Identification
NameTesmilifene
Accession NumberDB04905
TypeSmall Molecule
GroupsInvestigational
Description

Tesmilifene is a novel potentiator of chemotherapy which, when added to doxorubicin, achieved an unexpected and very large survival advantage over doxorubicin alone in a randomized trial in advanced breast cancer.

Structure
Thumb
Synonyms
Depmpe
DPPE
N,N-diethyl-2-((4-phenylmethyl)phenoxy)ethanamine
External IDs Not Available
Product Ingredients Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNIII43T3ID6G2
CAS number98774-23-3
WeightAverage: 283.4079
Monoisotopic: 283.193614427
Chemical FormulaC19H25NO
InChI KeyNFIXBCVWIPOYCD-UHFFFAOYSA-N
InChI
InChI=1S/C19H25NO/c1-3-20(4-2)14-15-21-19-12-10-18(11-13-19)16-17-8-6-5-7-9-17/h5-13H,3-4,14-16H2,1-2H3
IUPAC Name
[2-(4-benzylphenoxy)ethyl]diethylamine
SMILES
CCN(CC)CCOC1=CC=C(CC2=CC=CC=C2)C=C1
Pharmacology
Indication

Intended for the treatment of various forms of cancer.

Structured Indications Not Available
PharmacodynamicsNot Available
Mechanism of action

Although the exact mechanism of action is not known, one study (PMID: 16413681) proposes that tesmilifene may be an activating p-gp substrate, which enables the p-gp pump to extrude typical p-gp substrates (such as anthracyclines or taxanes) more efficiently. This process consumes ATP, since the p-gp is absolutely, and highly dependent on ATP hydrolysis. The mechanism of cell death is likely to result not from the presence of chemotherapy inside the cell (in fact the chemotherapy is extruded) but, directly or indirectly, from the enhanced consumption of ATP. The ATP may be consumed below a threshold necessary for survival, or, (more likely) the enhanced ATP production required to maintain ATP levels may result in the generation of reactive oxygen species (ROS) to an extent that overwhelms the cell’s ability to inactivate them. The result would be additional cell death, but only in the mdr+ population. The doxorubicin would continue to act on the drug sensitive remainder of the cell population, but without the help of tesmilifene.

TargetKindPharmacological actionActionsOrganismUniProt ID
Multidrug resistance protein 1Proteinyes
inducer
HumanP08183 details
Histamine H1 receptorProteinunknown
antagonist
HumanP35367 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Tesmilifene.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Tesmilifene.Experimental, Illicit
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Tesmilifene.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Tesmilifene.Experimental, Illicit
AbciximabTesmilifene may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Tesmilifene can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Tesmilifene.Approved
AcenocoumarolTesmilifene may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Acetaminophen can be decreased when it is combined with Tesmilifene.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Acetylsalicylic acid.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be decreased when it is combined with Tesmilifene.Approved
AldosteroneThe serum concentration of Aldosterone can be decreased when it is combined with Tesmilifene.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be decreased when it is combined with Tesmilifene.Approved, Investigational
AlprostadilAlprostadil may increase the antiplatelet activities of Tesmilifene.Approved, Investigational
AlteplaseTesmilifene may increase the anticoagulant activities of Alteplase.Approved
ALX-0081Tesmilifene may increase the anticoagulant activities of ALX-0081.Investigational
AmbrisentanThe serum concentration of Ambrisentan can be decreased when it is combined with Tesmilifene.Approved, Investigational
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Aminosalicylic Acid.Approved
AmiodaroneThe metabolism of Tesmilifene can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be decreased when it is combined with Tesmilifene.Approved
AmphetamineAmphetamine may decrease the sedative activities of Tesmilifene.Approved, Illicit
AnagrelideTesmilifene may increase the anticoagulant activities of Anagrelide.Approved
AncrodTesmilifene may increase the anticoagulant activities of Ancrod.Investigational
AnistreplaseTesmilifene may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanTesmilifene may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Apixaban.Approved
AprepitantThe serum concentration of Tesmilifene can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinTesmilifene may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanTesmilifene may increase the anticoagulant activities of Argatroban.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Tesmilifene.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be decreased when it is combined with Tesmilifene.Approved, Investigational
ArtemetherThe metabolism of Tesmilifene can be decreased when combined with Artemether.Approved
AstaxanthinTesmilifene may increase the anticoagulant activities of Astaxanthin.Investigational
AtazanavirThe metabolism of Tesmilifene can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be decreased when it is combined with Tesmilifene.Approved
AtomoxetineThe metabolism of Tesmilifene can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be decreased when it is combined with Tesmilifene.Approved, Investigational
