Drug intelligence / Profile preview

tretinoin + carfilzomib + pomalidomide + dexamethasone

Development stage
Unknown
Lead developer
First Affiliated Hospital of Xiamen University
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

All-trans retinoic acid + KPD is an investigational combination regimen consisting of tretinoin (all-trans retinoic acid), carfilzomib, pomalidomide, and dexamethasone. Tretinoin is a vitamin A derivative that acts as a ligand for retinoic acid receptors (RARs), modulating gene expression and down-regulating the interleukin-6 receptor (IL-6R) to inhibit myeloma cell growth. Carfilzomib is a second-generation proteasome inhibitor that irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, leading to the accumulation of ubiquitinated proteins and induction of apoptosis. Pomalidomide is an immunomodulatory imide drug (IMiD) that binds to cereblon, part of the E3 ubiquitin ligase complex, resulting in the degradation of transcription factors such as Ikaros and Aiolos. Dexamethasone is a synthetic corticosteroid with potent anti-inflammatory and immunosuppressive effects. This four-drug combination is being evaluated in Phase 2 clinical trials for the treatment of relapsed or refractory multiple myeloma.

Other names
all-trans retinoic acid + KPDATRA + Carfilzomib + Pomalidomide + Dexamethasoneall-trans retinoic acid + carfilzomib + pomalidomide + dexamethasone
02

Targets

RARA (Retinoic acid receptor alpha)CRBN (Cereblon)PSMB5 (Proteasome subunit beta Type-5)GR (Glucocorticoid receptor)

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