Peringatan Keamanan

Data regarding overdose is not readily available.L15326 However, keratopathy was seen in 71% of patients.A216756,A216761,A216766,L15326

Belantamab mafodotin

DB15719

biotech approved

Deskripsi

Belantamab mafodotin, or GSK2857916, is an afucosylated monoclonal antibody that targets B cell maturation antigen conjugated to the microtubule disrupter monomethyl auristatin-F (MMAF).A216756

Belantamab mafodotin was granted FDA accelerated approval on 5 August 2020 for the treatment of multiple myeloma;L15326 however, its manufacturer began the process for withdrawal of the US marketing authorization in November 2022. In the meantime, belantamab mafodotin will be available for patients in the Risk Evaluation and Mitigation Strategy (REMS) program who can enrol in a compassionate use program.L44236

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) The terminal half life of belantamab mafodotin was 12 days after the first dose and 14 days at steady state.[L15326]
Volume Distribusi The mean steady state volume of distribution of belantamab mafodotin was 11 L.[L15326]
Klirens (Clearance) The clearance of belantamab mafodotin was 0.9 L/day after the first dose and 0.7 L/day at steady state.[L15326]

Absorpsi

Belantamab mafodotin at a dose of 2.5mg/kg reaches a Cmax of 42 µg/mL, with a Tmax of 0.78 hours, and an AUC of 4666 µg\*h/mL.L15326

Metabolisme

Monoclonal antibodies are expected to be metabolized to smaller peptides and amino acids.L15326 MMAF is expected to be metabolized by oxidation and demethylation, however further data is not readily available.A216781,A216776

Rute Eliminasi

Monoclonal antibodies are eventually phagocytosed and broken down to smaller peptides and amino acids which are eliminated in a similar fashion to other proteins.A31470,A177074 Monoclonal antibodies are generally not eliminated in the urine, and only a small amount is excreted in bile.A40006

Interaksi Obat

724 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Troglitazone Troglitazone may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Erythromycin Erythromycin may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Tamoxifen Tamoxifen may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Quinidine Quinidine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Tipranavir Tipranavir may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Ketoconazole Ketoconazole may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Nifedipine Nifedipine may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Letermovir The excretion of Belantamab mafodotin can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Belantamab mafodotin which could result in a higher serum level.
Ranolazine The serum concentration of Belantamab mafodotin can be increased when it is combined with Ranolazine.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Belantamab mafodotin.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Belantamab mafodotin.
Estrone Estrone may increase the thrombogenic activities of Belantamab mafodotin.
Estradiol Estradiol may increase the thrombogenic activities of Belantamab mafodotin.
Dienestrol Dienestrol may increase the thrombogenic activities of Belantamab mafodotin.
Mestranol Mestranol may increase the thrombogenic activities of Belantamab mafodotin.
Estriol Estriol may increase the thrombogenic activities of Belantamab mafodotin.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Belantamab mafodotin.
Quinestrol Quinestrol may increase the thrombogenic activities of Belantamab mafodotin.
Hexestrol Hexestrol may increase the thrombogenic activities of Belantamab mafodotin.
Tibolone Tibolone may increase the thrombogenic activities of Belantamab mafodotin.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Belantamab mafodotin.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Belantamab mafodotin.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Belantamab mafodotin.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Belantamab mafodotin.
Zeranol Zeranol may increase the thrombogenic activities of Belantamab mafodotin.
Equol Equol may increase the thrombogenic activities of Belantamab mafodotin.
Promestriene Promestriene may increase the thrombogenic activities of Belantamab mafodotin.
Methallenestril Methallenestril may increase the thrombogenic activities of Belantamab mafodotin.
Epimestrol Epimestrol may increase the thrombogenic activities of Belantamab mafodotin.
Moxestrol Moxestrol may increase the thrombogenic activities of Belantamab mafodotin.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Belantamab mafodotin.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Belantamab mafodotin.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Belantamab mafodotin.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Belantamab mafodotin.
Biochanin A Biochanin A may increase the thrombogenic activities of Belantamab mafodotin.
Formononetin Formononetin may increase the thrombogenic activities of Belantamab mafodotin.
Estetrol Estetrol may increase the thrombogenic activities of Belantamab mafodotin.
Lumacaftor The serum concentration of Belantamab mafodotin can be decreased when it is combined with Lumacaftor.
Vemurafenib The serum concentration of Belantamab mafodotin can be increased when it is combined with Vemurafenib.
Apalutamide The serum concentration of Belantamab mafodotin can be decreased when it is combined with Apalutamide.
Pitolisant The serum concentration of Belantamab mafodotin can be increased when it is combined with Pitolisant.
Isavuconazonium The serum concentration of Belantamab mafodotin can be increased when it is combined with Isavuconazonium.
Isavuconazole The serum concentration of Belantamab mafodotin can be increased when it is combined with Isavuconazole.
Fluconazole The serum concentration of Belantamab mafodotin can be increased when it is combined with Fluconazole.
Sildenafil The serum concentration of Belantamab mafodotin can be increased when it is combined with Sildenafil.
Sorafenib The serum concentration of Belantamab mafodotin can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Belantamab mafodotin can be increased when it is combined with Loxapine.
Quinine The serum concentration of Belantamab mafodotin can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Belantamab mafodotin can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Belantamab mafodotin can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Belantamab mafodotin can be increased when it is combined with Simvastatin.
Verapamil The serum concentration of Belantamab mafodotin can be increased when it is combined with Verapamil.
Mifepristone The serum concentration of Belantamab mafodotin can be increased when it is combined with Mifepristone.
Clofazimine The serum concentration of Belantamab mafodotin can be increased when it is combined with Clofazimine.
Vardenafil The serum concentration of Belantamab mafodotin can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Belantamab mafodotin can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Belantamab mafodotin can be increased when it is combined with Conivaptan.
Zonisamide The serum concentration of Belantamab mafodotin can be increased when it is combined with Zonisamide.
Norgestimate The serum concentration of Belantamab mafodotin can be increased when it is combined with Norgestimate.
Amiodarone The serum concentration of Belantamab mafodotin can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Belantamab mafodotin can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Belantamab mafodotin can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Belantamab mafodotin can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Belantamab mafodotin can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Belantamab mafodotin can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Belantamab mafodotin can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Belantamab mafodotin can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Belantamab mafodotin can be increased when it is combined with Mibefradil.
Lopinavir The serum concentration of Belantamab mafodotin can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Belantamab mafodotin can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Belantamab mafodotin can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Belantamab mafodotin can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Belantamab mafodotin can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Belantamab mafodotin can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Belantamab mafodotin can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Belantamab mafodotin can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Belantamab mafodotin can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Belantamab mafodotin can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Belantamab mafodotin can be increased when it is combined with Temsirolimus.
Lonafarnib The serum concentration of Belantamab mafodotin can be increased when it is combined with Lonafarnib.
Brefeldin A The serum concentration of Belantamab mafodotin can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Belantamab mafodotin can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Belantamab mafodotin can be increased when it is combined with Ivacaftor.

