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 |
|---|---|---|---|---|---|---|---|
| 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 |
| 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 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... |
| 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 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 |
| 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 | 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 |
| 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 |
| 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 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 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 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 |
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- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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