Lazcluze (Lazertinib)
Third-Generation EGFR Tyrosine Kinase Inhibitor for Advanced Non-Small Cell Lung Cancer
Quick Facts About Lazcluze
Key Takeaways About Lazcluze (Lazertinib)
- Targeted EGFR therapy: Lazcluze selectively blocks mutated EGFR proteins (exon 19 deletions and exon 21 L858R mutations) that drive non-small cell lung cancer growth
- Used in combination: Always prescribed together with amivantamab for dual EGFR pathway blockade, providing both intracellular and extracellular EGFR inhibition
- Blood clot risk: When combined with amivantamab, there is a significant risk of venous thromboembolism; your doctor will prescribe anticoagulants to reduce this risk
- Skin protection essential: Proactive skin care including sunscreen (UVA/UVB), moisturisers, and protective clothing is critical to reduce skin-related side effects
- Not for pregnancy: Lazcluze may harm an unborn baby; effective contraception is required during treatment and for at least 3 weeks after the last dose
What Is Lazcluze and What Is It Used For?
Lazcluze (lazertinib) is a targeted cancer medicine that belongs to the protein kinase inhibitor class. It is used in combination with amivantamab to treat adults with advanced non-small cell lung cancer (NSCLC) that has specific mutations in the EGFR gene (epidermal growth factor receptor).
Non-small cell lung cancer is the most common type of lung cancer, accounting for approximately 80–85% of all lung cancer diagnoses worldwide. In a subset of patients, the cancer cells harbour activating mutations in the EGFR gene, most commonly exon 19 deletions or exon 21 L858R substitution mutations. These mutations cause the EGFR protein to become permanently switched on, sending continuous growth signals that drive cancer cell proliferation and survival.
Lazertinib is a third-generation, irreversible EGFR tyrosine kinase inhibitor (TKI). It works by binding to and blocking the aberrant EGFR protein inside cancer cells, disrupting the signalling pathways that promote tumour growth. Unlike earlier-generation EGFR inhibitors, lazertinib has been designed to target the mutant EGFR protein more selectively while having less effect on normal (wild-type) EGFR. This selectivity helps reduce certain off-target side effects that are more prominent with less selective EGFR inhibitors.
When used in combination with amivantamab – a bispecific antibody that targets both the extracellular domain of EGFR and the MET receptor – lazertinib provides a dual mechanism of EGFR pathway blockade. While lazertinib inhibits EGFR signalling from inside the cell, amivantamab blocks the receptor from outside the cell and can also engage the immune system against cancer cells. This combined approach has been shown in clinical trials to provide superior outcomes compared to standard EGFR TKI monotherapy in the first-line treatment setting.
Lazcluze is prescribed when the cancer has advanced to a stage where curative treatment (such as surgery) is unlikely to be effective. Patients must have confirmed EGFR exon 19 deletion or exon 21 L858R substitution mutation, typically identified through tumour biopsy or liquid biopsy testing, before treatment can be initiated.
What Should You Know Before Taking Lazcluze?
Before starting Lazcluze, your doctor must confirm the presence of EGFR mutations in your cancer. You should inform your doctor about all medical conditions, medications, and if you are pregnant, breastfeeding, or planning to become pregnant.
Contraindications
Do not take Lazcluze if you are allergic to lazertinib or any of the other ingredients in the tablet. If you are uncertain about any of the ingredients, consult your doctor or pharmacist before taking the medicine. An allergic reaction may include symptoms such as rash, itching, swelling, or difficulty breathing.
Warnings and Precautions
Talk to your doctor, pharmacist or nurse before taking Lazcluze if you have a history of lung inflammation (a condition called interstitial lung disease or pneumonitis). This is particularly important because lazertinib can cause inflammation and scarring in the lungs, which may be life-threatening in some cases.
