Identification

Name
Vinblastine
Accession Number
DB00570  (APRD00708)
Type
Small Molecule
Groups
Approved
Description

Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)

Structure
Thumb
Synonyms
  • Vinblastin
  • Vinblastina
  • Vinblastine
  • Vinblastinum
  • Vincaleukoblastine
External IDs
NSC-47842
Product Ingredients
IngredientUNIICASInChI Key
Vinblastine sulfateN00W22YO2B143-67-9KDQAABAKXDWYSZ-PNYVAJAMSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Velbe 1mg/mlPowder, for solution10 mgIntravenousEli Lilly & Co. Ltd.1994-11-152000-10-02Canada
Vinblastine Sulfate Inj 1mg/mlLiquid1 mgIntravenousDavid Bull Laboratories (Pty) Ltd.1992-12-311998-08-13Canada
Vinblastine Sulfate InjectionSolution1 mgIntravenousPfizer1998-04-14Not applicableCanada
Vinblastine Sulfate InjectionSolution1 mgIntravenousSandoz Canada IncorporatedNot applicableNot applicableCanada
Vinblastine Sulphate InjectionSolution1 mgIntravenousTeva2013-02-08Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Vinblastine SulfateInjection1 mg/mLIntravenousFresenius Kabi2000-07-12Not applicableUs
International/Other Brands
Blastivin (Pharmachemie) / Cytoblastin (Cipla) / Lemblastine / Oncostin (Cipla) / Velban (ABL Antibióticos do Brasil) / Velbastin (Korea United Pharm) / Velbe (STADA) / Vinblasin (Teva) / Vinblastin (Gedeon Richter) / Vinko (Koçak) / Weibaoding (Hospira) / Xintoprost (Richmond)
Categories
UNII
5V9KLZ54CY
CAS number
865-21-4
Weight
Average: 810.9741
Monoisotopic: 810.420379474
Chemical Formula
C46H58N4O9
InChI Key
JXLYSJRDGCGARV-CFWMRBGOSA-N
InChI
InChI=1S/C46H58N4O9/c1-8-42(54)23-28-24-45(40(52)57-6,36-30(15-19-49(25-28)26-42)29-13-10-11-14-33(29)47-36)32-21-31-34(22-35(32)56-5)48(4)38-44(31)17-20-50-18-12-16-43(9-2,37(44)50)39(59-27(3)51)46(38,55)41(53)58-7/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3/t28-,37-,38+,39+,42-,43+,44+,45-,46-/m0/s1
IUPAC Name
methyl (1R,9R,10S,11R,12R,19R)-11-(acetyloxy)-12-ethyl-4-[(13S,15R,17S)-17-ethyl-17-hydroxy-13-(methoxycarbonyl)-1,11-diazatetracyclo[13.3.1.0⁴,¹².0⁵,¹⁰]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.0¹,⁹.0²,⁷.0¹⁶,¹⁹]nonadeca-2,4,6,13-tetraene-10-carboxylate
SMILES
[H][C@@]12N(C)C3=CC(OC)=C(C=C3[C@@]11CCN3CC=C[C@](CC)([C@@]13[H])[C@@]([H])(OC(C)=O)[C@]2(O)C(=O)OC)[C@]1(C[C@@]2([H])CN(C[C@](O)(CC)C2)CCC2=C1NC1=CC=CC=C21)C(=O)OC

Pharmacology

Indication

For treatment of breast cancer, testicular cancer, lymphomas, neuroblastoma, Hodgkin's and non-Hodgkin's lymphomas, mycosis fungoides, histiocytosis, and Kaposi's sarcoma.

Associated Conditions
Pharmacodynamics

Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 multiringed units: vindoline and catharanthine. The vinca alkaloids have become clinically useful since the discovery of their antitumour properties in 1959. Initially, extracts of the periwinkle plant (Catharanthus roseus) were investigated because of putative hypoglycemic properties, but were noted to cause marrow suppression in rats and antileukemic effects in vitro. Vinblastine has some immunosuppressant effect. The vinca alkaloids are considered to be cell cycle phase-specific.

Mechanism of action

The antitumor activity of vinblastine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Vinblastine binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.

TargetActionsOrganism
ATubulin alpha-1A chain
adduct
Human
ATubulin beta chain
adduct
Human
ATubulin delta chain
adduct
Human
ATubulin gamma-1 chain
adduct
Human
ATubulin epsilon chain
adduct
Human
NTranscription factor AP-1
other/unknown
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

98-99%

Metabolism

Hepatic. Metabolism of vinblastine has been shown to be mediated by hepatic cytochrome P450 3A isoenzymes.

Route of elimination

The major route of excretion may be through the biliary system.

Half life

Triphasic: 35 min, 53 min, and 19 hours

Clearance
Not Available
Toxicity

Oral, mouse: LD50 = 423 mg/kg; Oral, rat: LD50 = 305 mg/kg.

