Peringatan Keamanan

In the few toxicity reports, it has been shown an increased in the development of cutaneous squamous cell carcinomas or acceleration in pre-existant tumor growth.FDA label

Vemurafenib

DB08881

small molecule approved

Deskripsi

Vemurafenib is a competitive kinase inhibitor with activity against BRAF kinase with mutations like V600E.A31269 It exerts its function by binding to the ATP-binding domain of the mutant BRAF.A31270 Vemurafenib was co-developed by Roche and Plexxikon and it obtained its FDA approval on August 17, 2011, under the company Hoffmann La Roche. After approval, Roche in collaboration with Genentech launched a broad development program. L1012

Struktur Molekul 2D

Berat 489.922
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of Vemurafenib is estimated to be 57 hours (range of 30-120 hours).[A31274]
Volume Distribusi The estimation of the volume of distribution for Vemurafenib is 106 L.[A31274]
Klirens (Clearance) The total body clearance is 31 L/day.[A31274]

Absorpsi

Vemurafenib is well absorbed after oral administration.A31273 Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. In the same conditions, Vemurafenib presents a Cmax of 62 mcg/ml and AUC of 601 mcg h/ml.FDA label It is unknown how food affects the absorption of vemurafenib. It presents an accumulation ratio of 7.36 after repeating doses of 960 mg L1014

Metabolisme

Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.A31274

Rute Eliminasi

Analysis showed that 94% of administered Vemurafenib is excreted via feces and 1% is excreted by urine.A31274

Interaksi Makanan

5 Data
  • 1. Do not take with or immediately after a high-fat meal. Taking vemurafenib with a high-fat meal may increase the AUC and Cmax by approximately 5 fold and 2.5 fold, respectively.
  • 2. Exercise caution with grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of vemurafenib, which may increase its serum concentration.
  • 3. Exercise caution with St. John's Wort. This herb induces the CYP3A4 metabolism of vemurafenib and may reduce its serum concentration.
  • 4. Limit caffeine intake. Vemurafenib inhibits CYP1A2, which may increase the serum levels and adverse effects of caffeine.
  • 5. Take with or without food.

