Ascimib Asciminib Hydrochloride

[Key Drug Information]

Generic Name: Asciminib Tablets / Asciminib Hydrochloride Tablets

Brand Name: Shanbeili / Scemblix / Ascimib

English Name: Asciminib

Dosage Form & Strength: Film-coated tablets

Strength: 40 mg per tablet; 30 tablets per box

Manufacturer: Everest Pharma Ltd (Everest Pharma, Bangladesh)

[Indications & Unique Mechanism]

Asciminib is a novel, highly selective BCR-ABL1 tyrosine kinase inhibitor (TKI). Its mechanism of action differs from that of traditional TKIs (such as imatinib, dasatinib, etc.); it functions by binding to the myristoyl pocket of the ABL1 kinase, thereby classifying it as a STAMP inhibitor (Specifically Targeting the ABL Myristoyl Pocket).

Official Approved Indications for Asciminib (based on US FDA and EU EMA approvals; applicable to adult patients):

Philadelphia chromosome-positive Chronic Myeloid Leukemia (Ph+ CML) in the Chronic Phase (CP),

provided that it meets either of the following conditions:

(a) Patients who have previously received two or more tyrosine kinase inhibitors (TKIs)—

—e.g., imatinib, nilotinib, dasatinib, bosutinib, etc.—and for whom treatment failed (due to insufficient efficacy) or was not tolerated due to toxicity.

(b) Patients harboring the BCR-ABL1 T315I mutation (regardless of the number of prior TKI treatments received)—

—The T315I mutation is one of the most refractory drug-resistant mutations in CML; it confers high resistance to most traditional TKIs (with the exception of ponatinib), whereas Asciminib demonstrates potent inhibitory activity against this specific mutation.

Supplementary Note:

Asciminib is not indicated for CML in the Accelerated Phase (AP) or Blast Phase (BP) (unless administered within the context of a clinical trial). Molecular testing (e.g., qPCR + mutation analysis) must be performed to confirm the *BCR-ABL1* status and the presence of specific mutations—such as T315I—before determining whether Asciminib is an appropriate treatment option.

Clinical Significance:

Asciminib offers a new therapeutic option for patients with Chronic Myeloid Leukemia (CML) who have developed multi-drug resistance or are intolerant to Tyrosine Kinase Inhibitors (TKIs); it holds particular breakthrough value for patients harboring the T315I mutation. Characterized by superior target specificity and a more favorable side-effect profile (e.g., a lower incidence of pleural effusion, vascular events, etc.), Asciminib significantly improves the quality of life and long-term prognosis for a subset of patients with refractory disease.

[Dosage and Administration]

Asciminib is a targeted therapy indicated for the treatment of Philadelphia chromosome-positive Chronic Myeloid Leukemia (Ph+ CML). Its dosage and administration must strictly adhere to the approved indications and the individual patient's clinical status. The following represents key prescribing information based on clinical guidelines:

I. Recommended Dosage Based on Indication

1. Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia (Ph+ CML-CP)

*   For patients previously treated with ≥2 Tyrosine Kinase Inhibitors (TKIs):

*   Recommended Dosage: 80 mg orally once daily; OR 40 mg orally twice daily.

*   Administration: May be taken with or without food. Tablets must be swallowed whole; do not break, crush, or chew.

*   For patients with Chronic Phase Ph+ CML harboring the T315I mutation:

*   Recommended Dosage: 200 mg orally twice daily. 

*   Administration: Must be taken with food. Tablets must be swallowed whole; avoid administration on an empty stomach.

2. Principles for Dosage Adjustment

If a patient experiences Grade 3 or higher adverse reactions, treatment must be temporarily suspended. Once symptoms have resolved to Grade 1 or returned to baseline levels, treatment may be resumed at a reduced dosage (the specific dosage reduction regimen should be determined by a physician).

Patients with Hepatic Impairment: No dosage adjustment is required for patients with mild to moderate hepatic impairment. Asciminib should be used with caution in patients with severe hepatic impairment, as there is currently no established recommended dosage for this population. Patients with Renal Impairment: No dose adjustment is required for patients with mild to moderate renal impairment; data are limited for patients with severe renal impairment, and use should be guided by a physician.

II. Precautions for Use

1.  Fixed Dosing Schedule: When administered once daily, it is recommended to take the medication at the same time each day; when administered twice daily, the two doses should be spaced approximately 12 hours apart.

2.  Management of Missed Doses:

If more than 12 hours remain before the next scheduled dose, take the missed dose as soon as possible.

If less than 12 hours remain before the next scheduled dose, skip the missed dose entirely; do not take a double dose at the next scheduled time.

3.  Drug Interactions: Avoid concomitant use with strong CYP3A4 inhibitors (e.g., itraconazole, clarithromycin) or inducers (e.g., rifampin, carbamazepine). If concomitant use is necessary, consult a physician regarding dose adjustment.

III. Important Reminders

Asciminib is a prescription medication. The specific dosage and administration schedule must be determined by a physician based on the patient's disease subtype, treatment history, genetic mutation status, and physical tolerance. Patients must not independently increase or decrease the dosage, nor discontinue the medication without medical advice.

