Drug reference

Nilotinib

Tyrosine Kinase Inhibitor · Antineoplastic

Also known as Tasigna, Nilotinib hydrochloride monohydrate

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Manufacturer advises avoid unless potential

FDA category + note

Top interactionssee all 12 →

AbarelixSevereDatabaseDDInter
AbirateroneSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter
AdenosineSevereDatabaseDDInter

Mechanism

Nilotinib inhibits Bcr-Abl tyrosine kinase. It also inhibits other receptor tyrosine kinases, including PDGFR and c-kit.

Indications

Untreated chronic phase Philadelphia-chromosome-positive CML in adultsChronic or accelerated phase Philadelphia-chromosome-positive CML in adults who cannot tolerate imatinib or have imatinib-resistant diseaseCML with resistance to or intolerance of imatinibChronic CML (nonresponsive to imatinib, first line)Accelerated phase of CMLAll phases of CML except blastic phase

Dosing

Adult: accelerated and blast phase Philadelphia-chromosomepositive CML in adults, when: . they have previously been treated with 1 or more tyrosine kinase inhibitor, and . imatinib, nilotinib and dasatinib are not appropriate, and . the manufacturer provides bosutinib with the discount agreed in the patient access scheme.…

Pharmacokinetics

Half-life

about 17 h (plasma)

Bioavailability

approximately 30% (oral); increases significantly with food

Metabolism

CYP3A4

Contraindications

History or risk factors for QT prolongation
Increased risk of bleeding
Patients at high risk of cardiovascular disease
Previous abdominal surgery
Recent history of hollow organ perforation
Impaired wound healing
Concomitant use with Itraconazole

Side effects

Common

FatigueAnorexiaGI symptoms (diarrhea, nausea, vomiting)fluid retentionedemaperiorbital swellingSimilar to imatinibhyperglycemia (10–20%)pruritusskin rasheshyperbilirubinemiaheadaches

Serious

Myelosuppression
QT prolongation
Electrolyte abnormalities (hypophosphatemia, hypokalemia, hypocalcemia, hyponatremia)
Hepatotoxicity
Cardiovascular events
QT interval prolongation
cardiac and vascular events (including ischemia)
Q-T prolongation
diabetes
arterio-occlusive events
pancreatitis (<5%)
cardiovascular complications (10-year cumulative incidence of 25–35%)
vasospastic or vaso-occlusive events