Asciminib is a kinase inhibitor that inhibits tyrosine kinase activity by targeting the ABL sarcomere binding pocket (STAMP inhibitor) of BCR-ABL1 fusion protein.

1、 Drug name

1. Common name: Asciminib

2. Product Name: SCEMBLIX ®

2、 Indications

1. Used to treat 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 inhibitors (TKIs) treatment.

2. Used to treat adult patients with Ph+CML-CP carrying T315I mutation.

3、 Specifications and characteristics

40mg, film coated tablets

4、 Main components

1. Active ingredient: Aximini hydrochloride (21.62 mg hydrochloride in 20 mg tablets, 43.24 mg hydrochloride in 40 mg tablets).

2. Auxiliary materials include colloidal silica, cross-linked carboxymethyl cellulose sodium, iron oxide, etc.

5、 Usage and dosage

1. Ph+CML-CP patients (previously received ≥ 2 TKIs): 80mg orally once daily or 40mg orally twice daily.

2. T315I mutation patients: Take 200mg orally twice daily.

3. Medication requirements: Swallow the entire tablet and avoid eating for 2 hours and 1 hour before and after.

6、 Dose adjustment

1. Thrombocytopenia/Neutropenia: If ANC<1.0 × 10 ⁹/L or PLT<50 × 10 ⁹/L, suspend administration until recovery. In severe cases, reduce to 40mg once daily or 20mg twice daily.

2. Elevated pancreatic enzymes: paused when asymptomatic and>2 × ULN, reduced after recovery; If accompanied by abdominal pain, pancreatitis should be ruled out.

3. Non hematological toxicity level ≥ 3: Pause until recovery to level ≤ 1 before reducing dosage.

7、 Medication precautions

1. Omission handling: Skip daily plan if missed for more than 12 hours; If the missed dose exceeds 6 hours twice a day, skip and take the next dose according to the original plan.

2. Vomiting treatment: If vomiting occurs on the same day, take the same dose as soon as possible and take the medication normally the next day.

3. Dietary taboos: Fasting for 2 hours and 1 hour before and after taking medication.

8、 Medication for special populations

1. Pregnancy period: Prohibited, may cause fetal malformation. Pregnancy status should be verified before medication, and effective contraception should be used during treatment and one week after discontinuation.

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and one week after the last dose.

3. Elderly individuals (≥ 65 years old): No dose adjustment is required, but close monitoring is necessary.

9、 Adverse reactions

1. Common (≥ 20%): Upper respiratory tract infection, musculoskeletal pain, fatigue, nausea, rash, diarrhea.

2. Laboratory abnormalities: thrombocytopenia, elevated triglycerides, decreased neutrophils, elevated ALT, etc.

3. Serious adverse reactions: bone marrow suppression (28% thrombocytopenia), pancreatic toxicity (2.5% pancreatitis), hypertension (19%).

10、 Contraindications

There are no clear contraindications, but it is absolutely prohibited during pregnancy.

11、 Drug interactions

1. Strong CYP3A4 inhibitor: 200mg twice daily regimen requires close monitoring of adverse reactions.

2. Itraconazole oral solution (containing hydroxypropyl - β - cyclodextrin): All doses should be avoided in combination.

3. CYP2C9 substrates: The 80mg daily regimen requires a reduction in the dosage of co administered drugs, while the 200mg twice daily regimen suggests switching to non CYP2C9 substrates.

12、 Storage method

1. Original bottle storage, built-in desiccant, moisture-proof.

2. Store at room temperature (20 ° C-25 ° C) and allow short-term storage at 15 ° C-30 ° C.

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