Identification

Name
Vinorelbine
Accession Number
DB00361  (APRD00101)
Type
Small Molecule
Groups
Approved, Investigational
Description

Vinorelbine is an anti-mitotic chemotherapy drug that is used in the treatment of several types of malignancies, including breast cancer and non-small cell lung cancer (NSCLC) [5]. It was initially approved in the USA in 1990's for the treatment of NSCLC [13].

It is a third-generation vinca alkaloid. The introduction of third-generation drugs (vinorelbine, gemcitabine, taxanes) in platinum combination improved survival of patients with advanced NSCLC, with very similar results from the various drugs. Treatment toxicities are considerable in the combination treatment setting [2].

A study was done on the clearance rate of vinorelbine on individuals with various single polymorphonuclear mutations. It was found that there was 4.3-fold variation in vinorelbine clearance across the cohort, suggesting a strong influence of genetics on the clearance of this drug [7].

Structure
Thumb
Synonyms
  • 5'-Noranhydrovinblastine
  • Vinorelbin
  • Vinorelbina
  • Vinorelbine
  • Vinorelbinum
External IDs
KW 2307 base
Product Ingredients
IngredientUNIICASInChI Key
Vinorelbine tartrate253GQW851Q125317-39-7CILBMBUYJCWATM-KRQCOKQWSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NavelbineInjection10 mg/mLIntravenousPierre Fabre Laboratories2005-11-15Not applicableUs
NavelbineSolution10 mgIntravenousPierre Fabre Pharma Canada Inc1994-12-312012-10-01Canada
Vinorelbine InjectionSolution10 mgIntravenousFresenius Kabi2009-03-31Not applicableCanada
Vinorelbine Injection, USPSolution10 mgIntravenousGeneric Medical Partners Inc2017-08-01Not applicableCanada
Vinorelbine Injection, USPSolution10 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Vinorelbine Tartrate for InjectionSolution10 mgIntravenousTeva2007-05-09Not applicableCanada
Vinorelbine Tartrate for InjectionSolution10 mgIntravenousPfizer2004-12-22Not applicableCanada
Vinorelbine Tartrate Injection USPSolution10 mgIntravenousSandoz Canada IncorporatedNot applicableNot applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aj-vinorelbineSolution10 mgIntravenousAgila Jamp Canada IncNot applicableNot applicableCanada
VinorelbineInjection, solution10 mg/mLIntravenousPfizer Laboratories Div Pfizer Inc.2012-09-012017-09-29Us
VinorelbineInjection, solution, concentrate10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2003-03-012018-01-31Us
VinorelbineInjection, solution10 mg/mLIntravenousMylan Institutional2012-09-012017-09-29Us
VinorelbineInjection, solution10 mg/mLIntravenousPfizer Laboratories Div Pfizer Inc.2012-09-012017-09-29Us
VinorelbineInjection, solution10 mg/mLIntravenousMylan Institutional2012-09-012017-09-28Us
VinorelbineInjection, solution10 mg/mLIntravenousActavis Pharma Company2009-09-14Not applicableUs
VinorelbineInjection, solution10 mg/mLIntravenousPfizer Laboratories Div Pfizer Inc.2012-09-012017-09-29Us
VinorelbineInjection, solution, concentrate50 mg/5mLIntravenousTeva Parenteral Medicines, Inc.2003-03-012018-01-31Us
VinorelbineInjection, solution10 mg/mLIntravenousMylan Institutional2012-09-012017-09-29Us
International/Other Brands
Bendarelbin (Bendalis) / Eberelbin (Ebewe) / Eunexon (AC Farma) / Eurovinorelbin (Lapharm) / Filcrin (Filaxis) / Navelbin (Pierre Fabre) / Navildez (Cryopharma) / Navin (Cancernova) / Navirel (medac) / Neocitec (Sandoz) / Renovel (Mustafa Nevzat) / Riborelbin (Ribosepharm) / Vilne (Dosa) / Vinelbine (GP-Pharm) / Vinorayne (Hospira) / Vinorel (Eriochem) / Vinorgen (Bago) / Vinotel (Fresenius) / Zinavin (Novamed)
Categories
UNII
Q6C979R91Y
CAS number
71486-22-1
Weight
Average: 778.947
Monoisotopic: 778.394164715
Chemical Formula
C45H54N4O8
InChI Key
GBABOYUKABKIAF-IELIFDKJSA-N
InChI
InChI=1S/C45H54N4O8/c1-8-27-19-28-22-44(40(51)55-6,36-30(25-48(23-27)24-28)29-13-10-11-14-33(29)46-36)32-20-31-34(21-35(32)54-5)47(4)38-43(31)16-18-49-17-12-15-42(9-2,37(43)49)39(57-26(3)50)45(38,53)41(52)56-7/h10-15,19-21,28,37-39,46,53H,8-9,16-18,22-25H2,1-7H3/t28-,37-,38+,39+,42+,43+,44-,45-/m0/s1
IUPAC Name
methyl (1R,9R,10S,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(12S,14R)-16-ethyl-12-(methoxycarbonyl)-1,10-diazatetracyclo[12.3.1.0^{3,11}.0^{4,9}]octadeca-3(11),4,6,8,15-pentaen-12-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.0^{1,9}.0^{2,7}.0^{16,19}]nonadeca-2,4,6,13-tetraene-10-carboxylate
SMILES
[H][[email protected]@]12N(C)C3=CC(OC)=C(C=C3[[email protected]@]11CCN3CC=C[[email protected]](CC)([[email protected]@]13[H])[[email protected]@]([H])(OC(C)=O)[[email protected]]2(O)C(=O)OC)[[email protected]]1(C[[email protected]@]2([H])CN(CC(CC)=C2)CC2=C1NC1=CC=CC=C21)C(=O)OC

Pharmacology

Indication

Vinorelbine tartrate is indicated for adults in the treatment of advanced non-small cell lung cancer (NSCLC), as a single therapy or in combination with other chemotherapeutic drugs [5].

Used in relapsed or refractory Hodgkin lymphoma, in combination with other chemotherapy agents [14].

For the treatment of desmoid tumor or aggressive fibromatosis, in combination with methotrexate [14].

For the treatment of recurrent or metastatic squamous cell head and neck cancer [14].

For the treatment of recurrent ovarian cancer [14].

For the treatment of metastatic breast cancer, in patients previously treated with anthracyline and/or taxane therapy [14].

For the treatment of HER2-positive, trastuzumab-resistant, advanced breast cancer in patients previously treated with a taxane, in combination with trastuzumab and everolimus [14].

