selpercatinib

E561036

Selpercatinib is a targeted cancer therapy drug that selectively inhibits RET kinase to treat certain RET-altered thyroid and non-small cell lung cancers.

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Statements (47)

Predicate Object
instanceOf RET inhibitor
small molecule drug
targeted cancer therapy
tyrosine kinase inhibitor
approvedBy U.S. Food and Drug Administration NERFINISHED
belongsToChemicalClass small-molecule kinase inhibitors
developedBy Eli Lilly and Company NERFINISHED
firstApprovalYear 2020
firstApprovedIn United States NERFINISHED
hasAdministrationFrequency twice daily in many regimens
hasApprovalType accelerated approval (initial US approval)
hasATCCode L01EX19
hasBlackBoxWarning none (as of initial approval)
hasBrandName Retevmo NERFINISHED
hasCommonAdverseEffect constipation
diarrhea
dry mouth
edema
elevated liver enzymes
fatigue
hypertension
hasDosageForm capsule
hasDrugInteraction strong CYP3A inducers
strong CYP3A inhibitors
hasIndicationPopulation adult patients
pediatric patients 12 years and older
hasINN selpercatinib
hasMechanismOfAction inhibition of RET-mediated signaling pathways
selective RET kinase inhibition
hasMolecularTargetType receptor tyrosine kinase
hasPregnancyRisk may cause fetal harm
hasRouteOfAdministration oral
hasSelectivity highly selective for RET over many other kinases
hasSeriousAdverseEffect QT interval prolongation
hemorrhagic events
hepatotoxicity
interstitial lung disease
hasTarget RET kinase NERFINISHED
rearranged during transfection proto-oncogene
indicatedFor RET fusion-positive non-small cell lung cancer
RET-mutant medullary thyroid carcinoma
advanced RET fusion-positive thyroid cancer
metastatic RET fusion-positive non-small cell lung cancer
metastatic RET-mutant medullary thyroid cancer
isAdministered by mouth
isMetabolizedBy CYP3A4 NERFINISHED
isTakenWithFood may be taken with or without food

Referenced by (2)

Full triples — surface form annotated when it differs from this entity's canonical label.

Loxo Oncology (acquired) developedDrug selpercatinib
subject surface form: Loxo Oncology
Loxo Oncology (acquired) secondMajorProduct selpercatinib
subject surface form: Loxo Oncology