Identification

Name
Conjugated estrogens
Accession Number
DB00286  (APRD00396)
Type
Small Molecule
Groups
Approved
Description

Conjugated estrogens, or Conjugated Equine Estrogens (CEEs) are composed of a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids that are purified from pregnant horse urine. Available as the product Premarin (FDA), this combination of equine-derived estrogenic compounds is indicated for the following conditions: treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy associated with menopause; hypoestrogenism due to hypogonadism, castration or primary ovarian failure; palliation of metastatic breast cancer; palliation of advanced androgen-dependent carcinoma of the prostate; and for prevention of postmenopausal osteoporosis.

All estrogen products mimic the effects of endogenous estrogens in the body which are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act by binding to estrogen receptors on a wide variety of tissues in the body and modulating the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. Prior to menopause, the primary source of estrogen is the ovarian follicle, which secretes 70-500 micrograms of estradiol daily, depending on the phase of the menstrual cycle. However, once a woman stops ovulating there is a sharp decline in the production of progesterone and estradiol by the ovaries and a consequent fluctuation in LH and FSH due to a lack of feedback control. This shift in hormone production is largely responsible for many of the symptoms experienced during and after menopause and includes hot flashes and other vasomotor symptoms, painful intercourse, vaginal dryness, and vulvovaginal atrophy. These symptoms are able to be reduced by replacing many of the hormones lost during and following menopause with synthetic or naturally occurring forms, in a therapy known as Hormone Replacement Therapy (HRT).

Pharmacologic estrogen products are available in a variety of formats. Although many of them contain several compounds in common (such as the estrogen derivatives sodium estrone sulfate and sodium equilin sulfate), they vary by their original source (such as horse-, human-, or plant-derived), and the remaining mixture of estrogenic derivatives. Conjugated Equine Estrogens (CEEs) are derived from the urine of pregnant mares and contain a blend of at least 10 estrogen derivatives. Marketed under the brand name Premarin, CEEs are the most frequently used form of conjugated estrogens. There is currently no generic form of CEEs available as a detailed analytical characterization of the active ingredients or of their estrogenic activity is not available at this time. Conjugated estrogens are also available in a plant-derived synthetic form that replicates the naturally occurring, horse-derived forms. Available as either "Synthetic Conjugated Estrogens, A" containing 9 estrogen derivatives (available as Cenestin) or as "Synthetic Conjugated Estrogens, B" containing 10 estrogen derivatives (available as Enjuvia), these products are isolated as precursors from yam or soy plants and then chemically modified to mimic the products available in their naturally occurring form.

