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    Bortezomib (Velcade) is a proteasome inhibitor drug used to treat multiple myeloma and lymphoma. It works by reversibly binding to and inhibiting the 26S proteasome, which prevents degradation of proteins that induce apoptosis. This disrupts signaling pathways involved in cell survival and proliferation. It is administered intravenously every 3-4 weeks in cycles, with doses spaced 3 days apart to allow for recovery of platelet and neutrophil counts. Common side effects include thrombocytopenia, neuropathy, and gastrointestinal issues. It interacts with CYP3A4 enzymes and should be used cautiously with other drugs that induce or inhibit these enzymes.

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    Bortezomib

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    Bortezomib (Velcade) is a proteasome inhibitor drug used to treat multiple myeloma and lymphoma. It works by reversibly binding to and inhibiting the 26S proteasome, which prevents degradation of proteins that induce apoptosis. This disrupts signaling pathways involved in cell survival and proliferation. It is administered intravenously every 3-4 weeks in cycles, with doses spaced 3 days apart to allow for recovery of platelet and neutrophil counts. Common side effects include thrombocytopenia, neuropathy, and gastrointestinal issues. It interacts with CYP3A4 enzymes and should be used cautiously with other drugs that induce or inhibit these enzymes.

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    67 views2 pages

    Bortezomib

    Uploaded by

    BigBoosting
    Bortezomib (Velcade) is a proteasome inhibitor drug used to treat multiple myeloma and lymphoma. It works by reversibly binding to and inhibiting the 26S proteasome, which prevents degradation of proteins that induce apoptosis. This disrupts signaling pathways involved in cell survival and proliferation. It is administered intravenously every 3-4 weeks in cycles, with doses spaced 3 days apart to allow for recovery of platelet and neutrophil counts. Common side effects include thrombocytopenia, neuropathy, and gastrointestinal issues. It interacts with CYP3A4 enzymes and should be used cautiously with other drugs that induce or inhibit these enzymes.

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    DRUG STUDY AND INFORMATION FORM Generic Name: Bortezomib Trade Name: Velcade Drug Class: Proteasome Inhibition

    Structure/Chemistry: Has a unique boron-containing structure.

    Pharmacodynamics

    Mechanism of Action: Inhibits proteasome-mediation protein degradation. Binds to the 5 subunit of the 20S core of the 26S proteasome and reversibly inhibits its chymotrypsin-like activity which disrupts multiple signaling cascades leading to apoptosis. Specifically, blocks proteasomal degradation of IB (binds NF-B and restricts it to the cytosol) which prevents the transcriptional activity of NF-B and downregulates cell survival responses. Also, blocks ubiquitn-proteasomal degradation of p21, p27, p53, and other key regulators of the cell cycle and initators of apoptosis.

    Pharmacologic Effects: Inhibition of proteasomes which lead to decreased survival of malignant cells.

    Drug Resistance or Tolerance:

    Pharmacokinetics

    Absorption: 1.3 mg/m2 given as IV bolus on days 1, 4, 8, and 11 of every 21-day cycle (with a 10-day rest period). 72 hours should elapse between doses.

    Distribution:

    Elimination: t1/2 of 5.5 hours in plasma. Functional t1/2 of 24 hours.

    Metabolism: Deboronation followed by hydroxylation via CYPs 3A4 and 2D6

    Adverse Side Effects/Toxicity: Thrombocytopenia, fatigue, peripheral neuropathy (most chronic of toxicities), neutropenia, anemia, vomiting, diarrhea, limb pain, dehydration, nausea, and/or weakness. Injection may precipitate hypotension. Possibly congestive heart failure and prolonged QT-interval. Drug Interactions: Caution if used with inducers or inhibitors/substrates of CYP3A4

    Therapeutic uses: Treatment of myeloid metaplasia (myelofibrosis) before or after relapse from other drugs. Also used for mantle cell lymphoma and myeloma.

    Miscellaneous:

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