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Velcade (bortezomib)

Shilpa · FDA-approved approved Verified Quality 76/100

Reversible inhibitor of 26S proteasome chymotrypsin-like activity preventing ubiquitinated protein degradation.

Bortezomib is a proteasome inhibitor approved for multiple myeloma and mantle cell lymphoma in adult patients. It reversibly inhibits 26S proteasome activity, disrupting protein homeostasis and inducing cancer cell death through multiple signaling pathways. Key risks include hypersensitivity reactions and increased toxicity with strong CYP3A4 inhibitors; intrathecal administration is contraindicated due to fatal outcomes. The drug demonstrates variable pharmacokinetics with half-lives of 40-193 hours and requires dose adjustment in moderate-to-severe hepatic impairment.

At a glance

Generic namebortezomib
SponsorShilpa
Drug classProteasome inhibitor
Target26S proteasome chymotrypsin-like activity
Therapeutic areaOncology
PhaseFDA-approved
First approval2003

Mechanism of action

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Experiments have demonstrated that bortezomib is cytotoxic to a variety of cancer cell types in vitro and causes a delay in tumor growth in vivo in nonclinical tumor models, including multiple myeloma.

Approved indications

Common side effects

Drug interactions

Key clinical trials

Patents

PatentExpiryType
117521642042-09-23Method of Use
116791192042-09-23Method of Use
120050692042-09-23Formulation
89625722032-11-03Formulation

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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