Drug intelligence / Profile preview

bortezomib + gemcitabine

Development stage
Phase 2
Lead developer
Takeda
Modality
Small Molecules
Administration
Intravenous
01

Overview

This combination therapy consists of the proteasome inhibitor bortezomib and the antimetabolite chemotherapy agent gemcitabine. Bortezomib (formerly PS-341) works by reversibly inhibiting the 26S proteasome, leading to cell cycle arrest and apoptosis, particularly in cancer cells. Gemcitabine is a pyrimidine nucleoside analog that inhibits DNA synthesis by replacing cytidine during DNA replication and inhibiting ribonucleotide reductase. This specific combination was evaluated in a Phase II clinical trial sponsored by the National Cancer Institute (NCI) for the treatment of recurrent or metastatic nasopharyngeal carcinoma, where bortezomib was administered first, followed by the addition of gemcitabine upon disease progression.

Brand names
Velcade + Gemzar
Other names
bortezomib + gemcitabine hydrochloride
02

Targets

PSMB1 (26S Proteasome (β1-Subunit))PSMB5 (Proteasome subunit beta Type-5)DNA polymerase familyDNARNR (Ribonucleotide reductase)

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