Peringatan Keamanan

Use of neratinib may produce diarrhea and hepatotoxicity as clinically significant adverse effects FDA Label. Serious adverse reactions in the neratinib arm of the clinical trials included diarrhea (1.6%), vomiting (0.9%), dehydration (0.6%), cellulitis (0.4%), renal failure (0.4%), erysipelas (0.4%), alanine aminotransferase increase (0.3%), aspartate aminotransferase increase (0.3%), nausea (0.3%), fatigue (0.2%), and abdominal pain (0.2%).

Neratinib

DB11828

small molecule approved investigational

Deskripsi

Neratinib was approved in July 2017 for use as an extended adjuvant therapy in Human Epidermal Growth Factor Receptor 2 (HER2) positive breast cancer. Approval was granted to Puma Biotechnology Inc. for the tradename Nerlynx. Neratinib is currently under investigation for use in many other forms of cancer.

Struktur Molekul 2D

Berat 557.05
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 half life of elimination ranges from 7-17 h following a single dose [FDA Label]. The mean plasma half life during multiple doses is 14.6 h for neratinib, 21.6 h for M3, 13.8 h for M6, and 10.4 h for M7.
Volume Distribusi The apparent volume of distribution at steady state is 6433 L [FDA Label].
Klirens (Clearance) The total clearance during multiple doses is 216 L/h for after the first dose and 281 L/h during steady state [FDA Label].

Absorpsi

Neratinib and its major active metabolites M3. M6, and M7 have a Tmax of 2-8 h FDA Label. Administration with a high fat meal increases Cmax by 1.7-fold and total exposure by 2.2-fold. Administration with a standard meal increases Cmax by 1.2-fold and total exposure by 1.1-fold. Administration with gastric acid reducing agents such as proton pump inhibitors reduces Cmax by 71% and total exposure by 65%.

Metabolisme

Neratinib is mainly undergoes metabolism via CYP3A4 FDA Label. It is also metabolized by flavin-containing monooxygenase to a lesser extent. The systemic exposures of neratinib's active metabolites M3, M6, M7, and M11 are 15%, 33%, 22%, and 4%.

Rute Eliminasi

97.1% of the total dose is excreted in the feces and 1.13% in the urine FDA Label.

Interaksi Makanan

5 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of neratinib.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of neratinib.
  • 3. Take at the same time every day.
  • 4. Take separate from antacids. Take antacids at least 3 hours before or after neratinib.
  • 5. Take with food.