Synonyms
  • Conjugated equine estrogens
  • conjugated estrogens
  • Estrogens, Conjugated
  • Estrogens,conjugated
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
C.E.S. TabletsTablet1.25 mgOralValeant Canada Lp Valeant Canada S.E.C.1963-12-312014-07-30Canada
C.E.S. TabletsTablet0.9 mgOralValeant Canada Lp Valeant Canada S.E.C.1997-03-142014-07-30Canada
C.E.S. TabletsTablet0.625 mgOralValeant Canada Lp Valeant Canada S.E.C.1963-12-31Not applicableCanada
C.E.S. TabletsTablet0.3 mgOralValeant Canada Lp Valeant Canada S.E.C.1997-03-142014-07-30Canada
Congest Tab 0.3mgTablet0.3 mgOralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 0.625mgTablet0.625 mgOralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 0.9mgTablet0.9 mgOralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 1.25mgTablet1.25 mgOralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 2.5mgTablet2.5 mgOralLaboratoires Trianon Inc1990-12-31Not applicableCanada
PMS-conjugated Estrogens C.S.D.Tablet0.3 mgOralPharmascience Inc1999-03-03Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-conest Tab 0.3mgTablet0.3 mgOralApotex Corporation1994-12-312009-10-09Canada
Apo-conest Tab 0.625mgTablet0.625 mgOralApotex Corporation1994-12-312009-10-09Canada
Apo-conest Tab 0.9mgTablet0.9 mgOralApotex Corporation1994-12-312009-10-09Canada
Apo-conest Tab 1.25mgTablet1.25 mgOralApotex Corporation1994-12-312009-10-09Canada
Apo-conest Tab 2.5mgTablet2.5 mgOralApotex Corporation1994-12-312009-10-09Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
DuaveeConjugated estrogens (.45 mg/1) + Bazedoxifene acetate (20 mg/1)Tablet, film coatedOralU.S. Pharmaceuticals2013-11-15Not applicableUs
DuaveeConjugated estrogens (.45 mg/1) + Bazedoxifene acetate (20 mg/1)Tablet, film coatedOralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2013-10-03Not applicableUs
DuaveeConjugated estrogens (.45 mg/1) + Bazedoxifene acetate (20 mg/1)Tablet, film coatedOralU.S. Pharmaceuticals2013-11-15Not applicableUs
DuaviveConjugated estrogens (0.45 mg) + Bazedoxifene (20 mg)Tablet, multilayer, extended releaseOralPfizer2016-12-20Not applicableCanada
DuaviveConjugated estrogens (0.45 mg) + Bazedoxifene (20 mg)Tablet, multilayer, extended releaseOralPfizer2014-12-16Not applicableEu
Esterified Estrogens and MethyltestosteroneConjugated estrogens (.625 mg/1) + Methyltestosterone (1.25 mg/1)TabletOralAmneal Pharmaceuticals2010-09-22Not applicableUs53746 0077 01 nlmimage10 6605b34d
Esterified Estrogens and MethyltestosteroneConjugated estrogens (1.25 mg/1) + Methyltestosterone (2.5 mg/1)Tablet, film coatedOralSeton Pharmaceuticals2010-05-05Not applicableUs
Esterified Estrogens and MethyltestosteroneConjugated estrogens (1.25 mg/1) + Methyltestosterone (2.5 mg/1)TabletOralAmneal Pharmaceuticals2010-09-22Not applicableUs53746 0078 01 nlmimage10 5f05afed
Esterified Estrogens and MethyltestosteroneConjugated estrogens (.625 mg/1) + Methyltestosterone (1.25 mg/1)Tablet, film coatedOralSeton Pharmaceuticals2005-10-10Not applicableUs
PremphaseConjugated estrogens + Medroxyprogesterone acetateKitWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2012-03-01Not applicableUs
Categories
UNII
IU5QR144QX
CAS number
12126-59-9
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Conjugated Equine Estrogens (CEEs) are indicated for the following conditions: treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy associated with menopause; hypoestrogenism due to hypogonadism, castration or primary ovarian failure; palliation of metastatic breast cancer; palliation of advanced androgen-dependent carcinoma of the prostate; and for prevention of postmenopausal osteoporosis.

Structured Indications
Pharmacodynamics
Not Available
Mechanism of action

All estrogen products mimic the effects of endogenous estrogens in the body which are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estrogens act by binding to estrogen receptors on a wide variety of tissues in the body and modulating the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH) through a negative feedback mechanism. Prior to menopause, the primary source of estrogen is the ovarian follicle, which secretes 70-500 micrograms of estradiol daily, depending on the phase of the menstrual cycle. However, once a woman stops ovulating there is a sharp decline in the production of progesterone and estradiol by the ovaries and a consequent fluctuation in LH and FSH due to a lack of feedback control. This shift in hormone production is largely responsible for many of the symptoms experienced during and after menopause and includes hot flashes and other vasomotor symptoms, painful intercourse, vaginal dryness, and vulvovaginal atrophy. These symptoms are able to be reduced by replacing many of the hormones lost during and following menopause with synthetic or naturally occurring forms, in a therapy known as Hormone Replacement Therapy (HRT).

TargetActionsOrganism
AEstrogen receptor alpha
agonist
Human
Absorption

Conjugated estrogens are water-soluble and are well-absorbed from the gastrointestinal tract after release from the drug formulation. Tablets release conjugated estrogens slowly over several hours.

Volume of distribution

The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentration in the sex hormone target organs.

Protein binding

Estrogens circulate in the blood largely bound to sex hormone-binding globulin (SHBG) and albumin.

Metabolism

Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is a major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the intestine followed by reabsorption. In postmenopausal women a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens. In vitro and in vivo studies have shown that estrogens are metabolized partially by cytochrome P450 3A4 (CYP3A4).

Route of elimination

Estradiol, estrone, and estriol are excreted in the urine, along with glucuronide and sulfate conjugates. Exogenous estrogens are metabolized in the same manner as endogenous estrogens.

