Lazertinib is a targeted therapy drug for specific mutated non-small cell lung cancer, mainly exerting anti-tumor effects by inhibiting EGFR mutations. It has significant clinical effects and can penetrate the blood-brain barrier.

1. Main indications

(1) Non small cell lung cancer: Used in combination with bevacizumab for first-line treatment of locally advanced or metastatic adult non-small cell lung cancer patients confirmed by FDA approved testing methods to have EGFR exon 19 deletion or exon 21 L858R substitution mutation.

2 Core mechanisms of action

(1) Targeted inhibition: Specifically inhibits EGFRT790M resistant mutations and exon 19 deletion/L858R activation mutations to avoid the influence of wild-type EGFR.

(2) Blood brain barrier penetration: The unique molecular structure can effectively enter the central nervous system and control brain metastases.

3 target points of action

(1) EGFR exon 19 deletion mutation.

(2) EGFR exon 21L858R substitution mutation.

(3) T790M resistance mutation (Korean version of indication).

4 Drug characteristics

(1) Third generation EGFR tyrosine kinase inhibitors can penetrate the blood-brain barrier.

(2) Selective inhibition of mutant EGFR has little effect on wild-type EGFR.

(3) Genetic testing is required to confirm the mutation status before use.

5 Clinical efficacy data

(1) Indications: Approved for EGFRT790M positive advanced/metastatic non-small cell lung cancer in South Korea, with an objective response rate of 54%.

(2) Combination therapy: When used in combination with first-line treatment with bevacizumab, the median progression free survival is significantly better than traditional chemotherapy.

6 Special Treatment Advantages

(1) Drug resistance management: Overcoming the common issue of T790M resistance after first/second-generation EGFR-TKI treatment.

(2) Convenient administration: The oral dosage form has stable pharmacokinetics, and food has no significant effect on absorption.

7 Precautions related to therapeutic efficacy

(1) Genetic testing: EGFR sensitive mutation status must be confirmed through tumor tissue or plasma testing.

(2) Therapeutic efficacy monitoring: Regular evaluation of imaging response and control of central nervous system lesions is required.