Drug intelligence / Profile preview

TTI-2341

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

TTI-2341 is a second-generation, brain-penetrant, covalent small molecule inhibitor of the epidermal growth factor receptor (EGFR). Developed by Trillium Therapeutics (acquired by Pfizer), it is designed to target both wild-type and mutant forms of EGFR, including the resistance-associated L858R and T790M variants. The compound is specifically engineered for high central nervous system (CNS) penetration, demonstrating superior oral bioavailability (86%) and significantly higher brain exposure compared to earlier inhibitors like afatinib. It is primarily being investigated for the treatment of glioblastoma multiforme (GBM) and brain metastases originating from non-small cell lung cancer (NSCLC).

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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