Belatacept

DB06681

biotech approved investigational

Deskripsi

Belatacept is a soluble fusion protein, which links the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) to the modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1 (IgG1). Structurally, abatacept is a glycosylated fusion protein with a MALDI-MS molecular weight of 92,300 Da and it is a homodimer of two homologous polypeptide chains of 357 amino acids each. It is produced through recombinant DNA technology in mammalian CHO cells. The drug has activity as a selective co-stimulation modulator with inhibitory activity on T lymphocytes. It is approved for the treatment of rheumatoid arthritis. Belatacept selectively blocks the process of T-cell activation. It was developed by Bristol-Myers-Squibb. Belatacept is only 2 amino acids different from abatacept (Orencia). FDA approved on June 15, 2011.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean terminal elimination half-life: 10 mg/kg, kidney transplant recipients= 9.8 days; 5 mg/kg, kidney transplant recipient = 8.2 days
Volume Distribusi Vd, steady state, transplant patients, 10 mg/kg = 0.11 L/kg; Vd, steady state, transplant patients, 5 mg/kg = 0.12 L/kg
Klirens (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.

Absorpsi

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 µg/mL; Cmax, 5 mg/kg = 139 µg/mL; AUC, 10 mg/kg = 22,252 µg · h/mL; AUC, 5 mg/kg = 14,090 µg · h/mL; Belatacept had linear and dose-dependent pharmacokinetic profile.

Metabolisme

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.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

353 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Belatacept.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Belatacept.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Belatacept.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Belatacept.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Belatacept.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Belatacept.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Belatacept.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Belatacept.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Belatacept.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Belatacept.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Belatacept.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Belatacept.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Belatacept.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Belatacept.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Belatacept.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Belatacept.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Belatacept.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Belatacept.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Belatacept.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Belatacept.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Belatacept.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Belatacept.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Belatacept.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Belatacept.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Belatacept.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Belatacept.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Belatacept.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Belatacept.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Belatacept.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Belatacept.
Cladribine Belatacept may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Belatacept.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Belatacept.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Belatacept.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Belatacept.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Belatacept.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Belatacept.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Belatacept.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Belatacept.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Belatacept.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Belatacept.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Belatacept.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Belatacept.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Belatacept.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Belatacept.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Belatacept.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Belatacept.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Belatacept.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Belatacept.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Belatacept.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Belatacept.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Belatacept.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Belatacept.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Belatacept.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Belatacept.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Belatacept.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Belatacept.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Belatacept.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Belatacept.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Belatacept.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Belatacept.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Belatacept.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Belatacept.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Belatacept.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Belatacept.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Belatacept.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Belatacept.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Belatacept.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Belatacept.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Belatacept.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Belatacept.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Belatacept.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Belatacept.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Belatacept.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Belatacept.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Belatacept.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Belatacept.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Belatacept.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Belatacept.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Belatacept.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Belatacept.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Belatacept.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Belatacept.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Belatacept.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Belatacept.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Belatacept.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Belatacept.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Belatacept.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Belatacept.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Belatacept.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Belatacept.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Belatacept.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Belatacept.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Belatacept.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Belatacept.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Belatacept.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Belatacept.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Belatacept.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Belatacept.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Belatacept.

Target Protein

T-lymphocyte activation antigen CD86 CD86
T-lymphocyte activation antigen CD80 CD80

Referensi & Sumber

Artikel (PubMed)
  • PMID: 22151353
    Wekerle T, Grinyo JM: Belatacept: from rational design to clinical application. Transpl Int. 2012 Feb;25(2):139-50. doi: 10.1111/j.1432-2277.2011.01386.x. Epub 2011 Dec 7.
  • PMID: 22928660
    Garnock-Jones KP: Belatacept: in adult kidney transplant recipients. BioDrugs. 2012 Dec 1;26(6):413-24. doi: 10.2165/11208900-000000000-00000.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
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    Injection, powder, lyophilized, for solution • 250 mg/1 • Intravenous • US • Approved
  • Nulojix
    Injection, powder, for solution • 250 mg • Intravenous • EU • Approved
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    Injection, powder, for solution • 250 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

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