Drug intelligence / Profile preview

AUY922 + bortezomib

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

Overview

**AUY922 + bortezomib** is an experimental combination of two small molecule antineoplastic agents being investigated for the treatment of relapsed or refractory multiple myeloma. AUY922 (also known as NVP-AUY922 or luminespib) is a heat shock protein 90 (HSP90) inhibitor, which disrupts multiple oncogenic signaling pathways by inhibiting this molecular chaperone, leading to cancer cell death. Bortezomib (marketed as Velcade) is a proteasome inhibitor that blocks the activity of the 26S proteasome, preventing proteolysis of proteins involved in cell cycle regulation and apoptosis, thereby promoting cancer cell death. The combination was evaluated in early-phase clinical trials to determine maximum tolerated dose, adverse events, and preliminary efficacy for multiple myeloma, but concomitant administration was limited by tolerability, especially ocular toxicities and other adverse events[2][3][5][6][7].

Brand names
Velcade (bortezomib)
Other names
AUY922 and bortezomibAUY-922 and bortezomibAUY 922 and bortezomibNVP-AUY922 + bortezomib
02

Targets

PSMB5 (Proteasome subunit beta Type-5)Heat shock protein 90 (HSP90) N-terminal ATPase domainHSP90AA1 (Heat shock protein HSP90-alpha)

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