Interaksi Obat

1377 Data
Modafinil The metabolism of Vemurafenib can be increased when combined with Modafinil.
Armodafinil The metabolism of Vemurafenib can be increased when combined with Armodafinil.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Vemurafenib.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Vemurafenib.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Vemurafenib.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Vemurafenib.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Vemurafenib.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Vemurafenib.
Silodosin The excretion of Silodosin can be decreased when combined with Vemurafenib.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Vemurafenib.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Vemurafenib.
Porfimer sodium Vemurafenib may increase the photosensitizing activities of Porfimer sodium.
Verteporfin Vemurafenib may increase the photosensitizing activities of Verteporfin.
Mecamylamine The risk or severity of adverse effects can be increased when Vemurafenib is combined with Mecamylamine.
Pentolinium The risk or severity of adverse effects can be increased when Vemurafenib is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Vemurafenib is combined with Trimethaphan.
Hexamethonium The risk or severity of adverse effects can be increased when Vemurafenib is combined with Hexamethonium.
Cyclopentamine The risk or severity of adverse effects can be increased when Vemurafenib is combined with Cyclopentamine.
Nicotine The risk or severity of adverse effects can be increased when Vemurafenib is combined with Nicotine.
Metreleptin The metabolism of Vemurafenib can be increased when combined with Metreleptin.
Methotrexate The protein binding of Methotrexate can be increased when combined with Vemurafenib.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Vemurafenib.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Vemurafenib.
Perampanel The metabolism of Perampanel can be increased when combined with Vemurafenib.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
Doxorubicin The serum concentration of Doxorubicin can be decreased when it is combined with Vemurafenib.
Dexketoprofen The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Vemurafenib.
Ketoprofen The risk or severity of adverse effects can be increased when Ketoprofen is combined with Vemurafenib.
Lumacaftor The serum concentration of Vemurafenib can be decreased when it is combined with Lumacaftor.
Erlotinib The serum concentration of Erlotinib can be decreased when it is combined with Vemurafenib.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Vemurafenib.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Vemurafenib.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Vemurafenib.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Vemurafenib.
Sulpiride The risk or severity of QTc prolongation can be increased when Sulpiride is combined with Vemurafenib.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Vemurafenib.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Vemurafenib.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Vemurafenib.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Vemurafenib.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Vemurafenib.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Vemurafenib.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Vemurafenib.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Vemurafenib.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Vemurafenib.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Vemurafenib.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Vemurafenib.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Vemurafenib.
Levosimendan The risk or severity of QTc prolongation can be increased when Levosimendan is combined with Vemurafenib.
Mesoridazine The risk or severity of QTc prolongation can be increased when Mesoridazine is combined with Vemurafenib.
Desloratadine The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Vemurafenib.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Vemurafenib.
Papaverine The risk or severity of QTc prolongation can be increased when Papaverine is combined with Vemurafenib.
Chlorpheniramine The risk or severity of QTc prolongation can be increased when Chlorpheniramine is combined with Vemurafenib.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Gemifloxacin is combined with Vemurafenib.
Ofloxacin The risk or severity of QTc prolongation can be increased when Ofloxacin is combined with Vemurafenib.
Probucol The risk or severity of QTc prolongation can be increased when Probucol is combined with Vemurafenib.
Aceprometazine The risk or severity of QTc prolongation can be increased when Aceprometazine is combined with Vemurafenib.
Terlipressin The risk or severity of QTc prolongation can be increased when Terlipressin is combined with Vemurafenib.
Prenylamine The risk or severity of QTc prolongation can be increased when Prenylamine is combined with Vemurafenib.
Fluspirilene The risk or severity of QTc prolongation can be increased when Fluspirilene is combined with Vemurafenib.
Azimilide The risk or severity of QTc prolongation can be increased when Azimilide is combined with Vemurafenib.
Pracinostat The risk or severity of QTc prolongation can be increased when Pracinostat is combined with Vemurafenib.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Technetium Tc-99m ciprofloxacin is combined with Vemurafenib.
Garenoxacin The risk or severity of QTc prolongation can be increased when Garenoxacin is combined with Vemurafenib.
Tedisamil The risk or severity of QTc prolongation can be increased when Tedisamil is combined with Vemurafenib.
Tucidinostat The risk or severity of QTc prolongation can be increased when Tucidinostat is combined with Vemurafenib.
Telavancin The risk or severity of QTc prolongation can be increased when Telavancin is combined with Vemurafenib.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Nemonoxacin is combined with Vemurafenib.
Antazoline The risk or severity of QTc prolongation can be increased when Antazoline is combined with Vemurafenib.
Bedaquiline The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Bedaquiline.
Fendiline The risk or severity of QTc prolongation can be increased when Fendiline is combined with Vemurafenib.
Eperisone The risk or severity of QTc prolongation can be increased when Eperisone is combined with Vemurafenib.
Butriptyline The risk or severity of QTc prolongation can be increased when Butriptyline is combined with Vemurafenib.
Melperone The risk or severity of QTc prolongation can be increased when Melperone is combined with Vemurafenib.
Dexchlorpheniramine maleate The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine maleate is combined with Vemurafenib.
Amifampridine The risk or severity of QTc prolongation can be increased when Amifampridine is combined with Vemurafenib.
Mocetinostat The risk or severity of QTc prolongation can be increased when Mocetinostat is combined with Vemurafenib.
Entinostat The risk or severity of QTc prolongation can be increased when Entinostat is combined with Vemurafenib.
CUDC-101 The risk or severity of QTc prolongation can be increased when CUDC-101 is combined with Vemurafenib.
Simendan The risk or severity of QTc prolongation can be increased when Simendan is combined with Vemurafenib.
Ricolinostat The risk or severity of QTc prolongation can be increased when Ricolinostat is combined with Vemurafenib.
Mizolastine The risk or severity of QTc prolongation can be increased when Mizolastine is combined with Vemurafenib.
Abexinostat The risk or severity of QTc prolongation can be increased when Abexinostat is combined with Vemurafenib.
Oxatomide The risk or severity of QTc prolongation can be increased when Oxatomide is combined with Vemurafenib.
Sitafloxacin The risk or severity of QTc prolongation can be increased when Sitafloxacin is combined with Vemurafenib.
Sultopride The risk or severity of QTc prolongation can be increased when Sultopride is combined with Vemurafenib.
Otilonium The risk or severity of QTc prolongation can be increased when Otilonium is combined with Vemurafenib.
Nizofenone The risk or severity of QTc prolongation can be increased when Nizofenone is combined with Vemurafenib.
Bunaftine The risk or severity of QTc prolongation can be increased when Bunaftine is combined with Vemurafenib.
Lorcainide The risk or severity of QTc prolongation can be increased when Lorcainide is combined with Vemurafenib.
Dexchlorpheniramine The risk or severity of QTc prolongation can be increased when Dexchlorpheniramine is combined with Vemurafenib.
Penfluridol The risk or severity of QTc prolongation can be increased when Penfluridol is combined with Vemurafenib.
Dexverapamil The risk or severity of QTc prolongation can be increased when Dexverapamil is combined with Vemurafenib.
Prochlorperazine The risk or severity of QTc prolongation can be increased when Prochlorperazine is combined with Vemurafenib.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Vemurafenib.
Quetiapine The risk or severity of QTc prolongation can be increased when Quetiapine is combined with Vemurafenib.
Levofloxacin The risk or severity of QTc prolongation can be increased when Levofloxacin is combined with Vemurafenib.
Emedastine The risk or severity of QTc prolongation can be increased when Emedastine is combined with Vemurafenib.
Encorafenib The serum concentration of Encorafenib can be increased when it is combined with Vemurafenib.

