Identification

Name
Testosterone undecanoate
Accession Number
DB13946  (DBSALT001033)
Type
Small Molecule
Groups
Approved, Investigational
Description

Testosterone undecanoate is an esterified form of testosterone which is attached to a long fatty acid chain. The lack of a methylated site on the carbon 17 eliminates the adverse effects on the liver found in other testosterone analogs.[5] It is currently getting further developed to be an alternative to testosterone enanthate or testosterone cypionate by Paddock labs, and this new injectable has an FDA status of tentative approval. The original approval by the FDA of a product from testosterone undecanoate was done in 1953.

Structure
Thumb
Synonyms
  • Testosterone undeconate
  • Testosterone undecylate
External IDs
BAY 86-5037 / BRN 3176734 / CLR-610 / ORG 538 / ORG-538
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AndriolCapsule40 mgOralMerck Ltd.1992-12-31Not applicableCanada
AveedInjection250 mg/mLIntramuscularEndo Pharmaceuticals Solutions Inc.2014-03-05Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PMS-testosteroneCapsule40 mgOralPharmascience Inc2009-10-08Not applicableCanada
Taro-testosteroneCapsule40 mgOralTaro Pharmaceuticals, Inc.2014-09-02Not applicableCanada
Categories
UNII
H16A5VCT9C
CAS number
5949-44-0
Weight
Average: 456.711
Monoisotopic: 456.360345406
Chemical Formula
C30H48O3
InChI Key
UDSFVOAUHKGBEK-CNQKSJKFSA-N
InChI
InChI=1S/C30H48O3/c1-4-5-6-7-8-9-10-11-12-28(32)33-27-16-15-25-24-14-13-22-21-23(31)17-19-29(22,2)26(24)18-20-30(25,27)3/h21,24-27H,4-20H2,1-3H3/t24-,25-,26-,27-,29-,30-/m0/s1
IUPAC Name
(1S,3aS,3bR,9aR,9bS,11aS)-9a,11a-dimethyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl undecanoate
SMILES

Pharmacology

Indication

Testosterone undecanoate is indicated as a testosterone replacement therapy in adult males that present conditions of deficiency or absence of endogenous testosterone. The approved conditions for the use of testosterone undecanoate are 1) primary hypogonadism, defined as a testicular failure due to cryptorchidism, bilateral torsion, orchitis, vanishing testis syndrome, orchiectomy, Klinefelter's syndrome, chemotherapy or toxic damage from alcohol or heavy metals: or 2) hypogonadotropic hypogonadism caused by idiopathic gonadotropin or luteinizing hormone-releasing hormone deficiency or pituitary-hypothalamic injuries from tumors, trauma or radiation.[FDA Label]

Structured Indications
Pharmacodynamics

Clinical studies with testosterone undecanoate have shown a constant level of plasma testosterone over the weeks without falling on levels under the lower normal limit and briefly being over the normal upper limit. The levels of dihydrotestosterone and estradiol were suppressed but also remain within the normal limits. All these hormonal alterations remain stable even two weeks after the administration cease.[2]

Mechanism of action

The effects of testosterone in humans and other vertebrates occur by way of two primary mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of specific estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5-alpha-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5-alpha-reductase. The T-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.[1]

TargetActionsOrganism
AAndrogen receptor
agonist
Human
UEstrogen receptor alphaNot AvailableHuman
UMineralocorticoid receptorNot AvailableHuman
Absorption

The absorption of testosterone undecanoate relies on the presence of fat as it is only soluble in it. Thus, the bioavailability of this testosterone derivative is very low of just 7%.[4] This highly lipophilic profile delineates the absorption of testosterone to be done via the lymphatic system.[5] The reported Cmax in steady state for testosterone undecanoate is 32 nmol/L after 7 days of administration.[2]

Volume of distribution

The distribution of testosterone undecanoate was limited to the liver, kidney and large and small intestine. Half of the administered dose remain near the injection site after 8 weeks of injection.[7] Following intravenous infusion of testosterone undecanoate, the reported volume of distribution was approximately 1 L/kg.[8]

Protein binding

Testosterone undecanoate is rapidly modified to form testosterone in plasma where 40% is bound to sex hormone-binding globulin and 2% remains unbound or bound to albumin and other proteins.[6]

Metabolism

To start its activity, testosterone undecanoate has to be processed by enzymes in the bloodstream. These enzymes will break the bond between the ester part of the molecule and the testosterone. Once separated, testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT). Testosterone is metabolized to DHT by steroid 5α-reductase in skin, liver and urogenital tract. In reproductive tissues, DHT is further metabolized to androstanediol.[6]

Route of elimination

About 90% of a dose of testosterone given intramuscularly is excreted in the urine as glucuronic and sulfuric acid conjugates of testosterone and its metabolites; about 6% of a dose is excreted in the feces, mostly in the unconjugated form.[1] In the case of testosterone undecanoate, most of the administered dose is excreted in feces and to a lesser extent in the urine.[7]

Half life

The reported elimination half-life of testosterone undecanoate is very long and it ranges between 18-24 days.[3]

Clearance

After intravenous administration of testosterone undecanoate, the observed clearance rate was 24.5 ml min/kg. This clearance rate indicated a fast metabolic elimination and explained the low bioavailability of this derivate of testosterone.[4]

