Drug intelligence / Profile preview

AT-IAP

Development stage
Preclinical
Lead developer
Taiho Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

AT-IAP is a non-peptidomimetic, small molecule dual antagonist of cellular inhibitor of apoptosis protein 1 (cIAP1) and X-linked inhibitor of apoptosis protein (XIAP). Developed by Astex Pharmaceuticals using their fragment-based Pyramid™ technology, AT-IAP is designed to lack the traditional alanine-mimetic "warhead" common in many SMAC mimetics. By binding to the BIR domains of IAPs, it promotes the formation of ripoptosome complexes, leading to caspase activation and the induction of apoptosis in cancer cells. Preclinical studies have demonstrated its oral bioavailability and potent antitumor activity in melanoma and breast cancer models, particularly when sensitized by TNF-α.

02

Targets

cIAP1 BIR3 (Cellular inhibitor of apoptosis protein 1 (cIAP1) BIR3 domain)XIAP BIR3 (XIAP BIR3 domain)cIAP2 BIR3 (Cellular inhibitor of apoptosis protein 2 (cIAP2) BIR3 domain)

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