Drug intelligence / Profile preview

ezatiostat

Development stage
Phase 2
Lead developer
Telik
Modality
Peptides, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Ezatiostat is a small molecule peptidomimetic inhibitor of glutathione S-transferase P1-1 (GSTP1-1), designed to stimulate hematopoiesis by promoting the formation and differentiation of bone marrow progenitor cells into granulocytes, monocytes, erythrocytes, and platelets. It acts intracellularly on the MAPK signaling pathway by activating ERK2 and disrupting GSTP1–1 interactions with JNK1. Ezatiostat has demonstrated myelostimulant activity in preclinical models and human bone marrow cultures. It is being investigated primarily for the treatment of myelodysplastic syndrome (MDS), a condition characterized by insufficient production of blood cells due to dysfunctional bone marrow. The drug may also have potential as an adjunct therapy to counteract cytopenias caused by chemotherapy[1][2][4][5].

Brand names
Telintra
Other names
gamma-Glutamyl-S-(benzyl)-cysteinyl-R(-)-phenylglycine diethyl esterezatiostat hydrochloride
02

Targets

GSTP1 (Glutathione S-transferase P)

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