During treatment with Lazcluze, tell your doctor immediately if you experience any of the following serious side effects:
- Skin problems: Rash (including acne-like rash), dry skin, itching, pain, or redness. To reduce the risk and severity of skin problems, use protective clothing, apply broad-spectrum sunscreen (protecting against both UVA and UVB rays), and use moisturising creams (ceramide-based or other long-lasting formulations without drying ingredients) regularly on the face and entire body (except the scalp). You will need to avoid direct sun exposure and continue these precautions for 2 months after completing treatment. Your doctor may recommend starting prophylactic antibiotics and an antiseptic wash for hands and feet.
- Breathing difficulties: Sudden shortness of breath, cough, or fever may indicate pneumonitis (lung inflammation). This condition can be life-threatening and your healthcare team will monitor you for these symptoms.
- Blood clots (venous thromboembolism): When Lazcluze is used with amivantamab, life-threatening blood clots in veins can occur, particularly in the lungs or legs. Your doctor will prescribe additional medication to prevent blood clots during treatment and will monitor you closely. Seek immediate medical attention if you experience severe chest pain, shortness of breath, rapid breathing, leg pain, or swelling in the arms or legs.
- Eye problems: Contact your doctor or nurse immediately if you experience vision changes or eye pain. If you wear contact lenses and develop new eye symptoms, stop wearing your contact lenses and seek medical attention promptly.
Pregnancy and Breastfeeding
Lazcluze may cause harm to an unborn baby. If you are pregnant, think you may be pregnant, or are planning to have a baby, talk to your doctor before taking this medicine. If you become pregnant during treatment, inform your doctor immediately so that you can discuss whether to continue treatment.
Women of childbearing potential must use effective contraception during treatment with Lazcluze and for at least 3 weeks after the last dose. Male patients with partners who can become pregnant must use effective contraception, such as condoms, during treatment and for 3 weeks after the last dose. Male patients must not donate sperm during this period.
Do not breastfeed during treatment with Lazcluze or for 3 weeks after the last dose. It is not known whether lazertinib passes into breast milk and a risk to the nursing infant cannot be excluded.
Children and Adolescents
Lazcluze has not been studied in children or adolescents under 18 years of age. Do not give this medicine to patients under 18 years old.
Driving and Using Machines
Lazcluze may have a minor effect on your ability to drive and use machines. If you feel tired after taking Lazcluze, do not drive or operate machinery until you feel well enough to do so safely.
Sodium Content
This medicine contains less than 1 mmol (23 mg) sodium per tablet and is therefore essentially sodium-free.
How Does Lazcluze Interact with Other Drugs?
Lazcluze can interact with several medications that either reduce its effectiveness or whose effects may be altered by lazertinib. Always inform your doctor about all medications you are taking, including prescription, over-the-counter medicines and herbal supplements.
Drug interactions with Lazcluze fall into two main categories: medicines that reduce how well Lazcluze works (by increasing its metabolism), and medicines whose effects are increased or altered by Lazcluze. Understanding these interactions is essential for safe and effective treatment.
Drugs That Reduce Lazcluze Effectiveness
The following medicines are strong or moderate CYP enzyme inducers and can significantly reduce lazertinib blood levels, potentially making the treatment less effective. Avoid using these during Lazcluze treatment whenever possible:
| Drug | Therapeutic Use | Interaction Mechanism |
|---|---|---|
| Carbamazepine | Anticonvulsant (epilepsy, seizures) | Strong CYP3A4 inducer; reduces lazertinib levels |
| Phenytoin | Anticonvulsant (seizures) | Strong CYP3A4 inducer; reduces lazertinib levels |
| Rifampicin | Antibiotic (tuberculosis) | Strong CYP3A4 inducer; reduces lazertinib levels |
| St John’s Wort | Herbal remedy (mild depression, anxiety) | CYP3A4 inducer; reduces lazertinib levels |
| Bosentan | Pulmonary arterial hypertension | Moderate CYP3A4 inducer; may reduce lazertinib levels |
| Efavirenz | Antiretroviral (HIV treatment/prevention) | Moderate CYP3A4 inducer; may reduce lazertinib levels |
| Modafinil | Wakefulness-promoting agent (sleep disorders) | Moderate CYP3A4 inducer; may reduce lazertinib levels |
Drugs Whose Effects May Be Altered by Lazcluze
Lazertinib may affect how the following medicines work and/or increase their risk of side effects. Your doctor may need to adjust doses or monitor you more closely:
| Drug | Therapeutic Use | Potential Effect |
|---|---|---|
| Tizanidine | Muscle relaxant | Increased blood levels and risk of side effects |
| Ciclosporin | Immunosuppressant | Increased blood levels; may require dose adjustment |
| Sirolimus | Immunosuppressant | Increased blood levels; may require dose adjustment |
| Tacrolimus | Immunosuppressant | Increased blood levels; may require dose adjustment |
| Everolimus | Cancer treatment (breast, kidney, neuroendocrine) | Increased blood levels and risk of side effects |
| Pimozide | Antipsychotic (Tourette syndrome) | Increased blood levels; risk of cardiac effects |
| Quinidine | Antimalarial / antiarrhythmic | Increased blood levels; risk of cardiac effects |
| Sunitinib | Cancer treatment (GIST, renal cell carcinoma) | Increased blood levels and risk of side effects |
This is not a complete list of drug interactions. Always tell your doctor about all medicines you are currently taking, including vitamins and herbal supplements. Your doctor will advise you on the most appropriate treatment plan.
