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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors
asciminib
L01EA06
Forms & Strengths
- Oral tablets: 10 mg
- Oral tablets: 20 mg
- Oral tablets: 40 mg
- Oral tablets: 50 mg
Adult Dosing
- Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase, previously treated with >=2 tyrosine kinase inhibitors: 80 mg orally once daily or 40 mg twice daily
- Ph+ CML in chronic phase with T315I mutation: 200 mg orally twice daily
Pediatric Dosing
- Safety and efficacy in pediatric patients (<18 years) have not been established
Indications
- Treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors
- Treatment of adult patients with Ph+ CML in CP harboring the T315I mutation
Mechanism of Action
- Specifically targets the N-myristoyl transferase (NMT) activity of BCR::ABL1
- Acts as an STAMP (specifically targeting ABL myristoyl pocket) inhibitor, locking the enzyme in an inactive conformation
Contraindications
- Hypersensitivity to asciminib or any of its excipients
Adverse Reactions
- Upper respiratory tract infections
- Musculoskeletal pain
- Fatigue
- Nausea
- Diarrhea
- Thrombocytopenia
- Neutropenia
- Hypertension
- Pancreatitis
Drug Interactions
- Strong CYP3A4 inhibitors: May increase asciminib exposure and toxicity
- Strong CYP3A4 inducers: May decrease asciminib efficacy
- Strong CYP2C9 inhibitors: May increase exposure of asciminib
- Drugs that prolong the QT interval: May increase risk of QT prolongation
Curated Content: Needs Vetting Before Put to Clinical Use