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

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Vinblastine can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Vinblastine can be increased when it is combined with Acetaminophen.Approved
Acetyl sulfisoxazoleThe metabolism of Vinblastine can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Vinblastine.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Vinblastine.Experimental
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Vinblastine.Approved
AmiodaroneThe serum concentration of Vinblastine can be increased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Vinblastine can be increased when it is combined with Amlodipine.Approved
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Vinblastine.Approved, Investigational, Withdrawn
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Vinblastine is combined with Anthrax immune globulin human.Approved
ApalutamideThe serum concentration of Vinblastine can be decreased when it is combined with Apalutamide.Approved, Investigational
AprepitantThe serum concentration of Vinblastine can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Vinblastine can be decreased when combined with Artemether.Approved
AsunaprevirThe serum concentration of Asunaprevir can be increased when it is combined with Vinblastine.Approved, Investigational, Withdrawn
AtazanavirThe metabolism of Vinblastine can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Vinblastine can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Vinblastine is combined with Atorvastatin.Approved
Bacillus calmette-guerin substrain connaught live antigenThe risk or severity of adverse effects can be increased when Vinblastine 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 Vinblastine 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 Vinblastine.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Vinblastine is combined with Beclomethasone dipropionate.Approved, Investigational
Benzyl alcoholThe serum concentration of Vinblastine can be increased when it is combined with Benzyl alcohol.Approved
BepridilThe serum concentration of Vinblastine can be increased when it is combined with Bepridil.Approved, Withdrawn
BetaxololThe metabolism of Vinblastine can be decreased when combined with Betaxolol.Approved, Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Vinblastine.Approved, Investigational
BoceprevirThe metabolism of Vinblastine can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Vinblastine can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Vinblastine can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Vinblastine.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Vinblastine.Approved, Investigational
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Vinblastine.Approved, Investigational
BudesonideThe risk or severity of adverse effects can be increased when Vinblastine is combined with Budesonide.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Vinblastine.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Vinblastine.Approved
CaffeineThe serum concentration of Vinblastine can be increased when it is combined with Caffeine.Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Carbamazepine.Approved, Investigational
CarbomycinThe serum concentration of Vinblastine can be increased when it is combined with Carbomycin.Vet Approved
CarvedilolThe serum concentration of Vinblastine can be increased when it is combined with Carvedilol.Approved, Investigational
CelecoxibThe metabolism of Vinblastine can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Vinblastine can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Vinblastine.Approved, Withdrawn
ChloroquineThe metabolism of Vinblastine can be decreased when combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorpromazineThe metabolism of Vinblastine can be decreased when combined with Chlorpromazine.Approved, Investigational, Vet Approved
CholecalciferolThe metabolism of Vinblastine can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
Cholic AcidVinblastine may decrease the excretion rate of Cholic Acid which could result in a higher serum level.Approved
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Vinblastine.Approved, Investigational
CinacalcetThe metabolism of Vinblastine can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Vinblastine.Approved, Investigational
CitalopramThe metabolism of Vinblastine can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Vinblastine can be decreased when combined with Clarithromycin.Approved
ClobazamThe metabolism of Vinblastine can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Vinblastine 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 Vinblastine is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).Approved
ClotrimazoleThe metabolism of Vinblastine can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Clozapine.Approved
CobicistatThe serum concentration of Vinblastine can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Vinblastine can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Vinblastine.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Vinblastine.Approved, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Vinblastine is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CrizotinibThe metabolism of Vinblastine can be decreased when combined with Crizotinib.Approved
CurcuminThe metabolism of Vinblastine can be decreased when combined with Curcumin.Approved, Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Vinblastine.Approved, Investigational
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Vinblastine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Vinblastine.Experimental
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Vinblastine.Approved
DabrafenibThe serum concentration of Vinblastine can be decreased when it is combined with Dabrafenib.Approved, Investigational
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Vinblastine.Approved
DarifenacinThe metabolism of Vinblastine can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Vinblastine can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Vinblastine can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Vinblastine can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Vinblastine can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Vinblastine.Approved
DesipramineThe metabolism of Vinblastine can be decreased when combined with Desipramine.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Vinblastine.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Vinblastine is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexniguldipineThe serum concentration of Vinblastine can be increased when it is combined with Dexniguldipine.Experimental
DexverapamilThe serum concentration of Vinblastine can be increased when it is combined with Dexverapamil.Experimental
DigitoxinDigitoxin may decrease the cardiotoxic activities of Vinblastine.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Vinblastine.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Vinblastine.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Vinblastine.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Vinblastine.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Vinblastine.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Vinblastine.Approved, Investigational
DiltiazemThe metabolism of Vinblastine can be decreased when combined with Diltiazem.Approved, Investigational
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Vinblastine.Approved, Investigational
DosulepinThe metabolism of Vinblastine can be decreased when combined with Dosulepin.Approved
DoxazosinThe serum concentration of Vinblastine can be increased when it is combined with Doxazosin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Vinblastine.Approved, Investigational
DoxycyclineThe metabolism of Vinblastine can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Vinblastine can be decreased when combined with Dronedarone.Approved
DuloxetineThe metabolism of Vinblastine can be decreased when combined with Duloxetine.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Vinblastine.Approved
EliglustatThe metabolism of Vinblastine can be decreased when combined with Eliglustat.Approved
EmopamilThe serum concentration of Vinblastine can be increased when it is combined with Emopamil.Experimental
EnzalutamideThe serum concentration of Vinblastine 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 Vinblastine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Vinblastine.Approved
ErythromycinThe serum concentration of Vinblastine can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Vinblastine.Approved, Investigational, Vet Approved
Ethinyl EstradiolThe risk or severity of liver damage can be increased when Ethinyl Estradiol is combined with Vinblastine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Vinblastine.Approved
FelodipineThe serum concentration of Vinblastine can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Vinblastine can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vinblastine.Approved
FingolimodVinblastine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe metabolism of Vinblastine can be decreased when combined with Fluconazole.Approved, Investigational
FluoxetineThe serum concentration of Vinblastine can be increased when it is combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Vinblastine is combined with Fluticasone propionate.Approved
FluvastatinThe excretion of Fluvastatin can be decreased when combined with Vinblastine.Approved
FluvoxamineThe serum concentration of Vinblastine can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Vinblastine can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Vinblastine can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Vinblastine can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Vinblastine can be increased when it is combined with Fusidic Acid.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Vinblastine is combined with G17DT.Investigational
GallopamilThe serum concentration of Vinblastine can be increased when it is combined with Gallopamil.Investigational
GemcitabineThe risk or severity of adverse effects can be increased when Gemcitabine is combined with Vinblastine.Approved
GI-5005The risk or severity of adverse effects can be increased when Vinblastine is combined with GI-5005.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Vinblastine.Experimental
GlyburideThe risk or severity of liver damage can be increased when Glyburide is combined with Vinblastine.Approved
GlycerinThe serum concentration of Vinblastine can be increased when it is combined with Glycerin.Approved, Investigational
HaloperidolThe metabolism of Vinblastine can be decreased when combined with Haloperidol.Approved
Hepatitis A VaccineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Vinblastine is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
Human rabies virus immune globulinThe risk or severity of adverse effects can be increased when Vinblastine is combined with Human rabies virus immune globulin.Approved
HydrocodoneThe serum concentration of the active metabolites of Hydrocodone can be reduced when Hydrocodone is used in combination with Vinblastine resulting in a loss in efficacy.Approved, Illicit
HydrocortisoneThe risk or severity of adverse effects can be increased when Vinblastine is combined with Hydrocortisone.Approved, Vet Approved
Hydrocortisone acetateThe risk or severity of adverse effects can be increased when Vinblastine is combined with Hydrocortisone acetate.Approved, Vet Approved
Hydrocortisone butyrateThe risk or severity of adverse effects can be increased when Vinblastine is combined with Hydrocortisone butyrate.Approved, Vet Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Vinblastine.Approved
IbuprofenThe serum concentration of Vinblastine can be increased when it is combined with Ibuprofen.Approved
IdelalisibThe metabolism of Vinblastine can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Vinblastine can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Vinblastine can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Vinblastine can be decreased when combined with Indinavir.Approved
INGN 201The risk or severity of adverse effects can be increased when Vinblastine is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Vinblastine is combined with INGN 225.Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Vinblastine is combined with Irinotecan.Approved, Investigational
IsavuconazoleThe serum concentration of Vinblastine can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Vinblastine can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Vinblastine can be decreased when combined with Isoniazid.Approved, Investigational
IsradipineThe serum concentration of Vinblastine can be increased when it is combined with Isradipine.Approved, Investigational
ItraconazoleThe serum concentration of Vinblastine can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Vinblastine 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 Vinblastine is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated).Approved
JosamycinThe serum concentration of Vinblastine can be increased when it is combined with Josamycin.Approved, Investigational
KetoconazoleThe metabolism of Vinblastine can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe serum concentration of Vinblastine can be increased when it is combined with Kitasamycin.Experimental