Half life

Following a dose of 0.625 mg of conjugated estrogens, the half life of estrone, baseline-adjusted estrone, and equilin was found to be 26.7 hr, 14.8 hr, and 11.4 hr, respectively.

Clearance
Not Available
Toxicity

Nausea and vomiting

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

Interactions

Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe serum concentration of Conjugated estrogens can be decreased when it is combined with 1,10-Phenanthroline.Experimental
16-BromoepiandrosteroneThe serum concentration of 16-Bromoepiandrosterone can be increased when it is combined with Conjugated estrogens.Investigational
19-norandrostenedioneThe serum concentration of 19-norandrostenedione can be increased when it is combined with Conjugated estrogens.Experimental, Illicit
3,4-DichloroisocoumarinThe serum concentration of Conjugated estrogens can be decreased when it is combined with 3,4-Dichloroisocoumarin.Experimental
4-(2-Aminoethyl)Benzenesulfonyl FluorideThe serum concentration of Conjugated estrogens can be decreased when it is combined with 4-(2-Aminoethyl)Benzenesulfonyl Fluoride.Experimental
5-androstenedioneThe serum concentration of 5-androstenedione can be increased when it is combined with Conjugated estrogens.Experimental, Illicit
AbciximabConjugated estrogens may decrease the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Conjugated estrogens can be increased when it is combined with Abiraterone.Approved
AcenocoumarolConjugated estrogens may decrease the anticoagulant activities of Acenocoumarol.Approved
AcitretinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Acitretin.Approved
AdapaleneThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Adapalene.Approved
AlclometasoneThe serum concentration of Alclometasone can be increased when it is combined with Conjugated estrogens.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Conjugated estrogens.Experimental, Investigational
AlitretinoinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Alitretinoin.Approved, Investigational
AlogliptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Alogliptin.Approved
Alpha-1-proteinase inhibitorThe serum concentration of Conjugated estrogens can be decreased when it is combined with Alpha-1-proteinase inhibitor.Approved
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be increased when it is combined with Conjugated estrogens.Experimental, Investigational
AmcinonideThe serum concentration of Amcinonide can be increased when it is combined with Conjugated estrogens.Approved
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Conjugated estrogens.Approved
AmiodaroneThe metabolism of Conjugated estrogens can be decreased when combined with Amiodarone.Approved, Investigational
AmobarbitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Amobarbital.Approved, Illicit
AmprenavirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Amprenavir.Approved
AnastrozoleThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Conjugated estrogens.Approved, Investigational
AncrodConjugated estrogens may decrease the anticoagulant activities of Ancrod.Investigational
AndrostenedioneThe serum concentration of Androstenedione can be increased when it is combined with Conjugated estrogens.Experimental, Illicit
AnecortaveThe serum concentration of Anecortave can be increased when it is combined with Conjugated estrogens.Investigational
anecortave acetateThe serum concentration of anecortave acetate can be increased when it is combined with Conjugated estrogens.Investigational
Anthrax immune globulin humanConjugated estrogens may increase the thrombogenic activities of Anthrax immune globulin human.Approved
Antithrombin III humanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Antithrombin III human.Approved
ApixabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Apixaban.Approved
AprepitantThe serum concentration of Conjugated estrogens can be decreased when it is combined with Aprepitant.Approved, Investigational
AprotininThe serum concentration of Conjugated estrogens can be decreased when it is combined with Aprotinin.Approved, Withdrawn
ArdeparinConjugated estrogens may decrease the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Argatroban.Approved, Investigational
ArmodafinilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Armodafinil.Approved, Investigational
ArtemetherThe serum concentration of Conjugated estrogens can be decreased when it is combined with Artemether.Approved
AsunaprevirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Asunaprevir.Approved, Investigational
AtamestaneThe serum concentration of Atamestane can be increased when it is combined with Conjugated estrogens.Investigational
AtazanavirThe metabolism of Conjugated estrogens can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Conjugated estrogens can be decreased when combined with Atomoxetine.Approved
AzithromycinThe metabolism of Conjugated estrogens can be decreased when combined with Azithromycin.Approved
BarbexacloneThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Barbexaclone.Experimental
BarbitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Barbital.Illicit
BatimastatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Batimastat.Experimental
BecaplerminConjugated estrogens may decrease the anticoagulant activities of Becaplermin.Approved, Investigational
Beclomethasone dipropionateThe serum concentration of Beclomethasone dipropionate can be increased when it is combined with Conjugated estrogens.Approved, Investigational
BenazeprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Benazepril.Approved, Investigational
BenzamidineThe serum concentration of Conjugated estrogens can be decreased when it is combined with Benzamidine.Experimental
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
BexaroteneThe serum concentration of Conjugated estrogens can be decreased when it is combined with Bexarotene.Approved, Investigational
BivalirudinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Bivalirudin.Approved, Investigational
BoceprevirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Conjugated estrogens can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Bosentan.Approved, Investigational
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Conjugated estrogens.Approved
CaffeineThe metabolism of Conjugated estrogens can be decreased when combined with Caffeine.Approved
CamostatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Camostat.Experimental
CandoxatrilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Candoxatril.Experimental
CandoxatrilatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Candoxatrilat.Experimental
Capromab pendetideConjugated estrogens may decrease effectiveness of Capromab pendetide as a diagnostic agent.Approved
CaptoprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Captopril.Approved
CarbamazepineThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Carbamazepine.Approved, Investigational
CelecoxibCelecoxib may increase the thrombogenic activities of Conjugated estrogens.Approved, Investigational
CeritinibThe serum concentration of Conjugated estrogens can be increased when it is combined with Ceritinib.Approved
CertoparinConjugated estrogens may decrease the anticoagulant activities of Certoparin.Approved, Investigational
Chenodeoxycholic acidThe therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Conjugated estrogens.Approved
CholesterolThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cholesterol.Experimental, Investigational
CholestyramineThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cholestyramine.Approved
ChymostatinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Chymostatin.Experimental
CiclesonideThe serum concentration of Ciclesonide can be increased when it is combined with Conjugated estrogens.Approved, Investigational
CilastatinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cilastatin.Approved
CilazaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cilazapril.Approved
CitalopramThe metabolism of Conjugated estrogens can be decreased when combined with Citalopram.Approved
Citric AcidConjugated estrogens may decrease the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Conjugated estrogens can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Conjugated estrogens can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Conjugated estrogens can be decreased when it is combined with Clobazam.Approved, Illicit
ClobetasolThe serum concentration of Clobetasol can be increased when it is combined with Conjugated estrogens.Investigational
Clobetasol propionateThe serum concentration of Clobetasol propionate can be increased when it is combined with Conjugated estrogens.Approved
ClobetasoneThe serum concentration of Clobetasone can be increased when it is combined with Conjugated estrogens.Approved
ClocortoloneThe serum concentration of Clocortolone can be increased when it is combined with Conjugated estrogens.Approved
ClorindioneConjugated estrogens may decrease the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Conjugated estrogens can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cobicistat.Approved
ColesevelamThe serum concentration of Conjugated estrogens can be decreased when it is combined with Colesevelam.Approved
ColestipolThe serum concentration of Conjugated estrogens can be decreased when it is combined with Colestipol.Approved
Conestat alfaConjugated estrogens may increase the thrombogenic activities of Conestat alfa.Approved
ConivaptanThe serum concentration of Conjugated estrogens can be increased when it is combined with Conivaptan.Approved, Investigational
Cortexolone 17α-propionateThe serum concentration of Cortexolone 17α-propionate can be increased when it is combined with Conjugated estrogens.Investigational
CorticosteroneThe serum concentration of Corticosterone can be increased when it is combined with Conjugated estrogens.Experimental
Cortisone acetateThe serum concentration of Cortisone acetate can be increased when it is combined with Conjugated estrogens.Approved
CrizotinibThe metabolism of Conjugated estrogens can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Conjugated estrogens can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Conjugated estrogens can be decreased when it is combined with Dabrafenib.Approved
DalteparinConjugated estrogens may decrease the anticoagulant activities of Dalteparin.Approved
DanaparoidConjugated estrogens may decrease the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Darexaban.Investigational
DarunavirThe metabolism of Conjugated estrogens can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Conjugated estrogens can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Conjugated estrogens can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortThe serum concentration of Deflazacort can be increased when it is combined with Conjugated estrogens.Approved
DelanzomibThe serum concentration of Conjugated estrogens can be decreased when it is combined with Delanzomib.Investigational
DelaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Delapril.Experimental
