Lazertinib

Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.

ID	`DRUG-LAZERTINIB`
Type	Drug
Aliases	JNJ-73841937LazcluzeLeclazaYH25448Лазертініб
Status	reviewed 2026-04-27 \| pending_clinical_signoff
Diseases	`DIS-NSCLC`
Sources	`SRC-ESMO-NSCLC-METASTATIC-2024` `SRC-NCCN-NSCLC-2025`

Drug Facts

Class	Third-generation EGFR tyrosine kinase inhibitor
Mechanism	Irreversible third-generation EGFR-TKI that covalently binds the cysteine residue (C797) of mutant EGFR, selective for sensitizing EGFR mutations (exon-19 deletions, L858R) and the T790M resistance-conferring mutation while sparing wild-type EGFR (so reduced rash / GI toxicity vs first-generation TKIs). Brain- penetrant (CSF/plasma ratio similar to osimertinib), enabling intracranial activity. Mechanism of action and target spectrum are pharmacologically analogous to osimertinib. Clinical evidence: MARIPOSA (lazertinib + amivantamab vs osimertinib in 1L EGFR ex19del / L858R NSCLC): mPFS 23.7 vs 16.6 mo, HR 0.70 — added FDA approval Aug 2024 for the combination. Korean approval as monotherapy preceded the Western combo registration (2021).
Typical dosing	240 mg PO once daily, with or without food, in combination with amivantamab IV/SC dosed per MARIPOSA schedule. Continuous until progression / unacceptable toxicity. Dose level -1 = 160 mg daily; -2 = 80 mg daily; permanent discontinuation if recurrent G3-4 at -2. Hold for ILD/pneumonitis (any grade — workup); permanently discontinue for confirmed ILD ≥G2. Hold for QTc >500 ms; correct K+/Mg++ and reassess. No formal renal adjustment.
Ukraine registered	False
NSZU reimbursed	False
Ukraine last verified	2026-04-27

Notes

Currently approved in the West only in fixed combination with amivantamab (MARIPOSA — superior PFS vs osimertinib but more AE, notably VTE / IRR / rash / hepatotoxicity). Korean approval as monotherapy (2021) is not reflected in EMA/FDA labels. VTE prophylaxis with prophylactic-dose LMWH or DOAC for the first 4 months is mandated by MARIPOSA protocol when combined with amivantamab. Baseline workup: ECG (QTc), LFTs, CBC, electrolytes (K, Mg, Ca), CT chest (ILD baseline), echo if cardiac history. Monitor LFTs / ECG q2 weeks first 8 weeks then monthly; CT chest at any new respiratory symptoms (high suspicion for ILD). Premed for amivantamab IRR as per ami protocol (steroid + antihistamine + antipyretic). Compared with osimertinib alone, the combo increases PFS at the cost of toxicity — patient selection (younger, fitter, willing to accept IV therapy and VTE prophylaxis) is critical.

Used By

Indications

IND-NSCLC-EGFR-1L-AMI-LAZ - IND-NSCLC-EGFR-1L-AMI-LAZ

Regimens

REG-AMI-LAZ-NSCLC - Amivantamab + Lazertinib (MARIPOSA) — 1L EGFR-mut NSCLC
REG-AMIVANTAMAB-LAZERTINIB-NSCLC-2L - Amivantamab + Lazertinib (MARIPOSA-2) — 2L EGFR-mut NSCLC post-osimertinib