larotrectinib
E561035
breakthrough therapy
orphan drug
small molecule drug
targeted cancer therapy
tyrosine kinase inhibitor
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.
Statements (49)
| Predicate | Object |
|---|---|
| instanceOf |
breakthrough therapy
ⓘ
orphan drug ⓘ small molecule drug ⓘ targeted cancer therapy ⓘ tyrosine kinase inhibitor ⓘ |
| approvedBy |
European Medicines Agency
NERFINISHED
ⓘ
U.S. Food and Drug Administration NERFINISHED ⓘ |
| blackBoxWarning | no boxed warning in U.S. labeling as of initial approval ⓘ |
| coDeveloper | Bayer NERFINISHED ⓘ |
| commonAdverseEffect |
dizziness
ⓘ
fatigue ⓘ increased liver enzymes ⓘ nausea ⓘ vomiting ⓘ |
| developer | Loxo Oncology NERFINISHED ⓘ |
| dosageForm |
oral capsules
ⓘ
oral solution ⓘ |
| eliminationRoute |
feces
ⓘ
urine ⓘ |
| firstFDAApprovalDate | 2018-11 ⓘ |
| hasATCCode | L01EX09 ⓘ |
| hasCASNumber | 1223405-08-0 ⓘ |
| hasClinicalTrial |
NCT02122913
ⓘ
NCT02576431 ⓘ NCT02637687 ⓘ |
| hasINN | larotrectinib NERFINISHED ⓘ |
| 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 NERFINISHED ⓘ |
| 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 NERFINISHED ⓘ TRKC NERFINISHED ⓘ |
Referenced by (2)
Full triples — surface form annotated when it differs from this entity's canonical label.
subject surface form:
Loxo Oncology
subject surface form:
Loxo Oncology