larotrectinib

E561035

Larotrectinib is a targeted cancer therapy that selectively inhibits TRK fusion proteins and is used to treat solid tumors harboring NTRK gene fusions regardless of tumor site.

All labels observed (1)

Label Occurrences
larotrectinib canonical 7

How this entity was disambiguated

Statements (49)

Predicate Object
instanceOf breakthrough therapy ⓘ
orphan drug ⓘ
small molecule drug ⓘ
targeted cancer therapy ⓘ
tyrosine kinase inhibitor ⓘ
approvedBy European Medicines Agency ⓘ
U.S. Food and Drug Administration ⓘ
blackBoxWarning no boxed warning in U.S. labeling as of initial approval ⓘ
coDeveloper Bayer ⓘ
commonAdverseEffect dizziness ⓘ
fatigue ⓘ
increased liver enzymes ⓘ
nausea ⓘ
vomiting ⓘ
developer Loxo Oncology ⓘ
dosageForm oral capsules ⓘ
oral solution ⓘ
eliminationRoute feces ⓘ
urine ⓘ
firstFDAApprovalDate 2018-11 ⓘ
hasATCCode L01EX09 ⓘ
hasCASNumber 1223405-08-0 ⓘ
hasClinicalTrial NCT02122913 ⓘ
NCT02576431 ⓘ
NCT02637687 ⓘ
hasINN larotrectinib ⓘ
hasIUPACName (3R)-N-{5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyridin-3-yl}-3-(1H-1,2,4-triazol-1-yl)pyrrolidine-1-carboxamide ⓘ
hasMolecularFormula C21H22F2N6O ⓘ
hasMolecularWeight molar mass about 380.4 g/mol ⓘ
hasTradeName Vitrakvi ⓘ
indication treatment of metastatic solid tumors with NTRK gene fusions ⓘ
treatment of solid tumors with NTRK gene fusions ⓘ
treatment of unresectable solid tumors with NTRK gene fusions ⓘ
tumor-agnostic cancer therapy for NTRK fusion–positive tumors ⓘ
isTumorAgnostic true ⓘ
legalStatusEU prescription only ⓘ
legalStatusUS prescription only ⓘ
mechanismOfAction selective inhibitor of tropomyosin receptor kinase (TRK) fusion proteins ⓘ
metabolism primarily metabolized by CYP3A4 ⓘ
pregnancyCategory can cause fetal harm based on mechanism and animal data ⓘ
requiresBiomarker NTRK gene fusion ⓘ
routeOfAdministration oral ⓘ
selectivity highly selective for TRK over other kinases ⓘ
targets NTRK1 gene fusion proteins ⓘ
NTRK2 gene fusion proteins ⓘ
NTRK3 gene fusion proteins ⓘ
TRKA ⓘ
TRKB ⓘ
TRKC ⓘ

How these facts were elicited

Referenced by (7)

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

Loxo Oncology → developedDrug → larotrectinib ⓘ
subject linked to: Loxo Oncology (acquired)
Loxo Oncology → leadProduct → larotrectinib ⓘ
subject linked to: Loxo Oncology (acquired)
Loxo Oncology → notableDrugCandidate → larotrectinib ⓘ
subject linked to: LOXO
larotrectinib → hasINN → larotrectinib ⓘ
Vitrakvi → hasActiveIngredient → larotrectinib ⓘ
LOXO-195 → predecessorDrug → larotrectinib ⓘ