Bacrelba

Newly diagnosed or previously treated Philadelphia chromosome +ve chronic myeloid leukemia (Ph+ CML) in chronic phase (CP) in adults. Ph+ CML in CP harboring the T315I mutation in adults.

Ph+ CML-CP 80 mg once daily at approx the same time each day, or 40 mg bid at approx 12-hr intervals. Patient changing from 40 mg bid to 80 mg once daily Start taking once daily approx 12 hr after the last bid dose, & then continue at 80 mg once daily. Patient changing from 80 mg once daily to 40 mg bid Start taking bid approx 24 hr after the last once-daily dose, & then continue at 40 mg bid at approx 12-hr intervals. Ph+ CML-CP harboring the T315I mutation 200 mg bid at approx 12-hr intervals.

Should be taken on an empty stomach: Avoid food consumption for at least 2 hr prior & 1 hr after taking tab. Swallow tab whole & do not break/crush/chew.

Risk of hypersensitivity; thrombocytopenia, neutropenia, & anemia; pancreatitis & asymptomatic elevation of serum lipase & amylase; ECG QT prolongation; HTN; reactivation of HBV. Perform CBC every 2 wk for the 1st 3 mth of treatment & mthly thereafter or as clinically indicated. Perform ECG prior to start of treatment & monitor during treatment as clinically indicated. Monitor for signs & symptoms of myelosuppression; pancreatic toxicity & more frequently in patients w/ history of pancreatitis; hypersensitivity. Assess serum lipase & amylase levels mthly during treatment or as clinically indicated. Correct hypokalemia & hypomagnesemia prior to administration & monitor during treatment as clinically indicated. Monitor & manage HTN using standard antihypertensive therapy during treatment. Test for HBV infection prior to start of treatment & closely monitor HBV carriers for signs & symptoms of active HBV infection throughout & for several mth following termination of therapy. Medicinal products w/ known risk of torsades de pointes should be co-administered w/ caution w/ asciminib 80 mg total daily dose & should be avoided w/ 200 mg bid dose. Caution in patients w/ severe renal or hepatic impairment receiving the 200 mg bid dose. Risk of embryo-fetal harm when administered to a pregnant woman. Sexually active females of reproductive potential should use effective contraception during treatment & for at least 3 days after last dose. Breastfeeding is not recommended during treatment & for at least 3 days after last dose. Safety & efficacy have not been established in ped patients <18 yr.

URTI; thrombocytopenia, neutropenia, anaemia; dyslipidaemia; headache, dizziness; HTN; cough; increased pancreatic enzymes, vomiting, diarrhoea, nausea, abdominal pain; increased hepatic enzyme; rash, pruritus; musculoskeletal pain, arthralgia; fatigue. Lower resp tract infection, flu; hypothyroidism; decreased appetite; blurred vision, dry eye; palpitations; pleural effusion, dyspnoea, non-cardiac chest pain; pancreatitis; increased blood bilirubin; urticaria; oedema, pyrexia; increased blood creatine phosphokinase.

Plasma conc may be increased w/ strong CYP3A4 inhibitors (eg, clarithromycin, telithromycin, troleandomycin, itraconazole, ketoconazole, voriconazole, ritonavir, indinavir, nelfinavir, saquinavir). Plasma conc may be decreased w/ strong CYP3A4 inducers (eg, rifampicin, carbamazepine, phenobarb, phenytoin, St. John's wort). May alter plasma conc of CYP3A4 substrates w/ narrow therapeutic index (eg, midazolam, fentanyl, alfentanil, dihydroergotamine, ergotamine); CYP2C9 sensitive substrates or CYP2C9 substrates w/ narrow therapeutic index (eg, phenytoin, warfarin); substrates of OATP1B, of BCRP or of both (eg, pravastatin, atorvastatin, sulfasalazine, MTX, pitavastatin, rosuvastatin, simvastatin); P-gp substrates w/ narrow therapeutic index (eg, digoxin, dabigatran, colchicine). May have additive effect on QT interval w/ medicinal products w/ known risk of torsades de pointes (eg, bepridil, chloroquine, clarithromycin, halofantrine, haloperidol, methadone, moxifloxacin, pimozide). Decreased bioavailability w/ food.

Targeted Cancer Therapy

L01EA06 - asciminib ; Belongs to the class of BCR-ABL tyrosine kinase inhibitors. Used in the treatment of cancer.

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