Our pipeline
Our Pipeline
HER2, including oncogenic mutations
ENT-H1 is a highly potent and irreversible tyrosine kinase inhibitor (TKI) that selectively targets HER2 and HER2 mutants, while sparing EGFR. Amplification and mutations of HER2 drive a wide range of human cancers. HER2 TKIs have had limited success due to a compensatory mechanism that increases the required therapeutic index beyond that of available pan-ERBB and HER2 inhibitors.
ENT-H1 exhibits over 1000-fold selectivity against EGFR, favorable PK and safety profiles, preferential tumor enrichment, and effective CNS penetrance. Together these make ENT-H1 a breakthrough molecule for realizing the full therapeutic potential of inhibiting HER2 signaling, while avoiding EGFR-driven toxicity. In vivo, ENT-H1 has demonstrated favorable efficacy and tolerability across a range of HER2 tumor models, including intracranial models, outperforming benchmark TKIs and antibody-drug conjugates (ADCs).
A multi-center Phase I trial is scheduled to commence patient dosing in early 2024.
Challenging kinase selectivity profile
Non-kinase target
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Effector protein
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Our mission is to maximize positive impact on patient health
Unmet clinical need
Quality of the drug
Speed to approval