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Vinblastine.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Vinblastine.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Vinblastine.Experimental
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Vinblastine.Approved
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Vinblastine.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Vinblastine is combined with Leflunomide.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Vinblastine.Approved, Investigational
LidocaineThe serum concentration of Vinblastine can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Vinblastine.Approved
LipegfilgrastimVinblastine may increase the myelosuppressive activities of Lipegfilgrastim.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Vinblastine.Approved, Investigational
LomerizineThe serum concentration of Vinblastine can be increased when it is combined with Lomerizine.Experimental
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Vinblastine.Approved
LopinavirThe serum concentration of Vinblastine can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Vinblastine can be increased when it is combined with Loratadine.Approved, Investigational
LorcaserinThe metabolism of Vinblastine can be decreased when combined with Lorcaserin.Approved
LorpiprazoleThe serum concentration of Vinblastine can be increased when it is combined with Lorpiprazole.Approved
LosartanThe serum concentration of Vinblastine can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Vinblastine.Approved, Investigational
LuliconazoleThe serum concentration of Vinblastine can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Vinblastine can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Vinblastine 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 Vinblastine.Illicit, Investigational, Withdrawn
MetamizoleThe risk or severity of myelosuppression can be increased when Metamizole is combined with Vinblastine.Approved, Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Vinblastine.Experimental
MethadoneThe metabolism of Vinblastine can be decreased when combined with Methadone.Approved
MethimazoleThe risk or severity of adverse effects can be increased when Vinblastine is combined with Methimazole.Approved
MethotrimeprazineThe metabolism of Vinblastine can be decreased when combined with Methotrimeprazine.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Vinblastine.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Vinblastine is combined with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Vinblastine.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Vinblastine.Experimental
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Vinblastine.Approved, Investigational
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Vinblastine.Experimental
MibefradilThe metabolism of Vinblastine can be decreased when combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Vinblastine can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidostaurinThe metabolism of Vinblastine can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Vinblastine can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Vinblastine can be decreased when combined with Mirabegron.Approved
MitomycinThe risk or severity of adverse effects can be increased when Vinblastine is combined with Mitomycin.Approved
MitotaneThe serum concentration of Vinblastine can be decreased when it is combined with Mitotane.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Vinblastine.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Vinblastine is combined with Natalizumab.Approved, Investigational
NefazodoneThe metabolism of Vinblastine can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Vinblastine can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Vinblastine can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Vinblastine can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Vinblastine can be increased when it is combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Vinblastine.Approved, Investigational
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Vinblastine.Approved
NiguldipineThe serum concentration of Vinblastine can be increased when it is combined with Niguldipine.Experimental
NilotinibThe metabolism of Vinblastine can be decreased when combined with Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Vinblastine can be increased when it is combined with Nimodipine.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Vinblastine.Approved
NisoldipineThe serum concentration of Vinblastine can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Vinblastine can be increased when it is combined with Nitrendipine.Approved, Investigational
NystatinThe serum concentration of Vinblastine can be increased when it is combined with Nystatin.Approved, Vet Approved
OcrelizumabOcrelizumab may increase the immunosuppressive activities of Vinblastine.Approved, Investigational
OlaparibThe metabolism of Vinblastine can be decreased when combined with Olaparib.Approved
OleandomycinThe serum concentration of Vinblastine can be increased when it is combined with Oleandomycin.Vet Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Vinblastine.Experimental, Investigational
OmeprazoleThe serum concentration of Vinblastine can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Vinblastine.Approved
OsimertinibThe serum concentration of Vinblastine can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Vinblastine.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Vinblastine.Approved, Vet Approved
PalbociclibThe serum concentration of Vinblastine can be increased when it is combined with Palbociclib.Approved, Investigational
PanobinostatThe serum concentration of Vinblastine can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe serum concentration of Vinblastine can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vinblastine.Approved
Peginterferon alfa-2bThe serum concentration of Vinblastine can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Vinblastine 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 Vinblastine.Approved, Investigational, Vet Approved, Withdrawn
PeruvosidePeruvoside may decrease the cardiotoxic activities of Vinblastine.Experimental
PhenobarbitalThe metabolism of Vinblastine can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Vinblastine 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 Vinblastine.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Vinblastine.Approved
PitolisantThe serum concentration of Pitolisant can be increased when it is combined with Vinblastine.Approved, Investigational
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Vinblastine.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Vinblastine.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Vinblastine is combined with Prednisolone.Approved, Vet Approved
PrimidoneThe metabolism of Vinblastine can be increased when combined with Primidone.Approved, Vet Approved
PromazineThe metabolism of Vinblastine can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Vinblastine can be increased when it is combined with Promethazine.Approved, Investigational
PropafenoneThe serum concentration of Vinblastine can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Vinblastine.Approved, Investigational
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Vinblastine.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Vinblastine.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Vinblastine.Approved
QuinidineThe metabolism of Vinblastine can be decreased when combined with Quinidine.Approved, Investigational
QuinineThe metabolism of Vinblastine can be decreased when combined with Quinine.Approved
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Vinblastine 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 Vinblastine.Approved, Investigational
RanitidineThe serum concentration of Vinblastine can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Vinblastine.Approved, Investigational
RifabutinThe metabolism of Vinblastine can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe risk or severity of liver damage can be increased when Rifampicin is combined with Vinblastine.Approved
RifapentineThe metabolism of Vinblastine can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Vinblastine.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Vinblastine.Approved
RindopepimutThe risk or severity of adverse effects can be increased when Vinblastine is combined with Rindopepimut.Investigational
RitonavirThe serum concentration of Vinblastine can be increased when it is combined with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Vinblastine.Approved
RolapitantThe metabolism of Vinblastine can be decreased when combined with Rolapitant.Approved, Investigational
RosuvastatinThe excretion of Rosuvastatin can be decreased when combined with Vinblastine.Approved
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Rubella virus vaccine.Approved, Investigational
RucaparibThe metabolism of Vinblastine 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 Vinblastine 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 Vinblastine is combined with Salmonella typhi ty21a live antigen.Approved
SaquinavirThe metabolism of Vinblastine can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Vinblastine can be decreased when used in combination with Sarilumab.Approved, Investigational
SertralineThe metabolism of Vinblastine can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Vinblastine can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Vinblastine.Approved
SiltuximabThe serum concentration of Vinblastine can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Vinblastine can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Vinblastine.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Vinblastine.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Vinblastine.Approved
SolithromycinThe serum concentration of Vinblastine can be increased when it is combined with Solithromycin.Investigational
SpiramycinThe serum concentration of Vinblastine can be increased when it is combined with Spiramycin.Approved
SRP 299The risk or severity of adverse effects can be increased when Vinblastine is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Vinblastine can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Vinblastine can be increased when it is combined with Stiripentol.Approved
SulfasalazineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Sulfasalazine.Approved
SulfisoxazoleThe metabolism of Vinblastine can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Sumatriptan can be increased when it is combined with Vinblastine.Approved, Investigational
TacrolimusTacrolimus may increase the immunosuppressive activities of Vinblastine.Approved, Investigational
TecemotideThe risk or severity of adverse effects can be increased when Vinblastine is combined with Tecemotide.Investigational
TelaprevirThe metabolism of Vinblastine can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Vinblastine can be decreased when combined with Telithromycin.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Vinblastine.Experimental
TetracyclineThe serum concentration of Tetracycline can be increased when it is combined with Vinblastine.Approved, Vet Approved
TetrandrineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Tetrandrine.Experimental
TG4010The risk or severity of adverse effects can be increased when Vinblastine is combined with TG4010.Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Vinblastine.Approved, Withdrawn
TiclopidineThe metabolism of Vinblastine can be decreased when combined with Ticlopidine.Approved
TipiracilThe serum concentration of Tipiracil can be increased when it is combined with Vinblastine.Approved, Investigational
TipranavirThe metabolism of Vinblastine can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Vinblastine can be decreased when it is combined with Tocilizumab.Approved
TofacitinibVinblastine may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Vinblastine.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Vinblastine.Approved
TopiramateThe serum concentration of Topiramate can be increased when it is combined with Vinblastine.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Vinblastine.Approved, Investigational
TranylcypromineThe metabolism of Vinblastine can be decreased when combined with Tranylcypromine.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Vinblastine.Approved, Investigational
TylosinThe serum concentration of Vinblastine can be increased when it is combined with Tylosin.Vet Approved
Typhoid VaccineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Typhoid Vaccine.Approved
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Vinblastine is combined with Varicella Zoster Vaccine (Live/Attenuated).Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Vinblastine.Approved
VemurafenibThe serum concentration of Vinblastine can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Vinblastine can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Vinblastine can be increased when it is combined with Verapamil.Approved
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Vinblastine.Approved, Investigational
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Vinblastine.Approved, Investigational
Yellow Fever VaccineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Yellow Fever Vaccine.Approved, Investigational
ZidovudineThe risk or severity of adverse effects can be increased when Vinblastine is combined with Zidovudine.Approved
ZiprasidoneThe metabolism of Vinblastine can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