AzelastineAzelastine may increase the antiplatelet activities of Tesmilifene.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Balsalazide.Approved, Investigational
BatroxobinTesmilifene may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminTesmilifene may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinTesmilifene may increase the anticoagulant activities of Bemiparin.Approved
BenzphetamineBenzphetamine may decrease the sedative activities of Tesmilifene.Approved, Illicit
Benzylpenicilloyl PolylysineTesmilifene may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BeraprostTesmilifene may increase the anticoagulant activities of Beraprost.Investigational
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Tesmilifene.Approved
BetamethasoneThe serum concentration of Betamethasone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
BetaxololThe metabolism of Tesmilifene can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Tesmilifene can be decreased when it is combined with Bexarotene.Approved, Investigational
BivalirudinTesmilifene may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Tesmilifene can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Tesmilifene can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Tesmilifene can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be decreased when it is combined with Tesmilifene.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be decreased when it is combined with Tesmilifene.Approved
BromocriptineThe serum concentration of Bromocriptine can be decreased when it is combined with Tesmilifene.Approved, Investigational
BupropionThe metabolism of Tesmilifene can be decreased when combined with Bupropion.Approved
ButylphthalideTesmilifene may increase the antiplatelet activities of Butylphthalide.Investigational
CabazitaxelThe serum concentration of Cabazitaxel can be decreased when it is combined with Tesmilifene.Approved
CaffeineThe serum concentration of Caffeine can be decreased when it is combined with Tesmilifene.Approved
CamptothecinThe serum concentration of Camptothecin can be decreased when it is combined with Tesmilifene.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be decreased when it is combined with Tesmilifene.Approved
CangrelorTesmilifene may increase the anticoagulant activities of Cangrelor.Approved
CarbamazepineThe metabolism of Tesmilifene can be increased when combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be decreased when it is combined with Tesmilifene.Approved
CelecoxibThe metabolism of Tesmilifene can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Tesmilifene can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be decreased when it is combined with Tesmilifene.Withdrawn
CertoparinTesmilifene may increase the anticoagulant activities of Certoparin.Approved
ChloroquineThe metabolism of Tesmilifene can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorphentermineChlorphentermine may decrease the sedative activities of Tesmilifene.Illicit, Withdrawn
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
CholecalciferolThe metabolism of Tesmilifene can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolTesmilifene may increase the anticoagulant activities of Cilostazol.Approved
CimetidineThe serum concentration of Cimetidine can be decreased when it is combined with Tesmilifene.Approved
CinacalcetThe metabolism of Tesmilifene can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be decreased when it is combined with Tesmilifene.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be decreased when it is combined with Tesmilifene.Approved
CitalopramThe serum concentration of Citalopram can be decreased when it is combined with Tesmilifene.Approved
Citric AcidTesmilifene may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Tesmilifene can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Tesmilifene can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be decreased when it is combined with Tesmilifene.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be decreased when it is combined with Tesmilifene.Approved, Investigational
ClomipramineThe metabolism of Tesmilifene can be decreased when combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be decreased when it is combined with Tesmilifene.Approved
ClopidogrelThe serum concentration of Clopidogrel can be decreased when it is combined with Tesmilifene.Approved, Nutraceutical
ClotrimazoleThe metabolism of Tesmilifene can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be decreased when it is combined with Tesmilifene.Approved
CobicistatThe serum concentration of Tesmilifene can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be decreased when it is combined with Tesmilifene.Approved
CocaineThe metabolism of Tesmilifene can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be decreased when it is combined with Tesmilifene.Approved
ConivaptanThe serum concentration of Tesmilifene can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Tesmilifene.Approved
CrizotinibThe metabolism of Tesmilifene can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Tesmilifene can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be decreased when it is combined with Tesmilifene.Approved
