Delving into the Latest Updates on ASR-600 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

AR

Mechanism

AR antagonists(Androgen Receptor antagonists)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic Cancer

Inactive Indication-

Originator Organization

University of Louisville

Active Organization

The Pennsylvania State University

University of Louisville

The University of Texas System

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

We investigated the efficacy of a small molecule ASR-600, an analog of Urolithin A (Uro A), on blocking androgen receptor (AR) and its splice variant AR-variant 7 (AR-V7) signaling in castration-resistant prostate cancer (CRPC). ASR-600 effectively suppressed the growth of AR⁺ CRPC cells by inhibiting AR and AR-V7 expressions; no effect was seen in AR^- CRPC and normal prostate epithelial cells. Biomolecular interaction assays revealed ASR-600 binds to the N-terminal domain of AR, which was further confirmed by immunoblot and subcellular localization studies. Molecular studies suggested that ASR-600 promotes the ubiquitination of AR and AR-V7 resulting in the inhibition of AR signaling. Microsomal and plasma stability studies suggest that ASR-600 is stable, and its oral administration inhibits tumor growth in CRPC xenografted castrated and non-castrated mice. In conclusion, our data suggest that ASR-600 enhances AR ubiquitination in both AR⁺ and AR-V7 CRPC cells and inhibits their growth in vitro and in vivo models.

100 Deals associated with ASR-600

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Cancer	Preclinical	US	The University of Texas System	-
Prostatic Cancer	Preclinical	US	The Pennsylvania State University	-
Prostatic Cancer	Preclinical	US	University of Louisville	-