DelavirdineThe metabolism of Conjugated estrogens can be decreased when combined with Delavirdine.Approved
DesirudinConjugated estrogens may decrease the anticoagulant activities of Desirudin.Approved
DesonideThe serum concentration of Desonide can be increased when it is combined with Conjugated estrogens.Approved, Investigational
DesoximetasoneThe serum concentration of Desoximetasone can be increased when it is combined with Conjugated estrogens.Approved
Desoxycorticosterone acetateThe serum concentration of Desoxycorticosterone acetate can be increased when it is combined with Conjugated estrogens.Approved
Desoxycorticosterone PivalateThe serum concentration of Desoxycorticosterone Pivalate can be increased when it is combined with Conjugated estrogens.Experimental, Vet Approved
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Conjugated estrogens.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Conjugated estrogens.Vet Approved
DextranConjugated estrogens may decrease the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Conjugated estrogens may decrease the anticoagulant activities of Dextran 40.Approved
Dextran 70Conjugated estrogens may decrease the anticoagulant activities of Dextran 70.Approved
Dextran 75Conjugated estrogens may decrease the anticoagulant activities of Dextran 75.Approved
DicoumarolConjugated estrogens may decrease the anticoagulant activities of Dicoumarol.Approved
DiflorasoneThe serum concentration of Diflorasone can be increased when it is combined with Conjugated estrogens.Approved
DifluocortoloneThe serum concentration of Difluocortolone can be increased when it is combined with Conjugated estrogens.Approved, Investigational
DifluprednateThe serum concentration of Difluprednate can be increased when it is combined with Conjugated estrogens.Approved
DihydroergotamineThe metabolism of Conjugated estrogens can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Conjugated estrogens can be decreased when combined with Diltiazem.Approved
DiphenadioneConjugated estrogens may decrease the anticoagulant activities of Diphenadione.Experimental
DosulepinThe metabolism of Conjugated estrogens can be decreased when combined with Dosulepin.Approved
DoxycyclineThe metabolism of Conjugated estrogens can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Conjugated estrogens can be decreased when combined with Dronedarone.Approved
DyphyllineThe serum concentration of Dyphylline can be increased when it is combined with Conjugated estrogens.Approved
EcabetThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ecabet.Approved, Investigational
Edetic AcidConjugated estrogens may decrease the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Edoxaban.Approved
ElafinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Elafin.Investigational
EltrombopagThe serum concentration of Conjugated estrogens can be increased when it is combined with Eltrombopag.Approved
ElvitegravirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Elvitegravir.Approved
EnalaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Enalaprilat.Approved
EnalkirenThe serum concentration of Conjugated estrogens can be decreased when it is combined with Enalkiren.Experimental
EnoxaparinConjugated estrogens may decrease the anticoagulant activities of Enoxaparin.Approved
EntacaponeThe metabolism of Conjugated estrogens can be decreased when combined with Entacapone.Approved, Investigational
EnzalutamideThe serum concentration of Conjugated estrogens can be decreased when it is combined with Enzalutamide.Approved
Epigallocatechin GallateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Epigallocatechin Gallate.Investigational
EquileninThe serum concentration of Equilenin can be increased when it is combined with Conjugated estrogens.Experimental
EquilinThe serum concentration of Equilin can be increased when it is combined with Conjugated estrogens.Approved
ErythromycinThe metabolism of Conjugated estrogens can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Conjugated estrogens.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be increased when it is combined with Conjugated estrogens.Approved
Ethyl biscoumacetateConjugated estrogens may decrease the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the thrombogenic activities of Conjugated estrogens.Approved, Investigational, Vet Approved
EtoricoxibEtoricoxib may increase the thrombogenic activities of Conjugated estrogens.Approved, Investigational
ExemestaneThe therapeutic efficacy of Exemestane can be decreased when used in combination with Conjugated estrogens.Approved, Investigational
ExenatideThe serum concentration of Conjugated estrogens can be decreased when it is combined with Exenatide.Approved, Investigational
FaldaprevirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Faldaprevir.Investigational
FelbamateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Felbamate.Approved
Ferulic acidConjugated estrogens may decrease the anticoagulant activities of Ferulic acid.Experimental
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Conjugated estrogens.Approved
fluasteroneThe serum concentration of fluasterone can be increased when it is combined with Conjugated estrogens.Investigational
FluconazoleThe metabolism of Conjugated estrogens can be decreased when combined with Fluconazole.Approved
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Conjugated estrogens.Approved
FluindioneConjugated estrogens may decrease the anticoagulant activities of Fluindione.Investigational
FlumethasoneThe serum concentration of Flumethasone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Conjugated estrogens.Approved, Investigational