DabrafenibThe serum concentration of Tesmilifene can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be decreased when it is combined with Tesmilifene.Approved
DalteparinTesmilifene may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidTesmilifene may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DapagliflozinThe serum concentration of Dapagliflozin can be decreased when it is combined with Tesmilifene.Approved
DarexabanTesmilifene may increase the anticoagulant activities of Ym150.Investigational
DarifenacinThe metabolism of Tesmilifene can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Tesmilifene can be increased when it is combined with Darunavir.Approved
DasatinibDasatinib may increase the anticoagulant activities of Tesmilifene.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be decreased when it is combined with Tesmilifene.Approved
DebrisoquinThe serum concentration of Debrisoquin can be decreased when it is combined with Tesmilifene.Approved
DeferasiroxThe serum concentration of Tesmilifene can be decreased when it is combined with Deferasirox.Approved, Investigational
DefibrotideTesmilifene may increase the anticoagulant activities of Defibrotide.Approved, Investigational
DelavirdineThe metabolism of Tesmilifene can be decreased when combined with Delavirdine.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Deoxycholic Acid.Approved
dersalazineThe risk or severity of adverse effects can be increased when Tesmilifene is combined with dersalazine.Investigational
DesipramineThe metabolism of Tesmilifene can be decreased when combined with Desipramine.Approved
DesirudinTesmilifene may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseTesmilifene may increase the anticoagulant activities of Desmoteplase.Investigational
DexamethasoneThe serum concentration of Tesmilifene can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextranTesmilifene may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Tesmilifene may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Tesmilifene may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Tesmilifene may increase the anticoagulant activities of Dextran 75.Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Tesmilifene.Approved, Illicit
DiazepamThe serum concentration of Diazepam can be decreased when it is combined with Tesmilifene.Approved, Illicit, Vet Approved
DicoumarolTesmilifene may increase the anticoagulant activities of Dicoumarol.Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Tesmilifene.Approved, Illicit
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Tesmilifene.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Diflunisal.Approved
DigitoxinThe serum concentration of Digitoxin can be decreased when it is combined with Tesmilifene.Approved
DigoxinThe serum concentration of Digoxin can be decreased when it is combined with Tesmilifene.Approved
DihydroergotamineThe metabolism of Tesmilifene can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be decreased when it is combined with Tesmilifene.Illicit
DiltiazemThe metabolism of Tesmilifene can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Tesmilifene can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Dipyridamole can be decreased when it is combined with Tesmilifene.Approved
DitazoleTesmilifene may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DocetaxelThe serum concentration of Docetaxel can be decreased when it is combined with Tesmilifene.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be decreased when it is combined with Tesmilifene.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Tesmilifene.Approved, Investigational
DoxycyclineThe metabolism of Tesmilifene can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Tesmilifene can be decreased when combined with Dronedarone.Approved
Drotrecogin alfaTesmilifene may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
DuloxetineThe metabolism of Tesmilifene can be decreased when combined with Duloxetine.Approved
Edetic AcidTesmilifene may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be decreased when it is combined with Tesmilifene.Approved
EfavirenzThe serum concentration of Tesmilifene can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be decreased when it is combined with Tesmilifene.Approved, Investigational
EliglustatThe metabolism of Tesmilifene can be decreased when combined with Eliglustat.Approved
EnoxaparinTesmilifene may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Tesmilifene can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be decreased when it is combined with Tesmilifene.Approved, Investigational
eplivanserineTesmilifene may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolEpoprostenol may increase the antiplatelet activities of Tesmilifene.Approved
EptifibatideTesmilifene may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be decreased when it is combined with Tesmilifene.Approved, Investigational
ErythromycinThe metabolism of Tesmilifene can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Tesmilifene can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Tesmilifene.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be decreased when it is combined with Tesmilifene.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Tesmilifene.Approved
