Drug intelligence / Profile preview

tanespimycin + bortezomib

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous
01

Overview

**Tanespimycin + bortezomib** is an investigational **combination therapy** for multiple myeloma and other cancers, pairing the heat shock protein 90 (HSP90) inhibitor **tanespimycin** (also known as 17-AAG, KOS-953) with the proteasome inhibitor **bortezomib** (also known as PS-341). **Tanespimycin** inhibits HSP90, leading to destabilization and degradation of client oncoproteins, while **bortezomib** inhibits the 20S proteasome, disrupting protein homeostasis and inducing tumor cell apoptosis. The combination has shown **synergistic antitumor activity**, with tanespimycin sensitizing tumor cells to proteasome inhibition and reducing bortezomib-induced peripheral neuropathy. Developed primarily for relapsed/refractory multiple myeloma, the regimen was evaluated in various phase I/II/III trials, with the most common administration being intravenous dosing on days 1, 4, 8, and 11 of each 21-day cycle. While tolerability is generally favorable and efficacy was observed especially in bortezomib-naive populations, the development status is limited to clinical trials and the regimen is not approved for any indication[1][2][3][4][5][6][7].

Brand names
Velcade
Other names
tanespimycin + bortezomib
02

Targets

HSP90 (Heat shock protein 90 chaperone complex)26S proteasome

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