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Th1126 details

Primary information
ID 1596
ThPP ID Th1126
Therapeutic Peptide/Protein Name Belatacept
Sequence MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification IIa
Molecular Weight 92300
Chemical Formula C3508H5440N922O1096S32
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life Mean terminal elimination half-life- 9.8 days.
Description Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity N.A.
Metabolism The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories Antirheumatic Agents and Immunosuppressive Agents
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target T-lymphocyte activation antigen CD86,T-lymphocyte activation antigen CD80
Information of corresponding available drug in the market
Brand Name Nulojix
Company Bristol-Myers Squibb
Brand Discription NULOJIX (belatacept), a selective T-cell costimulation blocker, is a soluble fusion protein consisting of the modified extracellular domain of CTLA-4 fused to a portion (hinge-CH2-CH3 domains) of the Fc domain of a human immunoglobulin G1 antibody. Belatacept is produced by recombinant DNA technology in a mammalian cell expression system. Two amino acid substitutions (L104 to E; A29 to Y) were made in the ligand binding region of CTLA-4. As a result of these modifications, belatacept binds CD80 and CD86 more avidly than abatacept, the parent CTLA4-Immunoglobulin (CTLA4-Ig) molecule from which it is derived. The molecular weight of belatacept is approximately 90 kilodaltons.
Prescribed for NULOJIX (belatacept) is indicated for prophylaxis of organ rejection in adult patients receiving a kidney transplant. NULOJIX is to be used in combination with basiliximab induction, mycophenolate mofetil, and corticosteroids.
Chemical Name N.A.
Formulation Prior to use, the lyophile is reconstituted with a suitable fluid to obtain a clear to slightly opalescent, colorless to pale yellow solution, with a pH in the range of 7.2 to 7.8. Suitable fluids for constitution of the lyophile include SWFI, 0.9% NS, or D5W. Each 250 mg single-use vial of NULOJIX also contains: monobasic sodium phosphate (34.5 mg), sodium chloride (5.8 mg), and sucrose (500 mg).
Physcial Appearance NULOJIX is supplied as a sterile, white or off-white lyophilized powder for intravenous administration.
Route of Administration Intravenous Injection
Recommended Dosage N.A.
Contraindication Epstein-Barr virus (EBV) seronegative or with unknown EBV serostatus
Side Effects PTLD, predominantly CNS PTLD, and other malignancies, EBV Seropositive Subpopulation, Progressive Multifocal Leukoencephalopathy, Bacterial, Mycobacterial, Viral, and Fungal Infections, Proteinuria, Immunogenicity, New-Onset Diabetes After Transplantation, Hypertension, Dyslipidemia
Useful Link http://www.rxlist.com/nulojix-drug.htm http://www.nulojix.com/hcp/index.aspx http://www.drugs.com/nulojix.html
PubMed ID 25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure Th1126 (View) or (Download)

Primary information
ID 1597
ThPP ID Th1126
Therapeutic Peptide/Protein Name Belatacept
Sequence MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification IIa
Molecular Weight 92300
Chemical Formula C3508H5440N922O1096S32
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life Mean terminal elimination half-life- 9.8 days.
Description Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity N.A.
Metabolism The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories Antirheumatic Agents and Immunosuppressive Agents
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link N.A.
PubMed ID 25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure Th1126 (View) or (Download)

Primary information
ID 1598
ThPP ID Th1126
Therapeutic Peptide/Protein Name Belatacept
Sequence MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification IIa
Molecular Weight 92300
Chemical Formula C3508H5440N922O1096S32
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life Mean terminal elimination half-life- 9.8 days.
Description Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity N.A.
Metabolism The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories Antirheumatic Agents and Immunosuppressive Agents
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link N.A.
PubMed ID 25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure Th1126 (View) or (Download)