Ethyl biscoumacetateTesmilifene may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Etoposide can be decreased when it is combined with Tesmilifene.Approved
EtravirineThe serum concentration of Tesmilifene can be decreased when it is combined with Etravirine.Approved
EzetimibeThe serum concentration of Ezetimibe can be decreased when it is combined with Tesmilifene.Approved
FesoterodineThe serum concentration of Fesoterodine can be decreased when it is combined with Tesmilifene.Approved
FexofenadineThe serum concentration of Fexofenadine can be decreased when it is combined with Tesmilifene.Approved
FibrinolysinTesmilifene may increase the anticoagulant activities of Plasmin.Investigational
FidaxomicinThe serum concentration of Fidaxomicin can be decreased when it is combined with Tesmilifene.Approved
FluconazoleThe metabolism of Tesmilifene can be decreased when combined with Fluconazole.Approved
FluindioneTesmilifene may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe metabolism of Tesmilifene can be decreased when combined with Fluoxetine.Approved, Vet Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be decreased when it is combined with Tesmilifene.Approved
FluvoxamineThe metabolism of Tesmilifene can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxTesmilifene may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumTesmilifene may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe metabolism of Tesmilifene can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Tesmilifene can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Tesmilifene can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Tesmilifene can be increased when it is combined with Fusidic Acid.Approved
GabexateTesmilifene may increase the anticoagulant activities of Gabexate.Investigational
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Tesmilifene.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be decreased when it is combined with Tesmilifene.Approved
GlucosamineGlucosamine may increase the antiplatelet activities of Tesmilifene.Approved
GrazoprevirThe serum concentration of Grazoprevir can be decreased when it is combined with Tesmilifene.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be decreased when it is combined with Tesmilifene.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Tesmilifene.Approved
HeparinTesmilifene may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineTesmilifene may increase the anticoagulant activities of Higenamine.Investigational
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Tesmilifene.Approved, Investigational
HydrocortisoneThe serum concentration of Hydrocortisone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
HydroxyamphetamineHydroxyamphetamine hydrobromide may decrease the sedative activities of Tesmilifene.Approved
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Tesmilifene.Approved
IbudilastTesmilifene may increase the antiplatelet activities of Ibudilast.Approved, Investigational
IbuprofenThe serum concentration of Ibuprofen can be decreased when it is combined with Tesmilifene.Approved
Icosapent ethylTesmilifene may increase the antiplatelet activities of Icosapent ethyl.Approved, Nutraceutical
IdelalisibThe serum concentration of Tesmilifene can be increased when it is combined with Idelalisib.Approved
IdraparinuxTesmilifene may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilTesmilifene may increase the antiplatelet activities of Ifenprodil.Approved, Withdrawn
IloprostIloprost may increase the antiplatelet activities of Tesmilifene.Approved, Investigational
ImatinibThe metabolism of Tesmilifene can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be decreased when it is combined with Tesmilifene.Approved
IndacaterolThe serum concentration of Indacaterol can be decreased when it is combined with Tesmilifene.Approved
IndinavirThe metabolism of Tesmilifene can be decreased when combined with Indinavir.Approved
IndobufenTesmilifene may increase the anticoagulant activities of Indobufen.Investigational
IndomethacinThe serum concentration of Indomethacin can be decreased when it is combined with Tesmilifene.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be decreased when it is combined with Tesmilifene.Approved, Investigational
IsavuconazoniumThe metabolism of Tesmilifene can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Tesmilifene can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Tesmilifene can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Tesmilifene can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Tesmilifene can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
KetanserinTesmilifene may increase the antiplatelet activities of Ketanserin.Investigational
KetazolamThe serum concentration of Ketazolam can be decreased when it is combined with Tesmilifene.Approved
KetoconazoleThe metabolism of Tesmilifene can be decreased when combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be decreased when it is combined with Tesmilifene.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Tesmilifene.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be decreased when it is combined with Tesmilifene.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be decreased when it is combined with Tesmilifene.Approved
