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Therapy Name Selpercatinib
Synonyms
Therapy Description

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 locally advanced or metastatic non-small cell lung cancer harboring RET fusions, and in adult and pediatric patients of 12 years and older with RET-mutant medullary thyroid cancer or RET fusion-positive thyroid cancer refractory to radioactive iodine, and in patients with advanced or metastatic solid tumor harboring RET fusions (FDA.org).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Selpercatinib Retevmo LOXO-292|LOXO292|LOXO 292|Retsevmo RET Inhibitor 52 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 locally advanced or metastatic non-small cell lung cancer harboring RET fusions, and in adult and pediatric patients of 12 years and older with RET-mutant medullary thyroid cancer or RET fusion-positive thyroid cancer refractory to radioactive iodine, and in patients with advanced or metastatic solid tumor harboring RET fusions (FDA.org).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
RET rearrange lung non-small cell carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is in guidelines as a first-line and subsequent therapy for patients with advanced or metastatic non-small cell lung cancer harboring RET rearrangements (NCCN.org). detail...
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 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 fusion colon cancer sensitive Selpercatinib Case Reports/Case Series Actionable In a Phase I/II trial (LIBRETTO-001), Retevmo (selpercatinib) treatment resulted in an objective response rate (ORR) of 43.9% (18/41, 2 complete responses, 16 partial responses) with a median duration of response (mDOR) of 24.5 months in patients with RET fusion-positive advanced or metastatic solid tumors, and ORR and mDOR in patients with colon cancer were 20.0% (2/10) and 9.4 months, respectively (PMID: 36108661; NCT03157128). 36108661
RET fusion colon cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with metastatic colon cancer harboring RET fusions (NCCN.org). detail...
RET fusion Adenocarcinoma of Unknown Primary sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with adenocarcinoma of unknown primary harboring RET fusions (NCCN.org). detail...
RET T930P Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited growth of transformed cells expressing RET T930P in culture (PMID: 32284345). 32284345
RET D571N Advanced Solid Tumor sensitive Selpercatinib Preclinical - Biochemical Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling in transformed cells expressing RET D571N in culture (PMID: 36166639). 36166639
RET fusion small intestine adenocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with metastatic small bowel adenocarcinoma with RET fusion (NCCN.org). detail...
RET fusion thyroid cancer sensitive Selpercatinib FDA approved - On Companion Diagnostic 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... detail... 32846061
RET V804M RET Y806C Advanced Solid Tumor decreased response Selpercatinib Preclinical - Biochemical Actionable In a preclinical study, transformed human cells expressing RET V804M and Y806C in cis were less sensitive to Retevmo (selpercatinib) in culture (PMID: 35304457). 35304457
RET fusion ovary epithelial cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as systemic therapy for patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer harboring a RET fusion (NCCN.org). detail...
RET D584N Advanced Solid Tumor sensitive Selpercatinib Preclinical - Biochemical Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling in transformed cells expressing RET D584N in culture (PMID: 36166639). 36166639
RET fusion stomach cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with unresectable locally advanced, recurrent, or metastatic gastric cancer harboring RET fusion (NCCN.org). (NCCN.org). detail...
RET E632_L633del thyroid gland medullary carcinoma conflicting Selpercatinib Case Reports/Case Series Actionable In a clinical case study, Retevmo (selpercatinib) treatment resulted in limited activity in a patient with medullary thyroid carcinoma harboring RET E632_L633del, with a partial response achieved at cycle 9 but significant progressive disease observed at cycle 13 (PMID: 36416226; NCT03157128). 36416226
RET E632_L633del thyroid gland medullary carcinoma conflicting Selpercatinib Case Reports/Case Series Actionable In a Phase I trial, Retevmo (selpercatinib) resulted in a partial response in the target lesions and stable disease in the non-target lesions in a patient with sporadic medullary thyroid cancer harboring RET E632_L633del, and treatment continued for at least 17 months (PMID: 35616103; NCT03906331). 35616103
RET fusion intrahepatic cholangiocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as primary (category 2B) and subsequent-line therapy for patients with unresectable or metastatic biliary tract cancer harboring RET fusions, including intrahepatic cholangiocarcinoma (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 V804M RET Y806C RET M918T Advanced Solid Tumor predicted - resistant Selpercatinib Preclinical - Biochemical Actionable In a preclinical study, transformed human cells expressing RET M918T, V804M, and Y806C in cis were resistant to Retevmo (selpercatinib) in culture (PMID: 35304457). 35304457
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 fusion extrahepatic bile duct carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as primary (category 2B) and subsequent-line therapy for patients with unresectable or metastatic biliary tract cancer harboring RET fusions, including extrahepatic cholangiocarcinoma (NCCN.org). detail...
