Asciminib

Indications

Cancer

Asciminib is used to treat adults with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP) who have already been treated with two or more tyrosine kinase inhibitors (TKIs). This use was approved under accelerated approval, based on major molecular response (MMR). Continued approval for it may depend on a confirmatory trial or trials verifying and describing the clinical benefit. Asciminib is also used for adults with Ph+ CML in chronic phase (CP) who have the T315I mutation.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Asciminib is an ABL/BCR-ABL1 tyrosine kinase inhibitor. It blocks the ABL1 kinase activity of the BCRABL1 fusion protein by binding to the ABL myristoyl pocket. In studies done in vitro and in animal models of CML, asciminib was active against wild-type BCR-ABL1 and against several mutant forms of the kinase, including the T315I mutation.

Steady-state exposure to asciminib (AUC and Cmax) rises slightly more than dose proportionally across the dose range of 10 to 200 mg (0.25 to 5 times the recommended 80 mg daily dosage), given once or twice daily. Pharmacokinetic parameters are shown as geometric mean (CV%) unless otherwise stated.

Pregnancy & Breastfeeding

Pregnancy: Animal studies and the way Asciminib works suggest it can harm the embryo and fetus if a pregnant woman takes it. There are no data on its use in pregnant women, so a risk linked to the medicine can't be assessed. Lactation: No data exist on whether Asciminib or its metabolites pass into human milk, what effect they have on a breastfed child, or whether milk production changes. Because the breastfed child could have serious adverse reactions, women are advised not to breastfeed during treatment and for 1 week after the last dose. Females and Males of Reproductive Potential: Animal studies point to the same concern, which is harm to the embryo and fetus when a pregnant woman takes the medicine. Pregnancy Testing: Check the pregnancy status of females of reproductive potential before starting treatment. Contraception: Females of reproductive potential should use effective contraception during treatment with Asciminib and for 1 week after the last dose. Infertility Females: Findings in animals suggest the medicine may impair fertility in females of reproductive potential. Whether this effect on fertility can be reversed is unknown.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: Recommended dosage in patients with Ph+ CML-CP, previously treated with two or more TKIs: the dose of Asciminib is 80 mg taken orally once daily at approximately the same time each day, or 40 mg twice daily at approximately 12-hour intervals. Take it by mouth without food. Avoid eating for at least 2 hours before and 1 hour after taking Asciminib. Continue treatment as long as clinical benefit is seen or until unacceptable toxicity occurs. Recommended dosage in patients with Ph+ CML-CP with the T315I mutation: the dose of Asciminib is 200 mg taken orally twice daily at approximately 12-hour intervals. Again, take it without food, and avoid eating for at least 2 hours before and 1 hour after the dose. Missed dose: on the once daily dosage regimen, if a dose of Asciminib is missed by more than approximately 12 hours, skip that dose and take the next one as scheduled. On the twice daily dosage regimens, if a dose is missed by more than approximately 6 hours, skip it and take the next dose as scheduled. Dosage modifications: the recommended dosage reductions of Asciminib for adverse reactions are as follows. For patients with CP-CML previously treated with two or more TKIs, the reduced dosage is 40 mg once daily or 20 mg twice daily. Permanently discontinue Asciminib in patients who can't tolerate 40 mg once daily or 20 mg twice daily. For patients with Ph+ CML-CP with the T315I mutation, the reduced dosage is 160 mg twice daily, and Asciminib should be permanently discontinued in patients who can't tolerate 160 mg twice daily.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.

Key Interactions

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