Respiratory and thoracic cancers:
Indications for: LUMAKRAS
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.
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.
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).
RAS GTPase (family) inhibitor.
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.
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.
Fecal (74%), renal (6%).
Half-life: 5 hours. Apparent clearance at steady state: 26.2 L/hr.
Generic Drug Availability:
Tabs 120mg—240; 320mg—90