Detail

Vemurafenib

Description

Name: Vemurafenib
Type: small molecule
Groups: approved
Indication: Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
Accession Number: DB08881 ( DB08881)
Description: Vemurafenib is a BRAF enzyme inhibitor developed by Plexxikon and Genentech for the treatment of late-stage melanoma. [Wikipedia] The cobas® 4800 BRAF B600 mutation test provided by Roche Molecular Systems is the diagnostic test to confirm eligibility for treatment. FDA approved on August 17, 2011 under the company Hoffmann La Roche.
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Zelboraftablet240 mgoral05-03-2012Canada
Zelboraftablet, film coated240 mg/1oral17-08-2011US

Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
ZelborafVemurafenib
ZelborafVemurafenib

Categories
  • No Category

Pharmacology

Indication: Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
Pharmacodynamics: Not Available
Mechanism of action: Vemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
Absorption: After oral administration of vemurafenib, it is well absorbed. Bioavailability is unknown. Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. Exposure is highly variable between different patients. Gastrointestinal fluid content, pH, volumes, motility, transition time and bile composition may be factors affecting exposure. It is unknown how food affects the absorption of vemurafenib. Time to steady state = 15 - 22 days
Volume of distribution:
    106 L

Protein binding: >99% protein bound to serum albumin and alpha-1 acid glycoprotein.
Metabolism: Not Available
Route of elimination: Excreted via feces (94%) and urine (1%).
Half life: Elimination half-life = 57 hours (range of 30-120 hours)
Clearance: Not Available
Toxicity: Not Available
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Not Available

Packagers:
  • Not Available

Dosage forms
FormRouteStrength
Tabletoral240 mg
Tablet, film coatedoral240 mg/1

Prices
Unit descriptionCostUnit

Patents
CountryPatent NumberApprovedExpires (estimated)
7504509United States2011-08-172026-10-22
7863288United States2011-08-172029-06-20
8143271United States2011-08-172026-06-21

