Table 1.
Characteristics | Imatinib | Dasatinib | Nilotinib | Bosutinib | Ponatinib | Radotinib |
---|---|---|---|---|---|---|
Tab strength | 100 mg,400 mg | 20 mg,50 mg, 70 mg, | 50 mg,150 mg,200 mg | 100 mg, | 15 mg, 45 mg | 100 mg, |
80 mg,100 mg, 140 mg | 500 mg | 200 mg | ||||
Adult dose | ||||||
CML-CP | 400 mg OD | 100 mg OD | 300 mg BD | 500 mg OD | 45 mg OD | 300 mg BD |
CML-AP | 400 mg BD | 140 mg OD | 400 mg BD | 500 mg OD | Approved for T315I mutation | 400 mg BD |
CML-BC | 400 mg BD | 140 mg OD | 400 mg BD | 500 mg OD | 400 mg BD | |
Pediatric Dose | Not approved | Not approved | Not approved | |||
CML-CP | 340 mg/sqm OD | 60 mg/sqm OD | 230 mg/sqm BD | |||
CML-AP | 400 mg/sqmOD | 80 mg/sqm OD | 230 mg/sqm BD | |||
CML-BC | 500 mg/sqmOD | 80 mg/sqm OD | 230 mg/sqm BD | |||
Interaction with food | Taken with food | No interaction | Two hour before or one hour after food | Taken with food | No interaction | Not known |
Common adverse effect | Fluid retention, Myalgia, arthralgia,GI-related, cytopenia | Pleural effusion, | Hyperlipidemia, hyperglycemia, myocardial infarction, stroke,peripheral artery occlusion, pancreatitis, QT prolongation | Diarrhea, elevated liver enzymes | Hypertension, | Myelosuppression, hepatotoxicity, hyperglycemia |
Pulmonary artery hypertension,cytopenia Bleeding/platelet dysfunction | Abdominal pain, | |||||
Arterial thrombosis.hepatotoxicity | ||||||
Contraindication | None | None | Hypokalemia,hypomagnesemia, prolonged QT interval | Hypersensitivity | None | None |
Black box warning for arterial thrombosis, hepatotoxicity | ||||||
Drug interaction | Increased exposure: | Increased exposure: | Increased exposure: | Increased exposure: | Increased exposure: | Data not available |
PPI,quinolones,azoles, CSA, valproic acid | PPI, Beta blocker,ACE inhibitor, macrolide,azole, CSA | Macrolides, valproic acid, cyclosporine,azoles | Azoles | Azole, protease inhibitor, macrolide, SRI | ||
Decreased exposure: | Decreased exposure: | Decreased exposure: | Decreased exposure: | Decreaed exposure: | ||
Dexamethosone, rifampicin, protease inhibitor, phenytoin carbamazepine, lamivudine,metformin | Dexamethasone, phenytoin, carbamazepine | Dexamethasone, phenytoin, carbamazepine, rifampicin | PPI, rifampicin | Rifampicin, carbamazepine, phenytoin | ||
Drugs prolonging QT interval has additive effect | ||||||
Female of childbearing age | Contraception advised | Contraception advised | Contraception advised | Contraception advised | Contraception advised | Data not available |
Breast feeding | Contraindicated | Contraindicated | Contraindicated | Contraindicated | Contra-indicated | Data not available |
ACE angiotensin converting enzyme, AP accelerated phase, BC blast crisis, BD twice daily, CML chronic myeloid leukemia, CSA cyclosporine, GI gastrointestinal, OD once daily, PPI proton pump inhibitor, SRI serotononin reuptake inhibitor