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. It was the first proteasome inhibitor approved for cancer treatment and fundamentally changed the treatment landscape of multiple myeloma.
Key Research 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.
Subcutaneous injection, Intravenous
FDA Approved
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