Primary information
ID 1599
ThPP ID Th1126
Therapeutic Peptide/Protein Name Belatacept
Sequence MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification IIa
Molecular Weight 92300
Chemical Formula C3508H5440N922O1096S32
Isoelectric Point N.A.
Hydrophobicity N.A.
Melting Point (℃) N.A.
Half Life Mean terminal elimination half-life- 9.8 days.
Description Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity N.A.
Metabolism The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories Antirheumatic Agents and Immunosuppressive Agents
Patents Number N.A.
Date of Issue N.A.
Date of Expiry N.A.
Drug Interaction N.A.
Target N.A.
Information of corresponding available drug in the market
Brand Name N.A.
Company N.A.
Brand Discription N.A.
Prescribed for N.A.
Chemical Name N.A.
Formulation N.A.
Physcial Appearance N.A.
Route of Administration N.A.
Recommended Dosage N.A.
Contraindication N.A.
Side Effects N.A.
Useful Link N.A.
PubMed ID 25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure Th1126 (View) or (Download)

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

Primary information
ID	1596
ThPP ID	Th1126
Therapeutic Peptide/Protein Name	Belatacept
Sequence	MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	92300
Chemical Formula	C3508H5440N922O1096S32
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Mean terminal elimination half-life- 9.8 days.
Description	Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease	For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics	Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action	Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity	N.A.
Metabolism	The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption	Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution	Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance	Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories	Antirheumatic Agents and Immunosuppressive Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	T-lymphocyte activation antigen CD86,T-lymphocyte activation antigen CD80
Information of corresponding available drug in the market
Brand Name	Nulojix
Company	Bristol-Myers Squibb
Brand Discription	NULOJIX (belatacept), a selective T-cell costimulation blocker, is a soluble fusion protein consisting of the modified extracellular domain of CTLA-4 fused to a portion (hinge-CH2-CH3 domains) of the Fc domain of a human immunoglobulin G1 antibody. Belatacept is produced by recombinant DNA technology in a mammalian cell expression system. Two amino acid substitutions (L104 to E; A29 to Y) were made in the ligand binding region of CTLA-4. As a result of these modifications, belatacept binds CD80 and CD86 more avidly than abatacept, the parent CTLA4-Immunoglobulin (CTLA4-Ig) molecule from which it is derived. The molecular weight of belatacept is approximately 90 kilodaltons.
Prescribed for	NULOJIX (belatacept) is indicated for prophylaxis of organ rejection in adult patients receiving a kidney transplant. NULOJIX is to be used in combination with basiliximab induction, mycophenolate mofetil, and corticosteroids.
Chemical Name	N.A.
Formulation	Prior to use, the lyophile is reconstituted with a suitable fluid to obtain a clear to slightly opalescent, colorless to pale yellow solution, with a pH in the range of 7.2 to 7.8. Suitable fluids for constitution of the lyophile include SWFI, 0.9% NS, or D5W. Each 250 mg single-use vial of NULOJIX also contains: monobasic sodium phosphate (34.5 mg), sodium chloride (5.8 mg), and sucrose (500 mg).
Physcial Appearance	NULOJIX is supplied as a sterile, white or off-white lyophilized powder for intravenous administration.
Route of Administration	Intravenous Injection
Recommended Dosage	N.A.
Contraindication	Epstein-Barr virus (EBV) seronegative or with unknown EBV serostatus
Side Effects	PTLD, predominantly CNS PTLD, and other malignancies, EBV Seropositive Subpopulation, Progressive Multifocal Leukoencephalopathy, Bacterial, Mycobacterial, Viral, and Fungal Infections, Proteinuria, Immunogenicity, New-Onset Diabetes After Transplantation, Hypertension, Dyslipidemia
Useful Link	http://www.rxlist.com/nulojix-drug.htm http://www.nulojix.com/hcp/index.aspx http://www.drugs.com/nulojix.html
PubMed ID	25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure	Th1126 (View) or (Download)

Primary information
ID	1597
ThPP ID	Th1126
Therapeutic Peptide/Protein Name	Belatacept
Sequence	MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	92300
Chemical Formula	C3508H5440N922O1096S32
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Mean terminal elimination half-life- 9.8 days.
Description	Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease	For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics	Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action	Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity	N.A.
Metabolism	The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption	Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution	Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance	Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories	Antirheumatic Agents and Immunosuppressive Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	N.A.
PubMed ID	25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure	Th1126 (View) or (Download)

