Drug intelligence / Profile preview

AUY922 + bortezomib + dexamethasone

Development stage
Discontinued
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is an investigational combination therapy comprising **AUY922** (luminespib), **bortezomib**, and **dexamethasone**, studied primarily for relapsed or refractory multiple myeloma. - **AUY922 (luminespib)** is a selective inhibitor of the molecular chaperone **heat shock protein 90 (Hsp90)**, disrupting the folding and function of multiple oncogenic client proteins critical for tumor cell survival and proliferation. - **Bortezomib** is a reversible inhibitor of the **26S proteasome**, resulting in disruption of targeted protein degradation, induction of apoptosis, and inhibition of myeloma cell growth. - **Dexamethasone** is a synthetic glucocorticoid, exerting anti-inflammatory and anti-myeloma effects through glucocorticoid receptor–mediated transcriptional modulation. - The combination was designed to exploit potential synergistic effects: Hsp90 inhibition may sensitize myeloma cells to proteasome inhibitors, and corticosteroids further enhance cytotoxic response. - The regimen has been investigated in phase I-Ib/II studies for safety and efficacy in multiple myeloma but was not brought to approval and clinical development has been **terminated**[1][4][5].

Brand names
Luminespib
Other names
NVP-AUY922NVP-AUY-922NVP-AUY 922
02

Targets

HSP90AA1 (Heat shock protein HSP90-alpha)PSMB5 (Proteasome subunit beta Type-5)GR (Glucocorticoid receptor)

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