Lazertinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Lazertinib: clinical details
Prescribing considerations
- Initiation should be supervised by a clinician experienced in anticancer treatment.
- Confirm an eligible EGFR mutation using a validated tumour or plasma test; consider tumour testing after a negative plasma result where suitable tissue is available.
- Review the combination's measures for preventing and managing venous thromboembolism and skin or nail toxicity.
- Verify pregnancy status where relevant and counsel about contraception and reproductive risks.
Contraindications and cautions
- Hypersensitivity to lazertinib or any excipient.
- Exercise caution with previous interstitial lung disease or pneumonitis, previous venous thromboembolism, severe hepatic impairment or end-stage renal disease because experience is limited or absent.
Monitoring
- Assess promptly for interstitial lung disease or pneumonitis; interrupt treatment while suspected cases are investigated.
- Monitor for venous thromboembolism, particularly early in combination treatment.
- Review skin, nail and oral toxicity and reinforce sun protection and preventive skin care.
- Monitor eye symptoms; arrange prompt ophthalmology review for worsening symptoms and advise stopping contact-lens use pending assessment.
- Monitor liver enzymes and other laboratory parameters according to the oncology protocol.
- Review all medicines for CYP3A4 and BCRP interactions.
Clinical pharmacology
Lazertinib is a third-generation EGFR tyrosine kinase inhibitor targeting activating EGFR mutations and T790M. It is mainly metabolised through GSTM1-mediated glutathione conjugation, with a smaller CYP3A4 contribution, and inhibits CYP3A4 and BCRP.
Formulation and product differences
- The product is a yellow, oval film-coated tablet supplied in blister packaging.
- Tablets must be swallowed whole and are not suitable for crushing, splitting or chewing.
Lazertinib preparations and strengths
Tablet
Route: Oral
Strengths: 80 mg, 240 mg
Lazertinib interactions
Give the oncology team and pharmacist a complete list of prescribed, non-prescribed and herbal products.
Strong CYP3A4 inducers, including rifampicin, carbamazepine and phenytoin
These can substantially reduce lazertinib exposure and should be avoided.
St John's wort
This may reduce lazertinib exposure and should be avoided.
CYP3A4 substrates with a narrow therapeutic index, including tacrolimus, ciclosporin, sirolimus and everolimus
Lazertinib may increase their exposure, so adverse-effect or concentration monitoring may be needed.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.