Primary information
ID	1598
ThPP ID	Th1126
Therapeutic Peptide/Protein Name	Belatacept
Sequence	MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	92300
Chemical Formula	C3508H5440N922O1096S32
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Mean terminal elimination half-life- 9.8 days.
Description	Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease	For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics	Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action	Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity	N.A.
Metabolism	The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption	Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution	Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance	Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories	Antirheumatic Agents and Immunosuppressive Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	N.A.
PubMed ID	25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure	Th1126 (View) or (Download)

Primary information
ID	1599
ThPP ID	Th1126
Therapeutic Peptide/Protein Name	Belatacept
Sequence	MHVAQPAVVLASSRGIASFVCEYASPGKYTEVRVTVLRQADSQVTEVCAA view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	92300
Chemical Formula	C3508H5440N922O1096S32
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	Mean terminal elimination half-life- 9.8 days.
Description	Belatacept is a recombinant (CHO cells derived) soluble fusion protein, which links the extracellular domain of human cytotoxic CTLA-4 to the modified Fc portion of human IgG1, thereby selectively blocking the process of T-cell activation. It is a glycosylated fusion protein, which is a homodimer of two homologous polypeptide chains of 357 amino acids each. The drug acts as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It differs from abatacept (Orencia) by only 2 amino acids. It is approved for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers-Squibb. FDA approved on June 15, 2011.
Indication/Disease	For prophylaxis of organ rejection. It is also used concomitantly with basiliximumab for induction therapy, mycophenolate, and corticosteriods in kidney transplant recepients that are seropositive for the Epstein-Barr virus.
Pharmacodynamics	Belatacept binds to CD86 with a 4-fold higher affinity than abatacept. It also binds to CD80 with a 2-fold higher affinity than abatacept. It was observed in non-human primates that belatacept prolongs graft survival due to a decrease in antibody production against the donor organ. Furthermore, belatacept also inhibits the primary humoral immune response which is indicated by the decrease in post-transplant levels of IgG, IgM, and IgA. The magnitude of this effect is more significant in belatacept than it is in cyclosporine.
Mechanism of Action	Belatacept is a fusion protein in which the Fc portion of human IgG1 is attached onto the extracellular portion of human CTLA-4 (CD152). Belatacept specifically binds to CD80 and CD86 receptors that are found on the antigen-presenting cell (B cells, macrophages, dendritic cells) to block selective T-cell lymphocyte costimulation. CD80 and CD86 would normally act as the ligands to the CD28 receptor T-cells in which this interaction triggers the activation of T lymphocytes. However in the presence of belatacept, because the extracellular CTLA-4 component binds to CD28 with higher affinity than CD80 or CD86, T lymphyocyte anergy, a state of antigen specific tolerance, occurs instead. The T cell is also no longer able to respond to their antigen.
Toxicity	N.A.
Metabolism	The cytochrome P450 enzyme system or uridine diphosphate-glucuronosyltransferases are not expected to be involved with the metabolism of belatacept. Because the drug is a protein, belatacept is degraded into smaller peptides and amino acids by proteolytic enzymes.
Absorption	Following multiple intravenous doses of an initial 10 mg/kg dose and followed by a maintenance dose of 5 mg/kg in kidney transplant recipients, these are the following pharmacokinetic parameters: Cmax, 10 mg/kg = 247 Âµg/mL; Cmax, 5 mg/kg = 139 Âµg/mL; AUC, 10 mg/kg = 22,252 Âµg Â· h/mL; AUC, 5 mg/kg = 14,090 Âµg Â· h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.
Volume of Distribution	Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg;Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Clearance	Increased body weight may increase the clearance rate of belatacept.Mean systemic clearance:10 mg/kg, kidney transplant recipients= 0.49 mL/h/kg;5 mg/kg, kidney transplant recipient = 0.51 mL/h/kg.
Categories	Antirheumatic Agents and Immunosuppressive Agents
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	N.A.
Target	N.A.
Information of corresponding available drug in the market
Brand Name	N.A.
Company	N.A.
Brand Discription	N.A.
Prescribed for	N.A.
Chemical Name	N.A.
Formulation	N.A.
Physcial Appearance	N.A.
Route of Administration	N.A.
Recommended Dosage	N.A.
Contraindication	N.A.
Side Effects	N.A.
Useful Link	N.A.
PubMed ID	25611834, 25551406, 25448417, 25447131, 22928660, 22151353
3-D Structure	Th1126 (View) or (Download)

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