Structured Indications
Pharmacodynamics

Vinorelbine is a semi-synthetic vinca-alkaloid with a wide spectrum of anti-tumor activity. The vinca-alkaloids are considered spindle poisons. They work by interfering with the polymerization of tubulin, a protein responsible for building the microtubule system which appears during cell division in proliferating cancer cells [11].

Mechanism of action

Vinca alkaloids are structurally similar compounds composed of two multi-ringed units, vindoline, and catharanthine. Vinorelbine tartrate is a vinca alkaloid in which the catharanthine component is the target of structural modification [9], [10].

This structural modification contributes to unique pharmacologic properties.The antitumor activity of vinorelbine tartrate is believed to be owed to the inhibition of mitosis at metaphase via its interaction with tubulin [5].

Vinorelbine is a mitotic spindle poison that interferes with chromosomal segregation during mitosis, also known as cell division. It pauses cells at the G2/M phases, when present at concentrations close to the half maximal inhibitory concentration (IC50). Microtubules, which are derived from polymers of tubulin, are the main target of vinorelbine.

The chemical modification used to produce vinorelbine allows for the opening of the eight-member catharanthine ring with the formation of both a covalent and reversible bond with tubulin [11].

The relative contribution of different microtubule-associated proteins in the production of tubulin vary between neural tissue and proliferating cells and this has important functional implications. The ability of vinorelbine to bind specifically to mitotic rather than other microtubules has been shown and may suggest that neurotoxicity is less likely to be a problem than with the molecular mechanism of action [11].

As with other anti-microtubule agents, vinorelbine is known to contribute apoptosis in malignant cells. The exact mechanisms by which this process occurs are complex and many details are yet to be elucidated. The disarray of the microtubule structure has a number of effects, including the induction of tumor suppressor gene p53 and activation/inactivation of a number of protein kinases involved in essential signaling pathways, including p21 WAF1/CIP1 and Ras/Raf, PKC/PKA. These molecular changes lead to phosphorylation and consequently inactivation of the apoptosis inhibitor Bcl2. This, in turn, results in a decrease in the formation of heterodimers between Bcl2 and the pro-apoptotic gene BAX, stimulating the sequence of cell apoptosis [11].

Vinorelbine tartrate also possibly interferes with amino acid, cyclic AMP and glutathione metabolism, calmodulin-dependent Ca++-transport ATPase activity, cellular respiration, and nucleic acid and lipid biosynthesis [5].

TargetActionsOrganism
ATubulin beta chain
antagonist
inhibitor
Human
Absorption

Vinorelbine is rapidly absorbed with peak serum concentration reached within 2 hours [5].

Vinorelbine is highly bound to platelets and lymphocytes and is also bound to alpha 1-acid glycoprotein, albumin, and lipoproteins [4].

Volume of distribution

The volume of distribution is large, indicating extensive extravascular distribution [4].

The steady-state volume of distribution values range from 25.4 to 40.1 L/kg, according to one study [7].

Widely distributed, with highest amounts found in elimination organs such as liver and kidneys, minimal in heart and brain [7].

Protein binding

80-90% [6]

Metabolism

Vinorelbine undergoes substantial hepatic elimination in humans. Two metabolites of vinorelbine have been identified in human blood, plasma, and urine; vinorelbine N-oxide and deacetylvinorelbine. Deacetylvinorelbine has been demonstrated to be the primary metabolite of vinorelbine in humans, and has been shown to possess antitumor activity similar to vinorelbine [9], [10].

Vinorelbine is metabolized into two other minor metabolites, 20'-hydroxyvinorelbine and vinorelbine 6'-oxide [10].

Therapeutic doses of vinorelbine (30 mg/m2) yield very small, if any, quantifiable levels of either metabolite in blood or urine. The metabolism of vinorelbine is mediated by hepatic cytochrome P450 isoenzymes in the CYP3A subfamily [8], [4].

As the liver provides the main route for metabolism of the drug, patients with hepatic impairment may demonstrate increased toxicity with standard dosing, however, there are no available data on this. Likewise, the contribution of cytochrome P450 enzyme action to vinorelbine metabolism has potential implications in patients receiving other drugs metabolized by this route [11].

Route of elimination

Vinorelbine undergoes substantial hepatic elimination in humans, with large amounts recovered in feces after intravenous administration to humans [5].

Urinary excretion of unchanged drug accounts for less than 20% of an intravenous dose, with fecal elimination accounting for an additional 30% to 60% [4].

After intravenous administration of radioactive vinorelbine, approximately 18% and 46% of administered radioactivity was recovered in urine and feces, respectively [7].

Half life

The terminal phase half-life averaged 27.7 to 43.6 hours; the mean plasma clearances ranged from 0.97 to 1.26 L/hr/kg [4].

Clearance

The plasma clearance of vinorelbine is high, approaching the same as hepatic blood flow in humans, and its volume of distribution is large, indicating extensive extravascular distribution. In comparison to vinblastine or vincristine [4].

The clearance was found to be in the range of 0.29-1./26 L/ per kg in 4 clinical trials of patients receiving 30 mg/m2 of vinorelbine [12].

Toxicity

Due to the wide array of adverse effects of this drug, the toxicity of is categorized into organ systems [5].

Hematologic: Granulocytopenia was the primary dose-limiting toxicity with vinorelbine tartrate therapy; it is generally reversible and not cumulative. In one study, granulocytopenia resulted in hospitalizations for fever and/or sepsis in 8% of NSCLC and 9% of breast cancer patients [5]. Infectious (septic) deaths occurred in about 1% of patients. Grade 3 or 4 anemia occurred in about 1% of lung cancer and approximately 14% of breast cancer patients. Blood transfusions were administered to 18% of patients who received vinorelbine tartrate therapy. The incidence of Grade 3 and 4 thrombocytopenia was found to be less than 1% [5].

Neurologic: Mild to moderate peripheral neuropathy may occur. Symptoms of paresthesia and hypesthesia are reported as the most commonly reported neurologic toxicities of this drug. The loss of deep tendon reflexes (DTR) occurs in less than 5% of patients, according to one study. The development of severe peripheral neuropathy is rare [5].

Dermatologic: Alopecia has been reported in only about 12% of patients and is usually reported as mild. Vinorelbine tartrate is a moderate vesicant, leading to injection site reactions. Symptoms include erythema, pain at the injection site and vein discoloration occurred in about 1/3 of all patients. Chemical phlebitis along the vein, near the site of injection, has been reported [5].

Respiratory: Shortness of breath was reported in 3% of NSCLC and 9% of breast cancer patients, and was severe in 2% of each patient population. Interstitial pulmonary changes have been documented in a few patients [5].

