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lazertinib (Lazcluze)
Indications:
- for use in combination with amivantamab for first-line treatment of adults with locally advanced or metastatic non-small cell lung cancer with EGFR exon 19 deletions or exon 21 L858R substitution mutations
Dosage:
- 240 mg once daily in combination with amivantamab
- administer prior to amivantamab when given on the same day
- prophylaxis for venous thromboembolism for first 4 months of therapy
80 mg, 240 mg oral tablets
* no dosage adjustment in the elderly
Dosage adjustment in renal failure:
- has not been studied in patients with eGFR < 30 mL/min
Adverse effects:
- venous thromboembolism
- interstitial lung disease, pneumomitis
- acneiform dermatitis
- keratitis
- fetal toxicity
Pharmacokinetics:
- 99% bound to plasma protiens
- volume of distribution 2680 L
- terminal 1/2 life 3.7 days
- primarily metabolized by glutathione conjugation, either enzymatic via glutathione-S-transferase or non-enzymatic
- metabolized by CYP3A4 to a lesser extent
Mechanism of action:
- inhibits EGFR exon 19 deletions & exon 21 L858R substitution mutations at lower concentrations than wildtype EGFR
Interactions
drug adverse effects of pharmaceutical monoclonal antibodies
General
antineoplastic monoclonal antibody
Database Correlations
PUBCHEM cid=121269225
References
- HIGHLIGHTS OF PRESCRIBING INFORMATION
Laxcluze (lazertinib) tablets, for oral use
https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/LAZCLUZE-pi.pdf