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Th1162 details

Primary information
ID 1678
ThPP ID Th1162
Therapeutic Peptide/Protein Name Alirocumab
Sequence NA view full sequnce in fasta
Functional Classification Ic
Molecular Weight 146000
Chemical Formula C6472H9996N1736O2032S42
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance N.A.
Categories N.A.
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target Proprotein convertase subtilisin/kexin type 9
Information of corresponding available drug in the market
Brand Name Praluent
Company Sanofi Aventis U.S. Llc
Brand Discription PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name NA
Formulation 75 mg/mL
Physcial Appearance injection, solution
Route of Administration Subcutaneous
Recommended Dosage The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects Allergic Reactions
Useful Link http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID 27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure N.A.

Primary information
ID 1679
ThPP ID Th1162
Therapeutic Peptide/Protein Name Alirocumab
Sequence NA view full sequnce in fasta
Functional Classification Ic
Molecular Weight 146001
Chemical Formula C6472H9996N1736O2032S43
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance N.A.
Categories N.A.
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target Proprotein convertase subtilisin/kexin type 10
Information of corresponding available drug in the market
Brand Name Praluent
Company Sanofi Aventis Canada Inc
Brand Discription PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name NA
Formulation 150 mg
Physcial Appearance solution
Route of Administration Subcutaneous
Recommended Dosage The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects Allergic Reactions
Useful Link http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID 27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure N.A.

Primary information
ID 1680
ThPP ID Th1162
Therapeutic Peptide/Protein Name Alirocumab
Sequence NA view full sequnce in fasta
Functional Classification Ic
Molecular Weight 146002
Chemical Formula C6472H9996N1736O2032S44
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance N.A.
Categories N.A.
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target Proprotein convertase subtilisin/kexin type 11
Information of corresponding available drug in the market
Brand Name Praluent
Company Sanofi Aventis Canada Inc
Brand Discription PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name NA
Formulation 75 mg
Physcial Appearance solution
Route of Administration Subcutaneous
Recommended Dosage The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects Allergic Reactions
Useful Link http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID 27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure N.A.

Primary information
ID 1681
ThPP ID Th1162
Therapeutic Peptide/Protein Name Alirocumab
Sequence NA view full sequnce in fasta
Functional Classification Ic
Molecular Weight 146005
Chemical Formula C6472H9996N1736O2032S47
Isoelectric Point NA
Hydrophobicity NA
Melting Point (℃) NA
Half Life In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance N.A.
Categories N.A.
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target Proprotein convertase subtilisin/kexin type 14
Information of corresponding available drug in the market
Brand Name Praluent
Company Sanofi Aventis U.S. Llc
Brand Discription PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name NA
Formulation 150 mg/mL
Physcial Appearance injection, solution
Route of Administration Subcutaneous
Recommended Dosage The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects Allergic Reactions
Useful Link http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID 27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1678
ThPP ID	Th1162
Therapeutic Peptide/Protein Name	Alirocumab
Sequence	NA view full sequnce in fasta
Functional Classification	Ic
Molecular Weight	146000
Chemical Formula	C6472H9996N1736O2032S42
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description	Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease	Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics	Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action	Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity	During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism	Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption	Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution	Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance	N.A.
Categories	N.A.
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target	Proprotein convertase subtilisin/kexin type 9
Information of corresponding available drug in the market
Brand Name	Praluent
Company	Sanofi Aventis U.S. Llc
Brand Discription	PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for	It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name	NA
Formulation	75 mg/mL
Physcial Appearance	injection, solution
Route of Administration	Subcutaneous
Recommended Dosage	The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication	It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects	Allergic Reactions
Useful Link	http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID	27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure	N.A.

Primary information
ID	1679
ThPP ID	Th1162
Therapeutic Peptide/Protein Name	Alirocumab
Sequence	NA view full sequnce in fasta
Functional Classification	Ic
Molecular Weight	146001
Chemical Formula	C6472H9996N1736O2032S43
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description	Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease	Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics	Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action	Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity	During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism	Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption	Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution	Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance	N.A.
Categories	N.A.
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target	Proprotein convertase subtilisin/kexin type 10
Information of corresponding available drug in the market
Brand Name	Praluent
Company	Sanofi Aventis Canada Inc
Brand Discription	PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for	It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name	NA
Formulation	150 mg
Physcial Appearance	solution
Route of Administration	Subcutaneous
Recommended Dosage	The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication	It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects	Allergic Reactions
Useful Link	http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID	27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure	N.A.