Target Protein

Tumor necrosis factor receptor superfamily member 17 TNFRSF17

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30894515
    Trudel S, Lendvai N, Popat R, Voorhees PM, Reeves B, Libby EN, Richardson PG, Hoos A, Gupta I, Bragulat V, He Z, Opalinska JB, Cohen AD: Antibody-drug conjugate, GSK2857916, in relapsed/refractory multiple myeloma: an update on safety and efficacy from dose expansion phase I study. Blood Cancer J. 2019 Mar 20;9(4):37. doi: 10.1038/s41408-019-0196-6.
  • PMID: 32107339
    Popat R, Warcel D, O'Nions J, Cowley A, Smith S, Tucker WR, Yong K, Esposti SD: Characterization of response and corneal events with extended follow-up after belantamab mafodotin (GSK2857916) monotherapy for patients with relapsed multiple myeloma: a case series from the first-time-in-human clinical trial. Haematologica. 2020 May;105(5):e261-e263. doi: 10.3324/haematol.2019.235937. Epub 2020 Feb 27.
  • PMID: 32759303
    Authors unspecified: Anti-BCMA Therapy Endorsed, despite Eye Toxicity. Cancer Discov. 2020 Aug 5. pii: 2159-8290.CD-NB2020-074. doi: 10.1158/2159-8290.CD-NB2020-074.
  • PMID: 32729730
    McMillan A, Warcel D, Popat R: Antibody-drug conjugates for multiple myeloma. Expert Opin Biol Ther. 2020 Jul 30. doi: 10.1080/14712598.2020.1802422.
  • PMID: 16478695
    Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X.
  • PMID: 15389672
    Lobo ED, Hansen RJ, Balthasar JP: Antibody pharmacokinetics and pharmacodynamics. J Pharm Sci. 2004 Nov;93(11):2645-68. doi: 10.1002/jps.20178.
  • PMID: 28653357
    Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29.
  • PMID: 16417259
    Doronina SO, Mendelsohn BA, Bovee TD, Cerveny CG, Alley SC, Meyer DL, Oflazoglu E, Toki BE, Sanderson RJ, Zabinski RF, Wahl AF, Senter PD: Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24. doi: 10.1021/bc0502917.
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Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Blenrep
    Injection, powder, lyophilized, for solution • 50 mg/1mL • Intravenous • US • Approved
  • Blenrep
    Injection, powder, for solution • 100 mg • Intravenous • EU
International Brands
  • BLENREP

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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