Therapy Detail
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| Therapy Name | Selpercatinib |
| Synonyms | |
| Therapy Description |
Selpercatinib (LOXO-292) is an inhibitor of RET that specifically targets RET mutations and fusions, and may block the growth of cells with Ret activity (PMID: 29860229). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Selpercatinib | Retevmo | LOXO-292 | RET Inhibitor 39 | Retevmo (selpercatinib) is an inhibitor of RET that specifically targets RET mutations and fusions, and may block the growth of cells with increased Ret activity (PMID: 29860229). Retevmo (selpercatinib) is FDA approved for use in patients with metastatic non-small cell lung cancer harboring RET fusions, and in adult and pediatric patient of 12 years and older with RET-mutant medullary thyroid cancer or RET fusion-positive thyroid cancer refractory to radioactive iodine (FDA.org). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| RET fusion | thyroid gland papillary carcinoma | predicted - sensitive | Selpercatinib | Phase I | Actionable | In a Phase I trial, Retevmo (selpercatinib) treatment resulted in an objective response rate of 83% (5/6) in RET fusion-positive papillary thyroid cancer patients (J Clin Oncol 36, 2018 (suppl; abstr 102); NCT03157128). | detail... |
| RET M918T | Advanced Solid Tumor | sensitive | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing RET M918T were sensitive to treatment with Retevmo (selpercatinib) in culture, demonstrating decreased cell proliferation (PMID: 29912274). | 29912274 |
| RET V804M RET M918T | thyroid gland medullary carcinoma | predicted - sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with thyroid medullary cancer harboring RET M918T and RET V804M demonstrated an initial response to Retevmo (selpercatinib), which included a decrease in allelic fraction of RET M918T and RET V804M over 8 weeks and a radiographic response of nearly 54% post 6.9 months of treatment (PMID: 29912274; NCT03157128). | 29912274 |
| RET M918T | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, thyroid medullary carcinoma cells harboring RET M918T were sensitive to treatment with Retevmo (selpercatinib) in culture, demonstrating decreased cell proliferation (PMID: 29912274). | 29912274 |
| RET V804M | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Phase I | Actionable | In a Phase I trial, Retevmo (selpercatinib) treatment resulted in partial response in a thyroid medullary cancer patientharboring RET V804M (J Clin Oncol 36, 2018 (suppl; abstr 102); NCT03157128). | detail... |
| RET fusion | thyroid gland cancer | sensitive | Selpercatinib | FDA approved | Actionable | In a Phase I/II trial (LIBRETTO-001) that supported FDA approval, Retevmo (selpercatinib) treatment resulted in an objective response rate of 62% (16/26) in adult and pediatric patients of 12 years and older with RET fusion-positive thyroid cancer refractory to radio-iodine therapy (Ann Oncol, Oct 2019, 30 (Suppl 5): v933, Abstract LBA93; NCT03157128). | detail... detail... |
| RET C634W | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, thyroid medullary carcinoma cells harboring RET C634W were sensitive to treatment with Retevmo (selpercatinib), demonstrating decreased cell proliferation in culture and inhibition of tumor growth in cell line xenograft models (PMID: 29912274). | 29912274 |
| RET mutant | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Phase I | Actionable | In a Phase I trial, Retevmo (selpercatinib) treatment resulted in partial response in 14% (2/14) and tumor reduction in 79% (11/14) of RET mutant thyroid medullary cancer patients (J Clin Oncol 36, 2018 (suppl; abstr 102); NCT03157128). | detail... |
| RET mutant | thyroid gland medullary carcinoma | sensitive | Selpercatinib | FDA approved | Actionable | In a Phase I/II trial (LIBRETTO-001) that supported FDA approval, Retevmo (selpercatinib) treatment resulted in an objective response rate of 56% (31/55) in adult and pediatric patients of 12 years and older with medullary thyroid cancer harboring RET mutations (Ann Oncol, Oct 2019, 30 (Suppl 5): v933, Abstract LBA93; NCT03157128). | detail... detail... |
| RET fusion | lung non-small cell carcinoma | sensitive | Selpercatinib | FDA approved | Actionable | In a Phase I/II trial (LIBRETTO-001) that supported FDA approval, Retevmo (selpercatinib) treatment resulted in an objective response rate of 68% (71/105) in patients with RET fusion-positive non-small cell lung cancer (IASLC 2019 World Conference on Lung Cancer, Sep 2019, abstract# PL02.08; NCT03157128). | detail... detail... detail... |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| NCT03899792 | Phase Ib/II | Selpercatinib | A Study of Oral LOXO-292 in Pediatric Patients With Advanced Solid or Primary Central Nervous System Tumors (LIBRETTO-121) | Recruiting |
| NCT04211337 | Phase III | Vandetanib Cabozantinib Selpercatinib | A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer (LIBRETTO-531) | Recruiting |
| NCT04268550 | Phase II | Selpercatinib | Targeted Treatment for RET Fusion-Positive Advanced Non-Small Cell Lung Cancer (A LUNG-MAP Treatment Trial) | Recruiting |
| NCT04194944 | Phase III | Cisplatin + Pemetrexed Carboplatin + Pemetrexed Selpercatinib Carboplatin + Pembrolizumab + Pemetrexed Cisplatin + Pembrolizumab + Pemetrexed | A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer (LIBRETTO-431) | Recruiting |
| NCT03157128 | Phase Ib/II | Selpercatinib | Phase 1/2 Study of LOXO-292 in Patients With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRETTO-001)ET Activation (LIBRETTO-001)er | Recruiting |
| NCT03906331 | Expanded access | Selpercatinib | Expanded Access for the Treatment of Cancers With Rearranged During Transfection (RET) Activation | Available |
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