Primary information
ID	1680
ThPP ID	Th1162
Therapeutic Peptide/Protein Name	Alirocumab
Sequence	NA view full sequnce in fasta
Functional Classification	Ic
Molecular Weight	146002
Chemical Formula	C6472H9996N1736O2032S44
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description	Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease	Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics	Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action	Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity	During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism	Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption	Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution	Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance	N.A.
Categories	N.A.
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target	Proprotein convertase subtilisin/kexin type 11
Information of corresponding available drug in the market
Brand Name	Praluent
Company	Sanofi Aventis Canada Inc
Brand Discription	PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for	It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name	NA
Formulation	75 mg
Physcial Appearance	solution
Route of Administration	Subcutaneous
Recommended Dosage	The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication	It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects	Allergic Reactions
Useful Link	http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID	27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure	N.A.

Primary information
ID	1681
ThPP ID	Th1162
Therapeutic Peptide/Protein Name	Alirocumab
Sequence	NA view full sequnce in fasta
Functional Classification	Ic
Molecular Weight	146005
Chemical Formula	C6472H9996N1736O2032S47
Isoelectric Point	NA
Hydrophobicity	NA
Melting Point (℃)	NA
Half Life	In monotherapy, the median half-life of alirocumab at steady state was 17â€“20 days in patients rece
Description	Alirocumab is a biopharmaceutical drug approved by the FDA in July 2015 as a second line treatment for high cholesterol for adults whose LDL-cholesterol (LDL-C) is not controlled by diet and statin treatment. It is a human monoclonal antibody administered by subcutaneous injection that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors, and it was the first such agent to receive FDA approval. The FDA approval was contingent on the completion of further clinical trials to better determine efficacy and safety. PCSK9 inhibition facilitates more LDL-C clearance from the blood.
Indication/Disease	Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy in adults who require additional LDL-cholesterol (LDL-C) lowering due to heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease.
Pharmacodynamics	Alirocumab reduces levels of PCSK9 in a concentration-dependent manner.
Mechanism of Action	Alirocumab is a fully human IgG1 monoclonal antibody that binds and inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), an enzyme found to have gain of function mutations in autosomal dominant hypercholesterolemia. PCSK9 is secreted by the liver and typically binds to the LDL receptors in serum and marks them for lysosomal degradation. In result, the LDL receptors are not able to recycle to the plasma membrane, reducing their binding to LDL-C and therefore reducing the clearance of LDL-C from plasma. Therefore by inhibiting PCSK9's actions, alirocumab allows for more LDL-C reuptake by the liver and facilitates a higher rate of clearance. Lower LDL cholesterol concentrations are associated with a reduced risk of coronary heart disease.
Toxicity	During a 13-week toxicology study of 75 mg/kg once weekly alirocumab in combination with 40 mg/kg once daily atorvastatin in adult monkeys, there were no effects of PRALUENT on the humoral immune response to keyhole limpet hemocyanin (KLH) after one to two months at exposures 100-fold greater than the exposure at the maximum recommended human dose of 150 mg every two weeks, based on AUC.
Metabolism	Antibodies are generally metabolized by the reticuloendothelial system and degraded into small peptides and individual amino acids - therefore specific metabolism studies were not conducted. Alirocumab did not show evidence of affecting CYP 450 enzymes or transporter proteins in co-administration with statins.
Absorption	Following subcutaneous (SC) administration, alirocumab is absorbed into the bloodstream and maximum concentrations are reached at a median time of 3-7 days. The absolute availability after SC administration was 85%.
Volume of Distribution	Alirocumab is mainly distributed through the circulatory system, with minimal extravascular distribution.
Clearance	N.A.
Categories	N.A.
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	The risk or severity of adverse effects can be increased when Alirocumab is combined with Belimumab.
Target	Proprotein convertase subtilisin/kexin type 14
Information of corresponding available drug in the market
Brand Name	Praluent
Company	Sanofi Aventis U.S. Llc
Brand Discription	PRALUENT is a sterile, preservative-free, clear, colorless to pale yellow solution for subcutaneous injection. PRALUENT 75 mg/mL or 150 mg/mL solution for subcutaneous injection in a single-dose pre-filled pen or single-dose pre-filled syringe is supplied in a siliconized 1 mL Type-1 clear glass syringe. The needle shield is not made with natural rubber latex.
Prescribed for	It is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C.
Chemical Name	NA
Formulation	150 mg/mL
Physcial Appearance	injection, solution
Route of Administration	Subcutaneous
Recommended Dosage	The recommended starting dose of PRALUENT is 75 mg administered subcutaneously once every 2 weeks, since the majority of patients achieve sufficient LDL-C reduction with this dosage. If the LDL-C response is inadequate, the dosage may be increased to the maximum dosage of 150 mg administered every 2 weeks.
Contraindication	It is contraindicated in patients with a history of a serious hypersensitivity reaction to PRALUENT. Reactions have included hypersensitivity vasculitis and hypersensitivity reactions requiring hospitalization.
Side Effects	Allergic Reactions
Useful Link	http://www.rxlist.com/praluent-drug/clinical-pharmacology.htm
PubMed ID	27729681, 26651519, 25484055, 24284914, 23254906, 25484055, 24284914, 23254906, 25609019
3-D Structure	N.A.