Gastrointestinal: Mild or moderate nausea symptoms occurred in 32% of NSCLC and 47% of breast cancer patients treated with vinorelbine tartrate. Severe nausea was occurred infrequently (1% and 3% in NSCLC and breast cancer patients, respectively). Prophylactic administration of anti-emetics was not routine in patients treated with single-agent vinorelbine tartrate. Constipation occurred in about 28% of NSCLC and 38% of breast cancer patients. The paralytic ileus incidence of less than 2% of patients. Vomiting, diarrhea, anorexia and stomatitis were found to be mild or moderate and occurred in less than 20% of study patients [5].

Hepatic: Transient elevations of liver enzymes were reported without clinical symptoms. Cardiovascular: Chest pain was reported in 5% of NSCLC and 8% of breast cancer patients. Most reports of chest pain were in patients who had either a history of cardiovascular disease or tumor within the chest. There have been rare reports of myocardial infarction; however, these have not been shown definitely attributable to vinorelbine tartrate [8].

Other: Muscle weakness (asthenia) occurred in about 25% of patients with NSCLC and 41% of patients with breast cancer. It was usually mild or moderate but showed a linear increase with cumulative doses [8].

Several other toxicities reported in approximately 5% of patients include jaw pain, myalgia, arthralgia, headache, dysphagia, and skin rash. Hemorrhagic cystitis (bladder inflammation with blood in urine) and the syndrome of inappropriate ADH secretion were both reported in less than 1% of patients. The treatment of these entities are mainly symptomatic [8].

The carcinogenic potential of Vinorelbine has not been adequately studied. Vinorelbine has been demonstrated to affect chromosome number and likely the chromosome structure in vivo (polyploidy in bone marrow cells from Chinese hamsters and a positive micronucleus test in mice were observed) [8].