LenalidomideThe serum concentration of Lenalidomide can be decreased when it is combined with Tesmilifene.Approved
LenvatinibThe serum concentration of Lenvatinib can be decreased when it is combined with Tesmilifene.Approved
LepirudinTesmilifene may increase the anticoagulant activities of Lepirudin.Approved
LevetiracetamThe serum concentration of Levetiracetam can be decreased when it is combined with Tesmilifene.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be decreased when it is combined with Tesmilifene.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be decreased when it is combined with Tesmilifene.Approved
LimaprostLimaprost may increase the antiplatelet activities of Tesmilifene.Approved
LinagliptinThe serum concentration of Linagliptin can be decreased when it is combined with Tesmilifene.Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Tesmilifene.Approved, Investigational
LoperamideThe serum concentration of Loperamide can be decreased when it is combined with Tesmilifene.Approved
LopinavirThe metabolism of Tesmilifene can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Tesmilifene can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Losartan can be decreased when it is combined with Tesmilifene.Approved
LovastatinThe metabolism of Tesmilifene can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Tesmilifene can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Tesmilifene can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Tesmilifene can be decreased when combined with Lumefantrine.Approved
MannitolThe serum concentration of Mannitol can be decreased when it is combined with Tesmilifene.Approved, Investigational
MephedroneMephedrone may decrease the sedative activities of Tesmilifene.Investigational
MephentermineMephentermine may decrease the sedative activities of Tesmilifene.Approved
MesalazineThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Mesalazine.Approved
MethadoneThe metabolism of Tesmilifene can be decreased when combined with Methadone.Approved
MethamphetamineMethamphetamine may decrease the sedative activities of Tesmilifene.Approved, Illicit
MethotrexateThe serum concentration of Methotrexate can be decreased when it is combined with Tesmilifene.Approved
MethotrimeprazineThe metabolism of Tesmilifene can be decreased when combined with Methotrimeprazine.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Tesmilifene.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be decreased when it is combined with Tesmilifene.Approved, Illicit
MifepristoneThe serum concentration of Tesmilifene can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the antiplatelet activities of Tesmilifene.Approved
MirabegronThe serum concentration of Mirabegron can be decreased when it is combined with Tesmilifene.Approved
MitotaneThe serum concentration of Tesmilifene can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be decreased when it is combined with Tesmilifene.Approved, Investigational
MMDAMMDA may decrease the sedative activities of Tesmilifene.Experimental, Illicit
ModafinilThe serum concentration of Tesmilifene can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be decreased when it is combined with Tesmilifene.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Tesmilifene.Approved, Investigational
NadololThe serum concentration of Nadolol can be decreased when it is combined with Tesmilifene.Approved
NadroparinTesmilifene may increase the anticoagulant activities of Nadroparin.Approved
NafamostatTesmilifene may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NafcillinThe serum concentration of Tesmilifene can be decreased when it is combined with Nafcillin.Approved
NaftopidilTesmilifene may increase the antiplatelet activities of Naftopidil.Investigational
NaloxoneThe serum concentration of Naloxone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
NefazodoneThe metabolism of Tesmilifene can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Tesmilifene can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Tesmilifene can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Tesmilifene can be increased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be decreased when it is combined with Tesmilifene.Approved
NifedipineThe serum concentration of Nifedipine can be decreased when it is combined with Tesmilifene.Approved
NilotinibThe metabolism of Tesmilifene can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the antiplatelet activities of Tesmilifene.Approved, Withdrawn
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Tesmilifene.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Nitroaspirin.Investigational
NizatidineThe serum concentration of Nizatidine can be decreased when it is combined with Tesmilifene.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Obinutuzumab.Approved
OlanzapineThe serum concentration of Olanzapine can be decreased when it is combined with Tesmilifene.Approved, Investigational
OlaparibThe metabolism of Tesmilifene can be decreased when combined with Olaparib.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Olsalazine.Approved
