Peringatan Keamanan

There is no information regarding the acute toxicity (LD50) and overdose of lazertinib.

Lazertinib

DB16216

small molecule approved investigational

Deskripsi

Lazertinib is an oral, third-generation, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI).A264299, A264304 Lazertinib was first approved in South Korea on January 18, 2021, for the treatment of EGFR T790M mutation-positive non-small cell lung cancer (NSCLC) with EGFR mutations.A264289 It was approved by the FDA on August 19, 2024.L51189 Lazertinib is used alone or in combination with other chemotherapeutic agents.L51184

Struktur Molekul 2D

Berat 554.655
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean terminal half-life is 3.7 days (56%).[L51184]
Volume Distribusi The mean apparent volume of distribution is 2680 L (51%).[L51184] Lazertinib penetrates the blood-brain barrier.[A264289]
Klirens (Clearance) The mean apparent clearance is 36.4 L/h (47%).[L51184]

Absorpsi

Lazertinib maximum plasma concentration (Cmax) and area under the 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. Lazertinib steady-state plasma exposure was achieved by day 15 with approximately 2-fold accumulation for AUC. The Tmax ranges from two to four hours. A high-fat meal (800 to 1000 kcal, approximately 50% fat) did not have a clinically significant effect on lazertinib pharmacokinetics compared to that under fasted conditions.L51184

Metabolisme

In vitro studies demonstrate that lazertinib is primarily metabolized by glutathione conjugation, mediated by glutathione S-transferase M1. CYP3A4 also plays a minor role.A264289, L51184 Its metabolites have not been fully characterized.

Rute Eliminasi

Following a single oral dose of radiolabeled lazertinib, approximately 86% of the dose was recovered in feces (< 5% as unchanged) and 4% in urine (< 0.2% as unchanged).L51184

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not have a clinically significant effect on lazertinib pharmacokinetics.

Interaksi Obat

345 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Lazertinib.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Lazertinib.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Lazertinib.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Lazertinib.
Lidocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Tetrodotoxin.
Ambroxol The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Ambroxol.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Lazertinib is combined with Quinisocaine.
Etrasimod The risk or severity of immunosuppression can be increased when Lazertinib is combined with Etrasimod.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Lazertinib.
Phenytoin The metabolism of Lazertinib can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Lazertinib can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Lazertinib can be increased when combined with Carbamazepine.
Mitotane The metabolism of Lazertinib can be increased when combined with Mitotane.
Primidone The metabolism of Lazertinib can be increased when combined with Primidone.
Rifampin The metabolism of Lazertinib can be increased when combined with Rifampin.
Phenobarbital The metabolism of Lazertinib can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Lazertinib can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Lazertinib can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Lazertinib can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Lazertinib can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Lazertinib can be increased when combined with Midostaurin.
Enzalutamide The metabolism of Lazertinib can be increased when combined with Enzalutamide.
Lumacaftor The metabolism of Lazertinib can be increased when combined with Lumacaftor.
Apalutamide The metabolism of Lazertinib can be increased when combined with Apalutamide.
Cyclosporine The metabolism of Cyclosporine can be decreased when combined with Lazertinib.
Fluvoxamine The metabolism of Lazertinib can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Lazertinib can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Lazertinib can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Lazertinib can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Lazertinib can be decreased when combined with Isradipine.
Diltiazem The metabolism of Lazertinib can be decreased when combined with Diltiazem.
Clozapine The metabolism of Lazertinib can be decreased when combined with Clozapine.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Lazertinib.
Ciprofloxacin The metabolism of Lazertinib can be decreased when combined with Ciprofloxacin.
Voriconazole The metabolism of Lazertinib can be decreased when combined with Voriconazole.
Nicardipine The metabolism of Lazertinib can be decreased when combined with Nicardipine.
Verapamil The metabolism of Lazertinib can be decreased when combined with Verapamil.
Aprepitant The metabolism of Lazertinib can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Lazertinib can be decreased when combined with Isoniazid.
Primaquine The metabolism of Lazertinib can be decreased when combined with Primaquine.
Miconazole The metabolism of Lazertinib can be decreased when combined with Miconazole.
Danazol The metabolism of Lazertinib can be decreased when combined with Danazol.
Fusidic acid The metabolism of Lazertinib can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Lazertinib can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Dronedarone can be decreased when combined with Lazertinib.
Milnacipran The metabolism of Lazertinib can be decreased when combined with Milnacipran.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Lazertinib.
Isavuconazonium The metabolism of Lazertinib can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Lazertinib can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Lazertinib can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Lazertinib can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Lazertinib can be decreased when combined with Linagliptin.
Indalpine The metabolism of Lazertinib can be decreased when combined with Indalpine.
Netupitant The metabolism of Lazertinib can be decreased when combined with Netupitant.
Barnidipine The metabolism of Lazertinib can be decreased when combined with Barnidipine.
Benidipine The metabolism of Lazertinib can be decreased when combined with Benidipine.
Venetoclax The metabolism of Venetoclax can be decreased when combined with Lazertinib.
Isavuconazole The metabolism of Lazertinib can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Lazertinib can be decreased when combined with Fosnetupitant.
Berotralstat The serum concentration of Berotralstat can be increased when it is combined with Lazertinib.
Nelfinavir The metabolism of Lazertinib can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Lazertinib can be decreased when combined with Indinavir.
Terfenadine The metabolism of Lazertinib can be decreased when combined with Terfenadine.
Ritonavir The serum concentration of Lazertinib can be increased when it is combined with Ritonavir.
Efavirenz The metabolism of Lazertinib can be increased when combined with Efavirenz.
Ergotamine The metabolism of Ergotamine can be decreased when combined with Lazertinib.
Amprenavir The metabolism of Lazertinib can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Lazertinib can be decreased when combined with Delavirdine.
Methimazole The metabolism of Lazertinib can be decreased when combined with Methimazole.
Conivaptan The metabolism of Conivaptan can be decreased when combined with Lazertinib.

Target Protein

Epidermal growth factor receptor EGFR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34028784
    Dhillon S: Lazertinib: First Approval. Drugs. 2021 Jun;81(9):1107-1113. doi: 10.1007/s40265-021-01533-x.
  • PMID: 31587882
    Ahn MJ, Han JY, Lee KH, Kim SW, Kim DW, Lee YG, Cho EK, Kim JH, Lee GW, Lee JS, Min YJ, Kim JS, Lee SS, Kim HR, Hong MH, Ahn JS, Sun JM, Kim HT, Lee DH, Kim S, Cho BC: Lazertinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: results from the dose escalation and dose expansion parts of a first-in-human, open-label, multicentre, phase 1-2 study. Lancet Oncol. 2019 Dec;20(12):1681-1690. doi: 10.1016/S1470-2045(19)30504-2. Epub 2019 Oct 3.
  • PMID: 36031779
    Lee J, Hong MH, Cho BC: Lazertinib: on the Way to Its Throne. Yonsei Med J. 2022 Sep;63(9):799-805. doi: 10.3349/ymj.2022.63.9.799.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Lazcluze
    Tablet, film coated • 240 mg/1 • Oral • US • Approved
  • Lazcluze
    Tablet, film coated • 80 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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