APG-2449 is a novel, orally active, multi-targeted tyrosine kinase inhibitor, which inhibits FAK, ALK, and ROS1 with nanomolar potencies. In preclinical studies, APG-2449 demonstrated potent antiproliferative activity in various cancer cell lines as a single agent. In combination treatment, APG-2449 enhanced anti-proliferative activities of several chemotherapeutic and targeted agents. It is indicated that APG-2449 may have a broad therapeutic potential for the treatment of human cancer as a single agent and in combination with other classes of anticancer drugs. APG-2449 is intended for the treatment of patients with advanced solid tumors. Upon completion of the Phase 1 dose escalation study to establish the maximum tolerated dose (MTD), dose-limiting toxicities (DLTs), and/or recommended phase 2 dose (RP2D), several phase Ib/II studies will be implemented accordingly.
Dose exploration stage: non-small cell lung cancer diagnosed by histology and/or cytology and positive for ALK/ROS1 gene fusion (molecular diagnosis confirmed by the investigator) and malignant pleural mesothelioma, esophageal cancer and ovarian cancer. Kind of patients with advanced tumors.
ECOG Performance Status ≤ 1.
Expectation of life ≥ 3 months.
According to RECIST version 1.1, there is at least 1 measurable lesion.
Receiving concurrent anti-cancer therapy (chemotherapy, radiotherapy, immunotherapy, biologic therapy); or any investigational therapy within 28 days prior to the first dose of study drug.
Receiving TKI therapy within 8 days prior to the first dose of study drug.
Continuance of toxicities due to prior therapy that do not recover (CTCAE V5.0 Grade> 1).
Has difficulty in swallowing, absorbing barrier, or other diseases blocking APG-2449' taken.
Sequential
APG-2449
DrugCapsule, multiple dose cohorts, oral administration every day (QD) of a 28-day cycle
Maximum Tolerated Dose (MTD)
To determine the maximum tolerated dose (MTD) of APG-2449 in subjects with advanced solid tumors
Recommended Phase 2 dose (RP2D)
To determine the tentative recommended Phase 2 dose (RP2D) of APG-2449 in subjects with advanced solid tumors
Maximum plasma concentration (Cmax)
Maximum plasma concentration (Cmax) will be assessed on all participants with APG-2449 treatments
Area under the plasma concentration versus time curve (AUC)
Area under the plasma concentration versus time curve (AUC) will be assessed on all participants with APG-2449 treatments
Phosphorylation of FAK protein
Phosphorylation of FAK protein will be assessed in peripheral blood mononuclear cells on all participants with APG-2449 treatments
Preliminary efficacy assessment: Response Evaluation Criteria In Solid Tumors (RECIST) 1.1
To assess preliminary efficacy in subjects with solid tumors using Response Evaluation Criteria In Solid Tumors (RECIST) 1.1
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Ascentage Pharma Group Inc.
Lead sponsor
Suzhou Yasheng Pharmaceutical Co., Ltd.
Collaborator
