Olafertinib: An Oral, Third Generation, Irreversible Kinase Inhibitor

Olafertinib (CK-101) is an investigational oral, third-generation, irreversible kinase inhibitor against selective mutations of epidermal growth factor receptor (EGFR). Activating mutations in the tyrosine kinase domain of EGFR are found in approximately 20% of patients with advanced NSCLC.

Third-generation EGFR inhibitors are designed to be highly selective against one or more EGFR activating mutations and the T790M resistance mutation with minimal inhibition of wild-type EGFR, thereby potentially improving tolerability and safety profiles. In March 2015, we entered into an exclusive license agreement with NeuPharma, Inc. to develop and commercialize novel covalent third-generation EGFR inhibitors on a worldwide basis outside of certain Asian countries.

We believe that Olafertinib has the potential to be effective as a monotherapy or in combination with other anti-tumor immune response potentiating compounds, such as cosibelimab. NeuPharma commenced a Phase 3 clinical trial in China evaluating Olafertinib in treatment-naïve locally advanced or metastatic NSCLC patients whose tumors have an EGFR activating mutation.