Drug intelligence / Profile preview

ricolinostat + lenalidomide + dexamethasone

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

Overview

This drug is a combination therapy consisting of **ricolinostat** (ACY-1215), **lenalidomide**, and **dexamethasone**, investigated primarily for the treatment of relapsed or refractory multiple myeloma. \n- **Ricolinostat** is an oral, selective inhibitor of histone deacetylase 6 (HDAC6) with minimal class I HDAC activity. It disrupts protein homeostasis in malignant plasma cells by inhibiting HDAC6, facilitating the accumulation of acetylated tubulin, impairing aggresome function, and potentiating antimyeloma effects. \n- **Lenalidomide** is an immunomodulatory drug (IMiD) that acts through multiple mechanisms, including direct cytotoxicity, modulation of the immune response (enhancing T cell and NK cell activation), and inhibition of angiogenesis, primarily by modulating cereblon-mediated ubiquitin ligase activity and resulting in the degradation of transcription factors critical for myeloma survival. \n- **Dexamethasone** is a synthetic glucocorticoid corticosteroid that exhibits anti-inflammatory and cytotoxic effects on malignant plasma cells by modulating gene transcription via the glucocorticoid receptor. \nThis three-drug regimen has shown synergistic activity and enhanced efficacy compared to two-drug combinations in clinical studies for multiple myeloma. The combination is currently being evaluated in clinical trials, with selected dosing regimens for ricolinostat established based on phase 1b data[1][3][5].

Other names
ricolinostat + lenalidomide + dexamethasone
02

Targets

HDAC6 (Histone deacetylase 6)GR (Glucocorticoid receptor)CRBN (Cereblon)

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