Toxicity

Preclinical trials have shown induction of uterine tumors as well as an increase in the susceptibility to hepatoma. Testosterone undecanoate is known to increase the number of tumors and differentiation of chemically induced carcinomas. Administration of exogenous testosterone reversibly suppresses spermatogenesis.[7]

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-Bromoepiandrosterone16-Bromoepiandrosterone may increase the fluid retaining activities of Testosterone undecanoate.Investigational
19-norandrostenedione19-norandrostenedione may increase the fluid retaining activities of Testosterone undecanoate.Experimental, Illicit
5-androstenedione5-androstenedione may increase the fluid retaining activities of Testosterone undecanoate.Experimental, Illicit
AbciximabThe therapeutic efficacy of Abciximab can be increased when used in combination with Testosterone undecanoate.Approved
AbirateroneThe serum concentration of Testosterone undecanoate can be increased when it is combined with Abiraterone.Approved
AcarboseTestosterone undecanoate may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
Acetyl sulfisoxazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Acetyl sulfisoxazole.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Testosterone undecanoate.Approved
AlbiglutideTestosterone undecanoate may increase the hypoglycemic activities of Albiglutide.Approved
AlclometasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Alclometasone.Approved
AldosteroneAldosterone may increase the fluid retaining activities of Testosterone undecanoate.Experimental, Investigational
AlogliptinTestosterone undecanoate may increase the hypoglycemic activities of Alogliptin.Approved
AmcinonideThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Amcinonide.Approved
AmiodaroneThe metabolism of Testosterone undecanoate can be decreased when combined with Amiodarone.Approved, Investigational
AncrodThe therapeutic efficacy of Ancrod can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
AndrostenedioneAndrostenedione may increase the fluid retaining activities of Testosterone undecanoate.Experimental, Illicit
AnecortaveAnecortave may increase the fluid retaining activities of Testosterone undecanoate.Investigational
anecortave acetateanecortave acetate may increase the fluid retaining activities of Testosterone undecanoate.Investigational
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be increased when used in combination with Testosterone undecanoate.Approved
ApalutamideThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Apalutamide.Approved, Investigational
ApixabanThe therapeutic efficacy of Apixaban can be increased when used in combination with Testosterone undecanoate.Approved
AprepitantThe serum concentration of Testosterone undecanoate can be increased when it is combined with Aprepitant.Approved, Investigational
ArdeparinThe therapeutic efficacy of Ardeparin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational, Withdrawn
ArgatrobanThe therapeutic efficacy of Argatroban can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Testosterone undecanoate.Approved, Investigational
ArmodafinilThe metabolism of Testosterone undecanoate can be decreased when combined with Armodafinil.Approved, Investigational
AsunaprevirThe serum concentration of Asunaprevir can be decreased when it is combined with Testosterone undecanoate.Approved, Investigational, Withdrawn
AtamestaneAtamestane may increase the fluid retaining activities of Testosterone undecanoate.Investigational
AtazanavirThe metabolism of Testosterone undecanoate can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Testosterone undecanoate can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Testosterone undecanoate is combined with Atorvastatin.Approved
BecaplerminThe therapeutic efficacy of Becaplermin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Beclomethasone dipropionate.Approved, Investigational
BetamethasoneBetamethasone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
BivalirudinThe therapeutic efficacy of Bivalirudin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
BoceprevirThe metabolism of Testosterone undecanoate can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Testosterone undecanoate can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Testosterone undecanoate.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine is combined with Testosterone undecanoate.Approved, Investigational
BudesonideBudesonide may increase the fluid retaining activities of Testosterone undecanoate.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Testosterone undecanoate.Approved
CanagliflozinTestosterone undecanoate may increase the hypoglycemic activities of Canagliflozin.Approved
CapecitabineThe metabolism of Testosterone undecanoate can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Testosterone undecanoate can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Testosterone undecanoate can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Testosterone undecanoate can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Testosterone undecanoate.Approved, Withdrawn
CertoparinThe therapeutic efficacy of Certoparin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
ChloramphenicolThe metabolism of Testosterone undecanoate can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChlorpropamideTestosterone undecanoate may increase the hypoglycemic activities of Chlorpropamide.Approved, Investigational
CholecalciferolThe metabolism of Testosterone undecanoate can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CiclesonideCiclesonide may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
CimetidineThe metabolism of Testosterone undecanoate can be decreased when combined with Cimetidine.Approved, Investigational
CitalopramThe metabolism of Testosterone undecanoate can be decreased when combined with Citalopram.Approved
Citric AcidThe therapeutic efficacy of Citric Acid can be increased when used in combination with Testosterone undecanoate.Approved, Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Testosterone undecanoate can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Testosterone undecanoate can be decreased when combined with Clemastine.Approved, Investigational
ClobetasolThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Clobetasol.Approved, Investigational
Clobetasol propionateClobetasol propionate may increase the fluid retaining activities of Testosterone undecanoate.Approved
ClobetasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Clobetasone.Approved
ClocortoloneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Clocortolone.Approved
ClopidogrelThe metabolism of Testosterone undecanoate can be decreased when combined with Clopidogrel.Approved
ClorindioneTestosterone undecanoate may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Testosterone undecanoate can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Testosterone undecanoate.Approved
