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

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

Adverse effects

• venous thromboembolism
• interstitial lung disease, pneumomitis
• acneiform dermatitis
• keratitis
• fetal toxicity

• drug adverse effects of pharmaceutical monoclonal antibodies

Mechanism of action

• inhibits EGFR exon 19 deletions & exon 21 L858R substitution mutations at lower concentrations than wildtype EGFR

More general terms

• antineoplastic monoclonal antibody

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=121269225