Detailed description page of ThPDB2
This page displays user query in tabular form. |
Th1685 details |
Primary information | |
---|---|
ID | 16155 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Amino Acids, Peptides, and Proteins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | Ryplazim |
Company | Prometic Biotherapeutics, Inc. |
Brand Description | Prometic Biotherapeutics, Inc. |
Prescribed For | Intravenous |
Chemical Name | 68.8 mg/1 |
Formulation | RYPLAZIM is contraindicated in patients with known hypersensitivity to plasminogen or other components of RYPLAZIM [See Hypersensitivity Reactions]. |
Physical Appearance | abdominal pain, bloating, nausea, fatigue, pain in extremities, bleeding, constipation, dry mouth, headache, dizziness, joint pain, and back pain. |
Route of Administration | Ryplazim is a medicine containing human plasminogen and is used to increase the blood levels of plasminogen in people with plasminogen deficiency type 1 (hypoplasminogenemia). It is injected into a vein. |
Recommended Dosage | Ryplazim (plasminogen, human-tvmh) is plasma-derived human plasminogen used to treat patients with plasminogen deficiency type 1 (hypoplasminogenemia). |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | Link |
Remarks | NA |
Primary information | |
---|---|
ID | 16156 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Anticoagulants |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16157 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Beta-Globulins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16158 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Blood Proteins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16159 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Cardiovascular Agents |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16160 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Enzyme Precursors |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16161 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Enzymes and Coenzymes |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16162 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Fibrin Modulating Agents |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16163 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Fibrinolytic Agents |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16164 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Globulins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16165 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Hematologic Agents |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16166 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Proteins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |
Primary information | |
---|---|
ID | 16167 |
Therapeutic ID | Th1685 |
Protein Name | Plasminogen |
Sequence | >Th1685_Plasminogen MEHKEVVLLLLLFLKSGQGEPLDDYVNTQGASLFSVTKKQLGAGSIEECAAKCEEDEEFTCRAFQYHSKEQQCVIMAENRKSSIIIRMRDVVLFEKKVYLSECKTGNGKNYRGTMSKTKNGITCQKWSSTSPHRPRFSPATHPSEGLEENYCRNPDNDPQGPWCYTTDPEKRYDYCDILECEEECMHCSGENYDGKISKTMSGLECQAWDSQSPHAHGYIPSKFPNKNLKKNYCRNPDRELRPWCFTTDPNKRWELCDIPRCTTPPPSSGPTYQCLKGTGENYRGNVAVTVSGHTCQHWSAQTPHTHNRTPENFPCKNLDENYCRNPDGKRAPWCHTTNSQVRWEYCKIPSCDSSPVSTEQLAPTAPPELTPVVQDCYHGDGQSYRGTSSTTTTGKKCQSWSSMTPHRHQKTPENYPNAGLTMNYCRNPDADKGPWCFTTDPSVRWEYCNLKKCSGTEASVVAPPPVVLLPDVETPSEEDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPSFDCGKPQVEPKKCPGRVVGGCVAHPHSWPWQVSLRTRFGMHFCGGTLISPEWVLTAAHCLEKSPRPSSYKVILGAHQEVNLEPHVQEIEVSRLFLEPTRKDIALLKLSSPAVITDKVIPACLPSPNYVVADRTECFITGWGETQGTFGAGLLKEAQLPVIENKVCNRYEFLNGRVQSTELCAGHLAGGTDSCQGDSGGPLVCFEKDKYILQGVTSWGLGCARPNKPGVYVRVSRFVTWIEGVMRNN |
Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The mean half-life of Ryplazim at steady-state is approximately 39.2 hours.[L34620] |
Description | Plasminogen is a pro-enzyme (i.e. a zymogen) which is cleaved to form plasmin - also known as [fibrinolysin] - as part of the fibrinolytic pathway that breaks down fibrin blood clots.[A236035] This pathway is activated when a clot is no longer needed or to prevent a clot from extending beyond the site of injury.[L34635] In June 2021, the FDA approved a plasma-derived plasminogen (Ryplazim, human plasminogen-tvmh)[L34620] for the treatment of type 1 plasminogen deficiency (hypoplasminogenemia).[L34615] It is the first and only FDA-approved treatment for this condition, which causes wood-like lesions to form on the mucous membranes of patients, providing an unmet medical need for patients with this rare congenital disease. |
Indication/Disease | Plasma-derived human plasminogen, marketed under the brand name Ryplazim, is indicated for the treatment of patients with plasminogen deficiency type 1 (hypoplasminogenemia).[L34620] |
Pharmacodynamics | The intravenous administration of plasminogen temporarily increases levels of plasminogen in the blood, allowing for the reduction or resolution of the lignous lesions associated with plasminogen deficiency.[L34620] Therapy is administered periodically, every 2 to 4 days, to prevent any significant build-up of these lesions between doses. Plasminogen administration can lead to tissue sloughing at mucosal sites where lignous lesions have built up, which may lead to organ or airway obstruction depending on the site of the lesion(s). Patients should be monitored for at least 4 hours post-administration, especially patients with evidence of airway involvement, to ensure airway management and respiratory support is readily available.[L34620] |
Mechanism of Action | Plasminogen is a zymogen produced in the liver which, when cleaved into its active form, breaks down fibrin blood clots.[A236035] This active form, called plasmin or fibrinolysin, is generated when tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA) cleave plasminogen to begin the fibrinolytic pathway.[L34635] Blood clots are broken down by plasmin into soluble fibrin and fibrinogen degradation products when the clot is no longer needed.[L34635] Type 1 plasminogen deficiency, also called hypoplasminogenemia, is a congenital disorder in which patients are deficient in plasminogen. Interestingly, this disease does not increase the risk of clotting, but rather results in the formation of lignous pseudomembranous lesions on the mucous membranes of the body.[L34625] Lesions range in location and severity but can lead to severe long-term consequences if left untreated. For example, lignous conjunctivitis, the most common manifestation of type 1 plasminogen deficiency, may lead to corneal tearing and blindness.[A236040] Human plasminogen is administered topically (e.g. in eye drops) or intravenously (i.e. [Ryplazim](https://www.fda.gov/media/149806/download)) in order to temporarily increase local or serum levels of fibrinogen. When this therapy is administered every 2 to 4 days, it prevents the build-up of lignous lesions and allows existing lesions to be shed. |
Toxicity | There are no data regarding overdose of intravenously administered human plasminogen. |
Metabolism | Plasminogen is a zymogen which is converted into the active fibrinolytic plasmin, or fibrinolysin, by tissue plasminogen activator (tPA) or urokinase-like plasminogen activator (uPA).[L34635,A236035] |
Absorption | Following 12 weeks of intravenous administration every 2 to 4 days, the mean AUCinf of Ryplazim was 5731.8 hr*% and its Cmax was approximately 125% of the mean physiological level (normal: 70-130%).[L34620] After 12 weeks of therapy, physiological plasminogen levels were sustained for approximately 24 hours post-dose and patients maintained a 10% absolute increase in plasminogen concentration for up to 96 hours after administration.[L34620] |
The mean steady-state volume of distribution of Ryplazim is approximately 49.3 mL/kg.[L34620] | |
Clearance | The clearance of Ryplazim appears to slow with extended use. Following the first intravenous dose the mean clearance of Ryplazim was 1.4 mL/hr/kg, while following an intravenous dose at week 12 the mean clearance was 0.9 mL/hr/kg.[L34620] |
Categories | Serum Globulins |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | NA |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |