Scemblix

— THERAPEUTIC CATEGORIES —
  • Leukemias, lymphomas, and other hematologic cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Scemblix Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Asciminib 20mg, 40mg; tabs.

    Pharmacological Class

    Kinase inhibitor.

    How Supplied

    Tabs 20mg, 40mg—60; 40mg—300 (5×60)

    Manufacturer

    Novartis Pharmaceuticals Corp

    Generic Availability

    NO

    Mechanism of Action

    Asciminib inhibits the ABL1 kinase activity of the BCR-ABL1 fusion protein, by binding to the ABL myristoyl pocket. In studies conducted in vitro or in animal models of CML, asciminib showed activity against wild-type BCR-ABL1 and several mutant forms of the kinase, including the T315I mutation.

    Scemblix Indications

    Indications

    In adults with: Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with ≥2 tyrosine kinase inhibitors (TKIs); or Ph+ CML in CP with the T315I mutation.

    Scemblix Dosage and Administration

    Adult

    Swallow whole. Take on an empty stomach. Avoid food for at least 2hrs before and 1hr after dosing. Previously treated with ≥2 TKIs: 80mg once daily (at same time each day) or 40mg twice daily (at approx. 12hr intervals). With T315I mutation: 200mg twice daily (at approx. 12hr intervals). Dose modifications for adverse reactions: see full labeling.

    Children

    Not established.

    Scemblix Contraindications

    Not Applicable

    Scemblix Boxed Warnings

    Not Applicable

    Scemblix Warnings/Precautions

    Warnings/Precautions

    Monitor for myelosuppression, pancreatic toxicity (increase monitoring if history of pancreatitis), hypertension, hypersensitivity. Monitor for cardiovascular signs/symptoms in those with a history of cardiovascular risk factors. Reduce dose, temporarily withhold, or permanently discontinue based on severity of adverse reactions; see full labeling. Perform CBCs every 2 weeks for the 1st 3 months, then monthly thereafter or as clinically indicated. Assess serum lipase and amylase levels monthly during therapy, or as clinically indicated; temporarily withhold if lipase and amylase elevation are accompanied by abdominal symptoms. Embryo-fetal toxicity. Advise females of reproductive potential to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).

    Scemblix Pharmacokinetics

    Absorption

    Median Tmax of asciminib: 2.5 hours (range: 2–3 hours). 

    Distribution

    Plasma protein bound: 97%.

    Apprarent volume of distribution at steady state: 151 L.

    Metabolism

    CYP3A4-mediated oxidation, UGT2B7- and UGT2B17-mediated glucuronidation. 

    Elimination

    Fecal (80%), renal (11%). Half-life: 5.5 hours (80mg/day); 9 hours (400mg/day).

    Scemblix Interactions

    Interactions

    Potentiated by strong CYP3A4 inhibitors (eg, clarithromycin); monitor closely. Antagonized by itraconazole oral soln containing hydroxypropyl-β-cyclodextrin; avoid. Potentiates certain CYP3A4 substrates (eg, midazolam); avoid concomitant with Scemblix at 200mg twice daily; monitor closely with Scemblix at 80mg daily dose. Potentiates CYP2C9 substrates (eg, warfarin). Avoid concomitant with certain CYP2C9 substrates at Scemblix 80mg daily dose; if unavoidable, reduce CYP2C9 substrate dose. Avoid concomitant with sensitive or certain CYP2C9 substrates at Scemblix 200mg twice daily dose; if unavoidable, consider alternatives (eg, non-CYP2C9 substrate). Avoid concomitant with rosuvastatin, atorvastatin. Potentiates OATP1B and BCRP substrates; monitor closely and reduce substrate dose. Potentiates P-gp substrates; monitor closely.

    Scemblix Adverse Reactions

    Adverse Reactions

    Upper respiratory tract infections, musculoskeletal pain, headache, fatigue, nausea, rash, diarrhea, lab abnormalities (decreased platelet count, decreased neutrophil count, decreased hemoglobin, decreased lymphocyte count, increased triglycerides, increased creatine kinase, increased ALT/AST, increased lipase, increased amylase, increased uric acid); hypertension, myelosuppression, pancreatic, or cardiovascular toxicity.

    Scemblix Clinical Trials

    See Literature

    Scemblix Note

    Not Applicable

    Scemblix Patient Counseling

    See Literature

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