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Therapy Name	Zeteletinib
Synonyms
Therapy Description	Zeteletinib (DS-5010) is a multi-kinase inhibitor that inhibits RET and KDR (VEGFR2), which may lead to inhibition of tumor cell growth (Cancer Res 2019;79(13 Suppl):Abstract nr 2199).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
Zeteletinib		DS5010\|DS 5010\|BOS172738\|BOS-172738\|BOS 172738\|DS-5010	RET Inhibitor 53 VEGFR2 Inhibitor 37	Zeteletinib (DS-5010) is a multi-kinase inhibitor that inhibits RET and KDR (VEGFR2), which may lead to inhibition of tumor cell growth (Cancer Res 2019;79(13 Suppl):Abstract nr 2199).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
RET fusion	lung non-small cell carcinoma	predicted - sensitive	Zeteletinib	Phase I	Actionable	In a Phase I trial, Zeteletinib (DS-5010) treatment resulted in an objective response rate (ORR) of 33% (18/54) in patients with RET-altered advanced solid tumors including an ORR of 33% (10/30) in non-small cell lung cancer patients harboring a RET fusion, an ORR of 44% (7/16) in patients with medullary thyroid cancer harboring RET mutations, and a partial response in a pancreatic cancer patient (J Clin Oncol 2021 39: 15_suppl, 3008; NCT03780517).	detail...
RET mutant	medullary thyroid carcinoma	predicted - sensitive	Zeteletinib	Phase I	Actionable	In a Phase I trial, Zeteletinib (DS-5010) treatment resulted in an objective response rate (ORR) of 33% (18/54) in patients with RET-altered advanced solid tumors including an ORR of 33% (10/30) in non-small cell lung cancer patients harboring a RET fusion, an ORR of 44% (7/16) in patients with medullary thyroid cancer harboring RET mutations, and a partial response in a pancreatic cancer patient (J Clin Oncol 2021 39: 15_suppl, 3008; NCT03780517).	detail...
RET fusion	pancreatic cancer	predicted - sensitive	Zeteletinib	Case Reports/Case Series	Actionable	In a Phase I trial, Zeteletinib (DS-5010) treatment resulted in an objective response rate (ORR) of 33% (18/54) in patients with RET-altered advanced solid tumors including an ORR of 33% (10/30) in non-small cell lung cancer patients harboring a RET fusion, an ORR of 44% (7/16) in patients with medullary thyroid cancer harboring RET mutations, and a partial response in a pancreatic cancer patient (J Clin Oncol 2021 39: 15_suppl, 3008; NCT03780517).	detail...
RET G810S	Advanced Solid Tumor	predicted - sensitive	Zeteletinib	Preclinical - Cell culture	Actionable	In a preclinical study, cells expressing RET G810S in the context of KIF5B-RET were sensitive to Zeteletinib (DS-5010) treatment in culture (Cancer Res (2024) 84 (6_Supplement): 5833).	detail...

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT03780517	Phase I	Zeteletinib	Safety, Efficacy, and Tolerability of BOS172738 in Patients With Advanced Rearranged During Transfection (RET) Gene-Altered Tumors	Completed	USA \| FRA \| ESP \| BEL	3

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