Drug intelligence / Profile preview

everolimus + pomalidomide + dexamethasone

Development stage
Discontinued
Lead developer
New Mexico Cancer Research Alliance
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy consists of everolimus, pomalidomide, and dexamethasone, and was evaluated for the treatment of relapsed or refractory multiple myeloma. Everolimus is a small molecule inhibitor of the mechanistic target of rapamycin (mTOR), which plays a key role in regulating cell growth, proliferation, and survival. Pomalidomide is an immunomodulatory imide drug (IMiD) that binds to the cereblon E3 ubiquitin ligase complex, leading to the polyubiquitination and subsequent degradation of the lymphoid transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), which are critical for the survival of myeloma cells. Dexamethasone is a synthetic glucocorticoid that acts as an agonist of the glucocorticoid receptor, inducing anti-inflammatory and pro-apoptotic effects that synergize with pomalidomide. This triplet regimen was studied in a Phase I clinical trial (NCT01889420) sponsored by the New Mexico Cancer Research Alliance to establish safety and dosing in patients with advanced myeloma.

Other names
EPD regimenEverolimus, Pomalidomide, and Dexamethasone combination
02

Targets

GR (Glucocorticoid receptor)CRBN (Cereblon)Mechanistic target of rapamycin complex 1

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