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Vinorelbine Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Vinorelbine can be increased when it is combined with Abiraterone.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Vinorelbine.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Vinorelbine.Experimental
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Vinorelbine.Approved
AmiodaroneThe metabolism of Vinorelbine can be decreased when combined with Amiodarone.Approved, Investigational
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Vinorelbine.Approved, Investigational, Withdrawn
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Anthrax immune globulin human.Approved
ApalutamideThe serum concentration of Vinorelbine can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Vinorelbine can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Vinorelbine can be decreased when combined with Artemether.Approved
AsunaprevirThe serum concentration of Asunaprevir can be increased when it is combined with Vinorelbine.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Vinorelbine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Vinorelbine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Atorvastatin.Approved
Bacillus calmette-guerin substrain connaught live antigenThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Bacillus calmette-guerin substrain connaught live antigen.Approved, Investigational
Bacillus calmette-guerin substrain tice live antigenThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Bacillus calmette-guerin substrain tice live antigen.Approved
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Vinorelbine.Investigational
BetaxololThe metabolism of Vinorelbine can be decreased when combined with Betaxolol.Approved, Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Vinorelbine.Approved, Investigational
BoceprevirThe metabolism of Vinorelbine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Vinorelbine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Vinorelbine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Vinorelbine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Vinorelbine.Approved, Investigational
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Vinorelbine.Approved, Investigational
BupropionThe metabolism of Vinorelbine can be decreased when combined with Bupropion.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Vinorelbine.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Vinorelbine.Approved
CarbamazepineThe metabolism of Vinorelbine can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Vinorelbine can be increased when it is combined with Carbomycin.Vet Approved
CelecoxibThe metabolism of Vinorelbine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Vinorelbine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Vinorelbine.Approved, Withdrawn
ChloroquineThe metabolism of Vinorelbine can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorpromazineThe metabolism of Vinorelbine can be decreased when combined with Chlorpromazine.Approved, Investigational, Vet Approved
CholecalciferolThe metabolism of Vinorelbine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Vinorelbine can be decreased when combined with Cimetidine.Approved, Investigational
CinacalcetThe metabolism of Vinorelbine can be decreased when combined with Cinacalcet.Approved
CisplatinThe risk or severity of adverse effects can be increased when Cisplatin is combined with Vinorelbine.Approved
CitalopramThe metabolism of Vinorelbine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Vinorelbine can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Vinorelbine can be decreased when combined with Clemastine.Approved, Investigational
ClobazamThe metabolism of Vinorelbine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Vinorelbine can be decreased when combined with Clomipramine.Approved, Investigational, Vet Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Vinorelbine is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).Approved
ClotrimazoleThe metabolism of Vinorelbine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Clozapine.Approved
CobicistatThe serum concentration of Vinorelbine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Vinorelbine can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Vinorelbine.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Vinorelbine.Approved, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Vinorelbine is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CrizotinibThe metabolism of Vinorelbine can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Vinorelbine.Approved, Investigational
CyclosporineThe metabolism of Vinorelbine can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Vinorelbine.Experimental
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Vinorelbine.Approved
DabrafenibThe serum concentration of Vinorelbine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DarifenacinThe metabolism of Vinorelbine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Vinorelbine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Vinorelbine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Vinorelbine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Vinorelbine can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Vinorelbine.Approved
DesipramineThe metabolism of Vinorelbine can be decreased when combined with Desipramine.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Vinorelbine.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Vinorelbine.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Vinorelbine.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Vinorelbine.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Vinorelbine.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Vinorelbine.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Vinorelbine.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Vinorelbine.Approved, Investigational
DiltiazemThe metabolism of Vinorelbine can be decreased when combined with Diltiazem.Approved, Investigational
DiphenhydramineThe metabolism of Vinorelbine can be decreased when combined with Diphenhydramine.Approved, Investigational
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Vinorelbine.Approved, Investigational
DosulepinThe metabolism of Vinorelbine can be decreased when combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Vinorelbine.Approved, Investigational
DoxycyclineThe metabolism of Vinorelbine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Vinorelbine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Vinorelbine can be decreased when combined with Duloxetine.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Vinorelbine.Approved
EliglustatThe metabolism of Vinorelbine can be decreased when combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Vinorelbine can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Vinorelbine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Vinorelbine.Approved
ErythromycinThe serum concentration of Vinorelbine can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Vinorelbine.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vinorelbine.Approved
FingolimodVinorelbine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe metabolism of Vinorelbine can be decreased when combined with Fluconazole.Approved, Investigational
FluoxetineThe metabolism of Vinorelbine can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Vinorelbine.Approved
FluvoxamineThe metabolism of Vinorelbine can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Vinorelbine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Vinorelbine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Vinorelbine can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Vinorelbine can be increased when it is combined with Fusidic Acid.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Vinorelbine is combined with G17DT.Investigational
GefitinibGefitinib may increase the neutropenic activities of Vinorelbine.Approved, Investigational
GI-5005The risk or severity of adverse effects can be increased when Vinorelbine is combined with GI-5005.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Vinorelbine.Experimental
HaloperidolThe metabolism of Vinorelbine can be decreased when combined with Haloperidol.Approved
Hepatitis A VaccineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Vinorelbine is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
Human rabies virus immune globulinThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Human rabies virus immune globulin.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Vinorelbine.Approved
IdelalisibThe metabolism of Vinorelbine can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Vinorelbine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Vinorelbine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Vinorelbine can be decreased when combined with Indinavir.Approved
INGN 201The risk or severity of adverse effects can be increased when Vinorelbine is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Vinorelbine is combined with INGN 225.Investigational
IsavuconazoleThe serum concentration of Vinorelbine can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Vinorelbine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Vinorelbine can be decreased when combined with Isoniazid.Approved, Investigational
IsradipineThe metabolism of Vinorelbine can be decreased when combined with Isradipine.Approved, Investigational
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Vinorelbine.Approved, Investigational
IvacaftorThe serum concentration of Vinorelbine can be increased when it is combined with Ivacaftor.Approved
Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Vinorelbine is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated).Approved
JosamycinThe serum concentration of Vinorelbine can be increased when it is combined with Josamycin.Approved, Investigational
KetoconazoleThe metabolism of Vinorelbine can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Vinorelbine can be increased when it is combined with Kitasamycin.Experimental
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Vinorelbine.Experimental
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Vinorelbine.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Leflunomide.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Vinorelbine.Approved, Investigational
LopinavirThe metabolism of Vinorelbine can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Vinorelbine can be decreased when combined with Lorcaserin.Approved
LorpiprazoleThe serum concentration of Vinorelbine can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Vinorelbine.Approved, Investigational
LuliconazoleThe serum concentration of Vinorelbine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Vinorelbine can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Vinorelbine can be decreased when combined with Lumefantrine.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Vinorelbine.Illicit, Investigational, Withdrawn
ManidipineThe metabolism of Vinorelbine can be decreased when combined with Manidipine.Approved, Investigational
MetamizoleThe risk or severity of myelosuppression can be increased when Metamizole is combined with Vinorelbine.Approved, Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Vinorelbine.Experimental
MethadoneThe metabolism of Vinorelbine can be decreased when combined with Methadone.Approved
MethotrimeprazineThe metabolism of Vinorelbine can be decreased when combined with Methotrimeprazine.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Vinorelbine.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Vinorelbine.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Vinorelbine.Experimental
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Vinorelbine.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Vinorelbine.Experimental
MidostaurinThe metabolism of Vinorelbine can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Vinorelbine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Vinorelbine can be decreased when combined with Mirabegron.Approved
MitomycinThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Mitomycin.Approved
MitotaneThe serum concentration of Vinorelbine can be decreased when it is combined with Mitotane.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Vinorelbine.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Natalizumab.Approved, Investigational
NefazodoneThe metabolism of Vinorelbine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Vinorelbine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Vinorelbine can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Vinorelbine can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Vinorelbine can be decreased when combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Vinorelbine.Approved, Investigational
NilotinibThe metabolism of Vinorelbine can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Vinorelbine.Approved
OcrelizumabOcrelizumab may increase the immunosuppressive activities of Vinorelbine.Approved, Investigational
OlaparibThe metabolism of Vinorelbine can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Vinorelbine can be increased when it is combined with Oleandomycin.Vet Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Vinorelbine.Experimental, Investigational
OsimertinibThe serum concentration of Vinorelbine can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Vinorelbine.Approved
PaclitaxelPaclitaxel may increase the neurotoxic activities of Vinorelbine.Approved, Vet Approved
PalbociclibThe serum concentration of Vinorelbine can be increased when it is combined with Palbociclib.Approved, Investigational
PanobinostatThe serum concentration of Vinorelbine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Vinorelbine can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vinorelbine.Approved
Peginterferon alfa-2bThe serum concentration of Vinorelbine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Vinorelbine can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Vinorelbine.Approved, Investigational, Vet Approved, Withdrawn
PeruvosidePeruvoside may decrease the cardiotoxic activities of Vinorelbine.Experimental
PhenobarbitalThe metabolism of Vinorelbine can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Vinorelbine can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Vinorelbine.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Vinorelbine.Approved
PitolisantThe serum concentration of Pitolisant can be increased when it is combined with Vinorelbine.Approved, Investigational
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Vinorelbine.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Vinorelbine.Approved
PrimidoneThe metabolism of Vinorelbine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Vinorelbine can be decreased when combined with Promazine.Approved, Vet Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Vinorelbine.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Vinorelbine.Approved
QuinidineThe metabolism of Vinorelbine can be decreased when combined with Quinidine.Approved, Investigational
QuinineThe metabolism of Vinorelbine can be decreased when combined with Quinine.Approved
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Rabies virus inactivated antigen, A.Approved, Investigational
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Vinorelbine.Approved, Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Vinorelbine.Approved, Investigational
RifabutinThe metabolism of Vinorelbine can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Vinorelbine can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Vinorelbine can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Vinorelbine.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Vinorelbine.Approved
RindopepimutThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Rindopepimut.Investigational
RitonavirThe metabolism of Vinorelbine can be decreased when combined with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Vinorelbine.Approved
RolapitantThe metabolism of Vinorelbine can be decreased when combined with Rolapitant.Approved, Investigational
RopiniroleThe metabolism of Vinorelbine can be decreased when combined with Ropinirole.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Vinorelbine.Approved
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Rubella virus vaccine.Approved, Investigational
RucaparibThe metabolism of Vinorelbine can be decreased when combined with Rucaparib.Approved, Investigational
Salmonella typhi ty2 vi polysaccharide antigenThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Salmonella typhi ty2 vi polysaccharide antigen.Approved
Salmonella typhi ty21a live antigenThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Salmonella typhi ty21a live antigen.Approved
SaquinavirThe metabolism of Vinorelbine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Vinorelbine can be decreased when used in combination with Sarilumab.Approved, Investigational
SertralineThe metabolism of Vinorelbine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Vinorelbine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Vinorelbine.Approved
SiltuximabThe serum concentration of Vinorelbine can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Vinorelbine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Vinorelbine.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Vinorelbine.Approved, Investigational
SolithromycinThe serum concentration of Vinorelbine can be increased when it is combined with Solithromycin.Investigational
SpiramycinThe serum concentration of Vinorelbine can be increased when it is combined with Spiramycin.Approved
SRP 299The risk or severity of adverse effects can be increased when Vinorelbine is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Vinorelbine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Vinorelbine can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Vinorelbine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusTacrolimus may increase the immunosuppressive activities of Vinorelbine.Approved, Investigational
TecemotideThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Tecemotide.Investigational
TelaprevirThe metabolism of Vinorelbine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Vinorelbine can be decreased when combined with Telithromycin.Approved
TerbinafineThe metabolism of Vinorelbine can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Vinorelbine.Experimental
TG4010The risk or severity of adverse effects can be increased when Vinorelbine is combined with TG4010.Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Vinorelbine.Approved, Withdrawn
TiclopidineThe metabolism of Vinorelbine can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Vinorelbine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Vinorelbine can be decreased when it is combined with Tocilizumab.Approved
TofacitinibVinorelbine may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Vinorelbine.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Vinorelbine.Approved, Investigational
TranylcypromineThe metabolism of Vinorelbine can be decreased when combined with Tranylcypromine.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Vinorelbine.Approved, Investigational
TylosinThe serum concentration of Vinorelbine can be increased when it is combined with Tylosin.Vet Approved
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Vinorelbine is combined with Varicella Zoster Vaccine (Live/Attenuated).Approved
VemurafenibThe serum concentration of Vinorelbine can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Vinorelbine can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Vinorelbine can be decreased when combined with Verapamil.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Vinorelbine.Approved, Investigational
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Vinorelbine.Approved, Investigational
Yellow Fever VaccineThe risk or severity of adverse effects can be increased when Vinorelbine is combined with Yellow Fever Vaccine.Approved, Investigational
ZiprasidoneThe metabolism of Vinorelbine can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

