Features and properties of lazertinib

Alternative names	GNS-1480; JNJ 73841937; JNJ-1937; lazertinib mesylate monohydrate; LECLAZA®; YH25448
Class	Amides; aniline compounds; antineoplastics; dimethylamines; ethers; morpholines; pyrimidines; small molecules
Mechanism of action	EGFR tyrosine kinase inhibitor
Route of administration	Oral
Pharmacodynamics	Highly selective for EGFR single (Ex19del, L858R, T790M) and double (Ex19del/T790M and L858R/T790M) mutations
	High blood-brain permeability and more effective than osimertinib in inducing tumour regression in an EGFR-mutated mouse brain metastasis model
	Potent antitumour activity in a patient-derived xenograft model of EGFR-mutant NSCLC and in a patient with EGFR-mutant NSCLC
Pharmacokinetics	Median time to peak plasma concentration 2–4 h; steady state reached by day 15
	Average volume of distribution 4263.97 L; highly plasma protein bound (99.1–99.7%)
	Mean terminal half-life of 64.7 h; excreted largely in bile (60%) and faeces (24%)
Most common adverse reactions (240 mg dose)	Rash, itchiness, paresthesia, muscle spasms, headache, diarrhoea, decreased appetite
ATC codes
WHO ATC code	L01EB (EGFR tyrosine kinase inhibitors)
EphMRA ATC code	L1H2 (protein kinase inhibitor antineoplastics, EGFR)
Chemical name	N-{5-[(4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl)amino]-4-methoxy-2-(morpholin-4-yl)phenyl}prop-2-enamide

EGFR epidermal growth factor receptor