Conestat alfaTestosterone undecanoate may increase the thrombogenic activities of Conestat alfa.Approved, Investigational
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
Cortexolone 17α-propionateCortexolone 17α-propionate may increase the fluid retaining activities of Testosterone undecanoate.Investigational
CorticosteroneCorticosterone may increase the fluid retaining activities of Testosterone undecanoate.Experimental
Cortisone acetateThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Cortisone acetate.Approved, Investigational
CrisaboroleThe metabolism of Testosterone undecanoate can be decreased when combined with Crisaborole.Approved, Investigational
CrizotinibThe metabolism of Testosterone undecanoate can be decreased when combined with Crizotinib.Approved
CyclosporineTestosterone undecanoate may increase the hepatotoxic activities of Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Testosterone undecanoate.Approved
DabrafenibThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Dabrafenib.Approved, Investigational
DalteparinThe therapeutic efficacy of Dalteparin can be increased when used in combination with Testosterone undecanoate.Approved
DanaparoidThe therapeutic efficacy of Danaparoid can be increased when used in combination with Testosterone undecanoate.Approved, Withdrawn
DapagliflozinTestosterone undecanoate may increase the hypoglycemic activities of Dapagliflozin.Approved
DarexabanThe therapeutic efficacy of Darexaban can be increased when used in combination with Testosterone undecanoate.Investigational
DarunavirThe metabolism of Testosterone undecanoate can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Testosterone undecanoate can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortDeflazacort may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
DelavirdineThe metabolism of Testosterone undecanoate can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Testosterone undecanoate can be decreased when combined with Desipramine.Approved, Investigational
DesirudinThe therapeutic efficacy of Desirudin can be increased when used in combination with Testosterone undecanoate.Approved
DesonideThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Desonide.Approved, Investigational
DesoximetasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Desoximetasone.Approved
Desoxycorticosterone acetateDesoxycorticosterone acetate may increase the fluid retaining activities of Testosterone undecanoate.Approved
Desoxycorticosterone PivalateDesoxycorticosterone Pivalate may increase the fluid retaining activities of Testosterone undecanoate.Experimental, Vet Approved
DexamethasoneDexamethasone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateDexamethasone isonicotinate may increase the fluid retaining activities of Testosterone undecanoate.Vet Approved
DextranThe therapeutic efficacy of Dextran can be increased when used in combination with Testosterone undecanoate.Approved, Investigational, Vet Approved
DicoumarolThe therapeutic efficacy of Dicoumarol can be increased when used in combination with Testosterone undecanoate.Approved
DiflorasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Diflorasone.Approved
DifluocortoloneDifluocortolone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational, Withdrawn
DifluprednateThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Difluprednate.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Testosterone undecanoate.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Testosterone undecanoate.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Testosterone undecanoate.Experimental
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Testosterone undecanoate.Approved, Investigational
DiltiazemThe metabolism of Testosterone undecanoate can be decreased when combined with Diltiazem.Approved, Investigational
DiphenadioneTestosterone undecanoate may increase the anticoagulant activities of Diphenadione.Experimental
DisopyramideTestosterone undecanoate may increase the hypoglycemic activities of Disopyramide.Approved
DosulepinThe metabolism of Testosterone undecanoate can be decreased when combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
DoxorubicinThe metabolism of Testosterone undecanoate can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Testosterone undecanoate can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Testosterone undecanoate can be decreased when combined with Dronedarone.Approved
DulaglutideTestosterone undecanoate may increase the hypoglycemic activities of Dulaglutide.Approved, Investigational
Edetic AcidThe therapeutic efficacy of Edetic Acid can be increased when used in combination with Testosterone undecanoate.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Testosterone undecanoate.Approved
EfavirenzThe metabolism of Testosterone undecanoate can be decreased when combined with Efavirenz.Approved, Investigational
EltrombopagThe serum concentration of Testosterone undecanoate can be increased when it is combined with Eltrombopag.Approved
EmpagliflozinTestosterone undecanoate may increase the hypoglycemic activities of Empagliflozin.Approved
EnoxaparinThe therapeutic efficacy of Enoxaparin can be increased when used in combination with Testosterone undecanoate.Approved
EnzalutamideThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Enzalutamide.Approved
EquileninEquilenin may increase the fluid retaining activities of Testosterone undecanoate.Experimental
EquilinEquilin may increase the fluid retaining activities of Testosterone undecanoate.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Testosterone undecanoate.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Testosterone undecanoate.Approved
ErythromycinThe metabolism of Testosterone undecanoate can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
Eslicarbazepine acetateThe metabolism of Testosterone undecanoate can be decreased when combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Esomeprazole.Approved, Investigational
EstroneEstrone may increase the fluid retaining activities of Testosterone undecanoate.Approved
Estrone sulfateEstrone sulfate may increase the fluid retaining activities of Testosterone undecanoate.Approved
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be increased when used in combination with Testosterone undecanoate.Withdrawn
EtravirineThe metabolism of Testosterone undecanoate can be decreased when combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Testosterone undecanoate.Approved
ExenatideTestosterone undecanoate may increase the hypoglycemic activities of Exenatide.Approved, Investigational
FelodipineThe metabolism of Testosterone undecanoate can be decreased when combined with Felodipine.Approved, Investigational
Ferulic acidThe therapeutic efficacy of Ferulic acid can be increased when used in combination with Testosterone undecanoate.Experimental
FloxuridineThe metabolism of Testosterone undecanoate can be decreased when combined with Floxuridine.Approved