General References
  1. Marty M, Fumoleau P, Adenis A, Rousseau Y, Merrouche Y, Robinet G, Senac I, Puozzo C: Oral vinorelbine pharmacokinetics and absolute bioavailability study in patients with solid tumors. Ann Oncol. 2001 Nov;12(11):1643-9. [PubMed:11822766]
  2. Piccirillo MC, Daniele G, Di Maio M, Bryce J, De Feo G, Del Giudice A, Perrone F, Morabito A: Vinorelbine for non-small cell lung cancer. Expert Opin Drug Saf. 2010 May;9(3):493-510. doi: 10.1517/14740331003774078. [PubMed:20350282]
  3. Bahadori F, Topcu G, Eroglu MS, Onyuksel H: A new lipid-based nano formulation of vinorelbine. AAPS PharmSciTech. 2014 Oct;15(5):1138-48. doi: 10.1208/s12249-014-0146-3. Epub 2014 May 29. [PubMed:24871553]
  4. Wargin WA, Lucas VS: The clinical pharmacokinetics of vinorelbine (Navelbine). Semin Oncol. 1994 Oct;21(5 Suppl 10):21-7. [PubMed:7973765]
  5. Vinorelbine Tartrate [Link]
  6. Vinorelbine, Ontario Cancer Care [Link]
  7. Predictors of Vinorelbine Pharmacokinetics and Pharmacodynamics in Patients With Cancer [Link]
  8. Vinorelbine injection, Daily Med [Link]
  9. Metabolism pathway of vinorelbine (Navelbine®) in human: Characterisation of the metabolites by HPLC–MS/MS [Link]
  10. Vinca Alkaloid Pharmacokinetics [Link]
  11. Vinorelbine, a clinical review [Link]
  12. Vinorelbine FDA pharmacology review [Link]
  13. Drug Approval Package [Link]
  14. Navelbine, PDR [Link]
External Links
Human Metabolome Database
HMDB0014505
KEGG Drug
D08680
PubChem Compound
44424639
PubChem Substance
46507772
ChemSpider
4470974
ChEBI
480999
ChEMBL
CHEMBL553025
Therapeutic Targets Database
DAP000765
PharmGKB
PA451881
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Vinorelbine
ATC Codes
L01CA04 — Vinorelbine
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (102 KB)
MSDS
Download (155 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingBasic ScienceCancer, Breast1
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedPreventionLeukemias / Multiple Myeloma (MM)1
1CompletedTreatmentAdvanced Malignant Solid Tumors1
1CompletedTreatmentAdvanced Neoplasm1
1CompletedTreatmentBladder Cancers / Cervical Cancers / Endometrial Cancers / Vaginal Cancers1
1CompletedTreatmentCancer of the Ovary / Cancer, Breast / Cancers / Lung Cancers1
1CompletedTreatmentCancer, Breast4
1CompletedTreatmentCancer, Breast / Lung Cancer Non-Small Cell Cancer (NSCLC) / Non-Hodgkin's Lymphoma (NHL)1
1CompletedTreatmentEstrogen Receptor-negative Breast Cancer / HER2-Negative Breast Cancer / Hereditary Breast/Ovarian Cancer - BRCA1 / Hereditary Breast/Ovarian Cancer - BRCA2 / Male Breast Cancer / Progesterone Receptor-negative Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer / Triple-Negative Breast Cancer (TNBC)1
1CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Hereditary Paraganglioma / Male Breast Cancer / Metastatic Gastrointestinal Carcinoid Tumor / Metastatic Pheochromocytoma / Pancreatic Polypeptide Tumor / Paraganglion neoplasm malignant / Recurrent Breast Cancer / Recurrent Cervical Cancer / Recurrent Endometrial Carcinoma / Recurrent Gastrointestinal Carcinoid Tumor / Recurrent Islet Cell Carcinoma / Recurrent Neuroendocrine Carcinoma of the Skin / Recurrent Non-small Cell Lung Cancer / Recurrent Ovarian Epithelial Cancer / Recurrent Ovarian Germ Cell Tumor / Recurrent Pheochromocytoma / Recurrent Prostate Cancer / Recurrent Renal Cell Cancer / Recurrent Small Cell Lung Cancer / Recurrent Uterine Sarcoma / Regional Gastrointestinal Carcinoid Tumor / Regional Pheochromocytoma / Stage III Cervical Cancer / Stage III Endometrial Carcinoma / Stage III Neuroendocrine Carcinoma of the Skin / Stage III Ovarian Epithelial Cancer / Stage III Ovarian Germ Cell Tumor / Stage III Prostate Cancer / Stage III Renal Cell Cancer / Stage III Uterine Sarcoma / Stage IIIA Breast Cancer / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Breast Cancer / Stage IIIb Non-small Cell Lung Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Stage IV Endometrial Carcinoma / Stage IV Neuroendocrine Carcinoma of the Skin / Stage IV Non-Small Cell Lung Cancer / Stage IV Ovarian Epithelial Cancer / Stage IV Ovarian Germ Cell Tumor / Stage IV Prostate Cancer / Stage IV Renal Cell Cancer / Stage IV Uterine Sarcoma / Stage IVA Cervical Cancer / Stage IVB Cervical Cancer / Thyroid Gland Medullary Carcinoma1
1CompletedTreatmentLeukemias1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)4
1CompletedTreatmentLung Cancers1
1CompletedTreatmentMalignant Lymphomas1
1CompletedTreatmentMetastatic Breast Cancer (MBC)1
1CompletedTreatmentNon-Squamous Non-Small Cell Lung Cancer1
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Pleural Mesothelioma (MPM)1
1TerminatedTreatmentCancer, Breast1
1TerminatedTreatmentFailure or Contraindication of Trastuzumab Therapy / First or Second Line Therapy / HER2 Positive / Metastatic Breast Cancer (MBC)1
1TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1TerminatedTreatmentMalignant Solid Tumours1
1TerminatedTreatmentMetastatic Breast Cancer (MBC) / Metastatic Non Small Cell Lung Cancer1
1Unknown StatusTreatmentLung Cancers1
1Unknown StatusTreatmentLymphoma, Hodgkins1
1Unknown StatusTreatmentNonhematologic Malignancies1
1Unknown StatusTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentAdvanced Malignant Solid Tumors / Cancer, Breast1
1, 2Active Not RecruitingTreatmentCancer, Advanced / Cancer, Breast / Lung Cancer Small Cell Lung Cancer (SCLC) / Malignant Neoplasm of Pancreas / Ovarian / Sarcomas1
1, 2Active Not RecruitingTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
1, 2CompletedTreatmentBreast / Cancers1
1, 2CompletedTreatmentCancer, Breast3
1, 2CompletedTreatmentLeukemias / Malignant Lymphomas / Sarcomas / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2CompletedTreatmentLung Cancers1
1, 2CompletedTreatmentLung Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentMalignant Lymphomas1
1, 2CompletedTreatmentMetastatic Cancers1
1, 2CompletedTreatmentProstate Cancer1
1, 2TerminatedTreatmentCancer, Breast1
1, 2TerminatedTreatmentLung Cancers1
