TKI Product Portfolio

Indications: chronic myeloid leukemia (CML), gastrointestinal stromal tumors (GIST)

Being developed by Ascentage Pharma, HQP1351 is a novel, orally active, potent third-generation BCR-ABL tyrosine kinase inhibitor (TKI) designed to effectively target a spectrum of BCR-ABL mutants, including T315I, and the first China-developed third-generation BCR-ABL TKI targeting drug-resistant chronic myeloid leukemia (CML). Since 2018, the clinical results of HQP1351 have been selected for oral presentations at American Society of Clinical Oncology (ASCO) Annual Meeting for three years in a row. At present, a New Drug Application (NDA) for HQP1351 has been submitted in China, and the application was subsequently granted the Priority Review status. Moreover, HQP1351 was cleared by the US Food and Drug Administration (FDA) to enter a Phase Ib clinical study, and was subsequently granted an Orphan Drug Designation (ODD) and a Fast Track Designation (FTD) by the US FDA.

HQP8361 is a second-generation targeted c-Met kinase inhibitor being studied for the treatment of gastric cancer, non-small cell lung cancer (NSCLC) and liver cancer. We licensed HQP8361 Asia Pacific market rights from Merck Sharp & Dohme in 2013, which has completed a Phase I clinical trial in the U.S. A total of 47 patients received treatment with HQP8361, and the study results showed the compound is well tolerated and active in patients with advanced cancers. We are currently studying HQP8361 in a Phase I trial in China with advanced solid tumors. We are currently planning a Phase II trial for HQP8361 as a monotherapy in c-Met amplified solid tumors such as NSCLC, gastric cancer and hepatocellular cancer, as well as Phase II combination trials with an EGFR inhibitor in EGFR TKI resistant NSCLC patients.