FluasteroneFluasterone may increase the fluid retaining activities of Testosterone undecanoate.Investigational
FlucloroloneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluclorolone.Experimental
FluconazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Fluconazole.Approved, Investigational
FludrocortisoneFludrocortisone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
FluindioneThe therapeutic efficacy of Fluindione can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
FlumethasoneFlumethasone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
FlunisolideFlunisolide may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
Fluocinolone AcetonideThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluocinolone Acetonide.Approved, Investigational, Vet Approved
FluocinonideFluocinonide may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
FluocortinThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluocortin.Experimental
FluocortoloneFluocortolone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Withdrawn
FluorometholoneFluorometholone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational
FluorouracilThe metabolism of Testosterone undecanoate can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Testosterone undecanoate can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluperoloneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluperolone.Experimental
FluprednideneFluprednidene may increase the fluid retaining activities of Testosterone undecanoate.Approved, Withdrawn
FluprednisoloneFluprednisolone may increase the fluid retaining activities of Testosterone undecanoate.Approved
FlurandrenolideFlurandrenolide may increase the fluid retaining activities of Testosterone undecanoate.Approved
FluticasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluticasone.Approved, Experimental, Investigational
Fluticasone furoateFluticasone furoate may increase the fluid retaining activities of Testosterone undecanoate.Approved
Fluticasone propionateThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Fluvastatin can be increased when it is combined with Testosterone undecanoate.Approved
FluvoxamineThe metabolism of Testosterone undecanoate can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxThe therapeutic efficacy of Fondaparinux can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
FormestaneFormestane may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational, Withdrawn
FormocortalThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Formocortal.Experimental
FosamprenavirThe metabolism of Testosterone undecanoate can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Testosterone undecanoate can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Testosterone undecanoate can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Testosterone undecanoate can be increased when it is combined with Fusidic Acid.Approved, Investigational
GabexateThe therapeutic efficacy of Gabexate can be increased when used in combination with Testosterone undecanoate.Investigational
GemfibrozilThe metabolism of Testosterone undecanoate can be decreased when combined with Gemfibrozil.Approved
GliclazideTestosterone undecanoate may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideTestosterone undecanoate may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideTestosterone undecanoate may increase the hypoglycemic activities of Glipizide.Approved, Investigational
GlucoseThe serum concentration of Glucose can be decreased when it is combined with Testosterone undecanoate.Approved, Vet Approved
GlyburideTestosterone undecanoate may increase the hypoglycemic activities of Glyburide.Approved
HalcinonideThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Halcinonide.Approved, Investigational, Withdrawn
HalometasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Halometasone.Experimental
HE3286HE3286 may increase the fluid retaining activities of Testosterone undecanoate.Investigational
HeparinThe therapeutic efficacy of Heparin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
Human C1-esterase inhibitorTestosterone undecanoate may increase the thrombogenic activities of Human C1-esterase inhibitor.Approved
HydrocortisoneHydrocortisone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Testosterone undecanoate.Approved
IdelalisibThe metabolism of Testosterone undecanoate can be decreased when combined with Idelalisib.Approved
IdraparinuxThe therapeutic efficacy of Idraparinux can be increased when used in combination with Testosterone undecanoate.Investigational
ImatinibThe metabolism of Testosterone undecanoate can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Testosterone undecanoate can be decreased when combined with Indinavir.Approved
Insulin AspartTestosterone undecanoate may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirTestosterone undecanoate may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineTestosterone undecanoate may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineTestosterone undecanoate may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanTestosterone undecanoate may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproTestosterone undecanoate may increase the hypoglycemic activities of Insulin Lispro.Approved
IrbesartanThe metabolism of Testosterone undecanoate can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoleThe serum concentration of Testosterone undecanoate can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Testosterone undecanoate can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Testosterone undecanoate can be decreased when combined with Isoniazid.Approved, Investigational
IsradipineThe metabolism of Testosterone undecanoate can be decreased when combined with Isradipine.Approved, Investigational
IstaroximeIstaroxime may increase the fluid retaining activities of Testosterone undecanoate.Investigational
ItraconazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Testosterone undecanoate can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Ketoconazole.Approved, Investigational
LapatinibThe metabolism of Testosterone undecanoate can be decreased when combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Testosterone undecanoate.Approved
LeflunomideThe metabolism of Testosterone undecanoate can be decreased when combined with Leflunomide.Approved, Investigational
LepirudinThe therapeutic efficacy of Lepirudin can be increased when used in combination with Testosterone undecanoate.Approved
LetaxabanThe therapeutic efficacy of Letaxaban can be increased when used in combination with Testosterone undecanoate.Investigational
LiraglutideTestosterone undecanoate may increase the hypoglycemic activities of Liraglutide.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Testosterone undecanoate.Approved, Investigational
LobeglitazoneThe metabolism of Testosterone undecanoate can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Testosterone undecanoate can be decreased when combined with Lopinavir.Approved
