Bortezomib (Velcade)
Overview
A modified dipeptidyl boronic acid that reversibly inhibits the chymotrypsin-like activity of the 26S proteasome. Bortezomib disrupts the ubiquitin-proteasome pathway, stabilizing pro-apoptotic factors and inhibiting NF-kB activation, which is constitutively active in many hematologic malignancies.
Mechanism of Action
It was the first proteasome inhibitor approved for cancer treatment and fundamentally changed the treatment landscape of multiple myeloma..
Research Summary & Key Findings
FDA-approved for multiple myeloma and mantle cell lymphoma. VISTA trial established bortezomib-melphalan-prednisone (VMP) as a standard of care for transplant-ineligible myeloma patients. APEX trial demonstrated superior response rates and time to progression vs. dexamethasone in relapsed myeloma (Richardson et al., NEJM, 2005). Peripheral neuropathy is dose-limiting, mitigated by subcutaneous rather than IV administration.
Clinical Status
Bortezomib (Velcade) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.
Administration Routes
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