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Belantamab mafodotin API Manufacturers & Suppliers

General Description:

Belantamab mafodotin, identified by CAS number 2050232-20-5, is a notable compound with significant therapeutic applications. Belantamab mafodotin, or GSK2857916, is an afucosylated monoclonal antibody that targets B cell maturation antigen conjugated to the microtubule disrupter monomethyl auristatin-F (MMAF). Belantamab mafodotin was granted FDA accelerated approval on 5 August 2020 for the treatment of multiple myeloma; 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.

Indications:

This drug is primarily indicated for: 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. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Belantamab mafodotin undergoes metabolic processing primarily in: Monoclonal antibodies are expected to be metabolized to smaller peptides and amino acids. MMAF is expected to be metabolized by oxidation and demethylation, however further data is not readily available. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Belantamab mafodotin are crucial for its therapeutic efficacy: Belantamab mafodotin at a dose of 2.5mg/kg reaches a C_max of 42 µg/mL, with a T_max of 0.78 hours, and an AUC of 4666 µg\*h/mL. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Belantamab mafodotin is an important consideration for its dosing schedule: The terminal half life of belantamab mafodotin was 12 days after the first dose and 14 days at steady state. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Belantamab mafodotin exhibits a strong affinity for binding with plasma proteins: Monoclonal antibodies are generally not protein bound. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Belantamab mafodotin from the body primarily occurs through: Monoclonal antibodies are eventually phagocytosed and broken down to smaller peptides and amino acids which are eliminated in a similar fashion to other proteins. Monoclonal antibodies are generally not eliminated in the urine, and only a small amount is excreted in bile. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Belantamab mafodotin is distributed throughout the body with a volume of distribution of: The mean steady state volume of distribution of belantamab mafodotin was 11 L. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Belantamab mafodotin is a critical factor in determining its safe and effective dosage: The clearance of belantamab mafodotin was 0.9 L/day after the first dose and 0.7 L/day at steady state. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Belantamab mafodotin exerts its therapeutic effects through: Belantamab mafodotin treats multiple myeloma through antibody dependant cell mediated cytotoxicity as well as G2/M cell cycle arrest. 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. Patients should be counselled regarding the risk of keratopathy. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Belantamab mafodotin functions by: 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). Afucosylation of the Fc region of monoclonal antibodies enhances binding to the Fc region, which enhances antibody dependant cell mediated cytoxicity. BCMA is uniquely expressed on CD138-positive myeloma cells. Targeting BCMA allows belantamab mafodotin to be highly selective in its delivery of MMAF to multiple myeloma cells. Belantamab mafodotin binds to BCMA, is internalised into cells, and releases MMAF. The MMAF payload binds to tubulin, stopping the cell cycle at the DNA damage checkpoint between the G2 and M phases, resulting in apoptosis. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Belantamab mafodotin belongs to the None, classified under the direct parent group Peptides. This compound is a part of the Organic Compounds, falling under the Organic Acids superclass, and categorized within the Carboxylic Acids and Derivatives class, specifically within the Amino Acids, Peptides, and Analogues subclass.

Categories:

Belantamab mafodotin is categorized under the following therapeutic classes: Amino Acids, Peptides, and Proteins, Antibodies, Antibodies, Monoclonal, Antibodies, Monoclonal, Humanized, Antibody-drug Conjugates, Antineoplastic Agents, Antineoplastic and Immunomodulating Agents, Blood Proteins, BSEP/ABCB11 Substrates, Cancer immunotherapy, Globulins, Immunoglobulins, Immunoproteins, Immunotherapy, MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES, OATP1B1/SLCO1B1 Substrates, OATP1B3 substrates, P-glycoprotein substrates, Proteins, Serum Globulins, Tubulin Inhibiting Agent. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.