LorpiprazoleThe serum concentration of Testosterone undecanoate can be increased when it is combined with Lorpiprazole.Approved
LosartanThe metabolism of Testosterone undecanoate can be decreased when combined with Losartan.Approved
LoteprednolThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Loteprednol.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
LuliconazoleThe serum concentration of Testosterone undecanoate can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Testosterone undecanoate can be increased when it is combined with Lumacaftor.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Testosterone undecanoate.Illicit, Investigational, Withdrawn
ManidipineThe metabolism of Testosterone undecanoate can be decreased when combined with Manidipine.Approved, Investigational
ME-609ME-609 may increase the fluid retaining activities of Testosterone undecanoate.Investigational
MecaserminTestosterone undecanoate may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MedrysoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Medrysone.Approved
MelagatranThe therapeutic efficacy of Melagatran can be increased when used in combination with Testosterone undecanoate.Experimental
MelengestrolMelengestrol may increase the fluid retaining activities of Testosterone undecanoate.Vet Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Testosterone undecanoate.Experimental
MetforminTestosterone undecanoate may increase the hypoglycemic activities of Metformin.Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Testosterone undecanoate.Approved
MethylprednisoloneMethylprednisolone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Testosterone undecanoate.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Testosterone undecanoate.Experimental
MidostaurinThe metabolism of Testosterone undecanoate can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Testosterone undecanoate can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolTestosterone undecanoate may increase the hypoglycemic activities of Miglitol.Approved
MitotaneThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Testosterone undecanoate can be decreased when combined with Moclobemide.Approved, Investigational
ModafinilThe metabolism of Testosterone undecanoate can be decreased when combined with Modafinil.Approved, Investigational
MometasoneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Mometasone.Approved, Vet Approved
NabiloneThe metabolism of Testosterone undecanoate can be decreased when combined with Nabilone.Approved, Investigational
NadroparinThe therapeutic efficacy of Nadroparin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
NafamostatThe therapeutic efficacy of Nafamostat can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Testosterone undecanoate.Approved
NateglinideTestosterone undecanoate may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 1022NCX 1022 may increase the fluid retaining activities of Testosterone undecanoate.Investigational
NefazodoneThe metabolism of Testosterone undecanoate can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Testosterone undecanoate can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Testosterone undecanoate can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Testosterone undecanoate can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Testosterone undecanoate can be decreased when combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Testosterone undecanoate.Approved, Investigational
NilotinibThe metabolism of Testosterone undecanoate can be decreased when combined with Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Testosterone undecanoate.Approved
OlaparibThe metabolism of Testosterone undecanoate can be decreased when combined with Olaparib.Approved
Oleoyl-estroneOleoyl-estrone may increase the fluid retaining activities of Testosterone undecanoate.Investigational
OmeprazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Testosterone undecanoate can be increased when it is combined with Osimertinib.Approved
OtamixabanThe therapeutic efficacy of Otamixaban can be increased when used in combination with Testosterone undecanoate.Investigational
PalbociclibThe serum concentration of Testosterone undecanoate can be increased when it is combined with Palbociclib.Approved, Investigational
PantoprazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Pantoprazole.Approved
ParamethasoneParamethasone may increase the fluid retaining activities of Testosterone undecanoate.Approved
ParoxetineThe metabolism of Testosterone undecanoate can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Testosterone undecanoate.Approved
Pentaerythritol TetranitrateThe therapeutic efficacy of Pentaerythritol Tetranitrate can be increased when used in combination with Testosterone undecanoate.Approved
PentamidineTestosterone undecanoate may increase the hypoglycemic activities of Pentamidine.Approved, Investigational
PentobarbitalThe metabolism of Testosterone undecanoate can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
Pentosan PolysulfateThe therapeutic efficacy of Pentosan Polysulfate can be increased when used in combination with Testosterone undecanoate.Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Testosterone undecanoate.Approved, Investigational, Vet Approved, Withdrawn
PhenindioneThe therapeutic efficacy of Phenindione can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
PhenobarbitalThe metabolism of Testosterone undecanoate can be increased when combined with Phenobarbital.Approved, Investigational
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
PhenytoinThe metabolism of Testosterone undecanoate can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Testosterone undecanoate can be decreased when combined with Pioglitazone.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone undecanoate.Approved
PitolisantThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Pitolisant.Approved, Investigational
PosaconazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintideTestosterone undecanoate may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
PrasteronePrasterone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Investigational, Nutraceutical
Prasterone sulfatePrasterone sulfate may increase the fluid retaining activities of Testosterone undecanoate.Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Testosterone undecanoate.Approved
PrednicarbateThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Prednicarbate.Approved, Investigational
PrednisoloneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Prednisolone.Approved, Vet Approved
PrednisonePrednisone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
PregnenolonePregnenolone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Experimental, Investigational
PrimidoneThe metabolism of Testosterone undecanoate can be increased when combined with Primidone.Approved, Vet Approved
Protein CThe therapeutic efficacy of Protein C can be increased when used in combination with Testosterone undecanoate.Approved