Fluocinolone AcetonideThe serum concentration of Fluocinolone Acetonide can be increased when it is combined with Conjugated estrogens.Approved, Investigational, Vet Approved
FluocinonideThe serum concentration of Fluocinonide can be increased when it is combined with Conjugated estrogens.Approved, Investigational
FluocortoloneThe serum concentration of Fluocortolone can be increased when it is combined with Conjugated estrogens.Approved, Withdrawn
FluorometholoneThe serum concentration of Fluorometholone can be increased when it is combined with Conjugated estrogens.Approved
FluprednideneThe serum concentration of Fluprednidene can be increased when it is combined with Conjugated estrogens.Approved, Withdrawn
FluprednisoloneThe serum concentration of Fluprednisolone can be increased when it is combined with Conjugated estrogens.Approved
FlurandrenolideThe serum concentration of Flurandrenolide can be increased when it is combined with Conjugated estrogens.Approved
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Conjugated estrogens.Approved
Fluticasone propionateThe serum concentration of Fluticasone propionate can be increased when it is combined with Conjugated estrogens.Approved
FluvoxamineThe metabolism of Conjugated estrogens can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxConjugated estrogens may decrease the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumConjugated estrogens may decrease the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FormestaneThe serum concentration of Formestane can be increased when it is combined with Conjugated estrogens.Approved, Investigational, Withdrawn
FosamprenavirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Conjugated estrogens can be decreased when it is combined with Fosaprepitant.Approved
FosinoprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Fosinopril.Approved
FosphenytoinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Conjugated estrogens can be increased when it is combined with Fusidic Acid.Approved
GabexateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Gabexate.Investigational
GeldanamycinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Geldanamycin.Experimental, Investigational
GM6001The serum concentration of Conjugated estrogens can be decreased when it is combined with GM6001.Experimental
GriseofulvinThe metabolism of Conjugated estrogens can be increased when combined with Griseofulvin.Approved, Vet Approved
HalcinonideThe serum concentration of Halcinonide can be increased when it is combined with Conjugated estrogens.Approved, Investigational, Withdrawn
HE3286The serum concentration of HE3286 can be increased when it is combined with Conjugated estrogens.Investigational
HeparinConjugated estrogens may decrease the anticoagulant activities of Heparin.Approved, Investigational
HexobarbitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Hexobarbital.Approved
Human C1-esterase inhibitorConjugated estrogens may increase the thrombogenic activities of Human C1-esterase inhibitor.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Conjugated estrogens.Approved, Investigational
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
IdelalisibThe serum concentration of Conjugated estrogens can be increased when it is combined with Idelalisib.Approved
IdraparinuxThe serum concentration of Conjugated estrogens can be decreased when it is combined with Idraparinux.Investigational
ImatinibThe metabolism of Conjugated estrogens can be decreased when combined with Imatinib.Approved
ImidaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Imidapril.Investigational
IndinavirThe metabolism of Conjugated estrogens can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Conjugated estrogens can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoflurophateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Isoflurophate.Approved, Investigational, Withdrawn
IsotretinoinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Isotretinoin.Approved
IsradipineThe metabolism of Conjugated estrogens can be decreased when combined with Isradipine.Approved
IstaroximeThe serum concentration of Istaroxime can be increased when it is combined with Conjugated estrogens.Investigational
ItraconazoleThe metabolism of Conjugated estrogens can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Conjugated estrogens can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ixazomib.Approved
KetoconazoleThe metabolism of Conjugated estrogens can be decreased when combined with Ketoconazole.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Conjugated estrogens.Approved, Investigational
LenalidomideConjugated estrogens may increase the thrombogenic activities of Lenalidomide.Approved
LepirudinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Lepirudin.Approved
LetaxabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Letaxaban.Investigational
LevothyroxineThe therapeutic efficacy of Levothyroxine can be decreased when used in combination with Conjugated estrogens.Approved
LidocaineThe metabolism of Conjugated estrogens can be decreased when combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Linagliptin.Approved
LiothyronineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Conjugated estrogens.Approved, Vet Approved
LiotrixThe therapeutic efficacy of Liotrix can be decreased when used in combination with Conjugated estrogens.Approved
LisinoprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Lisinopril.Approved, Investigational