1, 2TerminatedTreatmentStage IV (Metastatic) Breast Cancer1
1, 2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)2
2Active Not RecruitingTreatmentAdvanced Non-Small Cell Lung Cancer / Non-Small Cell Lung Cancer Stage IIIB1
2Active Not RecruitingTreatmentCancer, Breast4
2Active Not RecruitingTreatmentHER-2 Positive Breast Cancer1
2Active Not RecruitingTreatmentLocally Advanced Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)3
2Active Not RecruitingTreatmentMalignant Lymphomas1
2Active Not RecruitingTreatmentMalignant Tumor of the Breast / Neoplasms, Breast1
2Active Not RecruitingTreatmentMesothelioma1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)3
2CompletedTreatmentAdenocarcinoma of Colon / Adenocarcinoma of Rectum / Metastatic Disease1
2CompletedTreatmentAdult Lymphocyte Depletion Hodgkin Lymphoma / Adult Lymphocyte Predominant Hodgkin Lymphoma / Adult Mixed Cellularity Hodgkin Lymphoma / Adult Nodular Lymphocyte Predominant Hodgkin Lymphoma / Adult Nodular Sclerosis Hodgkin Lymphoma / Childhood Lymphocyte Depletion Hodgkin Lymphoma / Childhood Lymphocyte Predominant Hodgkin Lymphoma / Childhood Mixed Cellularity Hodgkin Lymphoma / Childhood Nodular Lymphocyte Predominant Hodgkin Lymphoma / Childhood Nodular Sclerosis Hodgkin Lymphoma / Recurrent Adult Hodgkin's Lymphoma / Recurrent/Refractory Childhood Hodgkin Lymphoma / Stage I Adult Hodgkin Lymphoma / Stage I Childhood Hodgkin Lymphoma / Stage II Adult Hodgkin Lymphoma / Stage II Childhood Hodgkin Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage III Childhood Hodgkin Lymphoma / Stage IV Adult Hodgkin Lymphoma / Stage IV Childhood Hodgkin Lymphoma1
2CompletedTreatmentAdult Lymphocyte Depletion Hodgkin Lymphoma / Adult Lymphocyte Predominant Hodgkin Lymphoma / Adult Mixed Cellularity Hodgkin Lymphoma / Adult Nodular Sclerosis Hodgkin Lymphoma / Recurrent Adult Hodgkin's Lymphoma1
2CompletedTreatmentAdult Rhabdomyosarcoma / Childhood Alveolar Rhabdomyosarcoma / Childhood Pleomorphic Rhabdomyosarcoma / Childhood Rhabdomyosarcoma With Mixed Embryonal and Alveolar Features / Previously Treated Childhood Rhabdomyosarcoma / Recurrent Adult Soft Tissue Sarcoma / Recurrent Childhood Rhabdomyosarcoma1
2CompletedTreatmentBrain and Central Nervous System Tumors / Neuroblastomas / Sarcomas1
2CompletedTreatmentBreast Cancer Metastatic1
2CompletedTreatmentCancer of the Lung / Carcinoma NOS / Lung Cancer Non-Small Cell Cancer (NSCLC) / Neoplasms, Lung1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cancer1
2CompletedTreatmentCancer, Breast14
2CompletedTreatmentCancer, Breast / Lung Cancer Non-Small Cell Cancer (NSCLC) / Prostate Cancer1
2CompletedTreatmentCancer, Breast / Neoplasms Metastasis1
2CompletedTreatmentCancers2
2CompletedTreatmentCervical Cancers1
2CompletedTreatmentConcomitant Radiochemotherapy / NSCLC Stage IIIB1
2CompletedTreatmentEsophageal Cancers / Malignant Neoplasm of Stomach1
2CompletedTreatmentEstrogen Receptor-negative Breast Cancer / Estrogen Receptor-Positive Breast Cancer / Her2-Positive Breast Cancer / Progesterone Receptor-negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer1
2CompletedTreatmentHer2-negative Locally Advanced Breast Cancer / Her2-negative Metastatic Breast Cancer1
2CompletedTreatmentHodgkins Disease (HD)1
2CompletedTreatmentHodgkins Disease (HD) / Lymphoma, Hodgkin Disease / Lymphoma, Hodgkins / Malignant Lymphomas1
2CompletedTreatmentHodgkins Disease (HD) / Non-Hodgkin's Lymphoma (NHL)2
2CompletedTreatmentLow-Grade Gliomas1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)11
2CompletedTreatmentLung Cancers8
2CompletedTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2CompletedTreatmentMale Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentMalignant Lymphomas3
2CompletedTreatmentMalignant Pleural Mesothelioma (MPM)1
2CompletedTreatmentMelanoma (Skin)1
2CompletedTreatmentMetastatic Breast Cancer (MBC)4
2CompletedTreatmentMetastatic Melanoma1
2CompletedTreatmentNeoplasms Metastasis / Neoplasms, Breast1
2CompletedTreatmentNeoplasms, Breast2
2CompletedTreatmentNeoplasms, Lung1
2CompletedTreatmentNon Small Cell Lung Carcinoma (NSCLC)1
2CompletedTreatmentNon-Hodgkin's Lymphoma (CD20+)1
2CompletedTreatmentPlasma Cell Myeloma1
2CompletedTreatmentProstate Cancer4
2CompletedTreatmentRecurrent Non-small Cell Lung Cancer / Recurrent Non-Small Cell Lung Carcinoma / Stage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2CompletedTreatmentRenal Cancers1
2CompletedTreatmentSoft Tissue Sarcoma (STS)1
2Not Yet RecruitingTreatmentCancer of the Ovary / Fallopian Tube Cancer1
2Not Yet RecruitingTreatmentCancer, Breast1
2Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Not Yet RecruitingTreatmentMultiple Myeloma (MM)1
2Not Yet RecruitingTreatmentNon-small Cell Lung Cancer Stage Ⅱ / Non-small Cell Lung Cancer Stage ⅢA1
2RecruitingTreatmentAdvanced Triple-Negative Breast Cancer1
2RecruitingTreatmentAggressive Non-Hodgkin Lymphoma1
2RecruitingTreatmentAmyloidosis / Multiple Myeloma (MM)1
2RecruitingTreatmentAnaplastic Large Cell Lymphoma / Vinorelbine2
2RecruitingTreatmentBreast Cancer Metastatic1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentEffects of Chemotherapy / Lung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentLarge Cell Lung Carcinoma Metastatic / Lung adenocarcinoma metastatic / Lung Cancer Non-Small Cell Cancer (NSCLC) / Metastatic Lung Cancer1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentLung Cancers1
2RecruitingTreatmentLung neoplasm malignant1
2RecruitingTreatmentLymphoma, Large B-Cell, Diffuse (DLBCL)1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)3
2RecruitingTreatmentNeoplasms, Breast1
2RecruitingTreatmentNeoplasms, Head and Neck1
2RecruitingTreatmentNon-small Cell Lung Cancer Stage IIIA1
2RecruitingTreatmentSquamous Cell Carcinoma of Esophagus1
2RecruitingTreatmentSquamous Cell Esophageal Carcinoma1
2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
2SuspendedTreatmentLow-Grade Gliomas1
2TerminatedTreatmentAdvanced Stage IIIB / High Thymidylate Synthase Expression / Lung Cancer Non-Small Cell Cancer (NSCLC) / Secondary1