What Is the Correct Dosage of Lazcluze?
The recommended dose of Lazcluze is 240 mg (three 80 mg tablets) taken once daily by mouth, in combination with amivantamab. The dose may be reduced to 160 mg or 80 mg daily if you experience certain side effects.
Adults
Standard Dose
240 mg once daily (three 80 mg tablets or one 240 mg tablet), taken with or without food. Swallow the tablet(s) whole – do not crush, split, or chew.
Dose Reductions for Side Effects
If you experience certain side effects, your doctor may reduce your dose:
- First reduction: 160 mg once daily
- Second reduction: 80 mg once daily
Your doctor will determine the appropriate dose based on the type and severity of side effects you experience.
Lazcluze is always used in combination with amivantamab, which is given by intravenous infusion or subcutaneous injection. Your doctor will determine the dosing schedule for amivantamab separately.
Children
Lazcluze is not approved for use in children and adolescents under 18 years of age. No dosing recommendations can be made for this population, as clinical studies have not been conducted in paediatric patients.
Elderly
No dose adjustment is required based on age alone. However, elderly patients may be more susceptible to certain side effects, and your doctor will monitor you closely and may adjust the dose as needed based on your individual tolerance.
Missed Dose
If you forget to take a dose of Lazcluze, take it as soon as you remember. However, if it is less than 12 hours until your next scheduled dose, skip the missed dose entirely. Take your next dose at the usual time. Do not take a double dose to make up for a missed one.
Overdose
If you have taken more than your prescribed dose, contact your doctor immediately. You may have an increased risk of side effects. There is no specific antidote for lazertinib overdose; treatment is supportive and based on symptoms.
What Are the Side Effects of Lazcluze?
Like all medicines, Lazcluze can cause side effects, although not everybody gets them. The side effects listed below have been reported in clinical studies of Lazcluze used in combination with amivantamab. Some side effects can be serious and require immediate medical attention.
