Ascimib 80 mg, containing the active pharmaceutical ingredient Asciminib, is an advanced targeted therapy for chronic myeloid leukemia (CML). Classified as an ABL/BCR-ABL1 tyrosine kinase inhibitor, Ascimib offers a novel mechanism of action by selectively binding to the myristoyl pocket of the ABL1 kinase, effectively inhibiting the activity of the BCR-ABL1 fusion protein. This mechanism allows it to act against both wild-type BCR-ABL1 and resistant mutant forms, including the T315I mutation, providing a vital treatment option for patients with resistance or intolerance to previous tyrosine kinase inhibitors (TKIs).

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Therapeutic Class

Cytotoxic Chemotherapy / Tyrosine Kinase Inhibitor

Indications

Ascimib is indicated for the treatment of adult patients with:

• Chronic-phase CML (CP-CML) previously treated with two or more TKIs

• CML with the T315I mutation in the BCR-ABL1 kinase

Treatment should be guided and monitored by an oncologist or hematologist experienced in managing CML.

Pharmacology

Ascimib is a highly selective ABL/BCR-ABL1 tyrosine kinase inhibitor. By targeting the myristoyl pocket of ABL1, it stabilizes the inactive form of the BCR-ABL1 protein, blocking downstream signaling pathways responsible for malignant cell proliferation and survival.

• Demonstrates efficacy against wild-type and mutant BCR-ABL1, including T315I

• Shows dose-dependent pharmacokinetics across 10–200 mg

• Steady-state exposure (AUC and Cmax) increases slightly more than dose proportionally

• Metabolized primarily via CYP3A4, necessitating caution with inhibitors or inducers

Dosage & Administration

• Standard dose for CP-CML (after 2+ TKIs):

  • 80 mg once daily or 40 mg twice daily

• T315I mutation:

  • 200 mg twice daily

• Administration guidelines:

  • Take orally without food, avoiding food for 2 hours before and 1 hour after dosing

  • Swallow tablets whole; do not crush, chew, or split

  • Continue therapy as long as clinical benefit is observed or until unacceptable toxicity occurs

• Missed doses:

  • Once daily: skip if >12 hours late

  • Twice daily: skip if >6 hours late

• Dose adjustments:

  • Reduce dose or permanently discontinue in patients unable to tolerate recommended doses

Interactions

• CYP3A4 substrate: Concomitant strong CYP3A4 inhibitors may increase exposure, raising the risk of adverse reactions

• Avoid itraconazole oral solution containing hydroxypropyl-β-cyclodextrin due to reduced efficacy

• Monitor patients closely when used with CYP3A modulators

Side Effects

Common and clinically significant adverse reactions include:

• Myelosuppression: Thrombocytopenia, neutropenia, anemia

• Pancreatitis: Elevation of lipase/amylase; may be asymptomatic or Grade 3–4

• Hypertension: Monitor blood pressure regularly

• Hypersensitivity: Rash, edema, bronchospasm; severe reactions may require dose interruption or discontinuation

• Cardiovascular toxicity: Ischemic events, arterial thrombotic conditions, and cardiac failure

  রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Pregnancy & Lactation

• Fetal risk: Can cause embryo-fetal harm based on animal studies

• Verify pregnancy status in females of reproductive potential before starting therapy

• Contraception: Effective methods required during treatment and for 1 week after the last dose

• Lactation: Avoid breastfeeding during treatment and for 1 week after the final dose

Precautions & Warnings

• Monitor for myelosuppression, pancreatitis, hypertension, hypersensitivity, and cardiovascular events

• Permanently discontinue in severe adverse reactions (e.g., Grade ≥3 hypersensitivity or cardiac failure)

• Regular blood tests recommended for early detection of toxicities

Use in Special Populations

• Pediatric safety and efficacy not established

• No significant differences observed in patients ≥65 years; limited data for ≥75 years

Storage Conditions

• Store at or below 25°C, in a cool, dry place

• Protect from light and moisture

• Keep out of reach of children.