Drug intelligence / Profile preview

FAR09

Development stage
Preclinical
Lead developer
Indian Institute of Technology, Madras
Modality
Small Molecules
01

Overview

FAR09 is an experimental small molecule androgen receptor (AR) antagonist. It belongs to a series of 4,4-dimethylimidazolidin-2-one pharmacophore-based compounds (FAR01-FAR11) designed as flexible analogs of the second-generation AR antagonist enzalutamide. In these molecules, the rigid thiohydantoin ring found in enzalutamide is replaced by a more flexible 4,4-dimethylimidazolidin-2-one moiety, and a methylene group is introduced between the pharmacophore and one of the aromatic rings to further enhance flexibility. FAR09 was developed to target AR signaling, which is a fundamental driver of tumour growth in prostate cancer, including castration-resistant prostate cancer (CRPC). The compound has been evaluated in vitro using the androgen-dependent LNCaP prostate cancer cell line to assess its potential as a therapeutic agent for androgen deprivation therapy (ADT).

02

Targets

AR (Adrenergic receptors)

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