OmbitasvirThe serum concentration of Ombitasvir can be decreased when it is combined with Tesmilifene.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Tesmilifene.Approved, Nutraceutical
OsimertinibThe serum concentration of Tesmilifene can be increased when it is combined with Osimertinib.Approved
OtamixabanTesmilifene may increase the anticoagulant activities of Otamixaban.Investigational
OzagrelTesmilifene may increase the anticoagulant activities of Kct 0809.Investigational
PaclitaxelThe serum concentration of Paclitaxel can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
PalbociclibThe serum concentration of Tesmilifene can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Tesmilifene can be increased when it is combined with Panobinostat.Approved, Investigational
ParnaparinTesmilifene may increase the anticoagulant activities of Parnaparin.Approved
ParoxetineThe metabolism of Tesmilifene can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be decreased when it is combined with Tesmilifene.Approved
Peginterferon alfa-2bThe serum concentration of Tesmilifene can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Tesmilifene can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Tesmilifene.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Tesmilifene.Approved, Investigational
PhenindioneTesmilifene may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Tesmilifene can be increased when combined with Phenobarbital.Approved
PhenprocoumonTesmilifene may increase the anticoagulant activities of Phenprocoumon.Approved
PhenterminePhentermine may decrease the sedative activities of Tesmilifene.Approved, Illicit
PhenytoinThe metabolism of Tesmilifene can be increased when combined with Phenytoin.Approved, Vet Approved
PitavastatinThe serum concentration of Pitavastatin can be decreased when it is combined with Tesmilifene.Approved
PomalidomideThe serum concentration of Pomalidomide can be decreased when it is combined with Tesmilifene.Approved
PonatinibThe serum concentration of Ponatinib can be decreased when it is combined with Tesmilifene.Approved
PosaconazoleThe metabolism of Tesmilifene can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelTesmilifene may increase the anticoagulant activities of Prasugrel.Approved
PravastatinThe serum concentration of Pravastatin can be decreased when it is combined with Tesmilifene.Approved
PrazosinThe serum concentration of Prazosin can be decreased when it is combined with Tesmilifene.Approved
PrednisoloneThe serum concentration of Prednisolone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
PrimidoneThe metabolism of Tesmilifene can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be decreased when it is combined with Tesmilifene.Approved, Vet Approved
PromazineThe metabolism of Tesmilifene can be decreased when combined with Promazine.Approved, Vet Approved
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Tesmilifene.Approved, Investigational
Protein CTesmilifene may increase the anticoagulant activities of Protein C.Approved
Protein S humanTesmilifene may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeTesmilifene may increase the anticoagulant activities of Protocatechualdehyde.Approved
PseudoephedrinePseudoephedrine may decrease the sedative activities of Tesmilifene.Approved
QuetiapineThe serum concentration of Quetiapine can be decreased when it is combined with Tesmilifene.Approved
QuinidineThe metabolism of Tesmilifene can be decreased when combined with Quinidine.Approved
QuinineThe serum concentration of Quinine can be decreased when it is combined with Tesmilifene.Approved
RamatrobanTesmilifene may increase the antiplatelet activities of Ramatroban.Investigational
RanitidineThe serum concentration of Ranitidine can be decreased when it is combined with Tesmilifene.Approved
RanolazineThe metabolism of Tesmilifene can be decreased when combined with Ranolazine.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be decreased when it is combined with Tesmilifene.Approved
ResveratrolResveratrol may increase the antiplatelet activities of Tesmilifene.Experimental, Investigational
ReteplaseTesmilifene may increase the anticoagulant activities of Reteplase.Approved
ReviparinTesmilifene may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the antiplatelet activities of Tesmilifene.Approved
RifabutinThe metabolism of Tesmilifene can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Tesmilifene can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Tesmilifene can be increased when combined with Rifapentine.Approved
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Tesmilifene.Approved, Investigational
RitobegronRitobegron may decrease the sedative activities of Tesmilifene.Investigational
RitonavirThe metabolism of Tesmilifene can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanTesmilifene may increase the anticoagulant activities of Rivaroxaban.Approved
RolapitantThe metabolism of Tesmilifene can be decreased when combined with Rolapitant.Approved
RomidepsinThe serum concentration of Romidepsin can be decreased when it is combined with Tesmilifene.Approved, Investigational
RopiniroleThe metabolism of Tesmilifene can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneTesmilifene may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Salicylic acid.Approved, Vet Approved
