Gleevec
E584150
orphan drug
protein kinase inhibitor
small molecule drug
targeted cancer therapy
tyrosine kinase inhibitor
Gleevec is a groundbreaking targeted cancer therapy, best known for treating chronic myeloid leukemia by inhibiting the BCR-ABL tyrosine kinase.
Statements (60)
| Predicate | Object |
|---|---|
| instanceOf |
orphan drug
ⓘ
protein kinase inhibitor ⓘ small molecule drug ⓘ targeted cancer therapy ⓘ tyrosine kinase inhibitor ⓘ |
| approvedForIndication |
KIT-positive gastrointestinal stromal tumor
ⓘ
Philadelphia chromosome–positive acute lymphoblastic leukemia ⓘ Philadelphia chromosome–positive chronic myeloid leukemia ⓘ aggressive systemic mastocytosis with KIT mutation ⓘ chronic eosinophilic leukemia ⓘ chronic myeloid leukemia ⓘ dermatofibrosarcoma protuberans ⓘ gastrointestinal stromal tumor ⓘ hypereosinophilic syndrome ⓘ metastatic dermatofibrosarcoma protuberans ⓘ myelodysplastic/myeloproliferative diseases associated with PDGFR gene rearrangements ⓘ unresectable dermatofibrosarcoma protuberans ⓘ |
| considered | first successful targeted cancer therapy ⓘ |
| developedBy | Novartis NERFINISHED ⓘ |
| discoveredIn | 1990s ⓘ |
| firstApprovedBy | U.S. Food and Drug Administration NERFINISHED ⓘ |
| firstApprovedYear | 2001 ⓘ |
| hasAdministrationFrequency | once daily ⓘ |
| hasATCCode | L01EA01 ⓘ |
| hasBrandName | Glivec NERFINISHED ⓘ |
| hasChemicalClass | phenylaminopyrimidine derivative ⓘ |
| hasCommonSideEffect |
diarrhea
ⓘ
edema ⓘ fatigue ⓘ fluid retention ⓘ muscle cramps ⓘ nausea ⓘ rash ⓘ vomiting ⓘ |
| hasDosageForm | tablet ⓘ |
| hasGenericName | imatinib mesylate ⓘ |
| hasInternationalNonproprietaryName | imatinib ⓘ |
| hasLegalStatusInEU | prescription only ⓘ |
| hasLegalStatusInUS | prescription only ⓘ |
| hasMechanismOfAction |
BCR-ABL tyrosine kinase inhibition
ⓘ
KIT (CD117) tyrosine kinase inhibition ⓘ PDGFR tyrosine kinase inhibition ⓘ |
| hasMolecularTargetType | oncogenic fusion protein ⓘ |
| hasPregnancyCategoryUS | D ⓘ |
| hasPrimaryMolecularTarget | BCR-ABL1 fusion protein NERFINISHED ⓘ |
| hasRouteOfAdministration | oral ⓘ |
| isInhibitorOf |
CYP2C9
ⓘ
CYP2D6 NERFINISHED ⓘ CYP3A4 NERFINISHED ⓘ |
| isSubstrateOf | CYP3A4 NERFINISHED ⓘ |
| metabolizedBy |
CYP2C9
NERFINISHED
ⓘ
CYP2D6 NERFINISHED ⓘ CYP3A4 NERFINISHED ⓘ |
| targetsProtein |
ABL1
NERFINISHED
ⓘ
BCR-ABL NERFINISHED ⓘ KIT NERFINISHED ⓘ PDGFRα ⓘ PDGFRβ NERFINISHED ⓘ |
| usedAs |
first-line therapy for chronic-phase CML
ⓘ
second-line therapy for interferon-resistant CML ⓘ |
Referenced by (1)
Full triples — surface form annotated when it differs from this entity's canonical label.