LobeglitazoneThe metabolism of Conjugated estrogens can be decreased when combined with Lobeglitazone.Approved, Investigational
LopinavirThe metabolism of Conjugated estrogens can be decreased when combined with Lopinavir.Approved
LoteprednolThe serum concentration of Loteprednol can be increased when it is combined with Conjugated estrogens.Approved
LovastatinThe metabolism of Conjugated estrogens can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Conjugated estrogens can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Conjugated estrogens can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the thrombogenic activities of Conjugated estrogens.Approved, Investigational
ME-609The serum concentration of ME-609 can be increased when it is combined with Conjugated estrogens.Investigational
MedrysoneThe serum concentration of Medrysone can be increased when it is combined with Conjugated estrogens.Approved
MelagatranThe serum concentration of Conjugated estrogens can be decreased when it is combined with Melagatran.Experimental
MelengestrolThe serum concentration of Melengestrol can be increased when it is combined with Conjugated estrogens.Vet Approved
MethohexitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Methohexital.Approved
MethylphenobarbitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Methylphenobarbital.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
MetreleptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Metreleptin.Approved
MexiletineThe metabolism of Conjugated estrogens can be decreased when combined with Mexiletine.Approved
MidostaurinThe metabolism of Conjugated estrogens can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Conjugated estrogens can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Conjugated estrogens can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Moexipril.Approved
MometasoneThe serum concentration of Mometasone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
Mycophenolic acidThe serum concentration of Conjugated estrogens can be decreased when it is combined with Mycophenolic acid.Approved
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Conjugated estrogens can be decreased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.Experimental
NabumetoneNabumetone may increase the thrombogenic activities of Conjugated estrogens.Approved
NadroparinConjugated estrogens may decrease the anticoagulant activities of Nadroparin.Approved
NafamostatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Nafamostat.Approved, Investigational
NafcillinThe metabolism of Conjugated estrogens can be increased when combined with Nafcillin.Approved
NCX 1022The serum concentration of NCX 1022 can be increased when it is combined with Conjugated estrogens.Investigational
NefazodoneThe metabolism of Conjugated estrogens can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Conjugated estrogens can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Conjugated estrogens can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Conjugated estrogens can be decreased when it is combined with Nevirapine.Approved
NilotinibThe metabolism of Conjugated estrogens can be decreased when combined with Nilotinib.Approved, Investigational
NitroaspirinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Nitroaspirin.Investigational
OlaparibThe metabolism of Conjugated estrogens can be decreased when combined with Olaparib.Approved
Oleoyl-estroneThe serum concentration of Oleoyl-estrone can be increased when it is combined with Conjugated estrogens.Investigational
OmapatrilatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Omapatrilat.Investigational
OsimertinibThe serum concentration of Conjugated estrogens can be increased when it is combined with Osimertinib.Approved
OspemifeneThe risk or severity of adverse effects can be increased when Conjugated estrogens is combined with Ospemifene.Approved
OtamixabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Otamixaban.Investigational
OxcarbazepineThe serum concentration of Conjugated estrogens can be decreased when it is combined with Oxcarbazepine.Approved
PalbociclibThe serum concentration of Conjugated estrogens can be increased when it is combined with Palbociclib.Approved
ParamethasoneThe serum concentration of Paramethasone can be increased when it is combined with Conjugated estrogens.Approved
ParecoxibParecoxib may increase the thrombogenic activities of Conjugated estrogens.Approved
Peginterferon alfa-2bThe serum concentration of Conjugated estrogens can be increased when it is combined with Peginterferon alfa-2b.Approved
Pentaerythritol TetranitrateConjugated estrogens may decrease the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
PentobarbitalThe metabolism of Conjugated estrogens can be increased when combined with Pentobarbital.Approved, Vet Approved
Pentosan PolysulfateConjugated estrogens may decrease the anticoagulant activities of Pentosan Polysulfate.Approved
PerindoprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Perindopril.Approved
PhenindioneConjugated estrogens may decrease the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Conjugated estrogens can be increased when combined with Phenobarbital.Approved
PhenprocoumonConjugated estrogens may decrease the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenytoinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Phenytoin.Approved, Vet Approved
PhosphoramidonThe serum concentration of Conjugated estrogens can be decreased when it is combined with Phosphoramidon.Experimental