Target Protein

Serine/threonine-protein kinase B-raf BRAF

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23094782
    Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24.
  • PMID: 25096067
    Kim G, McKee AE, Ning YM, Hazarika M, Theoret M, Johnson JR, Xu QC, Tang S, Sridhara R, Jiang X, He K, Roscoe D, McGuinn WD, Helms WS, Russell AM, Miksinski SP, Zirkelbach JF, Earp J, Liu Q, Ibrahim A, Justice R, Pazdur R: FDA approval summary: vemurafenib for treatment of unresectable or metastatic melanoma with the BRAFV600E mutation. Clin Cancer Res. 2014 Oct 1;20(19):4994-5000. doi: 10.1158/1078-0432.CCR-14-0776. Epub 2014 Aug 5.
  • PMID: 22083257
    Luke JJ, Hodi FS: Vemurafenib and BRAF inhibition: a new class of treatment for metastatic melanoma. Clin Cancer Res. 2012 Jan 1;18(1):9-14. doi: 10.1158/1078-0432.CCR-11-2197. Epub 2011 Nov 14.
  • PMID: 27863476
    Schirosi L, Strippoli S, Gaudio F, Graziano G, Popescu O, Guida M, Simone G, Mangia A: Is immunohistochemistry of BRAF V600E useful as a screening tool and during progression disease of melanoma patients? BMC Cancer. 2016 Nov 18;16(1):905.
  • PMID: 27995058
    Stempel JM, Bustamante Alvarez JG, Carpio AM, Mittal V, Dourado C: Erdheim-Chester disease, moving away from the orphan diseases: A case report. Respir Med Case Rep. 2016 Dec 3;20:55-58. eCollection 2017.
  • PMID: 28255850
    Zhang W, Heinzmann D, Grippo JF: Clinical Pharmacokinetics of Vemurafenib. Clin Pharmacokinet. 2017 Mar 2. doi: 10.1007/s40262-017-0523-7.
  • PMID: 25729580
    Goldinger SM, Rinderknecht J, Dummer R, Kuhn FP, Yang KH, Lee L, Ayala RC, Racha J, Geng W, Moore D, Liu M, Joe AK, Bazan SP, Grippo JF: A single-dose mass balance and metabolite-profiling study of vemurafenib in patients with metastatic melanoma. Pharmacol Res Perspect. 2015 Mar;3(2):e00113. doi: 10.1002/prp2.113.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Zelboraf
    Tablet, film coated • 240 mg/1 • Oral • US • Approved
  • Zelboraf
    Tablet • 240 mg • Oral • Canada • Approved
  • Zelboraf
    Tablet, film coated • 240 mg • Oral • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul