Selpercatinib

Drug

Also known as: LOXO-292, Retevmo

Drug Profile

Selpercatinib is marketed as RETEVMO, a selective RET-targeted kinase inhibitor indicated across RET fusion-positive NSCLC, RET-mutant medullary thyroid cancer, RET fusion-positive thyroid cancer, and other RET fusion-positive solid tumors. Labeling includes both adult and pediatric indications for patients aged 2 years and older in several settings. U.S. initial approval was in 2020.

Drug Class
RET-targeted kinase inhibitor
Approval Status
FDA approved (Initial U.S. Approval: 2020; some solid tumor indication under accelerated approval)
Mechanism of Action
Inhibits wild-type and mutated RET isoforms (with additional kinase activity against VEGFR1/3 and FGFR1-3 at higher concentrations), suppressing RET-driven oncogenic signaling.
Brand Names
  • RETEVMO
Indications
  • \Locally advanced or metastatic RET fusion-positive NSCLC in adults\
  • \Advanced or metastatic RET-mutant medullary thyroid cancer in adults and pediatric patients >=2 years requiring systemic therapy\
  • \Advanced or metastatic RET fusion-positive thyroid cancer in adults and pediatric patients >=2 years requiring systemic therapy and radioactive iodine-refractory (if appropriate)\
  • \Locally advanced or metastatic RET fusion-positive solid tumors in adults and pediatric patients >=2 years after prior systemic treatment progression or no satisfactory alternatives\

Related News

Related Clinical Trials

NCT ID Title Status Phase
NCT07543887

Selpercatinib and Body Composition

COMPLETED
NCT07146893

Feasibility Study for Repurposing RET Inhibitors

NOT_YET_RECRUITING EARLY_PHASE1
NCT07010393

Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study

NOT_YET_RECRUITING PHASE4
NCT06532149

ERectile Dysfunctions, gOnadotoxicity and Sexual Health Assessment in Men With Lung Cancer

RECRUITING
NCT05906836

A Drug Drug Interaction (DDI) Study of Selpercatinib (LY3527723) and Rosuvastatin in Healthy Participants

COMPLETED PHASE1
NCT05668962

Restor. I-131 Upt. + Selpercatinib in RET F-P RAI-R TC

RECRUITING PHASE2
NCT05630287

A Study of Absorption, Metabolism, Excretion, and Absolute Bioavailability of Carbon-14-Labelled [14C] Selpercatinib (LY3527723) in Healthy Male Participants

COMPLETED PHASE1
NCT05630274

A Study of Effect of Selpercatinib (LY3527723) on Corrected QT (QTc) Interval in Healthy Participants

COMPLETED PHASE1
NCT05469113

A Study of Effects of Selpercatinib (LY3527723) on Repaglinide in Healthy Participants

COMPLETED PHASE1
NCT05469100

A Study of Effect of Selpercatinib (LY3527723) in Participants With Normal and Impaired Renal Function

COMPLETED PHASE1