Synthesis Reference

Pierre Potier, Pierre Mangeney, Nicole Langlois, Yves Langlois, "Process for the synthesis of vinblastine and leurosidine." U.S. Patent US4305875, issued October, 1977.

US4305875
General References
  1. Starling D: Two ultrastructurally distinct tubulin paracrystals induced in sea-urchin eggs by vinblastine sulphate. J Cell Sci. 1976 Jan;20(1):79-89. [PubMed:942954]
External Links
PubChem Compound
13342
PubChem Substance
46504550
ChemSpider
12773
BindingDB
50012278
ChEMBL
CHEMBL159
Therapeutic Targets Database
DAP000785
PharmGKB
PA451877
HET
VLB
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Vinblastine
ATC Codes
L01CA01 — Vinblastine
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
1z2b / 4eb6 / 5bmv / 5j2t
MSDS
Download (73.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentCentral Nervous System / Recurrent Lymphoma / Refractory Lymphomas / Tumors, Solid1
1CompletedTreatmentBrain and Central Nervous System Tumors / Neurofibromatosis Type 11
1CompletedTreatmentHodgkins Disease (HD)1
1CompletedTreatmentLymphoma, Hodgkins1
1CompletedTreatmentNeoplasms Metastasis / Neoplasms, Kidney1
1CompletedTreatmentStage IV Melanoma1
1CompletedTreatmentTumors, Central Nervous System / Tumors, Solid1
1RecruitingTreatmentRecurrent Low-grade Gliomas / Refractory Low-grade Gliomas1
1Unknown StatusTreatmentLung Cancers2
1, 2CompletedTreatmentHodgkins Disease (HD)1
1, 2CompletedTreatmentMetastatic Melanoma1
1, 2CompletedTreatmentRecurrent Melanoma / Stage IV Skin Melanoma1
1, 2Not Yet RecruitingTreatmentChildhood Lymphoma / Childhood Solid Tumors1
1, 2RecruitingTreatmentAIDS-Related Hodgkin Lymphoma / Ann Arbor Stage II Hodgkin Lymphoma / Ann Arbor Stage IIA Hodgkin Lymphoma / Ann Arbor Stage IIB Hodgkin Lymphoma / Ann Arbor Stage III Hodgkin Lymphoma / Ann Arbor Stage IIIA Hodgkin Lymphoma / Ann Arbor Stage IIIB Hodgkin Lymphoma / Ann Arbor Stage IV Hodgkin Lymphoma / Ann Arbor Stage IVA Hodgkin Lymphoma / Ann Arbor Stage IVB Hodgkin Lymphoma / CD30-Positive Neoplastic Cells Present / Classic Hodgkin Lymphoma / Classical Hodgkin Lymphoma / Human Immunodeficiency Virus (HIV) Infections / Stage II Hodgkin Lymphoma / Stage IIA Hodgkin Lymphoma / Stage IIB Hodgkin Lymphoma / Stage III Hodgkin Lymphoma / Stage IIIA Hodgkin Lymphoma / Stage IIIB Hodgkin Lymphoma / Stage IV Hodgkin Lymphoma / Stage IVA Hodgkin Lymphoma / Stage IVB Hodgkin Lymphoma1
1, 2RecruitingTreatmentHodgkins Disease (HD)1
1, 2RecruitingTreatmentLymphoma, Hodgkins1
2Active Not RecruitingTreatmentAdult Lymphocyte Depletion Hodgkin Lymphoma / Adult Lymphocyte Predominant Hodgkin Lymphoma / Adult Mixed Cellularity Hodgkin Lymphoma / Adult Nodular Sclerosis Hodgkin Lymphoma / Stage II Adult Hodgkin Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage IV Adult Hodgkin Lymphoma1
2Active Not RecruitingTreatmentGliomas1
2Active Not RecruitingTreatmentHIV-associated Hodgkin Lymphoma / Human Immunodeficiency Virus (HIV) Infections / Stage III Adult Hodgkin Lymphoma / Stage IV Adult Hodgkin Lymphoma1
2Active Not RecruitingTreatmentHodgkins Disease (HD)1
2Active Not RecruitingTreatmentLocalized Urothelial Carcinoma of the Renal Pelvis and Ureter / Recurrent Urothelial Carcinoma of the Renal Pelvis and Ureter / Regional Urothelial Carcinoma of the Renal Pelvis and Ureter1
2Active Not RecruitingTreatmentLymphoma, Hodgkins4
2Active Not RecruitingTreatmentMalignant Lymphomas / Nonneoplastic Condition1
2CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL) / Lymphoma, Lymphoblastic1
2CompletedTreatmentBladder Cancers2
2CompletedTreatmentBladder Cancers / Muscle-invasive Bladder Cancer1
2CompletedTreatmentDesmoid Tumors1
2CompletedTreatmentGliomas1
2CompletedTreatmentHigh Risk Urothelial Carcinoma of the Upper Urinary Tracts / Muscle Invasive Bladder Cancer1
2CompletedTreatmentHodgkins Disease (HD) / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHodgkins Disease (HD) / Lymphoma, Hodgkin Disease / Lymphoma, Hodgkins / Malignant Lymphomas1
2CompletedTreatmentHodgkins Disease (HD) / Pediatric1
2CompletedTreatmentIntraluminal Pulmonary Vein Stenosis1
2CompletedTreatmentLymphoma, Hodgkins1
2CompletedTreatmentMalignant Lymphomas9
2CompletedTreatmentMelanoma / Skin Cancers1
2CompletedTreatmentNeurofibromatosis Type 1 / Precancerous Conditions1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentRenal Cell Adenocarcinoma1
2CompletedTreatmentSarcomas1
