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ICTP-101

Development stage
Preclinical
Lead developer
InnoCure Therapeutics
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

ICTP-101 is an orally bioavailable proteolysis-targeting chimera (PROTAC) developed by InnoCure Therapeutics for the treatment of solid tumors, specifically non-small cell lung cancer (NSCLC) and gastric cancer. Utilizing InnoCure's proprietary MILPROTAC (Minimizing Linker PROTAC) technology platform, the drug is designed to overcome the common challenges of oral absorption associated with traditional PROTAC molecules. ICTP-101 functions by inducing the degradation of the hepatocyte growth factor receptor (c-MET). It consists of a c-MET-targeting moiety linked to a cereblon (CRBN) binding moiety, which recruits the E3 ubiquitin ligase complex to ubiquitinate and subsequently degrade c-MET via the proteasome. The candidate is intended for patients with c-MET amplification or overexpression and is also being explored as a combination strategy to address resistance to EGFR or MET tyrosine kinase inhibitors.

02

Targets

MET (Mesenchymal-epithelial transition factor receptor)CRBN (Cereblon)

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