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|LOXO292|LOXO 292 | RET Inhibitor 40 | 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 V804M RET G810C RET M918T | Advanced Solid Tumor | resistant | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing RET V804M, G810C, and M918T were resistant to Retevmo (selpercatinib) treatment in culture (PMID: 33161056). | 33161056 |
| RET V804M RET M918T | Advanced Solid Tumor | sensitive | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Retevmo (selpercatinib) inhibited cell growth and Ret phosphorylation in transformed cells expressing RET V804M and M918T in culture (PMID: 33161056). | 33161056 |
| RET V804L | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a Phase I/II trial (LIBRETTO-001), Retevmo (selpercatinib) treatment resulted in an objective response in three patients (3/5) and stable disease in two patients (2/5) with medullary thyroid cancer harboring RET V804L or RET V804M who had been treated previously (PMID: 32846061; NCT03157128). | 32846061 |
| RET V804M RET G810S RET L881V RET M918T | thyroid gland medullary carcinoma | predicted - resistant | Selpercatinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with hereditary medullary thyroid carcinoma harboring germline RET M918T demonstrated disease progression following an initial response to Retevmo (selpercatinib), and ctDNA sequencing revealed a decrease in RET L881V, but an increase in RET V804M and RET G810S (PMID: 31988000). | 31988000 |
| RET D378_G385delinsE | thyroid gland medullary carcinoma | predicted - sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a clinical case study, a pediatric patient with heavily pretreated medullary thyroid cancer harboring RET D378_G385delinsE achieved a partial response after 8 weeks of Retevmo (selpercatinib) treatment, with an 86% reduction in tumor size after 40 weeks, and remained progression-free after 27 months (PMID: 32923911; NCT03157128). | 32923911 |
| RET fusion | thyroid gland follicular carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines for patients with follicular thyroid carcinoma harboring RET fusions (NCCN.org). | detail... |
| RET fusion | thyroid gland papillary carcinoma | 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 fusion | thyroid gland papillary carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines for patients with papillary thyroid carcinoma harboring RET fusions (NCCN.org). | 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 79% (15/19), including one complete and 14 partial responses, with a median response duration of 18.4 months, and median progression-free survival of 20.1 months in adult and pediatric patients 12 years and older with RET fusion-positive thyroid cancer who were previously treated (PMID: 32846061; NCT03157128). | detail... 32846061 |
| RET fusion | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines for patients with medullary thyroid carcinoma harboring RET fusions (NCCN.org). | detail... |
| RET fusion | thyroid gland anaplastic carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines for patients with anaplastic thyroid carcinoma harboring RET fusions (NCCN.org). | detail... |
| RET fusion | Erdheim-Chester disease | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring RET fusions (NCCN Guidelines). | 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 fusion | thyroid gland Hurthle cell carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is included in guidelines for patients with thyroid Hurthle cell carcinoma harboring RET fusions (NCCN.org). | detail... |
| 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 patient harboring RET V804M (J Clin Oncol 36, 2018 (suppl; abstr 102); NCT03157128). | detail... |
| RET V804M | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a Phase I/II trial (LIBRETTO-001), Retevmo (selpercatinib) treatment resulted in an objective response in three patients (3/5) and stable disease in two patients (2/5) with medullary thyroid cancer harboring RET V804M or RET V804L who were previously treated (PMID: 32846061; NCT03157128). | detail... 32846061 |
| RET M918T | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a clinical case study, a pediatric patient with previously treated metastatic medullary thyroid cancer harboring germ line RET M918T mutation achieved stable disease and remained on treatment after 5.2 months with Retevmo (selpercatinib) therapy (PMID: 32923911). | 32923911 |
| 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 M918T | thyroid gland medullary carcinoma | sensitive | Selpercatinib | Case Reports/Case Series | Actionable | In a clinical case study, Retevmo (selpercatinib) treatment resulted in rapid clinical improvement and complete resolution of the brain metastasis in a patient with metastatic medullary thyroid carcinoma harboring RET M918T whose disease progressed on prior Cometriq (cabozantinib) treatment, an official partial extracranial response was achieved at 1 year of treatment, until disease progression at 17 months (PMID: 33154983). | 33154983 |
| 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 M918T | Advanced Solid Tumor | sensitive | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, Retevmo (selpercatinib) inhibited cell growth and Ret phosphorylation in transformed cells expressing RET M918T in culture (PMID: 33161056). | 33161056 |
| RET V804M RET G810S RET M918T | Advanced Solid Tumor | resistant | Selpercatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing RET V804M, G810S, and M918T were resistant to Retevmo (selpercatinib) treatment in culture (PMID: 33161056). | 33161056 |
| RET rearrange | lung non-small cell carcinoma | sensitive | Selpercatinib | Guideline | Actionable | Retevmo (selpercatinib) is in guidelines for non-small cell lung cancer patients with RET rearrangements (NCCN.org). | 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 (ORR) of 64% (64/105) in patients with RET fusion-positive non-small cell lung cancer, with a median duration of response of 17.5 months, ORR was 85% (33/39) and 91% (10/11) in previously treated patients and patients with measurable CNS metastasis, respectively (PMID: 32846060; NCT03157128). | detail... 32846060 |
| 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 (ORR) of 69% (38/55), with five complete and 33 partial responses, in adult and pediatric patients of 12 years and older with medullary thyroid cancer harboring RET mutations who were previously treated, while patients who had not been previously treated demonstrated an ORR of 73% (64/88), with ten complete and 54 partial responses (PMID: 32846061; NCT03157128). | detail... 32846061 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04819100 | Phase III | Selpercatinib | A Study of Selpercatinib After Surgery or Radiation in Participants With Non-Small Cell Lung Cancer (NSCLC) (LIBRETTO-432) | Recruiting | USA | CAN | 29 |
| 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) | Recruiting | USA | CAN | 14 |
| NCT04268550 | Phase II | Selpercatinib | Targeted Treatment for RET Fusion-Positive Advanced Non-Small Cell Lung Cancer (A LUNG-MAP Treatment Trial) | Recruiting | USA | 0 |
| 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 | USA | CAN | 8 |
| NCT04759911 | Phase II | Selpercatinib | Selpercatinib Before Surgery for the Treatment of RET-Altered Thyroid Cancer | Recruiting | USA | 0 |
| NCT03906331 | Expanded access | Selpercatinib | Expanded Access for the Treatment of Cancers With Rearranged During Transfection (RET) Activation | Available | USA | 12 |
| NCT04320888 | Phase II | Selpercatinib | Selpercatinib for the Treatment of Advanced Solid Tumors, Lymphomas, or Histiocytic Disorders With Activating RET Gene Alterations, a Pediatric MATCH Treatment Trial | Recruiting | USA | 1 |
| NCT04211337 | Phase III | Vandetanib Cabozantinib Selpercatinib | A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer (LIBRETTO-531) | Recruiting | USA | CAN | 19 |
| NCT04194944 | Phase III | Cisplatin + Pemetrexed Disodium Carboplatin + Pemetrexed Disodium Selpercatinib Carboplatin + Pembrolizumab + Pemetrexed Disodium Cisplatin + Pembrolizumab + Pemetrexed Disodium | A Study of Selpercatinib (LY3527723) in Participants With Advanced or Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer (LIBRETTO-431) | Recruiting | CAN | 25 |
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