RET D898_E901del thyroid gland medullary carcinoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a Phase I/II trial (LIBRETTO-001), Retevmo (selpercatinib) treatment resulted in a clinical response after one month, with a partial response in liver lesions and abdominal lymph nodes that was maintained for 24 months, in a patient with metastatic medullary thyroid carcinoma harboring RET D898_E901del (PMID: 38438731; NCT03157128). 38438731
RET D898_E901del thyroid gland medullary carcinoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a clinical case study, Retevmo (selpercatinib) treatment resulted in a 61% reduction in the sum of the diameters of the target lesions in a patient with metastatic medullary thyroid carcinoma harboring RET D898_E901del, with treatment lasting 1 year (PMID: 37535881). 37535881
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 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 Erk phosphorylation and growth of transformed cells expressing RET M918T in culture (PMID: 32284345). 32284345
RET M918T Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET M918T in culture (PMID: 36166639). 36166639
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 vaginal carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with recurrent or metastatic vaginal squamous cell carcinoma or adenocarcinoma harboring an RET fusion (NCCN.org). detail...
RET G810N RET M918T thyroid gland medullary carcinoma predicted - resistant Selpercatinib Case Reports/Case Series Actionable In a retrospective analysis, a medullary thyroid carcinoma patient harboring RET M918T progressed on treatment with Retevmo (selpercatinib) and was found to have acquired RET G810N (PMID: 38127829; NCT03157128, NCT03037385, NCT03780517). 38127829
RET fusion sarcoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as first-line therapy for patients with advanced or metastatic soft tissue sarcoma harboring RET fusions (NCCN.org). detail...
RET E574D Advanced Solid Tumor sensitive Selpercatinib Preclinical - Biochemical Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling in transformed cells expressing RET E574D in culture (PMID: 36166639). 36166639
RET fusion ampulla of Vater adenocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as first-line or subsequent therapy for patients with metastatic ampullary adenocarcinoma harboring RET fusions (NCCN.org). detail...
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 fusion cervical cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with cervical cancer harboring RET fusions (NCCN.org). 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 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 Advanced Solid Tumor 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 44% (18/41, 2 complete responses, 16 partial responses), a clinical benefit rate of 63% (26/41), a median duration of response of 24.5 months, and a median progression-free survival of 13.2 months in patients with RET fusion-positive advanced solid tumors (PMID: 36108661; NCT03157128). 36108661 detail...
RET C620R Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET C620R in culture (PMID: 36166639). 36166639
RET D898_E901del Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret phosphorylation and proliferation in a transformed cell line expressing RET D898_E901del in culture (PMID: 37535881). 37535881
RET D898_E901del Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Erk phosphorylation and growth of transformed cells expressing RET D898_E901del in culture (PMID: 32284345). 32284345
RET amp lung non-small cell carcinoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a clinical case study, Retevmo (selpercatinib) treatment resulted in a complete response in the axillary lymph node and a partial response in the brain metastases in a patient with RET-amplified (CN=28) non-small cell lung cancer (PMID: 37972337). 37972337
RET fusion lung non-small cell carcinoma sensitive Selpercatinib FDA approved - On Companion Diagnostic 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 detail...
RET fusion lung non-small cell carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as a first-line therapy for patients with metastatic non-small cell lung cancer harboring RET fusions (PMID: 36872130; ESMO.org). 36872130 detail...
RET D631_L633delinsE Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET D631_L633delinsE in culture (PMID: 36166639). 36166639
RET D567N Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling and viability in transformed cells expressing RET D567N in culture and inhibited tumor growth in a cell line xenograft model (PMID: 36166639). 36166639
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 esophagus adenocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic esophageal adenocarcinoma harboring RET fusions (NCCN.org). detail...
