Drug intelligence / Profile preview

EL102

Development stage
Preclinical
Lead developer
Ayala Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

EL102 is a novel, broad-spectrum anti-cancer small molecule originally developed by Elara Pharmaceuticals. Identified through a systems biology approach targeting the hypoxia signaling cascade, EL102 acts as a potent inhibitor of HIF-1α signaling (IC50 ~13 nM). Beyond its effects on hypoxia pathways, the compound functions as an antagonist for several nuclear receptors, including the androgen receptor (AR), progesterone receptor (PR), and estrogen-related receptor alpha (ERRα), as well as the adenosine A3 receptor (ADORA3). Preclinical studies demonstrated significant anti-proliferative and pro-apoptotic activity across a variety of solid and liquid tumor models, including multiple myeloma. EL102 was developed as an oral formulation and was positioned for Phase I clinical entry in 2011.

02

Targets

ADORA3 (Adenosine A3 receptor)AR (Adrenergic receptors)ESRRA (Estrogen-related receptor alpha)HIF1A (Hypoxia-inducible factor 1-alpha)PR (Progesterone receptor)

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