Drug intelligence / Profile preview

C-14207

Development stage
Preclinical
Lead developer
Cyrus Therapeutics
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

C-14207 is a novel, orally bioavailable molecular glue degrader (MGD) targeting the translation termination factor GSPT1 (G1 to S phase transition 1). Developed by Cyrus Therapeutics, the compound functions by hijacking the Cereblon (CRBN) E3 ubiquitin ligase to induce the rapid and potent proteasomal degradation of GSPT1. This degradation leads to dysregulated protein translation termination, activation of the integrated stress response, and subsequent TP53-independent apoptosis. C-14207 has demonstrated significant preclinical anti-tumor activity in models of acute myeloid leukemia (AML) and MYC-driven solid tumors, including non-small cell lung cancer (NSCLC). It is characterized by a favorable rodent pharmacokinetic profile and a safer toxicity profile in normal cells compared to earlier generations of GSPT1 degraders.

02

Targets

CRBN (Cereblon)GSPT1 (G1 to S phase transition 1)

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