Lazertinib is a kinase inhibitor indicated in combination with Amivantamab for the first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring specific epidermal growth factor receptor (EGFR) mutations (exon 19 deletions or exon 21 L858R substitution mutations).
Dosage and Administration of Lazertinib, Recommended Dosage
Standard Dosage and Administration
(1) Lazertinib must be administered in combination with Amivantamab as part of a complete treatment regimen.
(2) Recommended dose: The recommended dosage of Lazertinib is 240 mg, administered orally once daily, with or without food.
(3) Administration method: Lazertinib tablets should be swallowed whole; they must not be crushed, split or chewed. When Lazertinib and Amivantamab are administered on the same day, Lazertinib may be taken at any time prior to Amivantamab infusion.
(4) Treatment duration: Treatment should continue until disease progression or unacceptable toxicity occurs.
(5) Missed dose: If a dose is missed and is remembered within 12 hours of the scheduled time, the patient should be instructed to take the missed dose immediately. If more than 12 hours have elapsed since the scheduled dose time, the patient should skip the missed dose and take the next dose at the regularly scheduled time.
(6) Management of vomiting: If vomiting occurs at any time following administration of Lazertinib, the patient should take the next dose at the regularly scheduled time; an additional dose should not be taken to make up for the vomited dose.
Dosage Modifications for Lazertinib
Venous Thromboembolic (VTE) Events
(1) Grade 2 or 3 VTE: Interrupt Lazertinib and Amivantamab. Initiate anticoagulant therapy per clinical indication. Once anticoagulant therapy is initiated, resume Lazertinib and Amivantamab at the same dose level.
(2) Grade 4 VTE or recurrent Grade 2/3 VTE (despite adequate anticoagulation): Interrupt Lazertinib and permanently discontinue Amivantamab. Lazertinib may be continued at the same dose level upon initiation of anticoagulant therapy, at the physician’s discretion.
(3) Prophylactic therapy: To reduce the risk of VTE, prophylactic anticoagulation is recommended for the first four months following initiation of the combination therapy.
Interstitial Lung Disease (ILD)/Pneumonitis
(1) ILD/pneumonitis of any grade (suspected): Immediately interrupt Lazertinib and Amivantamab.
(2) For confirmed ILD/pneumonitis, permanently discontinue Lazertinib and Amivantamab.
Use in Specific Populations
Patients with Hepatic or Renal Impairment
(1) Mild or moderate renal impairment: No dosage adjustment is recommended. Studies have not been conducted in patients with severe renal impairment or end-stage renal disease.(2) Mild or moderate hepatic impairment: No dosage adjustment is recommended. Studies have not been conducted in patients with severe hepatic impairment.(3) Pediatric patients: The efficacy of Lazertinib in pediatric patients has not been established.
Pregnant Women
(1) Animal studies have demonstrated that Lazertinib may cause fetal harm.
(2) Pregnant women and females of reproductive potential should be informed of the potential risk to the fetus.
(3) Females of reproductive potential are advised to use effective contraception during treatment and for 3 weeks following the last dose of Lazertinib.
Lactating Women
(1) It is unknown whether Lazertinib or its metabolites are excreted in human milk.
(2) Due to the potential risk of serious adverse reactions in breastfed infants, lactating women are advised not to breastfeed during treatment and for 3 weeks following the last dose of Lazertinib.
