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Idarubicin Hydrochloride
    Publish time 2024-10-17 14:29    

CAS Number: 57852-57-0

Idarubicin Hydrochloride

Basic Information

  • CAS Number: 57852-57-0

  • Product Name: Idarubicin hydrochloride

  • Molecular Formula: C26H28ClNO9

  • Molecular Weight: 533.95 (or 533.97, depending on the calculation method)

Physical Properties

  • Form: Solid, typically orange-red or red

  • Melting Point: 183-185°C (alternatively reported as 172-174°C)

  • Boiling Point: 725.4°C at 760 mmHg

  • Flash Point: 392.5°C

  • Density: No specific data (but rough estimates available)

  • Solubility: Highly soluble in DMSO (≥26.7 mg/mL), insoluble in ethanol, requires ultrasonic processing for solubility in water (≥2.39 mg/mL)

  • Stability: Hygroscopic, light-sensitive

Chemical Properties

  • Mechanism of Action: As an anthracycline-based non-specific cell cycle anticancer drug, idarubicin hydrochloride inhibits DNA synthesis, interferes with RNA polymerase, and inhibits topoisomerase II.

  • Potency: It has an 8-fold potency compared to daunorubicin and a 4-5 fold potency compared to doxorubicin.

Pharmaceutical Characteristics

  • Indications:

    • First-line treatment of adult acute non-lymphoblastic leukemia (ANLL) and induction remission therapy for relapsed and refractory patients.

    • Second-line treatment for adult and pediatric acute lymphoblastic leukemia (ALL).

    • Also used in the treatment of advanced breast cancer, myelodysplastic syndromes, and non-Hodgkin's lymphoma.

  • Dosage and Administration:

    • Adult acute myeloid leukemia: In combination with cytosine arabinoside, the recommended dose is 12 mg/m² intravenously per day for three consecutive days; or alone and in combination, the recommended dose is 8 mg/m² intravenously per day for five consecutive days.

    • Adult acute lymphoblastic leukemia: The recommended dose for monotherapy is 12 mg/m² intravenously per day for three consecutive days.

    • Pediatric acute lymphoblastic leukemia: The recommended dose is 10 mg/m² per day for three consecutive days.

  • Adverse Reactions:

    • Severe myelosuppression manifesting as leukopenia, anemia, and thrombocytopenia.

    • Cardiotoxicity manifesting as fatal congestive heart failure, acute arrhythmias, and cardiomyopathy.

    • Other adverse reactions include alopecia, acute nausea and vomiting, mucositis, esophagitis, diarrhea, fever, chills, rash, etc.