pharmacopeia
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/api/v1/drug/lazertinib

Mechanism of action

Sourced from openFDA

Lazertinib is a kinase inhibitor of epidermal growth factor receptor (EGFR) that inhibits EGFR exon 19 deletions and exon 21 L858R substitution mutations at lower concentrations than wild-type EGFR. In human NSCLC cells and mouse xenograft models of EGFR exon 19 deletions or EGFR L858R substitution mutations, lazertinib demonstrated anti-tumor activity.

Breast Cancer Resistance ProteinCytochrome P450 3A4Kinase

Indications

Sourced from openFDA
  • LAZCLUZE, in combination with amivantamab, is indicated for the first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations, as detected by an FDA-approved test [see Dosage and Administration (2.1) ] . LAZCLUZE 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) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations, as detected by an FDA-approved test.ICD-10: C34.90

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

The recommended dosage of LAZCLUZE is 240 mg orally once daily with or without food, given in combination with amivantamab. ( 2.2 ) Continue treatment until disease progression or unacceptable toxicity. ( 2.2 ) Administer LAZCLUZE any time prior to amivantamab when given on the same day. ( 2.2 ) Refer to the amivantamab prescribing information for recommended amivantamab dosing information. ( 2.2 ) Administer prophylactic and concomitant medications to reduce the risk of dermatologic adverse reactions. ( 2.3 ) Administer anticoagulant prophylaxis to reduce the risk of venous thromboembolic events (VTE) for the first four months of treatment. ( 2.3 ) 2.1 Patient Selection Select patients for the first-line treatment of NSCLC with LAZCLUZE, in combination with amivantamab, based on the presence of EGFR exon 19 deletions or exon 21 L858R substitution mutations in tumor or plasma specimens [see Clinical Studies (14) ] . If these mutations are not detected in a plasma specimen, test tumor tissue. Information on FDA-approved tests is available at: http://www.fda.gov/CompanionDiagnostics . 2.2 Recommended Dosage and Administration Recommended Dosage and Administration The recommended dosage of LAZCLUZE is 240 mg orally once daily administered in combination with amivantamab, with or without food. Swallow LAZCLUZE tablets whole. Do not crush, split, or chew. Continue treatment until disease progression or unacceptable toxicity. Administer LAZCLUZE any time prior to amivantamab when given on the same day.

Warnings & precautions

Sourced from openFDA

Venous Thromboembolic Events (VTE) : Prophylactic anticoagulation is recommended for the first four months of treatment. Monitor for signs and symptoms of VTE and treat as medically appropriate. Withhold LAZCLUZE and amivantamab based on severity. Once anticoagulant treatment has been initiated, resume LAZCLUZE and amivantamab at the same dose at the discretion of the healthcare provider. Permanently discontinue amivantamab and continue LAZCLUZE for recurrent VTE despite therapeutic anticoagulation. ( 2.3 , 2.4 , 5.1 ) Interstitial Lung Disease (ILD)/Pneumonitis : Monitor for new or worsening symptoms indicative of ILD/pneumonitis. Withhold LAZCLUZE and amivantamab in patients with suspected ILD/pneumonitis and permanently discontinue if ILD/pneumonitis is confirmed. ( 2.4 , 5.2 ) Dermatologic Adverse Reactions : Can cause severe rash including acneiform dermatitis. At treatment initiation, prophylactic and concomitant medications are recommended. Withhold, reduce the dose or permanently discontinue LAZCLUZE and amivantamab based on severity. ( 2.3 , 2.4 , 5.3 ) Hepatotoxicity : Can cause severe hepatotoxicity (including increased ALT and AST). Withhold, reduce the dose, or permanently discontinue LAZCLUZE and amivantamab based on severity. ( 2.4 , 5.4 ) Ocular Adverse Reactions : Promptly refer patients with new or worsening signs and symptoms of ocular adverse reactions, including keratitis, to an ophthalmologist for evaluation. Withhold, reduce the dose, or permanently discontinue amivantamab and continue LAZCLUZE based on severity.

