Drug intelligence / Profile preview

ezatiostat + lenalidomide

Development stage
Unknown
Lead developer
Telik
Modality
Small Molecules
Administration
Oral
01

Overview

**Ezatiostat + lenalidomide** is an investigational oral combination therapy composed of ezatiostat, a small molecule glutathione S-transferase P1-1 (GSTP1-1) inhibitor, and lenalidomide, an immunomodulatory agent. Ezatiostat promotes maturation of hematopoietic progenitors and induces apoptosis in malignant cells by inhibiting GSTP1-1, while lenalidomide modulates the immune microenvironment, inhibits angiogenesis, and exerts direct antineoplastic effects. The combination has been evaluated in phase 1 clinical trials for patients with non-deletion(5q) low to intermediate-1 risk myelodysplastic syndrome (MDS), showing tolerability and promising multilineage hematopoietic responses. The rationale is to leverage ezatiostat’s non-myelosuppressive stimulatory effects and lenalidomide’s established efficacy in MDS, potentially improving cytopenias and transfusion independence while maintaining manageable toxicity[1][2][4]. The combination regimen may also be considered for other hematologic malignancies responsive to lenalidomide[2].

Brand names
Telintra + Revlimid
Other names
ezatiostat plus lenalidomideezatiostat hydrochloride plus lenalidomide
02

Targets

CK1α (Casein kinase I alpha)GSTP1 (Glutathione S-transferase P)CRBN (Cereblon)IKZF3 (Zinc finger protein Aiolos)IKZF1 (Ikaros family zinc finger protein 1)

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