2TerminatedTreatmentCancer, Breast6
2TerminatedTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
2TerminatedTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Progesterone Receptor-positive Breast Cancer / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer1
2TerminatedTreatmentHodgkins Disease (HD)1
2TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)4
2TerminatedTreatmentMesothelioma1
2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
2TerminatedTreatmentNeoplasms, Breast2
2Unknown StatusDiagnosticLung Cancers1
2Unknown StatusSupportive CareChemotherapeutic Agent Toxicity / Lung Cancers / Musculoskeletal Complications / Tiredness1
2Unknown StatusTreatmentCancer, Breast1
2Unknown StatusTreatmentCancer, Breast / Stage II Breast Cancer / Stage III Breast Cancer1
2Unknown StatusTreatmentEwing's Tumor / Medulloblastomas / Neoplasms, Connective and Soft Tissue / Neuroblastomas / Rhabdomyosarcomas / Sarcoma, Osteogenic1
2Unknown StatusTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)4
2Unknown StatusTreatmentLung Cancers3
2Unknown StatusTreatmentLymphoma, Hodgkins1
2Unknown StatusTreatmentMesothelioma1
2Unknown StatusTreatmentMesothelioma, Malignant2
2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)1
2Unknown StatusTreatmentProstate Cancer1
2WithdrawnTreatmentMalignant Lymphomas1
2WithdrawnTreatmentNeoplasms, Breast1
2WithdrawnTreatmentProstate Cancer1
2, 3CompletedTreatmentLung Cancers1
2, 3Not Yet RecruitingTreatmentCancer, Breast / Chemotherapy Effect / Disease-Free Survival1
2, 3TerminatedTreatmentCancer, Breast1
2, 3TerminatedTreatmentCancer, Breast / HER2 Positive Breast Cancers1
2, 3TerminatedTreatmentMetastatic Breast Cancer (MBC)1
3Active Not RecruitingTreatmentCancer of Breast / Cancer, Breast / HER2-Negative Breast Cancer / Triple Negative Breast Cancer (TNBC) / Tumors, Breast1
3Active Not RecruitingTreatmentChildhood Favorable Prognosis Hodgkin Lymphoma / Childhood Lymphocyte Depletion Hodgkin Lymphoma / Childhood Mixed Cellularity Hodgkin Lymphoma / Childhood Nodular Sclerosis Hodgkin Lymphoma / Stage I Childhood Hodgkin Lymphoma / Stage II Childhood Hodgkin Lymphoma1
3Active Not RecruitingTreatmentChildhood Nodular Lymphocyte Predominant Hodgkin Lymphoma / Stage III Childhood Hodgkin Lymphoma / Stage IV Childhood Hodgkin Lymphoma1
3Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
3Active Not RecruitingTreatmentMetastatic Triple Negative Breast Cancer1
3Active Not RecruitingTreatmentNeoplasms, Breast1
3Active Not RecruitingTreatmentStage IB Non-Small Cell Lung Carcinoma / Stage IB Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIA Non-Small Cell Lung Carcinoma / Stage IIA Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIB Non-Small Cell Lung Carcinoma / Stage IIB Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v71
3CompletedPreventionCancers1
3CompletedTreatmentAdenocarcinoma of the Cervix / Adenosquamous carcinoma of the cervix / Cervical Squamous Cell Carcinoma / Recurrent Cervical Carcinoma / Stage IVB Cervical Cancer1
3CompletedTreatmentAdenocarcinoma of the Lung / Adenosquamous Cell Lung Cancer / Large Cell Lung Cancer / Squamous Cell Carcinoma of Lung / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIb Non-small Cell Lung Cancer1
3CompletedTreatmentAdvanced Non-Small Cell Lung Cancer1
3CompletedTreatmentCancer, Breast2
3CompletedTreatmentCancer, Breast / Stage IV Breast Cancer1
3CompletedTreatmentHER2/Neu Over-expressing Locally Advanced Breast Cancer / Metastatic Breast Cancer (MBC)1
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)7
3CompletedTreatmentLung Cancers7
3CompletedTreatmentMesothelioma, Malignant1
3CompletedTreatmentMetastatic Breast Cancer (MBC)1
3Not Yet RecruitingTreatment2-year Disease-Free Survival1
3Not Yet RecruitingTreatmentChemotherapy Effect / Susceptibility, Genetic1
3Not Yet RecruitingTreatmentCompletely Resected NSCLC With Common EGFR Mutations1
3Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Malignant Hydrothorax1
3RecruitingTreatmentBreast Cancer Model / Cancer, Breast / Effects of Chemotherapy1
3RecruitingTreatmentCancer, Breast3
3RecruitingTreatmentCancer, Breast / Metastasis1
3RecruitingTreatmentCarcinoma, Bronchogenic / Chronic Lung Diseases / Neoplasm, Bronchial / Neoplasms / Neoplasms, Lung / Respiratory Tract Diseases / Respiratory Tract Neoplasms / Stage IV, NSCLC / Thoracic Neoplasms1
3RecruitingTreatmentEsophageal Cancers / Malignant Neoplasm of Esophagus / Squamous Cell Carcinoma of Esophagus1
3RecruitingTreatmentHER-2 Positive Breast Cancer / Neoplasms, Metastatic1
3RecruitingTreatmentHER2-positive Locally Advanced or Metastatic Breast Cancer1
3RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)4
3RecruitingTreatmentMetastatic Breast Cancer (MBC)2
3RecruitingTreatmentPleural Mesothelioma Malignant Advanced1
3TerminatedNot AvailableStage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
3TerminatedTreatmentAdvanced Non-Small Cell Lung Cancer1
3TerminatedTreatmentMalignant Lymphomas1
3Unknown StatusTreatmentCancer, Breast1
3Unknown StatusTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3Unknown StatusTreatmentLung Cancers4
3Unknown StatusTreatmentSarcomas1
3WithdrawnTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3WithdrawnTreatmentLung Cancers1
4Active Not RecruitingTreatmentMetastatic Non-Small Cell Lung Cancer1
4CompletedTreatmentCancer, Breast1
4CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
4Not Yet RecruitingTreatmentPrimary Breast Cancer1
Not AvailableActive Not RecruitingNot AvailableCancer, Breast / Lung Cancer Non-Small Cell Cancer (NSCLC)1
Not AvailableAvailableNot AvailableMetastatic Breast Cancer With BRCA 1 or BRCA 2 Genetic Mutation / Triple-Negative Breast Cancer (TNBC)1
Not AvailableCompletedNot AvailableCancer, Breast / Metastatic Cancers1
Not AvailableCompletedTreatmentCancer, Breast1
Not AvailableCompletedTreatmentHypermethylation / Lung Cancers / Non Small Cell Lung Carcinoma (NSCLC)1
Not AvailableRecruitingNot AvailableCancer, Breast / Neoplasms, Breast1
Not AvailableTerminatedNot AvailableCancer, Breast1

