Primary information |
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ID | 15870 |
Therapeutic ID | Th1637 |
Protein Name | Belantamab mafodotin |
Sequence | >Th1637_Belantamab_mafodotin
QVQLVQSGAEVKKPGSSVKVSCKASGGTFSNYWMHWVRQAPGQGLEWMGATYRGHSDTYYNQKFKGRVTITADKSTSTAYMELSSLRSEDTAVYYCARGAIYDGYDVLDNWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Molecular Weight | NA |
Chemical Formula | NA |
Isoelectric Point | NA |
Hydrophobicity | NA |
Melting point | NA |
Half-life | The terminal half life of belantamab mafodotin was 12 days after the first dose and 14 days at steady state.[L15326] |
Description | Belantamab mafodotin, or GSK2857916, is an afucosylated monoclonal antibody that targets B cell maturation antigen conjugated to the microtubule distrupter monomethyl auristatin-F (MMAF).[A216756] Belantamab mafodotin was granted FDA approval on 5 August 2020.[L15326] |
Indication/Disease | Belantamab mafodotin is indicated in the treatment of adults with relapsed or refractory multiple myeloma who have received at least 4 prior therapies including an anti-CD38 monoclonal antibody, a proteasome inhibitor, and an immunomodulatory agent.[L15326] |
Pharmacodynamics | Belantamab mafodotin treats multiple myeloma through antibody dependant cell mediated cytotoxicity as well as G2/M cell cycle arrest.[A216771] It has a narrow therapeutic index due to the incidence of adverse effects, and a long duration of action as it is given every 3 weeks.[L15326] Patients should be counselled regarding the risk of keratopathy.[L15326] |
Mechanism of Action | Belantamab mafodotin, or GSK2857916, is an afucosylated monoclonal antibody that targets B cell maturation antigen (BCMA) conjugated to the microtubule distrupter monomethyl auristatin-F (MMAF).[A216756] Afucosylation of the Fc region of monoclonal antibodies enhances binding to the Fc region, which enhances antibody dependant cell mediated cytoxicity.[A216771] BCMA is uniquely expressed on CD138-positive myeloma cells.[A216756] Targeting BCMA allows belantamab mafodotin to be highly selective in its delivery of MMAF to multiple myeloma cells.[A216756] Belantamab mafodotin binds to BCMA, is internalised into cells, and releases MMAF.[A216756] The MMAF payload binds to tubulin, stopping the cell cycle at the DNA damage checkpoint between the G2 and M phases, resulting in apoptosis.[A216771] |
Toxicity | Data regarding overdose is not readily available.[L15326] However, keratopathy was seen in 71% of patients.[A216756,A216761,A216766,L15326] |
Metabolism | 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] |
Absorption | 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 |
| The mean steady state volume of distribution of belantamab mafodotin was 11 L.[L15326] |
Clearance | The clearance of belantamab mafodotin was 0.9 L/day after the first dose and 0.7 L/day at steady state.[L15326] |
Categories | BSEP/ABCB11 Substrates |
Patents Number | NA |
Date of Issue | NA |
Date of Expiry | NA |
Drug Interaction | NA |
Target | Tumor necrosis factor receptor superfamily member 17 |
Brand Name | NA |
Company | NA |
Brand Description | NA |
Prescribed For | NA |
Chemical Name | NA |
Formulation | NA |
Physical Appearance | NA |
Route of Administration | NA |
Recommended Dosage | NA |
Contraindication | NA |
Side Effects | NA |
Useful Link 1 | Link |
Useful Link 2 | NA |
Remarks | NA |