Protein S humanThe therapeutic efficacy of Protein S human can be increased when used in combination with Testosterone undecanoate.Approved
ProtocatechualdehydeThe therapeutic efficacy of Protocatechualdehyde can be increased when used in combination with Testosterone undecanoate.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Testosterone undecanoate.Approved
PyrimethamineThe metabolism of Testosterone undecanoate can be decreased when combined with Pyrimethamine.Approved, Investigational, Vet Approved
QuazepamThe serum concentration of Testosterone undecanoate can be increased when it is combined with Quazepam.Approved, Illicit
QuinineThe metabolism of Testosterone undecanoate can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
RepaglinideTestosterone undecanoate may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
ReviparinThe therapeutic efficacy of Reviparin can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
RifabutinThe metabolism of Testosterone undecanoate can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Testosterone undecanoate can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Testosterone undecanoate can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be decreased when it is combined with Testosterone undecanoate.Approved
RimexoloneThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Rimexolone.Approved
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be increased when used in combination with Testosterone undecanoate.Approved
RolapitantThe serum concentration of Testosterone undecanoate can be increased when it is combined with Rolapitant.Approved, Investigational
RosiglitazoneThe metabolism of Testosterone undecanoate can be decreased when combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Testosterone undecanoate.Approved
RucaparibThe metabolism of Testosterone undecanoate can be decreased when combined with Rucaparib.Approved, Investigational
SaquinavirThe metabolism of Testosterone undecanoate can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Testosterone undecanoate can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Testosterone undecanoate.Approved
SecobarbitalThe metabolism of Testosterone undecanoate can be increased when combined with Secobarbital.Approved, Vet Approved
SertralineThe metabolism of Testosterone undecanoate can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Testosterone undecanoate can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Testosterone undecanoate.Approved
SiltuximabThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Testosterone undecanoate can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Testosterone undecanoate.Approved
SitagliptinTestosterone undecanoate may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
SorafenibThe metabolism of Testosterone undecanoate can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Testosterone undecanoate can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Testosterone undecanoate can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Testosterone undecanoate can be decreased when combined with Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be increased when used in combination with Testosterone undecanoate.Approved, Investigational
SunitinibTestosterone undecanoate may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TamoxifenThe metabolism of Testosterone undecanoate can be decreased when combined with Tamoxifen.Approved
TelaprevirThe metabolism of Testosterone undecanoate can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Testosterone undecanoate can be decreased when combined with Telithromycin.Approved
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Testosterone undecanoate.Experimental
TeriflunomideThe serum concentration of Testosterone undecanoate can be increased when it is combined with Teriflunomide.Approved
ThiotepaThe metabolism of Testosterone undecanoate can be decreased when combined with Thiotepa.Approved, Investigational
TicagrelorThe metabolism of Testosterone undecanoate can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Testosterone undecanoate can be decreased when combined with Ticlopidine.Approved
TioclomarolTestosterone undecanoate may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolTixocortol may increase the fluid retaining activities of Testosterone undecanoate.Approved, Withdrawn
TocilizumabThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Tocilizumab.Approved
TolazamideTestosterone undecanoate may increase the hypoglycemic activities of Tolazamide.Approved, Investigational
TolbutamideThe metabolism of Testosterone undecanoate can be decreased when combined with Tolbutamide.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Testosterone undecanoate.Approved
TopiramateThe metabolism of Testosterone undecanoate can be decreased when combined with Topiramate.Approved
TopiroxostatThe metabolism of Testosterone undecanoate can be decreased when combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
TranylcypromineThe metabolism of Testosterone undecanoate can be decreased when combined with Tranylcypromine.Approved, Investigational
TriamcinoloneTriamcinolone may increase the fluid retaining activities of Testosterone undecanoate.Approved, Vet Approved
TrimethoprimThe metabolism of Testosterone undecanoate can be decreased when combined with Trimethoprim.Approved, Vet Approved
TroxerutinThe therapeutic efficacy of Troxerutin can be increased when used in combination with Testosterone undecanoate.Investigational
UlobetasolThe risk or severity of fluid retention can be increased when Testosterone undecanoate is combined with Ulobetasol.Approved
Valproic AcidThe metabolism of Testosterone undecanoate can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Testosterone undecanoate can be decreased when combined with Valsartan.Approved, Investigational
VemurafenibThe serum concentration of Testosterone undecanoate can be decreased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Testosterone undecanoate can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Testosterone undecanoate can be decreased when combined with Verapamil.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Testosterone undecanoate.Approved, Investigational
VoriconazoleThe metabolism of Testosterone undecanoate can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinThe therapeutic efficacy of Warfarin can be increased when used in combination with Testosterone undecanoate.Approved
XimelagatranThe therapeutic efficacy of Ximelagatran can be increased when used in combination with Testosterone undecanoate.Approved, Investigational, Withdrawn
ZafirlukastThe metabolism of Testosterone undecanoate can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Testosterone undecanoate can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe metabolism of Testosterone undecanoate can be decreased when combined with Zucapsaicin.Approved, Investigational
Food Interactions
Not Available