2Not Yet RecruitingTreatmentAdvanced Hodgkin's Lymphoma1
2Not Yet RecruitingTreatmentClassical Hodgkin Lymphoma1
2Not Yet RecruitingTreatmentCoexisting Medical Conditions / Lymphoma, Hodgkins1
2RecruitingTreatmentAnn Arbor Stage I Hodgkin Lymphoma / Ann Arbor Stage IA Hodgkin Lymphoma / Ann Arbor Stage IB Hodgkin Lymphoma / Ann Arbor Stage II Hodgkin Lymphoma / Ann Arbor Stage IIA Hodgkin Lymphoma / Ann Arbor Stage IIB Hodgkin Lymphoma / Stage I Hodgkin Lymphoma / Stage IA Hodgkin Lymphoma / Stage IB Hodgkin Lymphoma / Stage II Hodgkin Lymphoma / Stage IIA Hodgkin Lymphoma / Stage IIB Hodgkin Lymphoma1
2RecruitingTreatmentBladder Cancers1
2RecruitingTreatmentClassical Hodgkin Lymphoma2
2RecruitingTreatmentClassical Hodgkin Lymphoma / Hodgkin Lymphoma (Category) / Hodgkins Disease (HD) / Lymphoma, Hodgkins1
2RecruitingTreatmentClassical Hodgkin Lymphoma / Lymphocyte-Depleted Classical Hodgkin Lymphoma / Lymphocyte-Rich Classical Hodgkin Lymphoma / Mixed Cellularity Classical Hodgkin Lymphoma / Nodular Sclerosis Classical Hodgkin Lymphoma1
2RecruitingTreatmentLow Grade Glioma (LGG)1
2RecruitingTreatmentLymphoma, Hodgkins1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2RecruitingTreatmentRecurrent B-Cell Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood B-Lymphoblastic Lymphoma1
2RecruitingTreatmentRecurrent Low-grade Gliomas / Refractory Low-grade Gliomas1
2RecruitingTreatmentTumors, Solid1
2RecruitingTreatmentUrothelial Carcinoma of the Bladder1
2TerminatedTreatmentBladder Cancers3
2TerminatedTreatmentHodgkins Disease (HD)1
2TerminatedTreatmentLymphoma, Hodgkins1
2TerminatedTreatmentMalignant Lymphomas1
2TerminatedTreatmentMelanoma1
2TerminatedTreatmentMetastatic Melanoma1
2Unknown StatusDiagnosticLung Cancers1
2Unknown StatusTreatmentHIV-associated Hodgkin Lymphoma1
2Unknown StatusTreatmentHodgkins Disease (HD)1
2Unknown StatusTreatmentMalignant Lymphomas3
2Unknown StatusTreatmentMesothelioma, Malignant1
2Unknown StatusTreatmentRenal Cancers1
2WithdrawnTreatmentAnterior Urethral Cancer / Localized Transitional Cell Cancer of the Renal Pelvis and Ureter / Posterior Urethral Cancer / Recurrent Bladder Cancer / Recurrent Urethral Cancer / Regional Transitional Cell Cancer of the Renal Pelvis and Ureter / Stage III Bladder Cancer / Transitional Cell Carcinoma of the Bladder / Ureteral Cancer / Urethral Cancer Associated With Invasive Bladder Cancer1
2, 3CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter / Urethral Cancer1
2, 3RecruitingTreatmentLangerhans Cell Histiocytosis (LCH)1
3Active Not RecruitingTreatmentLymphoma, Hodgkins3
3Active Not RecruitingTreatmentMalignant Lymphomas5
3CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter / Urethral Cancer1
3CompletedTreatmentBladder Cancers / Urethral Cancer1
3CompletedTreatmentCervical Cancers1
3CompletedTreatmentElderly Patients (>65 Years) / Lymphoma, Large B-Cell, Diffuse (DLBCL)1
3CompletedTreatmentHodgkins Disease (HD)1
3CompletedTreatmentLeukemias1
3CompletedTreatmentLung Cancers3
3CompletedTreatmentLymphoma, Hodgkins4
3CompletedTreatmentMalignant Lymphomas4
3CompletedTreatmentMelanoma (Skin)2
3CompletedTreatmentMelanoma / Skin Cancers1
3CompletedTreatmentMetastatic Bladder Cancer / Stage III Bladder Cancer / Transitional Cell Carcinoma of the Bladder1
3CompletedTreatmentProstate Cancer2
3Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3RecruitingTreatmentLangerhans Cell Histiocytosis (LCH)1
3RecruitingTreatmentLymphoma, Hodgkins1
3TerminatedTreatmentExtragonadal Germ Cell Tumor / Testicular germ cell tumour1
3TerminatedTreatmentMalignant Lymphomas1
3TerminatedTreatmentProstate Cancer1
3Unknown StatusTreatmentBladder Cancers1
3Unknown StatusTreatmentCancer of the Ovary / Childhood Germ Cell Tumor / Extragonadal Germ Cell Tumor1
3Unknown StatusTreatmentExtragonadal Germ Cell Tumor / Testicular germ cell tumour1
3Unknown StatusTreatmentLung Cancers3
3Unknown StatusTreatmentLymphoma, Hodgkins1
3Unknown StatusTreatmentMalignant Lymphomas2
4RecruitingTreatmentMalignant Lymphomas1
Not AvailableActive Not RecruitingTreatmentMalignant Lymphomas1
Not AvailableCompletedTreatmentAtaxia-Telangiectasia1
Not AvailableCompletedTreatmentChildhood Langerhans Cell Histiocytosis1
Not AvailableCompletedTreatmentLymphoma, Large Cell / Non-Hodgkin's Lymphoma (NHL)1
Not AvailableRecruitingTreatmentLymphoma, Hodgkins1
Not AvailableUnknown StatusTreatmentMalignant Lymphomas2

