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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