TKI Product Portfolio



Third-generation BCR-ABL inhibitor
(has been approved in November 2021)

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

Developed by Ascentage Pharma with support from the National Major New Drug Discovery and Manufacturing program, the orally active, third-generation BCR-ABL inhibitor olverembatinib is the first China-approved third-generation BCR-ABL inhibitor targeting drug-resistant  chronic myeloid leukemia (CML). Olverembatinib can effectively target a spectrum of BCR-ABL mutants, including the T315I mutation.

In October 2020, olverembatinib was granted the Priority Review status by the Center for Drug Evaluation (CDE) in China for the treatment of adult patients resistant to TKIs and with T315I-mutant chronic phase CML (CML-CP) and accelerated phase CML (CML-AP). In March 2021, it was granted the Breakthrough Therapy designation by the CDE. In overseas, olverembatinib was cleared by the US FDA in July 2019 to directly enter a Phase Ib study. In May 2020, olverembatinib was sequentially granted an Orphan Drug designation and Fast Track designation by the US FDA. In November 2021, olverembatinib was granted an Orphan Designation by the European Union. Furthermore, since 2018, the clinical results of olverembatinib have been selected for oral presentations at the American Society of Hematology (ASH) Annual Meetings for four consecutive years, and was nominated for “Best of ASH” in 2019. (Olverembatinib has not been approved for any indication in the US.)

In July 2021, Ascentage Pharma and Innovent Biologics (1801.HK) reached the agreement regarding the joint development and commercialization of olverembatinib in China.



FAK/ROS1/ALK inhibitor

APG-2449 is a potent, orally bioavailable inhibitor of the focal adhesion kinase, or FAK, ROS1 and anaplastic lymphoma kinase, or ALK, kinases, which we are developing for the treatment of cancer. APG-2449 has demonstrated antitumor activity in multiple xenograft tumor models. Studies in preclinical tumor models have shown that APG-2449 overcomes the drug resistance to the first generation ALK inhibitors, and exhibits synergistic effects with EGFR inhibitors (especially the newly approved third generation AZD9291/osimertinib) in an EGFRT790M mutant NSCLC xenograft tumor model. We filed an IND application for APG-2449 in China in October 2018, which was approved in December 2018.



c-Met selective inhibitor

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.