Nilotinib

TASIGNA

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Pronunciation: nye-LOE-ti-nib

Nilotinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Nilotinib ballicule

What it isSecond-generation BCR-ABL inhibitor; chronic myeloid leukemia.

Why this oneDeeper molecular responses than imatinib, which supports attempting treatment-free remission.

What limits itQT prolongation and sudden death, so it must be taken fasting and ECG monitored. Vascular occlusive events; hyperglycemia.

Nilotinib molecular structure (skeletal formula) — Molecular structure: Nilotinib

FDA-approved for

CML (2007)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING QT prolongation and sudden deaths: correct hypokalemia/hypomagnesemia; ECG at baseline, day 7, periodically and after dose changes; do not use with hypokalemia, hypomagnesemia, or long QT; avoid QT-prolonging drugs and strong CYP3A4 inhibitors; no food 2 h before or 1 h after dose.

FDA dosing	Population	Start	Target	Max
Newly diagnosed Ph+ CML, chronic phase	Adults	300 mg BID	300 mg BID	300 mg BID
Ph+ CML-CP/AP resistant or intolerant to prior imatinib	Adults	400 mg BID	400 mg BID	400 mg BID
Newly diagnosed Ph+ CML, chronic phase	Pediatric ≥1 yr	230 mg/m2 BID (rounded to nearest 50 mg)	230 mg/m2 BID (rounded to nearest 50 mg)	400 mg per dose (800 mg/day)
Ph+ CML-CP/AP resistant or intolerant to prior TKI	Pediatric ≥1 yr	230 mg/m2 BID (rounded to nearest 50 mg)	230 mg/m2 BID (rounded to nearest 50 mg)	400 mg per dose (800 mg/day)

Renal Undefined

Hepatic Newly diagnosed CML-CP, any Child-Pugh: 200 mg BID, ↑300 mg BID as tolerated. Resistant/intolerant: mild–moderate 300 mg BID (↑400 mg BID); severe 200 mg BID (↑300 then 400 mg BID). Monitor QT.

ECG at baseline, 7 days after start, and after dose changes. Unavoidable strong CYP3A4 inhibitor: 200 mg QD (newly diagnosed) or 300 mg QD (resistant/intolerant). Treatment-free remission may be considered after ≥3 years with sustained MR4.5.

Instructions

BID ~12 h apart on empty stomach: no food ≥2 h before and ≥1 h after each dose
Swallow capsules whole with water; if unable, disperse contents in 1 teaspoon applesauce and take within 15 minutes
Correct hypokalemia/hypomagnesemia before starting

Available strengths

cap 50, 150, 200 mg
tab 71, 95 mg
ODT 60, 80 mg

Contraindications

Hypokalemia
Hypomagnesemia
Long QT syndrome

Cautions

Myelosuppression
QT prolongation
Sudden deaths
Cardiac and arterial vascular occlusive events
Pancreatitis and elevated serum lipase
Hepatotoxicity
Electrolyte abnormalities
Tumor lysis syndrome
Hemorrhage
Total gastrectomy
Lactose content
Monitoring laboratory tests
Fluid retention
Growth and development effects in pediatrics
Embryo-fetal toxicity
BCR-ABL monitoring after treatment discontinuation

Adverse reactions

Nausea
Rash
Headache
Fatigue
Pruritus
Vomiting
Diarrhea
Cough
Constipation
Arthralgia
Nasopharyngitis, pyrexia, night sweats
Myelosuppression (thrombocytopenia, neutropenia, anemia)

Pregnancy Can cause fetal harm (animal data and mechanism); no human data; advise effective contraception.

Lactation Present in rat milk; do not breastfeed during treatment and for 14 days after the last dose.

Cost

Nilotinib (TASIGNA)

Strength		#/mo	CostPlus
50 mg	cap	60 BID	offered
150 mg	cap	60 BID	offered
200 mg	cap	60 BID	out of stock

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Nilotinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2024

⚠ BOXED WARNING

QT prolongation and sudden death

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades4 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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