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Today, we will learn more about the third-generation non-small cell lung cancer (NSCLC) treatment that South Korea is proud of, Leclaza (Lazertinib).
Leclaza is emerging as a new hope for patients and their families suffering from lung cancer, especially EGFR mutant lung cancer, which is the number one cause of cancer deaths in Korea.
Leclaza, a domestic anticancer drug developed by Yuhan Corporation, has been recognized by the US FDA and Europe for its excellent efficacy and brain metastasis treatment effect.
In this article, we will organize the mechanism of action, pharmacodynamics, FDA-approved efficacy, side effects, and dosage of Lekrajajeong in an easy and accurate manner. Those interested in lung cancer treatment, read to the end! 😊
What is Leclaza? Everything about domestic EGFR lung cancer targeting treatment
Leclaza (ingredient name: Lazertinib) is a third-generation EGFR tyrosine kinase inhibitor (TKI) developed by Yuhan Corporation.
Designed for non-small cell lung cancer patients with EGFR mutations (Exon 19 deletion, Exon 21 L858R, T790M), this drug is the 31st new drug in Korea and is attracting attention on the global stage.
📌 Key features of Leclaza
✅ Domestic new drug: Lung cancer treatment developed with Korean technology
✅ Blood-brain barrier (BBB) passage: Effective even for patients with brain metastases
✅ 1st and 2nd line treatment: Key option for treating EGFR-mutated lung cancer
✅ Librivant combination therapy: Approved with Janssen's Librivant (Amivantamab) in January 2025
Mechanism of action of Leclaza: How does it block lung cancer cells?
Leclaza is a targeted anticancer drug that acts on EGFR (epidermal growth factor receptor) and blocks the growth signal of cancer cells.
🔹Main action
- Inhibits EGFR mutations: Targets Exon 19 deletion, Exon 21 L858R, T790M mutations
- Overcomes resistance: Effective for T790M mutations that occur after treatment with 1st and 2nd generation TKIs (e.g. Iressa, Tarceva)
- Brain metastasis treatment: Contributes to improving the survival rate of patients with brain metastases by crossing the blood-brain barrier (BBB).
Leclaza Pharmacokinetics: Process of action and half-life (30-72 hours)
Leclaza is an oral tablet that moves in the body as follows after taking it.
✔ Absorption: Rapidly absorbed in the stomach, can be taken without regard to food
✔ Distribution: Systemically transported in the blood, effective in treating brain metastases by passing through the blood-brain barrier (BBB)
✔ Metabolism: Metabolized by CYP3A4 enzyme in the liver → Caution when used together with CYP3A4 inhibitors (such as ketoconazole)
✔ Excretion: Metabolized through the liver, then excreted through bile (bile excretion) and urine excretion through the kidneys (renal excretion)
✔ Half-life: Approximately 30-40 hours → Maintain blood concentration by taking it once a day
💡 Q&A: "What's good about a long half-life?" → The efficacy lasts longer, making it more convenient to take!
Leclaza-based efficacy and effects: Complete summary of MFDS-approved indications
Leclaza has been approved by the Ministry of Food and Drug Safety (MFDS) of the Republic of Korea for the following indications.
📌 1st-line treatment (approved in June 2023)
- Non-small cell lung cancer patients with EGFR mutation (Exon 19 deletion, Exon 21 L858R)
- Monotherapy or combination therapy with Librevant (Amivantamab) possible
📌 2nd-line treatment (approved in January 2021)
- EGFR T790M mutation-positive non-small cell lung cancer
- Used when resistance occurs after 1st and 2nd generation TKI treatment
📌 Latest update (January 2025)
- Combination therapy with Librevant: Clinical results, progression-free survival (PFS) was approximately 23.7 months,
improving compared to existing monotherapy (12-18 months) (Source: 2024 ESMO announcement).
💡 Clinical Data: The tumor response rate (ORR) of 78% when combined with Leclaza and Librivant is providing great hope to patients with advanced lung cancer