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
Packagers
  • APP Pharmaceuticals
  • APPD
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Hospira Inc.
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous10 mg
InjectionIntravenous1 mg/mL
LiquidIntravenous1 mg
SolutionIntravenous1 mg
Prices
Unit descriptionCostUnit
Vinblastine sulf 10 mg vial18.6USD each
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)267 °CNot Available
water solubilityNegligibleNot Available
logP3.70SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0169 mg/mLALOGPS
logP4.22ALOGPS
logP4.18ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)10.87ChemAxon
pKa (Strongest Basic)8.86ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count9ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area154.1 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity222.42 m3·mol-1ChemAxon
Polarizability87.81 Å3ChemAxon
Number of Rings9ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9806
Blood Brain Barrier-0.9203
Caco-2 permeable+0.6283
P-glycoprotein substrateSubstrate0.9213
P-glycoprotein inhibitor IInhibitor0.7737
P-glycoprotein inhibitor IIInhibitor0.6817
Renal organic cation transporterNon-inhibitor0.771
CYP450 2C9 substrateNon-substrate0.816
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateSubstrate0.72
CYP450 1A2 substrateNon-inhibitor0.9198
CYP450 2C9 inhibitorNon-inhibitor0.9093
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8149
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.91
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9111 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9366
hERG inhibition (predictor II)Non-inhibitor0.5793
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as vinca alkaloids. These are alkaloids with a dimeric chemical structure composed of an indole nucleus (catharanthine), and a dihydroindole nucleus (vindoline), joined together.
Kingdom
Organic compounds
Super Class
Alkaloids and derivatives
Class
Vinca alkaloids
Sub Class
Not Available
Direct Parent
Vinca alkaloids
Alternative Parents
Carbazoles / 3-alkylindoles / Tricarboxylic acids and derivatives / Anisoles / Dialkylarylamines / Alkyl aryl ethers / Aralkylamines / Piperidines / N-alkylpyrrolidines / Tertiary alcohols
show 12 more
Substituents
Vinca alkaloid skeleton / Carbazole / 3-alkylindole / Tricarboxylic acid or derivatives / Indole or derivatives / Indole / Tertiary aliphatic/aromatic amine / Dialkylarylamine / Anisole / Aralkylamine
show 30 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Adduct
General 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.
Specific Function
Gtp binding
Gene Name
TUBA1A
Uniprot ID
Q71U36
Uniprot Name
Tubulin alpha-1A chain
Molecular Weight
50135.25 Da
References
  1. Jordan MA, Kamath K: How do microtubule-targeted drugs work? An overview. Curr Cancer Drug Targets. 2007 Dec;7(8):730-42. [PubMed:18220533]
  2. Correia JJ: Effects of antimitotic agents on tubulin-nucleotide interactions. Pharmacol Ther. 1991 Nov;52(2):127-47. [PubMed:1818332]
  3. Jordan A, Hadfield JA, Lawrence NJ, McGown AT: Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. [PubMed:9664292]
  4. Islam MN, Iskander MN: Microtubulin binding sites as target for developing anticancer agents. Mini Rev Med Chem. 2004 Dec;4(10):1077-104. [PubMed:15579115]
  5. Gupta S, Bhattacharyya B: Antimicrotubular drugs binding to vinca domain of tubulin. Mol Cell Biochem. 2003 Nov;253(1-2):41-7. [PubMed:14619954]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Adduct
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. Jordan MA, Kamath K: How do microtubule-targeted drugs work? An overview. Curr Cancer Drug Targets. 2007 Dec;7(8):730-42. [PubMed:18220533]
  2. Correia JJ: Effects of antimitotic agents on tubulin-nucleotide interactions. Pharmacol Ther. 1991 Nov;52(2):127-47. [PubMed:1818332]
  3. Jordan A, Hadfield JA, Lawrence NJ, McGown AT: Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. [PubMed:9664292]
  4. Islam MN, Iskander MN: Microtubulin binding sites as target for developing anticancer agents. Mini Rev Med Chem. 2004 Dec;4(10):1077-104. [PubMed:15579115]
  5. Gupta S, Bhattacharyya B: Antimicrotubular drugs binding to vinca domain of tubulin. Mol Cell Biochem. 2003 Nov;253(1-2):41-7. [PubMed:14619954]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Adduct
General Function
Structural constituent of cytoskeleton
Specific Function
In the elongating spermatid it is associated with the manchette, a specialized microtubule system present during reshaping of the sperm head.
Gene Name
TUBD1
Uniprot ID
Q9UJT1
Uniprot Name
Tubulin delta chain
Molecular Weight
51033.86 Da
References
  1. Jordan MA, Kamath K: How do microtubule-targeted drugs work? An overview. Curr Cancer Drug Targets. 2007 Dec;7(8):730-42. [PubMed:18220533]
  2. Correia JJ: Effects of antimitotic agents on tubulin-nucleotide interactions. Pharmacol Ther. 1991 Nov;52(2):127-47. [PubMed:1818332]
  3. Jordan A, Hadfield JA, Lawrence NJ, McGown AT: Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. [PubMed:9664292]
  4. Islam MN, Iskander MN: Microtubulin binding sites as target for developing anticancer agents. Mini Rev Med Chem. 2004 Dec;4(10):1077-104. [PubMed:15579115]
  5. Gupta S, Bhattacharyya B: Antimicrotubular drugs binding to vinca domain of tubulin. Mol Cell Biochem. 2003 Nov;253(1-2):41-7. [PubMed:14619954]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Adduct
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. The gamma chain is found at microtubule organizing centers (MTOC) such as the spindle poles or the centrosome. Pericentriolar matrix component that...
Gene Name
TUBG1
Uniprot ID
P23258
Uniprot Name
Tubulin gamma-1 chain
Molecular Weight
51169.48 Da
References
  1. Jordan MA, Kamath K: How do microtubule-targeted drugs work? An overview. Curr Cancer Drug Targets. 2007 Dec;7(8):730-42. [PubMed:18220533]
  2. Correia JJ: Effects of antimitotic agents on tubulin-nucleotide interactions. Pharmacol Ther. 1991 Nov;52(2):127-47. [PubMed:1818332]
  3. Jordan A, Hadfield JA, Lawrence NJ, McGown AT: Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. [PubMed:9664292]