RET D631Y Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET D631Y in culture (PMID: 36166639). 36166639
RET G607C Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET G607C in culture (PMID: 36166639). 36166639
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 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 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 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 fusion cholangiocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as primary (category 2B) or subsequent-line therapy (category 2A) for patients with unresectable or metastatic cholangiocarcinoma harboring RET fusions (NCCN.org). detail...
RET D631_L633delinsS thyroid gland medullary carcinoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a Phase I trial, Retevmo (selpercatinib) resulted in stable disease in the target lesions and a partial response in the non-target lesions in a patient with sporadic medullary thyroid cancer harboring RET D631_L633delinsS (PMID: 35616103; NCT03906331). 35616103
RET mutant thyroid gland medullary carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for adult or pediatric patients 12 years or older with advanced medullary thyroid gland carcinoma harboring RET mutations (PMID: 31549998, PMID: 35491008; ESMO.org). 31549998 detail... 35491008
RET mutant thyroid gland medullary carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with medullary thyroid carcinoma harboring RET mutations (NCCN.org). 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 (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... detail... 32846061
RET amp glioblastoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a clinical case study, Retevmo (selpercatinib) treatment resulted in a partial response in a patient with glioblastoma harboring RET amplification along with MDM2 and CDK4 amplification and an ATM splice mutation, who stayed on treatment for 8 months until disease progression (PMID: 36075388). 36075388
RET fusion esophagus squamous cell carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic esophageal squamous cell carcinoma harboring RET fusions (NCCN.org). detail...
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 Y806C RET M918T thyroid gland medullary carcinoma predicted - resistant Selpercatinib Case Reports/Case Series Actionable In a retrospective analysis, a medullary thyroid carcinoma patient harboring RET M918T progressed on treatment with Retevmo (selpercatinib) and was found to have acquired RET Y806C (PMID: 38127829; NCT03157128, NCT03037385, NCT03780517). 38127829
RET fusion gallbladder cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as primary (category 2B) and subsequent-line therapy for patients with unresectable or metastatic biliary tract cancer harboring RET fusions, including gallbladder cancer (NCCN.org). detail...
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 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.org). detail...
RET D567Y Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling and viability in transformed cells expressing RET D567Y in culture and inhibited tumor growth in a cell line xenograft model (PMID: 36166639). 36166639
RET fusion differentiated thyroid gland carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with advanced or metastatic differentiated thyroid gland carcinoma harboring RET fusions (PMID: 31549998, PMID: 35491008; ESMO.org). 35491008 31549998 detail...
RET fusion salivary gland cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with recurrent, unresectable, or metastatic salivary gland tumors harboring RET fusions (NCCN.org). detail...
RET C620Y lung small cell carcinoma predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a clinical case study, Retevmo (selpercatinib) treatment resulted in a partial response with rapid clinical improvement and shrinkage of brain, skin, and muscle metastases in a patient with small cell lung cancer harboring RET C620Y who remained on treatment after 6 months (PMID: 37922409). 37922409
RET fusion pancreatic adenocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as first-line or subsequent therapy for patients with locally advanced, metastatic, or recurrent pancreatic adenocarcinoma harboring RET fusions (NCCN.org). detail...
RET fusion gastroesophageal junction adenocarcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as second-line or subsequent therapy for patients with locally advanced, recurrent, or metastatic gastroesophageal junction adenocarcinoma harboring RET fusions (NCCN.org). detail...
RET fusion Squamous Cell Carcinoma of Unknown Primary sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with squamous cell carcinoma of unknown primary harboring RET fusions (NCCN.org). detail...
RET fusion pancreatic cancer predicted - sensitive Selpercatinib Case Reports/Case Series Actionable In a Phase I/II trial (LIBRETTO-001), Retevmo (selpercatinib) treatment resulted in an objective response rate (ORR) of 43.9% (18/41, 2 complete responses, 16 partial responses) with a median duration of response (mDOR) of 24.5 months in patients with RET fusion-positive advanced or metastatic solid tumors, and ORR and mDOR in patients with pancreatic cancer were 54.5% (6/11) and not reached, respectively (PMID: 36108661; NCT03157128). 36108661
RET fusion rectum cancer sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with metastatic rectum cancer harboring RET fusion (NCCN.org). detail...