Adverse reactions

Sourced from openFDA

The following adverse reactions are discussed elsewhere in the labeling: Venous Thromboembolic Events [see Warnings and Precautions (5.1) ] Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.2) ] Dermatologic Adverse Reactions [see Warnings and Precautions (5.3) ] Hepatotoxicity [see Warnings and Precautions (5.4) ] Ocular Toxicity [see Warnings and Precautions (5.5) ] LAZCLUZE in Combination with Amivantamab The most common adverse reactions (≥ 20%) were rash, nail toxicity, infusion-related reaction (amivantamab), musculoskeletal pain, edema, stomatitis, VTE, paresthesia, fatigue, diarrhea, constipation, COVID-19, hemorrhage, dry skin, decreased appetite, pruritus, and nausea. ( 6.1 ) The most common Grade 3 or 4 laboratory abnormalities (≥ 2%) were decreased albumin, decreased sodium, increased ALT, decreased potassium, decreased hemoglobin, increased AST, increased GGT, and increased magnesium. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Janssen Biotech, Inc. at 1-800-526-7736 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology (12.1) ] , LAZCLUZE can cause fetal harm when administered to a pregnant woman. There are no available data on the use of LAZCLUZE in pregnant women to inform a drug-associated risk. Oral administration of lazertinib to pregnant animals during the period of organogenesis resulted in reduced embryo-fetal survival and fetal body weight in rats and malformations in rabbits at exposures approximately 4 and 0.5 times, respectively, the human exposure at the recommended dose of 240 mg/day based on AUC (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study, pregnant rats received oral doses of 7.5, 30, or 60 mg/kg/day of lazertinib during the period of organogenesis (gestation day 6 to 17). Lazertinib decreased fetal body weights in association with maternal toxicity at 60 mg/kg/day (approximately 4 times the human exposure at the recommended dose of 240 mg/day based on AUC).

Pharmacokinetics

Sourced from openFDA
Metabolism
Lazertinib pharmacokinetics are presented as mean (CV%) for descriptive parameters unless otherwise specified. Lazertinib maximum plasma concentration (C max ) and area under plasma concentration time curve (AUC) increased dose proportionally from 20 mg to 320 mg (0.08 to 1.3 times the approved recommended dosage) following a single administration and once daily administration.

Approval history

Sourced from openFDA
  • Aug 19, 2024NDANDA219008Janssen Biotech

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
582 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Rash11420%
  2. 2Infusion Related Reaction6812%
  3. 3Neuropathy Peripheral366.2%
  4. 4Fatigue356.0%
  5. 5Off Label Use335.7%
  6. 6Paronychia335.7%
  7. 7Diarrhoea295.0%
  8. 8Dyspnoea244.1%
  9. 9Nausea223.8%
  10. 10Pruritus183.1%
  11. 11Decreased Appetite172.9%
  12. 12Oedema Peripheral172.9%
  13. 13Stomatitis172.9%
  14. 14Dermatitis Acneiform162.7%
  15. 15Dizziness162.7%

Clinical trials

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The 10 most recently updated of 45 ClinicalTrials.gov registrations naming Lazertinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Lazertinib work?
Lazertinib is a kinase inhibitor of epidermal growth factor receptor (EGFR) that inhibits EGFR exon 19 deletions and exon 21 L858R substitution mutations at lower concentrations than wild-type EGFR. In human NSCLC cells and mouse xenograft models of EGFR exon 19 deletions or EGFR L858R substitution mutations, lazertinib demonstrated anti-tumor activity.
What is Lazertinib used for?
According to FDA labeling, Lazertinib carries indications including: LAZCLUZE, in combination with amivantamab, is indicated for the first-line treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations, as detected by an FDA-approved test [see Dosage and Administration (2.1) ] . LAZCLUZE 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) with epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R substitution mutations, as detected by an FDA-approved test.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Lazertinib?
Lazertinib is classified as Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, Kinase Inhibitor, Breast Cancer Resistance Protein Inhibitors, Cytochrome P450 3A4 Inhibitors, Kinase Inhibitors.
What are the brand names for Lazertinib?
Lazertinib is marketed under brand names including Lazcluze.
What are the contraindications for Lazertinib?
Lazertinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for lazertinib is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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