  4. Islam MN, Iskander MN: Microtubulin binding sites as target for developing anticancer agents. Mini Rev Med Chem. 2004 Dec;4(10):1077-104. [PubMed:15579115]
  5. Gupta S, Bhattacharyya B: Antimicrotubular drugs binding to vinca domain of tubulin. Mol Cell Biochem. 2003 Nov;253(1-2):41-7. [PubMed:14619954]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Adduct
General Function
Structural constituent of cytoskeleton
Specific Function
Not Available
Gene Name
TUBE1
Uniprot ID
Q9UJT0
Uniprot Name
Tubulin epsilon chain
Molecular Weight
52931.4 Da
References
  1. Jordan MA, Kamath K: How do microtubule-targeted drugs work? An overview. Curr Cancer Drug Targets. 2007 Dec;7(8):730-42. [PubMed:18220533]
  2. Correia JJ: Effects of antimitotic agents on tubulin-nucleotide interactions. Pharmacol Ther. 1991 Nov;52(2):127-47. [PubMed:1818332]
  3. Jordan A, Hadfield JA, Lawrence NJ, McGown AT: Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle. Med Res Rev. 1998 Jul;18(4):259-96. [PubMed:9664292]
  4. Islam MN, Iskander MN: Microtubulin binding sites as target for developing anticancer agents. Mini Rev Med Chem. 2004 Dec;4(10):1077-104. [PubMed:15579115]
  5. Gupta S, Bhattacharyya B: Antimicrotubular drugs binding to vinca domain of tubulin. Mol Cell Biochem. 2003 Nov;253(1-2):41-7. [PubMed:14619954]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Other/unknown
General Function
Transcriptional activator activity, rna polymerase ii transcription factor binding
Specific Function
Transcription factor that recognizes and binds to the enhancer heptamer motif 5'-TGA[CG]TCA-3'. Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expre...
Gene Name
JUN
Uniprot ID
P05412
Uniprot Name
Transcription factor AP-1
Molecular Weight
35675.32 Da
References
  1. Brantley-Finley C, Lyle CS, Du L, Goodwin ME, Hall T, Szwedo D, Kaushal GP, Chambers TC: The JNK, ERK and p53 pathways play distinct roles in apoptosis mediated by the antitumor agents vinblastine, doxorubicin, and etoposide. Biochem Pharmacol. 2003 Aug 1;66(3):459-69. [PubMed:12907245]
  2. Bene A, Kurten RC, Chambers TC: Subcellular localization as a limiting factor for utilization of decoy oligonucleotides. Nucleic Acids Res. 2004 Oct 21;32(19):e142. [PubMed:15498923]
  3. Obey TB, Lyle CS, Chambers TC: Role of c-Jun in cellular sensitivity to the microtubule inhibitor vinblastine. Biochem Biophys Res Commun. 2005 Oct 7;335(4):1179-84. [PubMed:16111654]
  4. Martinez-Campa C, Casado P, Rodriguez R, Zuazua P, Garcia-Pedrero JM, Lazo PS, Ramos S: Effect of vinca alkaloids on ERalpha levels and estradiol-induced responses in MCF-7 cells. Breast Cancer Res Treat. 2006 Jul;98(1):81-9. Epub 2006 Mar 23. [PubMed:16555127]
  5. Duan L, Sterba K, Kolomeichuk S, Kim H, Brown PH, Chambers TC: Inducible overexpression of c-Jun in MCF7 cells causes resistance to vinblastine via inhibition of drug-induced apoptosis and senescence at a step subsequent to mitotic arrest. Biochem Pharmacol. 2007 Feb 15;73(4):481-90. Epub 2006 Oct 29. [PubMed:17126817]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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]
  2. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. [PubMed:10490933]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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
Substrate
Inhibitor
Inducer
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. Arora A, Shukla Y: Modulation of vinca-alkaloid induced P-glycoprotein expression by indole-3-carbinol. Cancer Lett. 2003 Jan 28;189(2):167-73. [PubMed:12490309]
  2. Gao J, Murase O, Schowen RL, Aube J, Borchardt RT: A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells. Pharm Res. 2001 Feb;18(2):171-6. [PubMed:11405287]
  3. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514]
  4. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):765-72. [PubMed:12134945]
  5. Horie K, Tang F, Borchardt RT: Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter. Pharm Res. 2003 Feb;20(2):161-8. [PubMed:12636153]
  6. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. [PubMed:12699389]
  7. Tanigawara Y, Okamura N, Hirai M, Yasuhara M, Ueda K, Kioka N, Komano T, Hori R: Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1). J Pharmacol Exp Ther. 1992 Nov;263(2):840-5. [PubMed:1359120]
  8. Tiberghien F, Loor F: Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. Anticancer Drugs. 1996 Jul;7(5):568-78. [PubMed:8862725]
  9. Pouliot JF, L'Heureux F, Liu Z, Prichard RK, Georges E: Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. Biochem Pharmacol. 1997 Jan 10;53(1):17-25. [PubMed:8960059]
  10. Smit JW, Weert B, Schinkel AH, Meijer DK: Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs. J Pharmacol Exp Ther. 1998 Jul;286(1):321-7. [PubMed:9655875]
  11. Shepard RL, Winter MA, Hsaio SC, Pearce HL, Beck WT, Dantzig AH: Effect of modulators on the ATPase activity and vanadate nucleotide trapping of human P-glycoprotein. Biochem Pharmacol. 1998 Sep 15;56(6):719-27. [PubMed:9751076]
  12. Golstein PE, Boom A, van Geffel J, Jacobs P, Masereel B, Beauwens R: P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999 Apr;437(5):652-60. [PubMed:10087141]
  13. Takara K, Tanigawara Y, Komada F, Nishiguchi K, Sakaeda T, Okumura K: Cellular pharmacokinetic aspects of reversal effect of itraconazole on P-glycoprotein-mediated resistance of anticancer drugs. Biol Pharm Bull. 1999 Dec;22(12):1355-9. [PubMed:10746169]
  14. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103]
  15. Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA: Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46. Epub 2004 Dec 22. [PubMed:15616150]
  16. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M, Lin JH: In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther. 2001 Mar;296(3):723-35. [PubMed:11181899]
  17. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684]
  18. Kumar S, Kwei GY, Poon GK, Iliff SA, Wang Y, Chen Q, Franklin RB, Didolkar V, Wang RW, Yamazaki M, Chiu SH, Lin JH, Pearson PG, Baillie TA: Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. J Pharmacol Exp Ther. 2003 Mar;304(3):1161-71. [PubMed:12604693]
