Names and pronunciation
(as-KIM-i-nib) Scemblix
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Drug reference
(as-KIM-i-nib) Scemblix
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Func. class.: Antineoplastic
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Chem. class.: Kinase inhibitor
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ACTION: Inhibits the ABL1 kinase activity of a fusion protein by binding to the ABL pocket, showed activity against wild-type BCR-ABL1 and several mutant forms of the kinase, including the T315I mutation
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USES: Philadelphia chromosome–positive myeloid leukemia
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CONTRAINDICATIONS Hypersensitivity, pregnancy, breast feeding Precautions: Myelosuppression, pancre- atic/CV toxicity, hypertension, pregnancy
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SIDE EFFECTS RESP: URI GI: Nausea, vomiting, diarrhea, abdomi- nal pain, anorexia, constipation MS: MS pain CNS: Fatigue, dizziness, fever INTEG: Rash
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INTERACTIONS Increase: adverse reactions—strong CYP3A4 inhibitors, certain substrates of CYP3A4, certain P-gp substrates Avoid use with itraconazole oral solution, with substrates of CYP2C9 Drug/Lab Test: Increase: Triglycerides, creatine kinase, alanine aminotransferase, lipase, amylase Decrease: Platelets, neutrophils, HCT
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DOSAGE AND ROUTES PH+ CML in CP • Adult: PO 80 mg daily or 40 mg bid Ph+ CML in CP with T315I Mutation • Adult: PO 200 mg bid
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Available forms: Film-coated tablets 20, 40 mg
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Administer: • Avoid food for at least 2 hr before and 1 hr after use • Swallow tablets whole; do not break, crush, or chew • Skip any missed dose and take the next dose at the regular time if missed by >12 hr for daily dosing or >6 hr with bid dosing
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Assess: • Hypersensitivity: Monitor patients for signs and symptoms of hypertension, B/P often and provide treatment as needed • CV toxicity: Monitor those with his- tory of CV risk factors for adverse reac- tions, QTc prolongation • Myelosuppression: Monitor CBC baseline and q2mo during first 3 mo and monthly thereafter during therapy and interrupt treatment or reduce dose if needed, severe thrombocytopenia and neutropenia may occur • Toxicity and pancreatitis: Monitor serum lipase and amylase baseline and during treatment. Interrupt, then resume at reduced dose or discontinue based on severity. Evaluate for pancreatitis when lipase elevation is accompanied by ab- dominal pain, nausea, vomiting • Hypertension: Monitor B/P baseline and often, manage hypertension with antihy- pertensives as prescribed, interrupt, reduce dose, or stop if not medically controlled • Pregnancy/breastfeeding: Obtain pregnancy test in females of reproductive potential, can cause fetal harm. Advise fe- males of reproductive potential of the po- tential risk and to use effective contracep- tion during and for 1 wk after last dose; to discontinue breastfeeding during and for 1 wk after last dose, may cause infertility
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Evaluate: • Therapeutic response: Prevention of increase in CML
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Hypersensitivity: Advise patient to A report immediately itching, rash, trouble breathing • CV toxicity: Teach patient to report • Myelosuppression: Advise patient to report excessive fatigue • Pancreatitis and toxicity: Teach pa- tient to report severe abdominal pain, nausea, vomiting • Pregnancy/breastfeeding: Teach pa- tient product can cause fetal harm, that females of reproductive potential should use effective contraception during and for 1 wk after last dose; to discontinue breast- feeding during and for 1 wk after last dose
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PHARMACOKINETICS 97% protein binding, half-life 5.5-9 hr, peak 2.5 hr, onset, duration unknown
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• Adult: PO 80 mg daily or 40 mg bid Ph+ CML in CP with T315I Mutation
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• Adult: PO 200 mg bid
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