|
| Primary information |
|---|
| ID | 15876 |
| Therapeutic ID | Th1637 |
| Protein Name | Belantamab mafodotin |
| Sequence | >Th1637_Belantamab_mafodotin
QVQLVQSGAEVKKPGSSVKVSCKASGGTFSNYWMHWVRQAPGQGLEWMGATYRGHSDTYYNQKFKGRVTITADKSTSTAYMELSSLRSEDTAVYYCARGAIYDGYDVLDNWGQGTLVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
|
| 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 | OATP1B1/SLCO1B1 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 |