Peringatan Keamanan

There has been a report of one patient who took 3,000 mg of lapatinib for 10 days. This patient had grade 3 diarrhea and vomiting on day 10.

Lapatinib

DB01259

small molecule approved investigational

Deskripsi

Lapatinib is an anti-cancer drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug capecitabine. Lapatinib is a human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1) tyrosine kinases inhibitor. It binds to the intracellular phosphorylation domain to prevent receptor autophosphorylation upon ligand binding.

Struktur Molekul 2D

Berat 581.058
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Single-dose terminal half life: 14.2 hours Effective multiple-dose half life: 24 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Absorption following oral administration of lapatinib is incomplete and variable.

Metabolisme

Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.

Rute Eliminasi

Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.

Farmakogenomik

4 Varian
HLA-DQA1 (None)

The presence of this polymorphism in TNXB may indicate an increased risk of drug-induced ALT-elevations leading to hepatotoxicity when treated with lapatinib.

HLA-DRB1 (None)

The presence of this polymorphism in TNXB may indicate an increased risk of drug-induced ALT-elevations leading to hepatotoxicity when treated with lapatinib.

HLA-DQB1 (None)

The presence of this polymorphism in TNXB may indicate an increased risk of drug-induced ALT-elevations leading to hepatotoxicity when treated with lapatinib.

TNXB (rs12153855)

The presence of this polymorphism in TNXB may indicate an increased risk of drug-induced ALT-elevations leading to hepatotoxicity when treated with lapatinib.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of lapatinib, increasing its serum levels.
  • 2. Take separate from meals. Take lapatinib at least 1 hour before or after eating, as lapatinib bioavailability is elevated by food.

Interaksi Obat

952 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Lapatinib.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Lapatinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Lapatinib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Lapatinib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Lapatinib.
Lomitapide The metabolism of Lomitapide can be decreased when combined with Lapatinib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Lapatinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Lapatinib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Lapatinib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Lapatinib.
Silodosin The excretion of Silodosin can be decreased when combined with Lapatinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Lapatinib.
Dabrafenib The serum concentration of Lapatinib can be decreased when it is combined with Dabrafenib.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Lapatinib.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Lapatinib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Lapatinib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Lapatinib.
Luliconazole The serum concentration of Lapatinib can be increased when it is combined with Luliconazole.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Lapatinib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Lapatinib.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Lapatinib.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Lapatinib.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Lapatinib.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Lapatinib.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Lapatinib.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Lapatinib.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Lapatinib.
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Lapatinib.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Lapatinib.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Lapatinib.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Lapatinib.
Mifepristone The serum concentration of Lapatinib can be increased when it is combined with Mifepristone.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Lapatinib.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Lapatinib.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Lapatinib.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Lapatinib.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Lapatinib.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Lapatinib.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Lapatinib.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Lapatinib.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Lapatinib.
Vincristine The excretion of Vincristine can be decreased when combined with Lapatinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Lapatinib.
St. John's Wort The serum concentration of Lapatinib can be decreased when it is combined with St. John's Wort.
Leuprolide The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Leuprolide.
Goserelin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Goserelin.
Azithromycin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Azithromycin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Sulfisoxazole.
Methadone The metabolism of Lapatinib can be decreased when combined with Methadone.
Sulpiride The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Sulpiride.
Nimodipine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Nimodipine.
Promazine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Promazine.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Prochlorperazine.
Droperidol The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Lapatinib.
Perflutren The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Perflutren.
Cinnarizine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Cinnarizine.
Atropine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Adenosine.
Pentamidine The metabolism of Lapatinib can be decreased when combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Gadobenic acid.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Carbinoxamine.
Dolasetron The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Dolasetron.
Roxithromycin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Roxithromycin.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Cinoxacin.
Granisetron The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Granisetron.
Levosimendan The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Dimenhydrinate.
Primaquine The metabolism of Lapatinib can be decreased when combined with Primaquine.
Papaverine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Papaverine.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Chlorpheniramine.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Ofloxacin.
Propafenone The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Propafenone.
Flecainide The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Flecainide.
Probucol The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Terlipressin.
Prenylamine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Prenylamine.
Fluspirilene The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Fluspirilene.
Lofexidine The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Lofexidine.
Azimilide The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Azimilide.
Pracinostat The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Nemonoxacin.
Antazoline The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Antazoline.
Bedaquiline The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Fendiline.
Eperisone The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Eperisone.
Butriptyline The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Butriptyline.
Melperone The risk or severity of QTc prolongation can be increased when Lapatinib is combined with Melperone.

Target Protein

Epidermal growth factor receptor EGFR
Eukaryotic elongation factor 2 kinase EEF2K
Receptor tyrosine-protein kinase erbB-2 ERBB2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16418322
    Nelson MH, Dolder CR: Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother. 2006 Feb;40(2):261-9. Epub 2006 Jan 17.
  • PMID: 15163842
    Burris HA 3rd: Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist. 2004;9 Suppl 3:10-5.
  • PMID: 15955900
    Burris HA 3rd, Hurwitz HI, Dees EC, Dowlati A, Blackwell KL, O'Neil B, Marcom PK, Ellis MJ, Overmoyer B, Jones SF, Harris JL, Smith DA, Koch KM, Stead A, Mangum S, Spector NL: Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol. 2005 Aug 10;23(23):5305-13. Epub 2005 Jun 13.
  • PMID: 17192538
    Geyer CE, Forster J, Lindquist D, Chan S, Romieu CG, Pienkowski T, Jagiello-Gruszfeld A, Crown J, Chan A, Kaufman B, Skarlos D, Campone M, Davidson N, Berger M, Oliva C, Rubin SD, Stein S, Cameron D: Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med. 2006 Dec 28;355(26):2733-43.
  • PMID: 16894399
    Johnston SR, Leary A: Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Barc). 2006 Jul;42(7):441-53.
  • PMID: 20110044
    Tevaarwerk AJ, Kolesar JM: Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer. Clin Ther. 2009;31 Pt 2:2332-48. doi: 10.1016/j.clinthera.2009.11.029.
  • PMID: 18803986
    Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008.

Contoh Produk & Brand

Produk: 12 • International brands: 1
Produk
  • Lapatinib
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Lapatinib
    Tablet, film coated • 250 mg/1 • Oral • US • Generic • Approved
  • Tykerb
    Tablet • 250 mg/1 • Oral • US • Approved
  • Tykerb
    Tablet • 250 mg/1 • Oral • US • Approved
  • Tykerb
    Tablet • 250 mg • Oral • Canada • Approved
  • Tyverb
    Tablet, film coated • 250 mg • Oral • EU • Approved
  • Tyverb
    Tablet, film coated • 250 mg • Oral • EU • Approved
  • Tyverb
    Tablet, film coated • 250 mg • Oral • EU • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Tycerb

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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