SaquinavirThe metabolism of Tesmilifene can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Tesmilifene.Approved
SelexipagThe serum concentration of Selexipag can be decreased when it is combined with Tesmilifene.Approved
SertralineThe metabolism of Tesmilifene can be decreased when combined with Sertraline.Approved
SevofluraneSevoflurane may increase the antiplatelet activities of Tesmilifene.Approved, Vet Approved
SildenafilThe metabolism of Tesmilifene can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be decreased when it is combined with Tesmilifene.Approved
SiltuximabThe serum concentration of Tesmilifene can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Tesmilifene can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Sitagliptin can be decreased when it is combined with Tesmilifene.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be decreased when it is combined with Tesmilifene.Approved
SorafenibThe serum concentration of Sorafenib can be decreased when it is combined with Tesmilifene.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be decreased when it is combined with Tesmilifene.Approved
SphingosineThe serum concentration of Sphingosine can be decreased when it is combined with Tesmilifene.Experimental
SRT501Tesmilifene may increase the antiplatelet activities of SRT501.Investigational
St. John's WortThe serum concentration of Tesmilifene can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Tesmilifene can be increased when it is combined with Stiripentol.Approved
StreptokinaseTesmilifene may increase the anticoagulant activities of Streptokinase.Approved
SulfisoxazoleThe metabolism of Tesmilifene can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideTesmilifene may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TacrolimusThe serum concentration of Tacrolimus can be decreased when it is combined with Tesmilifene.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Tesmilifene.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be decreased when it is combined with Tesmilifene.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be decreased when it is combined with Tesmilifene.Approved
TelaprevirThe metabolism of Tesmilifene can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Tesmilifene can be decreased when combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Temsirolimus can be decreased when it is combined with Tesmilifene.Approved
TenecteplaseTesmilifene may increase the anticoagulant activities of Tenecteplase.Approved
TerbinafineThe metabolism of Tesmilifene can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
ThioridazineThe metabolism of Tesmilifene can be decreased when combined with Thioridazine.Withdrawn
TicagrelorThe serum concentration of Ticagrelor can be decreased when it is combined with Tesmilifene.Approved
TiclopidineThe metabolism of Tesmilifene can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be decreased when it is combined with Tesmilifene.Approved
TinzaparinTesmilifene may increase the anticoagulant activities of Tinzaparin.Approved
TipranavirTipranavir may increase the antiplatelet activities of Tesmilifene.Approved, Investigational
TirofibanTesmilifene may increase the anticoagulant activities of Tirofiban.Approved
TocilizumabThe serum concentration of Tesmilifene can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Tolvaptan can be decreased when it is combined with Tesmilifene.Approved
TopotecanThe serum concentration of Topotecan can be decreased when it is combined with Tesmilifene.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be decreased when it is combined with Tesmilifene.Approved, Investigational
TositumomabThe risk or severity of adverse effects can be increased when Tesmilifene is combined with Tositumomab.Approved
TranilastTesmilifene may increase the antiplatelet activities of Tranilast.Approved, Investigational
TranylcypromineThe metabolism of Tesmilifene can be decreased when combined with Tranylcypromine.Approved
TrapidilTesmilifene may increase the antiplatelet activities of Trapidil.Approved
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be decreased when it is combined with Tesmilifene.Approved
TreprostinilTreprostinil may increase the antiplatelet activities of Tesmilifene.Approved, Investigational
TriflusalTesmilifene may increase the anticoagulant activities of Triflusal.Approved
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Tesmilifene.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be decreased when it is combined with Tesmilifene.Approved
UrokinaseTesmilifene may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
VecuroniumThe serum concentration of Vecuronium can be decreased when it is combined with Tesmilifene.Approved
VenetoclaxThe serum concentration of Venetoclax can be decreased when it is combined with Tesmilifene.Approved
VenlafaxineThe metabolism of Tesmilifene can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Tesmilifene can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be decreased when it is combined with Tesmilifene.Approved
