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Anticancer Drugs Asciminib Medicine Oncology Pharmacology Physiotherapy

Asciminib (Mechanism of Action)

In this article we will discuss Asciminib (Mechanism of Action)

In this article, we will discuss Asciminib (Mechanism of Action). So, let’s get started.

Mechanism of Action

Asciminib is an ABL/BCR-ABL1 tyrosine kinase inhibitor. Asciminib inhibits the ABL1 kinase activity of the BCR-ABL1 fusion protein, by binding to the ABL myristoyl pocket. In studies conducted in vitro or in animal models of CML, asciminib showed activity against wild-type BCR-ABL1 and several mutant forms of the kinase, including the T315I mutation.

Pharmacodynamics

Exposure-Response Relationships
Over asciminib dosages of 10 mg to 200 mg twice daily (0.25 to 5 times the recommended 80 mg daily dosage), a lower exposure was associated with a smaller decrease in BCR-ABL1 level and a lower MMR rate at Week 24. Over asciminib dosages of 10 mg to 280 mg twice daily (0.25 to 7 times the recommended 80 mg daily dosage), a higher exposure was associated with slightly higher incidence of some adverse reactions (e.g., Grade ≥3 lipase increase, Grade ≥3 hemoglobin decrease, Grade ≥2 ALT increase, Grade ≥2 AST increase, Grade ≥2 bilirubin increase, and any grade lipase increase).

Cardiac Electrophysiology
Asciminib does not cause a large mean increase in QTc interval (i.e., >20 msec) at the maximum recommended clinical dosage (200 mg twice daily). Based on available clinical data, small mean QTc increase (<10 msec) cannot be excluded.

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