Interactions

Drug Interactions
DrugInteraction
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Vemurafenib.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Vemurafenib.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Vemurafenib.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.
AprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Vemurafenib.
AtazanavirThe serum concentration of Vemurafenib can be increased when it is combined with Atazanavir.
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Vemurafenib.
BexaroteneThe serum concentration of Vemurafenib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Vemurafenib can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Vemurafenib.
BosentanThe serum concentration of Vemurafenib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Vemurafenib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Vemurafenib.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Vemurafenib.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Vemurafenib.
CarbamazepineThe serum concentration of Vemurafenib can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Vemurafenib can be increased when it is combined with Ceritinib.
CitalopramCitalopram may increase the QTc-prolonging activities of Vemurafenib.
ClarithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Clarithromycin.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Vemurafenib.
CobicistatThe serum concentration of Vemurafenib can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Vemurafenib.
ConivaptanThe serum concentration of Vemurafenib can be increased when it is combined with Conivaptan.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Vemurafenib.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Vemurafenib.
DabrafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Dabrafenib.
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Vemurafenib.
DarunavirThe serum concentration of Vemurafenib can be increased when it is combined with Darunavir.
DeferasiroxThe serum concentration of Vemurafenib can be decreased when it is combined with Deferasirox.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Vemurafenib.
DofetilideDofetilide may increase the QTc-prolonging activities of Vemurafenib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Vemurafenib.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Vemurafenib.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Vemurafenib.
EnzalutamideThe serum concentration of Vemurafenib can be decreased when it is combined with Enzalutamide.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Vemurafenib.
FluconazoleThe metabolism of Vemurafenib can be decreased when combined with Fluconazole.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Vemurafenib.
FluvoxamineThe serum concentration of Fluvoxamine can be increased when it is combined with Vemurafenib.
FosaprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Vemurafenib can be increased when it is combined with Fusidic Acid.
GoserelinGoserelin may increase the QTc-prolonging activities of Vemurafenib.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Vemurafenib.
IdelalisibThe serum concentration of Vemurafenib can be increased when it is combined with Idelalisib.
IndinavirThe serum concentration of Vemurafenib can be increased when it is combined with Indinavir.
IpilimumabIpilimumab may increase the hepatotoxic activities of Vemurafenib.
ItraconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Vemurafenib.
IvacaftorThe serum concentration of Vemurafenib can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Ketoconazole.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Vemurafenib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Vemurafenib.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Vemurafenib.
LuliconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Luliconazole.
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.
MifepristoneMifepristone may increase the QTc-prolonging activities of Vemurafenib.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Vemurafenib.
MitotaneThe serum concentration of Vemurafenib can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Vemurafenib.
NefazodoneThe serum concentration of Vemurafenib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Vemurafenib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Vemurafenib can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Vemurafenib.
OctreotideOctreotide may increase the QTc-prolonging activities of Vemurafenib.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Vemurafenib.
PalbociclibThe serum concentration of Vemurafenib can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.
PhenobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Phenytoin.
PirfenidoneThe serum concentration of Pirfenidone can be increased when it is combined with Vemurafenib.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Vemurafenib.
PorfimerVemurafenib may increase the photosensitizing activities of Porfimer.
PosaconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Vemurafenib can be decreased when it is combined with Primidone.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Vemurafenib.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Vemurafenib.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Vemurafenib.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Vemurafenib.
RifabutinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Vemurafenib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Vemurafenib.
RitonavirThe serum concentration of Vemurafenib can be increased when it is combined with Ritonavir.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Vemurafenib.
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Vemurafenib.
SaquinavirThe serum concentration of Vemurafenib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Vemurafenib.
SiltuximabThe serum concentration of Vemurafenib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Vemurafenib can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Vemurafenib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Vemurafenib can be increased when it is combined with Stiripentol.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Vemurafenib.
TelaprevirThe serum concentration of Vemurafenib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Telithromycin.
TesmilifeneThe serum concentration of Vemurafenib can be decreased when it is combined with Tesmilifene.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Vemurafenib.
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Vemurafenib.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
TocilizumabThe serum concentration of Vemurafenib can be decreased when it is combined with Tocilizumab.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Vemurafenib.
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Vemurafenib.
VerapamilThe serum concentration of Vemurafenib can be increased when it is combined with Verapamil.
VerteporfinVemurafenib may increase the photosensitizing activities of Verteporfin.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Vemurafenib.
VoriconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Vemurafenib.

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Acetophenones
  • Aminosulfonyl compounds
  • Aryl chlorides
  • Aryl fluorides
  • Aryl ketones
  • Azacyclic compounds
  • Benzoyl derivatives
  • Chlorobenzenes
  • Fluorobenzenes
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • Organochlorides
  • Organofluorides
  • Organonitrogen compounds
  • Pyrrolopyridines
  • Substituted pyrroles
  • Sulfanilides
  • Sulfonamides
  • Vinylogous amides
  • Vinylogous halides

substituent:
  • 3-phenylpyridine
  • Acetophenone
  • Aminosulfonyl compound
  • Aromatic heteropolycyclic compound
  • Aryl chloride
  • Aryl fluoride
  • Aryl halide
  • Aryl ketone
  • Azacycle
  • Benzenoid
  • Benzoyl
  • Chlorobenzene
  • Fluorobenzene
  • Halobenzene
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Ketone
  • Monocyclic benzene moiety
  • Organochloride
  • Organofluoride
  • Organohalogen compound
  • Organonitrogen compound
  • Organooxygen compound
  • Organosulfur compound
  • Pyrrole
  • Pyrrolopyridine
  • Substituted pyrrole
  • Sulfanilide
  • Sulfonamide
  • Sulfonic acid derivative
  • Sulfonyl
  • Vinylogous amide
  • Vinylogous halide

References

Synthesis Reference: Not Available
General Reference: # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23094782
External Links:
ResourceLink
RxListhttp://www.rxlist.com/zelboraf-drug.htm
Drugs.comhttp://www.drugs.com/mtm/vemurafenib.html

ATC Codes:
  • Array

AHFS Codes:
  • 10:00

MSDS: Download
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