Drug intelligence / Profile preview

CFT8919

Development stage
Phase 1
Lead developer
C4 Therapeutics, Inc.
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

CFT8919 is an orally bioavailable allosteric BiDAC™ degrader designed to be potent and selective against the epidermal growth factor receptor (EGFR) bearing the oncogenic L858R mutation. This small molecule functions as a proteolysis-targeting chimera (PROTAC), inducing targeted degradation of mutant EGFR proteins in non-small cell lung cancer (NSCLC). Preclinical studies demonstrate that CFT8919 degrades and inhibits mutant EGFR—including resistance-associated mutations such as T790M and C797S—resulting in significant tumor regression, including intracranial activity. The drug is being developed for patients with advanced or metastatic NSCLC harboring EGFR-L858R mutations, particularly those who have failed standard treatments or developed resistance to approved EGFR inhibitors[1][2][5][6][7][10].

02

Targets

EGFR L858R (Epidermal growth factor receptor L858R mutant)

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