Lumakras

— THERAPEUTIC CATEGORIES —
  • Respiratory and thoracic 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

    • Lumakras Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Sotorasib 120mg, 320mg; tabs.

    Pharmacological Class

    RAS GTPase (family) inhibitor.

    How Supplied

    Tabs 120mg—240; 320mg—90

    Manufacturer

    Amgen, Inc.

    Generic Availability

    NO

    Mechanism of Action

    Sotorasib forms an irreversible, covalent bond with the unique cysteine of KRASG12C, locking the protein in an inactive state that prevents downstream signaling without affecting wild-type KRAS. Sotorasib blocked KRAS signaling, inhibited cell growth, and promoted apoptosis only in KRAS G12C tumor cell lines.

    Lumakras Indications

    Indications

    In adults with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy.

    Lumakras Dosage and Administration

    Adult

    Confirm presence of KRAS G12C mutation in tumor or plasma specimens. Swallow whole. If difficulty swallowing, may disperse tabs in 120mL of room temperature water (without crushing). 960mg once daily until disease progression or unacceptable toxicity. Dose modifications for adverse reactions: see full labeling.

    Children

    Not established.

    Lumakras Contraindications

    Not Applicable

    Lumakras Boxed Warnings

    Not Applicable

    Lumakras Warnings/Precautions

    Warnings/Precautions

    Monitor LFTs prior to initiation, every 3 weeks during 1st 3 months of treatment, then once monthly or as clinically indicated; test more frequently if AST, ALT and/or bilirubin elevations develop. Monitor for pulmonary symptoms indicative of ILD/pneumonitis; withhold immediately if suspected and permanently discontinue if no other causes are identified. Hepatic impairment: monitor for adverse reactions more frequently. Pregnancy. Nursing mother: not recommended (during and for 1 week after the last dose).

    Lumakras Pharmacokinetics

    Absorption

    • Median time to peak plasma concentration: 1 hour.

    • Effect of Food:

      • Sotorasib AUC0-24h increased by 25% when administered with a high-fat, high-calorie meal compared to administration under fasted conditions.

    Distribution

    • Mean volume of distribution at steady state: 211 L.

    • 89% plasma protein bound. 

    Metabolism

    • Non-enzymatic conjugation and oxidative metabolism with CYP3As.

    Elimination

    • Fecal (74%), renal (6%). 

    • Half-life: 5 hours. Apparent clearance at steady state: 26.2 L/hr.

    Lumakras Interactions

    Interactions

    Avoid concomitant PPIs, H2-receptor antagonists, and locally acting antacids; if unavoidable, give Lumakras 4hrs before or 10hrs after antacid. Antagonized by strong CYP3A4 inducers (eg, rifampin); avoid. Avoid concomitant sensitive CYP3A4 substrates (eg, midazolam); if unavoidable, increase the CYP3A4 substrate dosage. Avoid concomitant P-gp substrates (eg, digoxin); if unavoidable, decrease the P-gp substrate dosage. Potentiates BCRP substrates; monitor for adverse reactions and decrease the BCRP substrate dose.

    Lumakras Adverse Reactions

    Adverse Reactions

    Diarrhea, musculoskeletal pain, nausea, fatigue, hepatotoxicity, cough, lab abnormalities (decreased lymphocytes, decreased hemoglobin, increased AST/ALT, decreased calcium, increased alkaline phosphatase, increased urine protein, decreased sodium); pneumonia.

    Lumakras Clinical Trials

    See Literature

    Lumakras Note

    Not Applicable

    Lumakras Patient Counseling

    See Literature

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