Delving into the Latest Updates on ARD-1693 with Synapse

Overview

Basic Info

Drug Type

Proteolysis-targeting chimeras (PROTAC)

Synonyms

Target

AR

Action

degraders

Mechanism

AR degraders(Androgen Receptor degraders)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic Cancer

Inactive Indication-

Originator Organization

University of Michigan

Active Organization

University of MichiganOncopia Therapeutics, Inc.

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC45H48ClN7O5

InChIKeyAWHKRHYGENDDAD-YNWFVEANSA-N

CAS Registry2632305-94-1

Author: Han, Xin ; Xu, Tianfeng ; Wang, Shaomeng ; Mckean, Robert ; Kirchhoff, Paul D. ; Qin, Chong ; Takyi-Williams, John ; Sun, Duxin ; McEachern, Donna ; Zhao, Lijie ; Xiang, Weiguo ; Bai, Longchuan ; Miao, Bukeyan ; Lu, Jianfeng ; Kregel, Steven ; Wen, Bo ; Wang, Mi ; Wang, Lu ; Ator, Mark ; Chinnaiyan, Arul M. ; Wang, Mingliang ; Yang, Chao-Yie

We report herein the discovery and extensive characterization of ARD-1676, a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR).ARD-1676 was designed using a new class of AR ligands and a novel cereblon ligand.It has DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, resp., and IC50 values of 11.5 and 2.8 nM in VCaP and LNCaP cell lines, resp.ARD-1676 effectively induces degradation of a broad panel of clin. relevant AR mutants.ARD-1676 has an oral bioavailability of 67, 44, 31, and 99% in mice, rats, dogs, and monkeys, resp.Oral administration of ARD-1676 effectively reduces the level of AR protein in the VCaP tumor tissue in mice and inhibits tumor growth in the VCaP mouse xenograft tumor model without any sign of toxicity.ARD-1676 is a highly promising development candidate for the treatment of AR+ human prostate cancer.

100 Deals associated with ARD-1693

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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	United States	Oncopia Therapeutics, Inc.	08 Sep 2023
Prostatic Cancer	Preclinical	United States	University of Michigan	08 Sep 2023