VincristineThe serum concentration of Vincristine can be decreased when it is combined with Tesmilifene.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be decreased when it is combined with Tesmilifene.Approved
Vitamin EVitamin E may increase the antiplatelet activities of Tesmilifene.Approved, Nutraceutical, Vet Approved
VorapaxarTesmilifene may increase the anticoagulant activities of Vorapaxar.Approved
VoriconazoleThe metabolism of Tesmilifene can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinTesmilifene may increase the anticoagulant activities of Warfarin.Approved
XimelagatranTesmilifene may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Tesmilifene.Approved
ZiprasidoneThe metabolism of Tesmilifene can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Liu J, Tu D, Dancey J, Reyno L, Pritchard KI, Pater J, Seymour LK: Quality of life analyses in a clinical trial of DPPE (tesmilifene) plus doxorubicin versus doxorubicin in patients with advanced or metastatic breast cancer: NCIC CTG Trial MA.19. Breast Cancer Res Treat. 2006 Dec;100(3):263-71. Epub 2006 Jul 6. [PubMed:16823511 ]
  2. Vincent M: Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31. Epub 2006 Jan 18. [PubMed:16413681 ]
  3. Raghavan D, Brandes LJ, Klapp K, Snyder T, Styles E, Tsao-Wei D, Lieskovsky G, Quinn DI, Ramsey EW: Phase II trial of tesmilifene plus mitoxantrone and prednisone for hormone refractory prostate cancer: high subjective and objective response in patients with symptomatic metastases. J Urol. 2005 Nov;174(5):1808-13; discussion 1813. [PubMed:16217292 ]
  4. Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. [PubMed:10755318 ]
  5. Brandes LJ, Hogg GR: Study of the in-vivo antioestrogenic action of N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine HCl (DPPE), a novel intracellular histamine antagonist and antioestrogen binding site ligand. J Reprod Fertil. 1990 May;89(1):59-67. [PubMed:2374133 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentMetastatic/Recurrent Breast Cancer1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00905 mg/mLALOGPS
logP4.65ALOGPS
logP4.64ChemAxon
logS-4.5ALOGPS
pKa (Strongest Basic)9.33ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity89.77 m3·mol-1ChemAxon
Polarizability33.95 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9935
Blood Brain Barrier+0.9482
Caco-2 permeable+0.8072
P-glycoprotein substrateSubstrate0.7041
P-glycoprotein inhibitor IInhibitor0.5341
P-glycoprotein inhibitor IINon-inhibitor0.885
Renal organic cation transporterInhibitor0.7133
CYP450 2C9 substrateNon-substrate0.7941
CYP450 2D6 substrateSubstrate0.6482
CYP450 3A4 substrateSubstrate0.5967
CYP450 1A2 substrateInhibitor0.9707
CYP450 2C9 inhibitorInhibitor0.5636
CYP450 2D6 inhibitorInhibitor0.9575
CYP450 2C19 inhibitorInhibitor0.6944
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8296
Ames testNon AMES toxic0.5749
CarcinogenicityNon-carcinogens0.657
BiodegradationNot ready biodegradable0.9877
Rat acute toxicity2.2808 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7258
hERG inhibition (predictor II)Inhibitor0.8407
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of chemical entities known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
KingdomChemical entities
Super ClassOrganic compounds
ClassBenzenoids
Sub ClassBenzene and substituted derivatives
Direct ParentDiphenylmethanes
Alternative ParentsPhenoxy compounds / Phenol ethers / Alkyl aryl ethers / Trialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
SubstituentsDiphenylmethane / Phenoxy compound / Phenol ether / Alkyl aryl ether / Tertiary aliphatic amine / Tertiary amine / Ether / Organic nitrogen compound / Organic oxygen compound / Organopnictogen compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
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. Vincent M: Tesmilifene may enhance breast cancer chemotherapy by killing a clone of aggressive, multi-drug resistant cells through its action on the p-glycoprotein pump. Med Hypotheses. 2006;66(4):715-31. Epub 2006 Jan 18. [PubMed:16413681 ]
  2. Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. [PubMed:10755318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Histamine receptor activity
Specific Function:
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
Uniprot Name:
Histamine H1 receptor
Molecular Weight:
55783.61 Da
References
  1. Brandes LJ, Bogdanovic RP, Cawker MD, LaBella FS: Histamine and growth: interaction of antiestrogen binding site ligands with a novel histamine site that may be associated with calcium channels. Cancer Res. 1987 Aug 1;47(15):4025-31. [PubMed:2886214 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da
References
  1. Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. [PubMed:10755318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Uniprot Name:
Cytochrome P450 2D6
Molecular Weight:
55768.94 Da
References
  1. Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. [PubMed:10755318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Uniprot Name:
Cytochrome P450 1A1
Molecular Weight:
58164.815 Da
References
  1. Brandes LJ, Queen GM, LaBella FS: N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs. Cancer Chemother Pharmacol. 2000;45(4):298-304. [PubMed:10755318 ]
Drug created on October 21, 2007 16:23 / Updated on September 01, 2017 11:23