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Bortezomib
    Publish time 2024-10-14 16:42    

CAS Number: 179324-69-7

Bortezomib

Basic Information

  • Product Name: Bortezomib

  • CAS Number: 179324-69-7

  • Molecular Formula: C19H25BN4O4

  • Molecular Weight: 384.23700 (alternatively, 384.24, with minor differences possibly due to measurement methods and precision)

Physical Properties

  • Appearance and Characteristics: Yellow solid

  • Melting Point: 122-124°C (alternatively, 139-143°C, which may be due to differences in batches or preparation methods)

  • Density: 1.214 (or 1.2±0.1 g/cm³)

  • Refractive Index: 1.564

  • Polarizability: 40.8±0.5 10^-24 cm³

  • Vapor Pressure: 5.1X10^-20 mm Hg at 25°C (estimated)

  • Solubility: Soluble in organic solvents such as DMSO (76 mg/l), but poorly soluble in water (<1 mg/ml)

Chemical Properties

  • Category: A dipeptide boronic acid that reversibly inhibits the 26S proteasome and is also an effective inhibitor of the 20S proteasome (20S proteasome) with a Ki of 0.6 nM

  • Mechanism of Action: Interferes with cancer cell growth and proliferation by inhibiting the activity of intracellular proteasomes, disrupting the cell cycle, inducing apoptosis, and inhibiting nuclear factor NF-κB

Pharmaceutical Properties

  • Indications:

    • Combined with melphalan and prednisone (MP regimen) for the treatment of previously untreated patients with multiple myeloma who are not suitable for high-dose chemotherapy and bone marrow suppression

    • As monotherapy for the treatment of patients with relapsed multiple myeloma who have received at least one prior therapy

    • For the treatment of patients with relapsed or refractory mantle cell lymphoma (safety and efficacy data for this indication are primarily from foreign clinical studies, and clinical study data for the Chinese population are lacking)

  • Route of Administration: For intravenous injection only; intrathecal injection can be fatal

  • Dosage and Administration:

    • When combined with melphalan and prednisone, the recommended dosage is a single injection of 1.3 mg/m², administered twice weekly for 2 weeks, followed by a 10-day rest period, with 3 weeks constituting one treatment cycle

    • For maintenance therapy beyond 8 cycles, the standard regimen may be followed, or a maintenance regimen of once weekly for 4 weeks, followed by a 13-day rest period, may be used

    • Dosage adjustments should be made based on the patient's actual condition and toxicity

  • Precautions:

    • During bortezomib treatment, patients require frequent blood tests to monitor its effects on the hematopoietic system

    • Patients should follow the doctor's advice, take medication according to the prescribed dosage and schedule, and pay close attention to possible adverse reactions

    • Store away from light and refrigerate to maintain stability