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Selpercatinib · Retevmo, LY-3527723

Small molecule · Inhibitor of RET proto-oncogene receptor tyrosine kinase (RET) · developed by Eli Lilly And Co

Approved FDA, May 2020

LLY Developer

1 Registered trials

What is Selpercatinib?

Selpercatinib is an orally bioavailable kinase inhibitor that binds wild-type RET and mutant and fusion forms of RET, blocking their constitutive activity in tumor cells. It also inhibits VEGFR1, VEGFR3 and FGFR1-3 at higher concentrations. It is studied in thyroid neoplasms and non-small cell lung carcinoma.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as: Retevmo, LY-3527723, LOXO-292
Drug type: Small molecule
Targets: RET proto-oncogene receptor tyrosine kinase (RET), VEGFR1 (FLT1) (FLT1) (secondary target), VEGFR3 (FLT4) (FLT4) (secondary target), FGFR1 (secondary target), FGFR2 (secondary target), FGFR3 (secondary target)
Mechanism: Inhibitor of RET proto-oncogene receptor tyrosine kinase (RET)
Pathways: RET kinase signaling, cell proliferation
Therapy area: Oncology
Developer: Eli Lilly And Co (LLY)
FDA status: Approved as Retevmo (May 8, 2020), NDA213246 · FDA label
UNII: CEGM9YBNGD

✅ FDA-approved uses

Non-small cell lung cancer with RET gene fusion
Medullary thyroid cancer with RET mutation
Thyroid cancer with RET gene fusion
Solid tumors with RET gene fusion

From the indications section of the FDA label (version of Jul 14, 2026). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trial	Phase	Condition	Status	Sponsor
NCT07822880	Phase 4	Thyroid Neoplasms	Not yet recruiting	LLY

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Carcinoma, Non-Small-Cell LungThyroid Neoplasms

Other drugs acting on RET

Regorafenib FDA approved

More from Eli Lilly And Co

Abemaciclib FDA approved Baricitinib FDA approved Donanemab FDA approved Dulaglutide FDA approved Imlunestrant FDA approved Lebrikizumab FDA approved Mirikizumab FDA approved Orforglipron FDA approved Pirtobrutinib FDA approved Tirzepatide FDA approved Brenipatide Phase 3 Clazakizumab Phase 2

Sources

Updated Oct 11, 2026. Something wrong or missing? Report it on the LLY page.

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Data: FDA (Drugs@FDA, Purple Book, DailyMed), NIH (NCI Thesaurus, GSRS, RxNorm), ClinicalTrials.gov • Informational purposes only, not medical or investment advice. • All drugs A–Z