Therapy Detail
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| Therapy Name | APS03118 |
| Synonyms | |
| Therapy Description |
APS03118 is a RET inhibitor with activity against RET fusions and gatekeeper mutations, potentially inhibiting phosphorylation, proliferation, and tumor growth (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| APS03118 | APS 03118|APS-03118 | RET Inhibitor 54 | APS03118 is a RET inhibitor with activity against RET fusions and gatekeeper mutations, potentially inhibiting phosphorylation, proliferation, and tumor growth (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| RET G810S | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Cell culture | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET G810S in an in vitro assay and inhibited proliferation of cells expressing RET G810S in culture (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET G810C | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Biochemical | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET G810C in an in vitro assay (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET V804E | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Biochemical | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET V804E in an in vitro assay (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET V804L | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Biochemical | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET V804L in an in vitro assay (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET C634W | thyroid cancer | predicted - sensitive | APS03118 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, APS03118 treatment inhibited proliferation of a thyroid cancer cell line harboring RET C634W in culture and inhibited tumor growth in a xenograft model (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET V804M | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Biochemical | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET V804M in an in vitro assay, inhibited Ret phosphorylation in cells expressing RET V804M in culture, and inhibited tumor growth in cell line xenograft models expressing RET V804M (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET G810R | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Cell culture | Actionable | In a preclinical study, APS03118 inhibited the enzymatic activity of RET G810R in an in vitro assay and inhibited Ret phosphorylation and proliferation of cells expressing RET G810R in culture (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
| RET fusion | lung non-small cell carcinoma | predicted - sensitive | APS03118 | Phase I | Actionable | In a Phase I trial, treatment with APS03118 demonstrated manageable safety and resulted in an objective response rate of 80% (20/22) and median progression-free survival not reached in treatment-naive non-small cell lung cancer patients harboring RET fusions, an ORR of 55% in patients with prior systemic therapy, and an ORR of 23% in patients with prior selective RET inhibitor treatment without known bypass mutations (J Clin Oncol 44: 16_Suppl, 8617; NCT05653869). | detail... |
| RET M918T | Advanced Solid Tumor | predicted - sensitive | APS03118 | Preclinical - Biochemical | Actionable | In a preclinical study, APS03118 treatment inhibited Ret phosphorylation in cells expressing RET M918T in culture (J Clin Oncol 40, no. 16_suppl (June 1, 2022)). | detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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