Drug information of Nilotinib
Nilotinib is a cancer medication that interferes with the growth and spread of cancer cells in the body. Nilotinib is used to treat a type of blood cancer called Philadelphia chromosome positive chronic myeloid leukemia (CML). Nilotinib is usually given after other medications have been tried without success.
Mechanism of effect
Binds to and stabilizes th.e inactive conformation of the kinase domain of Abl protein
Nilotinib is a transduction inhibitor that targets BCR-ABL, c-kit and PDGF, for the potential treatment of various leukemias, including chronic myeloid leukemia (CML)
C max is reached 3 h after oral administration. Steady state is reached in approximately 8 days. Bioavailability is increased when given with a meal. Compared with fasting, the AUC is increased by 82% when given 30 min after a high-fat meal. Serum protein binding is approximately 98%. The main metabolic pathways are oxidation and hydroxylation. The metabolites are inactive Elimination half-life is approximately 17 h. Approximately 93% of the administered dose is eliminated in feces within 7 days
Drug indicationsPh+ CML
Adults PO 400 mg twice daily for resistant or intolerant CML; 300 mg twice daily for newly diagnosed CML
Side effectsMigraine , nausea , Headache , insomnia , chest pain , Dermatit , dry mouth , constipation , abdominal pain , decreased appetite , dizziness , vomiting , fatigue , Blurred vision , Hepatic dysfunction , rash , flushing , Bradycardia , Depression , Diarrhea , Dyspnea , asthenia , Night sweats , urticaria , pruritus , Hypertension , Throat irritation , thrombocytopenia , neutropenia , lymphopenia , anemia , Erythema , cardiac arrhythmias , palpitations , paresthesia , acne , dyspepsia , Urinary tract infection , edema , Peripheral edema , Cough , Hyperthyroidism , hypothyroidism , weight decrease , myalgia , Hypomagnesemia , Bone pain , blood in stool , Alopecia , anorexia , malaise , conjunctivitis , Gynecomastia , gastritis , hyperlipidemia , Arthralgia , pain in the extremities , back pain , Upper respiratory tract infection , Tremor , Hyper-cholesteremia , Hyperkalemia , Hypokalemia , Hyperglycemia , Hypocalcemia , hemorrhage , stomatitis , dry eyes , Nasopharyngitis , eye irritation , hypercalcemia , hyponatremia , pneumonia , upper stomach pain , acute pancreatitis , ECG prolonged QT , coronary artery disease, , cyanosis , hematoma , hypertensive crisis , pericardial effusion , disturbance in attention , jaundice , diabetes mellitus
InteractionsErgotamine-C , Esomeprazole , Ipratropium bromide , Ifosfamide , Budesonide , Promethazine , Primidone , Pantoprazole , Tamsulosin , Trastuzumab , Topotecan , Daunorubicin , Domperidone , Rabeprazole , Salbutamol , Fluticasone propinate , Glibenclamide , Lansoprazole , Aluminium gel , Amiodarone , Itraconazole , Imatinib , Doxepin , Cimetidine , Quinidine , Midazolam , Hydroxychloroquine , Voriconazole , Ketoconazole , Clarithromycin , Clozapine , Sotalol , Phenobarbital , Phenytoin , Lithium carbonate , Maprotiline , Moxifloxacin , Carbamazepine , Disulfiram , Bisoprolol , Rifabutin , Ranolazine , Toremifene , Prochlorperazine , Histrelin , ISOPROTERENOL , ritonavir , mitotane , Dolasetron , Palonosetron , vandetanib , Droperidol , sparfloxacin , Procainamide , Mefloquine , Indapamide , Dofetilide , Inotuzumab , Promazine , Vasopressin , Arsenic trioxide , Halofantrine , Grepafloxacin , Mibefradil , cobicistat , Delavirdine , Terfenadine , Abarelix , Asenapine , Alfuzosin , Pazopanib , Perflutren , Pimavanserin , Dexlansoprazole , lenvatinib , Apalutamide , Edoxaban , Pitolisant , Entrectinib , Lorlatinib , gilteritinib , glasdegib , riociguat , oleandomycin , Bepridil , bedaquiline , Gefitinib , Dasatinib , Gemtuzumab , Remdesivir , lasmiditan , vemurafenib , Meningococcal conjugate vaccine , Fidaxomicin , Halaven
1-QT interval prolongation and sudden deaths have been reported. 2- Do not use nilotinib in patients with hypokalemia, hypomagnesemia, or long QT syndrome. Correct hypokalemia and hypomagnesemia prior to starting therapy and monitor serum levels periodically. 3-Avoid drugs known to prolong the QT interval and strong CYP3A4 inhibitors. Patients should avoid food 2 h before and 1 h after taking a dose. 4- A dose reduction is recommended in patients with hepatic impairment. Obtain ECGs at baseline, 7 days after initiation, and periodically thereafter, as well as following any dose adjustments
Points of recommendation
• For oral use only. Capsules should be swallowed whole with water only. • Do not administer with food. Food should not be consumed for at least 2 h before or at least 1 h after a dose is taken. • Administer twice daily at approximately 12-h intervals. • May be given in combination with hematopoietic growth factors, such as erythropoietin or granulocyte colony-stimulating factor, or with hydroxyurea or anagrelide if clinically indicated. • For patients who are unable to swallow capsules, the contents of each capsule may be dispersed in 1 tsp of applesauce (pureed apple). The mixture should be taken immediately (within 15 min) and should not be stored for future use.