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Asciminib is a kinase inhibitor that inhibits the tyrosine kinase activity of the BCR-ABL1 fusion protein by targeting its ABL myristoyl binding pocket (STAMP inhibitor).
1. Generic name: Asciminib
2. Trade name: SCEMBLIX®
1. For the treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia in the chronic phase (Ph+CML-CP) who have previously received two or more tyrosine kinase inhibitor (TKI) treatments.
2. For the treatment of adult patients with Ph+CML-CP carrying T315I mutation.
40 mg, film-coated tablets
1. Active ingredient: aceminib hydrochloride (20 mg tablet contains 21.62 mg hydrochloride, 40 mg tablet contains 43.24 mg hydrochloride).
2. Excipients include colloidal silica, croscarmellose sodium, iron oxide, etc.
1. Ph+CML-CP patients (previously receiving ≥2 TKIs): Take 80 mg orally once a day or 40 mg orally twice a day.
2. Patients with T315I mutation: Take 200 mg orally twice a day.
3. Medication requirements: Swallow the whole tablet and avoid 2 hours and 1 hour before and after eating.
1. Thrombocytopenia/neutropenia: If ANC<1.0×10⁹/L or PLT<50×10⁹/L, suspend administration until recovery. In severe cases, the dose needs to be reduced to 40 mg once a day or 20 mg twice a day.
2. Elevated pancreatic enzymes: Suspend when asymptomatic and >2×ULN, and reduce the dose after recovery; pancreatitis needs to be ruled out when accompanied by abdominal pain.
3. Non-hematological toxicity ≥ grade 3: Pause until recovery to ≤ grade 1 and then reduce the dose.
1. Treatment of missed doses: If you miss a dose for more than 12 hours in the once-daily regimen, skip it; if you miss a dose more than 6 hours in the twice-daily regimen, take the next dose as originally planned.
2. Treatment of vomiting: If you vomit on the same day, take the same dose as soon as possible and take the medicine normally the next day.
3. Dietary taboos: Fasting for 2 hours and 1 hour before and after taking the medicine.
1. Pregnancy: Contraindicated as it may cause fetal malformations. Pregnancy status needs to be verified before medication. Effective contraception is required during treatment and 1 week after stopping medication.
2. Lactation period: Breastfeeding is prohibited during treatment and 1 week after the last dose.
3. Elderly people (≥65 years old): No dose adjustment is required, but close monitoring is required.
1. Common (≥20%): Upper respiratory tract infection, musculoskeletal pain, fatigue, nausea, rash, diarrhea.
2. Laboratory abnormalities: Platelets decreased, triglycerides increased, neutrophils decreased, ALT increased, etc.
3. Serious adverse reactions: Bone marrow suppression (28% thrombocytopenia), pancreatic toxicity (2.5% pancreatitis), hypertension (19%).
There are no clear contraindications, but it is absolutely contraindicated during pregnancy.
1. Strong CYP3A4 inhibitor: The 200 mg twice daily regimen requires close monitoring of adverse reactions.
2. Itraconazole oral solution (containing hydroxypropyl-β-cyclodextrin): Avoid combined use of all doses.
3. CYP2C9 substrates: The 80 mg daily regimen requires reducing the dose of the combined drug, and the 200 mg twice daily regimen is recommended to use a non-CYP2C9 substrate.
1. Store in the original bottle with built-in desiccant to prevent moisture.
2. Store at room temperature (20°C-25°C). Short-term storage at 15°C-30°C is allowed.