  19. Atkinson DE, Greenwood SL, Sibley CP, Glazier JD, Fairbairn LJ: Role of MDR1 and MRP1 in trophoblast cells, elucidated using retroviral gene transfer. Am J Physiol Cell Physiol. 2003 Sep;285(3):C584-91. Epub 2003 Apr 30. [PubMed:12724138]
  20. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019]
  21. Dagenais C, Graff CL, Pollack GM: Variable modulation of opioid brain uptake by P-glycoprotein in mice. Biochem Pharmacol. 2004 Jan 15;67(2):269-76. [PubMed:14698039]
  22. Taipalensuu J, Tavelin S, Lazorova L, Svensson AC, Artursson P: Exploring the quantitative relationship between the level of MDR1 transcript, protein and function using digoxin as a marker of MDR1-dependent drug efflux activity. Eur J Pharm Sci. 2004 Jan;21(1):69-75. [PubMed:14706813]
  23. Hunter J, Hirst BH, Simmons NL: Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers. Pharm Res. 1993 May;10(5):743-9. [PubMed:8100632]
  24. Borgnia MJ, Eytan GD, Assaraf YG: Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J Biol Chem. 1996 Feb 9;271(6):3163-71. [PubMed:8621716]
  25. Dantzig AH, Shepard RL, Law KL, Tabas L, Pratt S, Gillespie JS, Binkley SN, Kuhfeld MT, Starling JJ, Wrighton SA: Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J Pharmacol Exp Ther. 1999 Aug;290(2):854-62. [PubMed:10411602]
  26. Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [PubMed:10617675]
  27. Fedoruk MN, Gimenez-Bonafe P, Guns ES, Mayer LD, Nelson CC: P-glycoprotein increases the efflux of the androgen dihydrotestosterone and reduces androgen responsive gene activity in prostate tumor cells. Prostate. 2004 Apr 1;59(1):77-90. [PubMed:14991868]
  28. Takara K, Sakaeda T, Kakumoto M, Tanigawara Y, Kobayashi H, Okumura K, Ohnishi N, Yokoyama T: Effects of alpha-adrenoceptor antagonist doxazosin on MDR1-mediated multidrug resistance and transcellular transport. Oncol Res. 2009;17(11-12):527-33. [PubMed:19806783]
  29. Jutabha P, Wempe MF, Anzai N, Otomo J, Kadota T, Endou H: Xenopus laevis oocytes expressing human P-glycoprotein: probing trans- and cis-inhibitory effects on [3H]vinblastine and [3H]digoxin efflux. Pharmacol Res. 2010 Jan;61(1):76-84. doi: 10.1016/j.phrs.2009.07.002. Epub 2009 Jul 21. [PubMed:19631272]
  30. Kugawa F, Suzuki T, Miyata M, Tomono K, Tamanoi F: Construction of a model cell line for the assay of MDR1 (multi drug resistance gene-1) substrates/inhibitors using HeLa cells. Pharmazie. 2009 May;64(5):296-300. [PubMed:19530439]
  31. Woodahl EL, Crouthamel MH, Bui T, Shen DD, Ho RJ: MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. doi: 10.1007/s00280-008-0906-4. Epub 2009 Jan 4. [PubMed:19123050]
  32. Ekins S, Kim RB, Leake BF, Dantzig AH, Schuetz EG, Lan LB, Yasuda K, Shepard RL, Winter MA, Schuetz JD, Wikel JH, Wrighton SA: Application of three-dimensional quantitative structure-activity relationships of P-glycoprotein inhibitors and substrates. Mol Pharmacol. 2002 May;61(5):974-81. [PubMed:11961114]
  33. Takara K, Sakaeda T, Yagami T, Kobayashi H, Ohmoto N, Horinouchi M, Nishiguchi K, Okumura K: Cytotoxic effects of 27 anticancer drugs in HeLa and MDR1-overexpressing derivative cell lines. Biol Pharm Bull. 2002 Jun;25(6):771-8. [PubMed:12081145]
  34. Henning U, Loffler S, Krieger K, Klimke A: Uptake of clozapine into HL-60 promyelocytic leukaemia cells. Pharmacopsychiatry. 2002 May;35(3):90-5. [PubMed:12107852]
  35. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):773-9. [PubMed:12134946]
  36. Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG: Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. J Pharmacol Exp Ther. 2002 Oct;303(1):323-32. [PubMed:12235267]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161]
  2. Loe DW, Almquist KC, Cole SP, Deeley RG: ATP-dependent 17 beta-estradiol 17-(beta-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids. J Biol Chem. 1996 Apr 19;271(16):9683-9. [PubMed:8621644]
  3. Flanagan SD, Cummins CL, Susanto M, Liu X, Takahashi LH, Benet LZ: Comparison of furosemide and vinblastine secretion from cell lines overexpressing multidrug resistance protein (P-glycoprotein) and multidrug resistance-associated proteins (MRP1 and MRP2). Pharmacology. 2002;64(3):126-34. [PubMed:11834888]
  4. Yildiz M, Celik-Ozenci C, Akan S, Akan I, Sati L, Demir R, Savas B, Ozben T, Samur M, Ozdogan M, Artac M, Bozcuk H: Zoledronic acid is synergic with vinblastine to induce apoptosis in a multidrug resistance protein-1 dependent way: an in vitro study. Cell Biol Int. 2006 Mar;30(3):278-82. Epub 2006 Feb 2. [PubMed:16458542]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161]
  2. Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA: Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46. Epub 2004 Dec 22. [PubMed:15616150]
  3. Ishikawa T, Muller M, Klunemann C, Schaub T, Keppler D: ATP-dependent primary active transport of cysteinyl leukotrienes across liver canalicular membrane. Role of the ATP-dependent transport system for glutathione S-conjugates. J Biol Chem. 1990 Nov 5;265(31):19279-86. [PubMed:2172249]
  4. Tang F, Horie K, Borchardt RT: Are MDCK cells transfected with the human MRP2 gene a good model of the human intestinal mucosa? Pharm Res. 2002 Jun;19(6):773-9. [PubMed:12134946]
  5. Baltes S, Gastens AM, Fedrowitz M, Potschka H, Kaever V, Loscher W: Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology. 2007 Feb;52(2):333-46. Epub 2006 Oct 10. [PubMed:17045309]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4...
Gene Name
ABCC6
Uniprot ID
O95255
Uniprot Name
Multidrug resistance-associated protein 6
Molecular Weight
164904.81 Da
References
  1. Cai J, Daoud R, Alqawi O, Georges E, Pelletier J, Gros P: Nucleotide binding and nucleotide hydrolysis properties of the ABC transporter MRP6 (ABCC6). Biochemistry. 2002 Jun 25;41(25):8058-67. [PubMed:12069597]
Details
5. Bile salt export pump
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759]
  2. Lecureur V, Sun D, Hargrove P, Schuetz EG, Kim RB, Lan LB, Schuetz JD: Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein. Mol Pharmacol. 2000 Jan;57(1):24-35. [PubMed:10617675]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]

Drug created on June 13, 2005 07:24 / Updated on August 15, 2018 09:41