Drug intelligence / Profile preview

VLX1570 + dexamethasone

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

Overview

VLX1570 + dexamethasone is an investigational drug combination studied primarily for the treatment of relapsed or refractory multiple myeloma. VLX1570 is a small molecule inhibitor targeting the deubiquitinases USP14 and UCHL5, which are components of the 19S regulatory subunit of the proteasome. By inhibiting these enzymes, VLX1570 disrupts protein degradation, leading to accumulation of polyubiquitylated proteins, induction of unfolded protein response (UPR), tumor cell apoptosis, and inhibition of tumor growth. Dexamethasone is a synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties that is commonly used in cancer regimens to reduce inflammation and manage side effects. The combination has been evaluated in phase 1/2 clinical trials for safety and efficacy in patients with multiple myeloma[1][2][3][5][6].

02

Targets

GR (Glucocorticoid receptor)UCHL5 (Ubiquitin carboxyl-terminal hydrolase isozyme L5)USP14 (Ubiquitin carboxyl-terminal hydrolase 14)

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