References

General References
  1. Freeman ER, Bloom DA, McGuire EJ: A brief history of testosterone. J Urol. 2001 Feb;165(2):371-3. [PubMed:11176375]
  2. Saad F, Kamischke A, Yassin A, Zitzmann M, Schubert M, Jockenhel F, Behre HM, Gooren L, Nieschlag E: More than eight years' hands-on experience with the novel long-acting parenteral testosterone undecanoate. Asian J Androl. 2007 May;9(3):291-7. doi: 10.1111/j.1745-7262.2007.00275.x. [PubMed:17486268]
  3. Zhang GY, Gu YQ, Wang XH, Cui YG, Bremner WJ: A pharmacokinetic study of injectable testosterone undecanoate in hypogonadal men. J Androl. 1998 Nov-Dec;19(6):761-8. [PubMed:9876028]
  4. Tauber U, Schroder K, Dusterberg B, Matthes H: Absolute bioavailability of testosterone after oral administration of testosterone-undecanoate and testosterone. Eur J Drug Metab Pharmacokinet. 1986 Apr-Jun;11(2):145-9. [PubMed:3770015]
  5. Steroidal [Link]
  6. Steroidal [Link]
  7. FDA pharmacology reviews [Link]
  8. Pfizer monograph [Link]
External Links
ChemSpider
58664
ChEBI
135741
ChEMBL
CHEMBL2107067
Wikipedia
Testosterone_undecanoate
AHFS Codes
  • 68:08.00 — Androgens
FDA label
Download (517 KB)
MSDS
Download (45.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableCompletedNot AvailableBone Density / Bone destruction / Hypogonadism / Paraplegia1
Not AvailableCompletedNot AvailableHypogonadism1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
InjectionIntramuscular250 mg/mL
CapsuleOral40 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8338395No2006-02-272026-02-27Us
US7718640No2007-03-142027-03-14Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)64-64ºC'MSDS'
water solubilityInsoluble'MSDS'
Predicted Properties
PropertyValueSource
Water Solubility7.4e-05 mg/mLALOGPS
logP6.74ALOGPS
logP8.06ChemAxon
logS-6.8ALOGPS
pKa (Strongest Acidic)18.52ChemAxon
pKa (Strongest Basic)-4.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area43.37 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity135.02 m3·mol-1ChemAxon
Polarizability57.8 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Steroid esters
Direct Parent
Steroid esters
Alternative Parents
Androgens and derivatives / 3-oxo delta-4-steroids / Delta-4-steroids / Cyclohexenones / Carboxylic acid esters / Monocarboxylic acids and derivatives / Organic oxides / Hydrocarbon derivatives
Substituents
Steroid ester / Androgen-skeleton / Androstane-skeleton / 3-oxosteroid / 3-oxo-delta-4-steroid / Oxosteroid / Delta-4-steroid / Cyclohexenone / Ketone / Carboxylic acid ester
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
Gene Name
AR
Uniprot ID
P10275
Uniprot Name
Androgen receptor
Molecular Weight
98987.9 Da
References
  1. Small EJ, Ryan CJ: The case for secondary hormonal therapies in the chemotherapy age. J Urol. 2006 Dec;176(6 Pt 2):S66-71. [PubMed:17084172]
  2. Omwancha J, Brown TR: Selective androgen receptor modulators: in pursuit of tissue-selective androgens. Curr Opin Investig Drugs. 2006 Oct;7(10):873-81. [PubMed:17086931]
  3. Petraki CD, Sfikas CP: Histopathological changes induced by therapies in the benign prostate and prostate adenocarcinoma. Histol Histopathol. 2007 Jan;22(1):107-18. [PubMed:17128417]
  4. Maudsley S, Davidson L, Pawson AJ, Freestone SH, Lopez de Maturana R, Thomson AA, Millar RP: Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5. Neuroendocrinology. 2006;84(5):285-300. Epub 2007 Jan 4. [PubMed:17202804]
  5. Lapauw B, Goemaere S, Crabbe P, Kaufman JM, Ruige JB: Is the effect of testosterone on body composition modulated by the androgen receptor gene CAG repeat polymorphism in elderly men? Eur J Endocrinol. 2007 Mar;156(3):395-401. [PubMed:17322500]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Kojima H, Iida M, Katsura E, Kanetoshi A, Hori Y, Kobayashi K: Effects of a diphenyl ether-type herbicide, chlornitrofen, and its amino derivative on androgen and estrogen receptor activities. Environ Health Perspect. 2003 Apr;111(4):497-502. [PubMed:12676605]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates targ...
Gene Name
NR3C2
Uniprot ID
P08235
Uniprot Name
Mineralocorticoid receptor
Molecular Weight
107066.575 Da
References
  1. Takeda AN, Pinon GM, Bens M, Fagart J, Rafestin-Oblin ME, Vandewalle A: The synthetic androgen methyltrienolone (r1881) acts as a potent antagonist of the mineralocorticoid receptor. Mol Pharmacol. 2007 Feb;71(2):473-82. Epub 2006 Nov 14. [PubMed:17105867]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
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. Zhang T, Zhu Y, Gunaratna C: Rapid and quantitative determination of metabolites from multiple cytochrome P450 probe substrates by gradient liquid chromatography-electrospray ionization-ion trap mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2002 Nov 25;780(2):371-9. [PubMed:12401364]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
  4. Source [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name
CYP19A1
Uniprot ID
P11511
Uniprot Name
Aromatase
Molecular Weight
57882.48 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Serotonin binding
Specific Function
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral...
Gene Name
MAOA
Uniprot ID
P21397
Uniprot Name
Amine oxidase [flavin-containing] A
Molecular Weight
59681.27 Da
References
  1. Sjoberg RL, Ducci F, Barr CS, Newman TK, Dell'osso L, Virkkunen M, Goldman D: A non-additive interaction of a functional MAO-A VNTR and testosterone predicts antisocial behavior. Neuropsychopharmacology. 2008 Jan;33(2):425-30. Epub 2007 Apr 11. [PubMed:17429405]
  2. Hoff KM: Interaction of testosterone with monoamineoxidase in mouse brain maturation. Gen Pharmacol. 1977;8(1):55-7. [PubMed:590724]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, nad(p)h as one donor, and incorporation of one atom of oxygen
Specific Function
Catalyzes the side-chain cleavage reaction of cholesterol to pregnenolone.
Gene Name
CYP11A1
Uniprot ID
P05108
Uniprot Name
Cholesterol side-chain cleavage enzyme, mitochondrial
Molecular Weight
60101.87 Da
References
  1. Kostic TS, Stojkov NJ, Bjelic MM, Mihajlovic AI, Janjic MM, Andric SA: Pharmacological doses of testosterone upregulated androgen receptor and 3-Beta-hydroxysteroid dehydrogenase/delta-5-delta-4 isomerase and impaired leydig cells steroidogenesis in adult rats. Toxicol Sci. 2011 Jun;121(2):397-407. doi: 10.1093/toxsci/kfr063. Epub 2011 Apr 6. [PubMed:21427060]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 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. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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 un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a coumarin 7-hydroxylase activity. Active in the metabolic activation of hexamethylphosphoramide, N,N-dimethylaniline, 2'-methoxyacetophenone, N-nitrosomethylphenylamine, and the tobacco-s...
Gene Name
CYP2A13
Uniprot ID
Q16696
Uniprot Name
Cytochrome P450 2A13
Molecular Weight
56687.095 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Steroid 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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid 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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Monooxygenase activity
Specific Function
Exhibits low testosterone 6-beta-hydroxylase activity.
Gene Name
CYP3A43
Uniprot ID
Q9HB55
Uniprot Name
Cytochrome P450 3A43
Molecular Weight
57669.21 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein group
Organism
Not Available
Pharmacological action
No
Actions
Substrate
General Function
Electron carrier activity
Specific Function
Converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and andro...