Pharmacoeconomics

Manufacturers
  • Pierre fabre medicament
  • Actavis totowa llc
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories div ben venue laboratories inc
  • Ebewe pharma ges mbh nfg kg
  • Hospira inc
  • Teva parenteral medicines inc
Packagers
  • APP Pharmaceuticals
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Ebewe Pharma
  • Hospira Inc.
  • Pierre Fabre
  • Sagent Pharmaceuticals
  • Sicor Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • Wyeth Pharmaceuticals
Dosage forms
FormRouteStrength
InjectionIntravenous10 mg/mL
Injection, solutionIntravenous10 mg/mL
Injection, solution, concentrateIntravenous10 mg/mL
Injection, solution, concentrateIntravenous50 mg/5mL
SolutionIntravenous10 mg
Prices
Unit descriptionCostUnit
Navelbine 50 mg/5 ml vial42.0USD ml
Vinorelbine 50 mg/5 ml vial27.6USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)181-183MSDS
water solubility10 mg/mL in waterMSDS
logP4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0122 mg/mLALOGPS
logP4.39ALOGPS
logP4.65ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)10.87ChemAxon
pKa (Strongest Basic)8.66ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area133.87 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity216.99 m3·mol-1ChemAxon
Polarizability84.31 Å3ChemAxon
Number of Rings9ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.974
Blood Brain Barrier-0.8815
Caco-2 permeable+0.5602
P-glycoprotein substrateSubstrate0.9283
P-glycoprotein inhibitor IInhibitor0.7488
P-glycoprotein inhibitor IIInhibitor0.7388
Renal organic cation transporterNon-inhibitor0.6979
CYP450 2C9 substrateNon-substrate0.8513
CYP450 2D6 substrateSubstrate0.6471
CYP450 3A4 substrateSubstrate0.7247
CYP450 1A2 substrateNon-inhibitor0.8415
CYP450 2C9 inhibitorNon-inhibitor0.7863
CYP450 2D6 inhibitorNon-inhibitor0.8369
CYP450 2C19 inhibitorNon-inhibitor0.8381
CYP450 3A4 inhibitorNon-inhibitor0.8095
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6672
Ames testNon AMES toxic0.8064
CarcinogenicityNon-carcinogens0.9299
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8350 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9014
hERG inhibition (predictor II)Non-inhibitor0.5171
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
Inhibitor
General Function
Ubiquitin protein ligase binding
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBB
Uniprot ID
P07437
Uniprot Name
Tubulin beta chain
Molecular Weight
49670.515 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Kruczynski A, Barret JM, Etievant C, Colpaert F, Fahy J, Hill BT: Antimitotic and tubulin-interacting properties of vinflunine, a novel fluorinated Vinca alkaloid. Biochem Pharmacol. 1998 Mar 1;55(5):635-48. [PubMed:9515574]
  4. Chang AY, Garrow GC: Pilot study of vinorelbine (Navelbine) and paclitaxel (Taxol) in patients with refractory breast cancer and lung cancer. Semin Oncol. 1995 Apr;22(2 Suppl 5):66-70; discussion 70-1. [PubMed:7740336]
  5. Seve P, Dumontet C: [Class III beta tubulin expression in nonsmall cell lung cancer]. Rev Mal Respir. 2010 Apr;27(4):383-6. doi: 10.1016/j.rmr.2010.03.006. Epub 2010 Mar 25. [PubMed:20403547]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]

Drug created on June 13, 2005 07:24 / Updated on April 23, 2018 22:58