RET C634R Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret phosphorylation and proliferation in a transformed cell line expressing RET C634R in culture (PMID: 37535881). 37535881
RET C634R Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Retevmo (selpercatinib) inhibited Ret signaling and viability in transformed cells expressing RET C634R in culture and inhibited tumor growth in a cell line xenograft model (PMID: 36166639). 36166639
RET T930K Advanced Solid Tumor sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited growth of transformed cells expressing RET T930K in culture (PMID: 32284345). 32284345
RET V804M RET M918T Advanced Solid Tumor predicted - 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 over exp pulmonary neuroendocrine tumor predicted - sensitive Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited proliferation of a lung neuroendocrine tumor cell line with high RET expression in 3D spheroid culture (Cancer Res (2023) 83 (7_Supplement): 4039). detail...
RET fusion neuroendocrine tumor sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines for patients with unresectable or metastatic extrapulmonary poorly differentiated neuroendocrine carcinoma, large or small cell carcinoma, or mixed neuroendocrine/non-neuroendocrine neoplasms harboring RET fusions who have progressed on or following prior treatment (NCCN.org). detail...
RET E632_L633del Advanced Solid Tumor conflicting Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, a cell line expressing RET E632_L633del was less sensitive to Retevmo (selpercatinib) than cells expressing wild-type RET in culture (PMID: 36416226). 36416226
RET E632_L633del Advanced Solid Tumor conflicting Selpercatinib Preclinical - Cell culture Actionable In a preclinical study, Retevmo (selpercatinib) inhibited viability in transformed cells expressing RET E632_L633del in culture (PMID: 36166639). 36166639
RET fusion hepatocellular carcinoma sensitive Selpercatinib Guideline Actionable Retevmo (selpercatinib) is included in guidelines as subsequent-line therapy (category 2B) for patients with hepatocellular carcinoma harboring RET fusions (NCCN.org). 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 V804M thyroid gland medullary carcinoma sensitive Selpercatinib Case Reports/Case Series 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...

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT03906331 Expanded access Selpercatinib Expanded Access for the Treatment of Cancers With Rearranged During Transfection (RET) Activation Available USA | NZL | ITA | FRA | ESP | DEU | AUS 5
NCT02925234 Phase II Palbociclib Ribociclib Lenvatinib Ipilimumab + Nivolumab Trametinib Crizotinib Niraparib Selpercatinib Olaparib Erlotinib Erdafitinib Dabrafenib Dacomitinib Rucaparib Axitinib Panitumumab Pemigatinib Durvalumab Afatinib Entrectinib Tepotinib Alpelisib Atezolizumab + Bevacizumab Alectinib Regorafenib Cobimetinib + Vemurafenib Nilotinib Vismodegib Abemaciclib Sunitinib Nivolumab Cabozantinib Lorlatinib Talazoparib Dabrafenib + Trametinib Pembrolizumab Pertuzumab + Trastuzumab The Drug Rediscovery Protocol (DRUP Trial) (DRUP) Recruiting NLD 0
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 | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUT | AUS 21
NCT05668962 Phase II Selpercatinib Restor. I-131 Upt. + Selpercatinib in RET F-P RAI-R TC Recruiting USA 0
NCT04211337 Phase III Vandetanib Cabozantinib Selpercatinib A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer (LIBRETTO-531) Active, not recruiting USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS 11
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) Active, not recruiting NLD | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS 17
NCT04268550 Phase II Selpercatinib Targeted Treatment for RET Fusion-Positive Advanced Non-Small Cell Lung Cancer (A LUNG-MAP Treatment Trial) Active, not recruiting USA 0
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 Active, not recruiting USA | AUS 1
NCT03899792 Phase Ib/II Selpercatinib A Study of Oral LOXO-292 (Selpercatinib) in Pediatric Participants With Advanced Solid or Primary Central Nervous System (CNS) Tumors (LIBRETTO-121) Recruiting USA | ITA | GBR | FRA | ESP | DEU | CAN | AUS 3
NCT04759911 Phase II Selpercatinib Selpercatinib Before Surgery for the Treatment of RET-Altered Thyroid Cancer Recruiting USA 0
NCT03157128 Phase Ib/II Selpercatinib A Study of Selpercatinib (LOXO-292) in Participants With Advanced Solid Tumors, RET Fusion-Positive Solid Tumors, and Medullary Thyroid Cancer (LIBRETTO-001) (LIBRETTO-001) Recruiting USA | ITA | GBR | FRA | ESP | DEU | CAN | AUS 8


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