Components:

Carriers

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Other/unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [PubMed:3521955]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Other/unknown
General Function
Androgen binding
Specific Function
Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
Gene Name
SHBG
Uniprot ID
P04278
Uniprot Name
Sex hormone-binding globulin
Molecular Weight
43778.755 Da
References
  1. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [PubMed:3521955]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Lu R, Kanai N, Bao Y, Wolkoff AW, Schuster VL: Regulation of renal oatp mRNA expression by testosterone. Am J Physiol. 1996 Feb;270(2 Pt 2):F332-7. [PubMed:8779895]
  2. Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [PubMed:8779894]
  3. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. Kobayashi Y, Hirokawa N, Ohshiro N, Sekine T, Sasaki T, Tokuyama S, Endou H, Yamamoto T: Differential gene expression of organic anion transporters in male and female rats. Biochem Biophys Res Commun. 2002 Jan 11;290(1):482-7. [PubMed:11779196]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
Gene Name
SLC22A7
Uniprot ID
Q9Y694
Uniprot Name
Solute carrier family 22 member 7
Molecular Weight
60025.025 Da
References
  1. Kobayashi Y, Hirokawa N, Ohshiro N, Sekine T, Sasaki T, Tokuyama S, Endou H, Yamamoto T: Differential gene expression of organic anion transporters in male and female rats. Biochem Biophys Res Commun. 2002 Jan 11;290(1):482-7. [PubMed:11779196]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Katoh M, Nakajima M, Yamazaki H, Yokoi T: Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport. Eur J Pharm Sci. 2001 Feb;12(4):505-13. [PubMed:11231118]
  2. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Virus receptor activity
Specific Function
The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
Gene Name
SLC10A1
Uniprot ID
Q14973
Uniprot Name
Sodium/bile acid cotransporter
Molecular Weight
38118.64 Da
References
  1. Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. [PubMed:9486191]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Tzvetkov MV, Vormfelde SV, Balen D, Meineke I, Schmidt T, Sehrt D, Sabolic I, Koepsell H, Brockmoller J: The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009 Sep;86(3):299-306. doi: 10.1038/clpt.2009.92. Epub 2009 Jun 17. [PubMed:19536068]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Symporter activity
Specific Function
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without...
Gene Name
SLC22A4
Uniprot ID
Q9H015
Uniprot Name
Solute carrier family 22 member 4
Molecular Weight
62154.48 Da
References
  1. Tzvetkov MV, Vormfelde SV, Balen D, Meineke I, Schmidt T, Sehrt D, Sabolic I, Koepsell H, Brockmoller J: The effects of genetic polymorphisms in the organic cation transporters OCT1, OCT2, and OCT3 on the renal clearance of metformin. Clin Pharmacol Ther. 2009 Sep;86(3):299-306. doi: 10.1038/clpt.2009.92. Epub 2009 Jun 17. [PubMed:19536068]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Janvilisri T, Venter H, Shahi S, Reuter G, Balakrishnan L, van Veen HW: Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51. Epub 2003 Mar 28. [PubMed:12668685]

Drug created on January 11, 2018 16:11 / Updated on May 22, 2018 23:59