Therapy Detail

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Therapy Name APG-2449
Synonyms
Therapy Description

APG-2449 is a multikinase inhibitor with activity against ALK, ROS1, and FAK, which potentially reduces tumor growth (PMID: 35820889).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
APG-2449 APG2449|APG 2449 ALK Inhibitor 32 FAK inhibitor 15 ROS1 Inhibitor 20 APG-2449 is a multikinase inhibitor with activity against ALK, ROS1, and FAK, which potentially reduces tumor growth (PMID: 35820889).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ALK G1202R Advanced Solid Tumor predicted - sensitive APG-2449 Preclinical - Biochemical Actionable In a preclinical study, APG-2449 inhibited the kinase activity of ALK G1202R in culture (PMID: 35820889). 35820889
ALK L1196M Advanced Solid Tumor predicted - sensitive APG-2449 Preclinical - Biochemical Actionable In a preclinical study, APG-2449 inhibited the kinase activity of ALK L1196M in culture (PMID: 35820889). 35820889
ALK S1206Y Advanced Solid Tumor predicted - sensitive APG-2449 Preclinical - Biochemical Actionable In a preclinical study, APG-2449 inhibited the kinase activity of ALK S1206Y in culture (PMID: 35820889). 35820889
EML4 - ALK lung non-small cell carcinoma sensitive APG-2449 Preclinical - Cell line xenograft Actionable In a preclinical study, APG-2449 inhibited proliferation of non-small cell lung cancer cell lines harboring EML4-ALK in culture and resulted in dose-dependent antitumor activity in a cell line xenograft model (PMID: 35820889). 35820889
ALK fusion lung non-small cell carcinoma predicted - sensitive APG-2449 Phase I Actionable In a Phase I trial, APG-2449 treatment was well tolerated and resulted in preliminary efficacy with 4 partial responses among 14 patients with non-small cell lung cancer harboring an ALK fusion who previously progressed on a second-generation ALK inhibitor, 1 intracranial complete response and 3 partial responses among 8 patients with brain metastases, and an overall response rate of 80% and a disease control rate of 100% among 10 TKI-naive patients (J Clin Oncol 40, no. 16_suppl (June 01, 2022) 9071-9071). detail...
EML4 - ALK ALK I1171T Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell culture Actionable In a preclinical study, APG-2449 inhibited proliferation of cells expressing EML4-ALK with ALK I1171T in culture (PMID: 35820889). 35820889
EML4 - ALK ALK F1174L Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell culture Actionable In a preclinical study, APG-2449 inhibited proliferation of a cell line expressing EML4-ALK with ALK F1174L in culture (PMID: 35820889). 35820889
EML4 - ALK ALK L1196M Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell line xenograft Actionable In a preclinical study, APG-2449 inhibited tumor growth in a cell line xenograft model expressing EML4-ALK with ALK L1196M (PMID: 35820889). 35820889
EML4 - ALK ALK G1202R Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell line xenograft Actionable In a preclinical study, APG-2449 inhibited tumor growth of a cell line xenograft model expressing EML4-ALK with ALK G1202R (PMID: 35820889). 35820889
ALK G1269A Advanced Solid Tumor predicted - sensitive APG-2449 Preclinical - Biochemical Actionable In a preclinical study, APG-2449 inhibited the kinase activity of ALK G1269A in culture (PMID: 35820889). 35820889
EML4 - ALK ALK R1275Q Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell culture Actionable In a preclinical study, APG-2449 inhibited proliferation of cells expressing EML4-ALK with ALK R1275Q in culture (PMID: 35820889). 35820889
EML4 - ALK Advanced Solid Tumor sensitive APG-2449 Preclinical - Cell culture Actionable In a preclinical study, APG-2449 inhibited proliferation of cells expressing EML4-ALK in culture (PMID: 35820889). 35820889

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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