Lazertinib

Class
Targeted therapy
Subclass
EGFR tyrosine kinase inhibitors
Substance name
Lazertinib
Brand names
Lazcluze®
Common formulations
Tablet
Dosage and administration
Adults patients
Treatment of non-small cell lung cancer in patients with EGFR exon 19 deletion, EGFR exon 21 L858R substitution • Locally advanced or metastatic
•
240 mg PO daily until disease progression or unacceptable toxicity
Taken with or without food. Administered in combination with amivantamab.
Indications for use
Labeled indications
Adults
•
Treatment of non-small cell lung cancer in patients with EGFR exon 19 deletion, EGFR exon 21 L858R substitution (locally advanced or metastatic)
Safety risks
Contraindications
Concomitant use of strong or moderate CYP3A4 inducers
Warnings and precautions
Cutaneous adverse reactions
•
Maintain a high level of suspicion, as lazertinib in combination with amivantamab has been associated with an increased risk of cutaneous adverse reactions, including severe rash, dermatitis, acneiform rash, pruritus, and dry skin. Advise using alcohol-free emollient cream to reduce dermatologic adverse reactions. Counsel patients to limit sun exposure during and for 2 months after treatment with lazertinib and amivantamab, advise wearing protective clothing and using broad-spectrum sunscreen. Consider offering prophylactic measures, such as oral antibiotics, to reduce the risk of cutaneous adverse reactions. Administer oral corticosteroids for the management of grade 3 reactions and consider seeking a dermatologic consultation. Refer patients with severe rash, atypical appearance, or lack of improvement within 2 weeks to a dermatologist. Withhold, reduce the dose, or permanently discontinue lazertinib and amivantamab based on severity. Decrease the dose to 160 mg for the first reduction and to 80 mg for the second reduction.
ILD
•
Maintain a high level of suspicion, as lazertinib in combination with amivantamab has been associated with an increased risk of ILD/pneumonitis. Discontinue lazertinib and amivantamab if ILD/pneumonitis develops.
Increased serum drug levels
•
Use caution in patients taking drugs that are CYP3A4 or BCRP substrates, as lazertinib is a weak CYP3A4 inhibitor and a BCRP inhibitor and can increase the serum concentrations of these drugs.
Ocular toxicity
•
Maintain a high level of suspicion, as lazertinib in combination with amivantamab has been associated with an increased risk of ocular toxicity, including keratitis. Refer patients to an ophthalmologist for new or worsening eye symptoms. Withhold lazertinib and amivantamab in cases of grade 3 and 4 reactions until resolution to grade ≤ 1 or baseline. Resume both drugs at reduced doses or continue only lazertinib. Consider permanently discontinuing if there is no recovery within 4 weeks. Decrease the dose to 160 mg for the first reduction and to 80 mg for the second reduction.
VTE
•
Maintain a high level of suspicion, as lazertinib in combination with amivantamab has been associated with an increased risk of serious and fatal venous thromboembolic events, including DVT and PE. Administer prophylactic anticoagulation, excluding VKAs, for the first 4 months of treatment. Withhold lazertinib and amivantamab in cases of grade 2 and 3 reactions and administer anticoagulants. Resume both drugs at the same dose level once anticoagulation is initiated. Withhold lazertinib and permanently discontinue amivantamab in cases of grade 4 or recurrent grade 2 or 3 reactions. Resume lazertinib after initiating anticoagulants.
Specific populations
Renal impairment
eGFR ≥ 30 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required.
eGFR < 30 mL/min/1.73 m²
•
No guidance available.
Renal replacement therapy
Any modality
•
No guidance available.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required.
Child-Pugh B (moderate)
•
Use acceptable. No dose adjustment required.
Child-Pugh C (severe)
•
No guidance available.
Pregnancy and breastfeeding
Pregnancy
All trimesters
•
Do not use. Evidence of fetal harm in humans. Verify pregnancy status in females of reproductive potential before initiating treatment. Advise using effective contraception during treatment and for at least 3 weeks after the last dose.
Breastfeeding
Do not use during breastfeeding.
•
Advise females not to breastfeed for 3 weeks after the last dose.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
May potentially cause adverse effects in breastfed infants.
Adverse reactions
Very common > 10%
•
Anemia, conjunctivitis, ↓ WBC count, ↓ blood neutrophil count, ↓ platelet count, ↓ serum albumin, ↓ serum calcium, ↓ serum magnesium, ↓ serum potassium, ↓ serum sodium, ↑ serum ALP, ↑ serum ALT, ↑ serum AST, ↑ serum creatinine, ↑ serum gamma-glutamyltransferase, ↑ serum magnesium, infusion-related reactions, nail abnormality, peripheral edema, abdominal pain, bleeding, constipation, cough, diarrhea, dizziness, dyspnea, fatigue, fever, headache, itching, loss of appetite, musculoskeletal pain, nausea, paresthesia, skin rash, vomiting, skin dryness, stomatitis, venous thromboembolism
Common 1-10%
•
Hemorrhoids, interstitial lung disease, pneumonitis, pleural effusion, pneumonia, insomnia
Interactions
Drug(s)
Check Interactions
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