Interaksi Obat

611 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Neratinib.
Modafinil The metabolism of Neratinib can be increased when combined with Modafinil.
Armodafinil The metabolism of Neratinib can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Neratinib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Neratinib.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Neratinib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Neratinib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Neratinib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Neratinib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Neratinib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Neratinib.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Neratinib.
Silodosin The excretion of Silodosin can be decreased when combined with Neratinib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Neratinib.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Neratinib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Neratinib.
Metreleptin The metabolism of Neratinib can be increased when combined with Metreleptin.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Neratinib.
Crizotinib The metabolism of Neratinib can be decreased when combined with Crizotinib.
Vincristine The excretion of Vincristine can be decreased when combined with Neratinib.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Neratinib.
Betrixaban The serum concentration of Betrixaban can be increased when it is combined with Neratinib.
Pitolisant The serum concentration of Neratinib can be decreased when it is combined with Pitolisant.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Neratinib.
Morphine The serum concentration of Morphine can be increased when it is combined with Neratinib.
Tenofovir disoproxil The serum concentration of Tenofovir disoproxil can be increased when it is combined with Neratinib.
Toremifene The serum concentration of Toremifene can be increased when it is combined with Neratinib.
Bisoprolol The serum concentration of Bisoprolol can be increased when it is combined with Neratinib.
Mannitol The serum concentration of Mannitol can be increased when it is combined with Neratinib.
Clomifene The serum concentration of Clomifene can be increased when it is combined with Neratinib.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Neratinib.
Tegaserod The serum concentration of Tegaserod can be increased when it is combined with Neratinib.
Sitagliptin The serum concentration of Sitagliptin can be increased when it is combined with Neratinib.
Paliperidone The serum concentration of Paliperidone can be increased when it is combined with Neratinib.
Belinostat The serum concentration of Belinostat can be increased when it is combined with Neratinib.
Indacaterol The serum concentration of Indacaterol can be increased when it is combined with Neratinib.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Neratinib.
Apixaban The serum concentration of Apixaban can be increased when it is combined with Neratinib.
Odanacatib The serum concentration of Odanacatib can be increased when it is combined with Neratinib.
Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Neratinib.
Canagliflozin The serum concentration of Canagliflozin can be increased when it is combined with Neratinib.
Dolutegravir The serum concentration of Dolutegravir can be increased when it is combined with Neratinib.
Sofosbuvir The serum concentration of Sofosbuvir can be increased when it is combined with Neratinib.
Umeclidinium The serum concentration of Umeclidinium can be increased when it is combined with Neratinib.
Technetium Tc-99m sestamibi The serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Neratinib.
Dasabuvir The serum concentration of Dasabuvir can be increased when it is combined with Neratinib.
Ombitasvir The serum concentration of Ombitasvir can be increased when it is combined with Neratinib.
Paritaprevir The serum concentration of Paritaprevir can be increased when it is combined with Neratinib.
Selexipag The serum concentration of Selexipag can be increased when it is combined with Neratinib.
Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Neratinib.
Velpatasvir The serum concentration of Velpatasvir can be increased when it is combined with Neratinib.
Tezacaftor The serum concentration of Tezacaftor can be increased when it is combined with Neratinib.
Talinolol The serum concentration of Talinolol can be increased when it is combined with Neratinib.
Revefenacin The serum concentration of Revefenacin can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Valspodar can be increased when it is combined with Neratinib.
Glasdegib The serum concentration of Glasdegib can be increased when it is combined with Neratinib.
Elagolix The serum concentration of Elagolix can be increased when it is combined with Neratinib.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Neratinib.
Omadacycline The serum concentration of Omadacycline can be increased when it is combined with Neratinib.
Grapiprant The serum concentration of Grapiprant can be increased when it is combined with Neratinib.
Lusutrombopag The serum concentration of Lusutrombopag can be increased when it is combined with Neratinib.
Pibrentasvir The serum concentration of Pibrentasvir can be increased when it is combined with Neratinib.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Neratinib.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Neratinib.
Vardenafil The serum concentration of Vardenafil can be increased when it is combined with Neratinib.
Rivaroxaban The serum concentration of Rivaroxaban can be increased when it is combined with Neratinib.
Fedratinib The serum concentration of Neratinib can be increased when it is combined with Fedratinib.
Lasmiditan The serum concentration of Lasmiditan can be increased when it is combined with Neratinib.
Enfortumab vedotin The serum concentration of Enfortumab vedotin can be increased when it is combined with Neratinib.
Darolutamide The serum concentration of Darolutamide can be increased when it is combined with Neratinib.
Lemborexant The serum concentration of Lemborexant can be increased when it is combined with Neratinib.
Selumetinib The serum concentration of Selumetinib can be increased when it is combined with Neratinib.
Ripretinib The serum concentration of Ripretinib can be increased when it is combined with Neratinib.
Fostemsavir The serum concentration of Fostemsavir can be increased when it is combined with Neratinib.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Neratinib.
Elbasvir The serum concentration of Elbasvir can be increased when it is combined with Neratinib.
Mefloquine The serum concentration of Mefloquine can be increased when it is combined with Neratinib.
Lenvatinib The serum concentration of Lenvatinib can be increased when it is combined with Neratinib.
Voclosporin The serum concentration of Voclosporin can be increased when it is combined with Neratinib.
Trilaciclib The serum concentration of Trilaciclib can be increased when it is combined with Neratinib.
Daptomycin The serum concentration of Daptomycin can be increased when it is combined with Neratinib.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Neratinib.
Tenofovir The serum concentration of Tenofovir can be increased when it is combined with Neratinib.
Tivozanib The serum concentration of Tivozanib can be increased when it is combined with Neratinib.
Loncastuximab tesirine The serum concentration of Loncastuximab tesirine can be increased when it is combined with Neratinib.
Dabigatran etexilate The serum concentration of Dabigatran etexilate can be increased when it is combined with Neratinib.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Neratinib.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Neratinib.
Quinidine The serum concentration of Quinidine can be increased when it is combined with Neratinib.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Neratinib.
Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Neratinib.
Vinblastine The serum concentration of Vinblastine can be increased when it is combined with Neratinib.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Neratinib.
Dactinomycin The serum concentration of Dactinomycin can be increased when it is combined with Neratinib.
Cobimetinib The serum concentration of Cobimetinib can be increased when it is combined with Neratinib.
Trastuzumab emtansine The serum concentration of Trastuzumab emtansine can be increased when it is combined with Neratinib.
Romidepsin The serum concentration of Romidepsin can be increased when it is combined with Neratinib.
Panobinostat The serum concentration of Panobinostat can be increased when it is combined with Neratinib.
Vemurafenib The serum concentration of Vemurafenib can be increased when it is combined with Neratinib.
Pomalidomide The serum concentration of Pomalidomide can be increased when it is combined with Neratinib.

Target Protein

Vascular endothelial growth factor receptor 2 KDR
Receptor tyrosine-protein kinase erbB-2 ERBB2
Epidermal growth factor receptor EGFR

Referensi & Sumber

Belum ada data referensi/link/attachment untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field referensi.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Nerlynx
    Tablet • 40 mg • Oral • Canada • Approved
  • Nerlynx
    Tablet • 40 mg/1 • Oral • US • Approved
  • Nerlynx
    Tablet, film coated • 40 mg • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

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