Serious Side Effects
Tell your doctor immediately if you experience any of the following serious side effects:
Very Common Serious Effects
- Skin reactions – rash (including acne-like rash), dry skin, itching, pain, redness; tell your doctor if skin problems worsen
- Venous thromboembolism (blood clots) – blood clots in veins, particularly in the lungs or legs; symptoms may include severe chest pain, shortness of breath, rapid breathing, leg pain, or swelling in arms or legs
Common Serious Effects
- Interstitial lung disease / pneumonitis – inflammation and scarring in the lungs; symptoms include sudden breathing difficulties, shortness of breath, cough, or fever; this can cause permanent damage and your doctor may need to stop Lazcluze treatment
- Keratitis – inflammation of the cornea (front of the eye); symptoms include eye redness, eye pain, vision problems, or light sensitivity
- Other eye problems – vision changes or increased eyelash growth
Other Side Effects
Very Common
- Nail problems (paronychia, nail changes)
- Infusion-related reactions (with amivantamab)
- Low albumin levels in the blood (hypoalbuminaemia)
- Liver function changes (elevated transaminases)
- Swelling due to fluid retention (oedema)
- Mouth sores (stomatitis)
- Peripheral neuropathy (tingling, numbness, pain, or loss of sensation)
- Severe tiredness (fatigue)
- Diarrhoea
- Constipation
- Decreased appetite
- Low calcium levels in the blood (hypocalcaemia)
- Nausea
- Muscle spasms
- Low potassium levels in the blood (hypokalaemia)
- Dizziness
- Muscle pain (myalgia)
- Vomiting
- Fever (pyrexia)
- Abdominal pain
Common
- Haemorrhoids
- Palmar-plantar erythrodysaesthesia (redness, swelling, peeling skin, or soreness, mainly on hands or feet)
- Low magnesium levels in the blood (hypomagnesaemia)
- Urticaria (itchy rash, hives)
If you experience any side effects, including any not listed above, talk to your doctor, pharmacist, or nurse. Reporting side effects helps regulatory authorities continuously monitor the benefit-risk balance of medicines.
How Should You Store Lazcluze?
Store Lazcluze at room temperature with no special storage conditions required. Keep the medicine out of the sight and reach of children.
Keep this medicine out of the sight and reach of children at all times. Do not use this medicine after the expiry date stated on the blister, inner carton, outer carton, bottle, and box after “EXP”. The expiry date refers to the last day of the stated month.
No special storage conditions are required for Lazcluze. Store the tablets in their original packaging to protect them from moisture. Do not remove the tablets from the blister or bottle until you are ready to take a dose.
Do not dispose of medicines via wastewater or household waste. Ask your pharmacist how to dispose of medicines you no longer use. These measures help to protect the environment and prevent accidental exposure.
What Does Lazcluze Contain?
The active substance is lazertinib (as mesylate monohydrate). Each film-coated tablet contains either 80 mg or 240 mg of lazertinib.
Active Ingredient
Lazertinib (as mesylate monohydrate). Available in two strengths: 80 mg and 240 mg film-coated tablets.
Other Ingredients
Tablet core: Colloidal anhydrous silica, croscarmellose sodium (E 468), microcrystalline cellulose (E 460i), mannitol (E 421), and magnesium stearate (E 572).
Film coating: Macrogol poly(vinyl alcohol) graft copolymer (E 1209), polyvinyl alcohol (E 1203), glycerol monocaprylocaprate type I (E 471), titanium dioxide (E 171), and talc (E 553b). The 80 mg tablet additionally contains yellow iron oxide (E 172). The 240 mg tablet additionally contains red iron oxide (E 172) and black iron oxide (E 172).
Tablet Appearance
Lazcluze 80 mg: Yellow, 14 mm long, oval, film-coated tablets, debossed with “LZ” on one side and “80” on the other. Available in cartons containing 56 film-coated tablets (two cartons of 28 tablets each) or bottles containing 60 or 90 tablets.
Lazcluze 240 mg: Reddish-purple, 20 mm long, oval, film-coated tablets, debossed with “LZ” on one side and “240” on the other. Available in cartons containing 14 film-coated tablets (one carton of 14 tablets), cartons containing 28 film-coated tablets (two cartons of 14 tablets each), or bottles containing 30 tablets.
Not all pack sizes may be marketed in your country.
Frequently Asked Questions About Lazcluze
Lazcluze is specifically indicated for advanced non-small cell lung cancer (NSCLC) that has activating mutations in the EGFR gene. The two types of EGFR mutations for which Lazcluze is approved are exon 19 deletions and exon 21 L858R substitution mutations. These mutations are found in approximately 10–15% of NSCLC cases in Western populations and up to 40–50% in East Asian populations. A confirmed mutation test result is required before treatment can begin.
Lazcluze and amivantamab work through complementary mechanisms to block the EGFR pathway more completely. Lazertinib blocks the mutated EGFR protein from inside the cancer cell (intracellular inhibition), while amivantamab targets EGFR from outside the cell (extracellular blockade) and also blocks the MET receptor, another pathway that cancer cells can use to grow. Clinical trial data from the MARIPOSA study demonstrated that this combination significantly improved progression-free survival compared to the standard EGFR TKI osimertinib alone.