During treatment, patients require regular monitoring of blood counts, liver function, bone marrow cytology, and other relevant parameters to facilitate the timely assessment of efficacy and safety.

[Important Warnings and Precautions]

The following constitute critical safety information for this medication, requiring close monitoring and management:

1.  Myelosuppression: May cause severe thrombocytopenia, neutropenia, and anemia. During treatment, blood counts must be monitored regularly (e.g., every 2 weeks for the first 3 months, and monthly thereafter); dose adjustments or temporary discontinuation of the medication may be required depending on the severity of the condition.

2.  Pancreatic Toxicity: May cause pancreatitis and elevated serum lipase/amylase levels. Lipase and amylase levels should be monitored regularly during treatment. Patients experiencing symptoms of pancreatitis—such as abdominal pain—should seek immediate medical evaluation.

3.  Hypertension: May cause or exacerbate hypertension. Blood pressure should be monitored regularly during treatment and controlled with antihypertensive medications as needed.

4.  Cardiovascular Toxicity: May increase the risk of cardiovascular events. Caution should be exercised when administering this medication to patients with a history of heart disease or relevant cardiovascular risk factors. 5.  Embryo-Fetal Toxicity: May cause harm to the fetus. Women of reproductive potential and their partners must use effective contraception during treatment and for at least 1 week after the last dose.

[Adverse Reactions]

In clinical studies, the most common adverse reactions (incidence ≥ 20%) included: musculoskeletal pain, thrombocytopenia, fatigue, upper respiratory tract infection, headache, neutropenia, and diarrhea.

The most common Grade 3 or 4 severe adverse reactions (incidence ≥ 5%) included: thrombocytopenia, neutropenia, elevated pancreatic enzymes, and hypertension.

[Drug Interactions]

Strong CYP3A4 Inhibitors (e.g., itraconazole, ketoconazole): May increase aciminib plasma concentrations, thereby increasing the risk of adverse reactions; use with caution.

Certain Specific Medications: Co-administration with oral formulations containing hydroxypropyl-beta-cyclodextrin (e.g., certain oral itraconazole solutions) may significantly reduce the bioavailability of aciminib, thereby compromising efficacy; co-administration should be avoided.

[Use in Specific Populations]

Pregnant Women: Based on animal data, may cause harm to the fetus; contraindicated.

Lactating Women: Breastfeeding is not recommended during treatment and for at least 1 week after the last dose.

Children and Adolescents: Safety and efficacy have not been established.

Geriatric Patients: No significant differences in overall safety were observed compared to younger patients.

[Storage]

Store at room temperature (20–25°C) in the original packaging, protected from moisture.

Keep out of reach of children.

[Important Note]

This package insert integrates official product information and patient guidelines from the Mayo Clinic; it is intended to serve as a comprehensive reference for you but does not substitute for the prescription and guidance of a professional physician.

To help you more clearly compare the differences between various targeted therapies, or to understand detailed data regarding aciminib in specific clinical studies, I can provide further analysis and organization for you upon request. Product Specifications

Product Name: Asciminib Hydrochloride Tablets (Asciminib) 40 mg × 30 Tablets/Box | Ascimib | Asciminib Hydrochloride

Common Name: Asciminib Hydrochloride Tablets

Active Ingredient: Asciminib Hydrochloride

Dosage Form: Oral Film-Coated Tablets

Specification: 40 mg per tablet; 30 tablets per box

Manufacturer: Everest Pharma Ltd (Bangladesh)

Indications: Officially approved indications for Asciminib (based on US FDA and EU EMA approvals; applicable to adult patients):

Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in the chronic phase (CP),

meeting either of the following conditions:

(a) Previously treated with two or more tyrosine kinase inhibitors (TKIs)—

e.g., Imatinib, Nilotinib, Dasatinib, Bosutinib, etc.—where treatment failed (due to insufficient efficacy) or was not tolerated due to toxicity.

(b) Harboring the BCR-ABL1 T315I mutation (regardless of the number of prior TKI treatments).

—The T315I mutation is one of the most difficult-to-treat resistance mutations in CML; it confers high resistance to most traditional TKIs (with the exception of Ponatinib), whereas Asciminib demonstrates potent inhibitory activity against this specific mutation.

Dosage and Administration: Chronic Phase Philadelphia Chromosome-Positive Chronic Myeloid Leukemia (Ph+ CML-CP)

For patients previously treated with ≥2 tyrosine kinase inhibitors (TKIs):

Recommended dosage: 80 mg orally once daily; OR 40 mg orally twice daily.

Administration: May be taken with or without food. Tablets must be swallowed whole; do not break, crush, or chew.

For patients with chronic phase Philadelphia chromosome-positive chronic myeloid leukemia harboring the T315I mutation:

Recommended dosage: 200 mg orally twice daily. Administration: Must be taken with a meal; swallow the tablet whole. Avoid taking on an empty stomach.