On August 29, 2016 Kadmon Holdings, Inc. (NYSE: KDMN) reported that the first patient has been dosed in a Phase 2 clinical trial of tesevatinib, the Company’s oral tyrosine kinase inhibitor, for the treatment of recurrent glioblastoma (Press release, Kadmon, AUG 29, 2016, View Source [SID:1234514791]). The open-label, multicenter study examines tesevatinib monotherapy administered at 300 mg once daily in up to 40 patients in the United States. Schedule your 30 min Free 1stOncology Demo! Tesevatinib is an oral inhibitor of epidermal growth factor receptor (EGFR), a cell surface receptor whose gene is amplified in more than 50% of gliomas. Unlike other EGFR inhibitors, tesevatinib has been observed in animal models to be highly blood-brain barrier penetrant, reaching equal concentrations in the brain and the blood. Published data have shown that other EGFR inhibitors have poor brain penetration, limiting their ability to reach and effectively treat brain tumors. We believe that tesevatinib may also penetrate the blood-brain barrier in humans, based on initial observations in certain patients exhibiting tumor shrinkage and improvement in neurological symptoms in our ongoing Phase 2 clinical trial in EGFR-mutant non-small cell lung cancer (NSCLC) that has metastasized to the brain. Based on its mechanism of action and brain penetrance, we believe tesevatinib is potentially well suited to treat glioblastoma.
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"We are encouraged by tesevatinib’s potential ability to cross the blood-brain barrier in humans, which may lead to meaningful clinical activity against brain tumors," said Harlan W. Waksal, M.D., President and Chief Executive Officer at Kadmon. "With its potent EGFR inhibition and biodistribution, we believe tesevatinib represents an ideal therapeutic candidate for this difficult-to-treat disease."
In addition to glioblastoma and the ongoing Phase 2 clinical trial in EGFR-mutant NSCLC that has metastasized to the central nervous system (the brain and leptomeninges), Kadmon is developing tesevatinib for the treatment of polycystic kidney disease, a genetic kidney disorder in which EGFR plays a central role.