Yes, when used in combination with amivantamab, Lazcluze carries a significant risk of venous thromboembolism (blood clots in veins). This is classified as a very common side effect, meaning it can occur in more than 1 in 10 patients. Blood clots can form in the deep veins of the legs (deep vein thrombosis) or travel to the lungs (pulmonary embolism), which can be life-threatening. Your doctor will prescribe anticoagulant medication to help prevent blood clots throughout your treatment. You should report any symptoms such as leg swelling, chest pain, or shortness of breath immediately.
Skin problems are very common with Lazcluze and amivantamab. Proactive skin care is essential: apply a broad-spectrum sunscreen (UVA/UVB) daily, use ceramide-based or other long-lasting moisturisers on your face and body (not the scalp), wear protective clothing, and avoid direct sunlight. Continue these measures for 2 months after completing treatment. Your doctor may prescribe prophylactic antibiotics and antiseptic hand/foot washes before you even start treatment. If you develop skin reactions, your doctor can prescribe additional treatments or refer you to a dermatologist.
Yes, Lazcluze can be taken with or without food. There is no requirement to take it at a specific time relative to meals. However, you should try to take your dose at approximately the same time each day to maintain consistent drug levels in your body. Swallow the tablets whole with water – do not crush, split, or chew them.
No, Lazcluze is not considered safe during pregnancy. It may harm the developing baby based on its mechanism of action. Women who are able to become pregnant must use effective contraception during treatment and for at least 3 weeks after the final dose. Male patients with female partners of childbearing potential should also use contraception (e.g., condoms) during treatment and for 3 weeks afterward. If you become pregnant while taking Lazcluze, tell your doctor immediately so you can discuss the risks and benefits of continuing treatment.
References
- European Medicines Agency (EMA). Lazcluze (lazertinib) – Summary of Product Characteristics. EMA/2025. Available at: www.ema.europa.eu
- Cho BC, et al. Amivantamab plus lazertinib vs osimertinib as first-line treatment in patients with EGFR-mutated advanced non-small cell lung cancer: primary results from MARIPOSA, a randomized, open-label, phase 3 trial. Annals of Oncology. 2024;35(1):77–90.
- National Comprehensive Cancer Network (NCCN). Clinical Practice Guidelines in Oncology: Non-Small Cell Lung Cancer. Version 3.2025. Available at: www.nccn.org
- European Society for Medical Oncology (ESMO). Metastatic Non-Small Cell Lung Cancer: ESMO Clinical Practice Guideline for diagnosis, treatment and follow-up. Annals of Oncology. 2024;35(7):611–630.
- World Health Organization (WHO). WHO Model List of Essential Medicines – 23rd List, 2023. Geneva: World Health Organization; 2023.
- Yun J, et al. Lazertinib, a third-generation EGFR tyrosine kinase inhibitor: preclinical characterization and clinical development. Cancer Research. 2021;81(13 Supplement):CT162.
- Planchard D, et al. Metastatic non-small cell lung cancer: ESMO Clinical Practice Guidelines. Annals of Oncology. 2023;29(Suppl 4):iv192–iv237.
- Sequist LV, et al. Osimertinib in EGFR-mutated non-small cell lung cancer: a review of the clinical evidence. Therapeutic Advances in Medical Oncology. 2023;15:17588359231196638.
Editorial Team
Medical Review
Content medically reviewed by the iMedic Medical Review Board, comprising board-certified oncologists and clinical pharmacologists with expertise in thoracic oncology, targeted cancer therapies, and drug safety. All content follows the GRADE evidence framework and adheres to international guidelines from ESMO, NCCN, and WHO.
Editorial Standards
This article is based on approved prescribing information (EMA Summary of Product Characteristics), published clinical trial data (MARIPOSA study), and international oncology guidelines. No commercial funding was received. For full editorial standards, see our Editorial Standards page.
Last fact-checked: | Evidence level: 1A (Systematic reviews and RCTs) | Conflict of interest: None declared