PosaconazoleThe metabolism of Conjugated estrogens can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Conjugated estrogens.Approved, Nutraceutical
Prasterone sulfateThe serum concentration of Prasterone sulfate can be increased when it is combined with Conjugated estrogens.Investigational
PrednicarbateThe serum concentration of Prednicarbate can be increased when it is combined with Conjugated estrogens.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
PregnenoloneThe serum concentration of Pregnenolone can be increased when it is combined with Conjugated estrogens.Experimental, Investigational
PrimidoneThe metabolism of Conjugated estrogens can be increased when combined with Primidone.Approved, Vet Approved
PrinomastatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Prinomastat.Investigational
Protein CConjugated estrogens may decrease the anticoagulant activities of Protein C.Approved
Protein S humanConjugated estrogens may decrease the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeConjugated estrogens may decrease the anticoagulant activities of Protocatechualdehyde.Approved
PrucaloprideThe serum concentration of Conjugated estrogens can be decreased when it is combined with Prucalopride.Approved
QuinaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Quinapril.Approved, Investigational
RacecadotrilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Racecadotril.Investigational
RamiprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ramipril.Approved
RanolazineThe serum concentration of Conjugated estrogens can be increased when it is combined with Ranolazine.Approved, Investigational
RemikirenThe serum concentration of Conjugated estrogens can be decreased when it is combined with Remikiren.Approved
ReviparinConjugated estrogens may decrease the anticoagulant activities of Reviparin.Approved, Investigational
RifabutinThe metabolism of Conjugated estrogens can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Conjugated estrogens can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Conjugated estrogens can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Rifaximin.Approved, Investigational
RimexoloneThe serum concentration of Rimexolone can be increased when it is combined with Conjugated estrogens.Approved
RivaroxabanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Rivaroxaban.Approved
RofecoxibRofecoxib may increase the thrombogenic activities of Conjugated estrogens.Investigational, Withdrawn
RolapitantThe serum concentration of Conjugated estrogens can be increased when it is combined with Rolapitant.Approved
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Conjugated estrogens.Approved, Investigational
S-3304The serum concentration of Conjugated estrogens can be decreased when it is combined with S-3304.Investigational
SaquinavirThe metabolism of Conjugated estrogens can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Saxagliptin.Approved
SecobarbitalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Selegiline can be increased when it is combined with Conjugated estrogens.Approved, Investigational, Vet Approved
SildenafilThe metabolism of Conjugated estrogens can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Conjugated estrogens can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Conjugated estrogens can be increased when it is combined with Simeprevir.Approved
SitagliptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Sitagliptin.Approved, Investigational
SivelestatThe serum concentration of Conjugated estrogens can be decreased when it is combined with Sivelestat.Investigational
SomatotropinThe therapeutic efficacy of Somatotropin can be decreased when used in combination with Conjugated estrogens.Approved, Investigational
SpiraprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Spirapril.Approved
St. John's WortThe serum concentration of Conjugated estrogens can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Conjugated estrogens can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Conjugated estrogens can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideConjugated estrogens may decrease the anticoagulant activities of Sulodexide.Approved, Investigational
TelaprevirThe serum concentration of Conjugated estrogens can be decreased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Conjugated estrogens can be decreased when combined with Telithromycin.Approved
TemocaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Temocapril.Experimental, Investigational
Tenofovir disoproxilThe metabolism of Conjugated estrogens can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TeriflunomideThe serum concentration of Conjugated estrogens can be increased when it is combined with Teriflunomide.Approved
Testosterone PropionateThe metabolism of Conjugated estrogens can be decreased when combined with Testosterone Propionate.Approved, Vet Approved
ThalidomideConjugated estrogens may increase the thrombogenic activities of Thalidomide.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Conjugated estrogens can be decreased when combined with Theophylline.Approved
ThiamylalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Thiamylal.Approved, Vet Approved
ThiopentalThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Thiopental.Approved, Vet Approved
ThiorphanThe serum concentration of Conjugated estrogens can be decreased when it is combined with Thiorphan.Experimental
Thyroid, porcineThe therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Conjugated estrogens.Approved
TiclopidineThe metabolism of Conjugated estrogens can be decreased when combined with Ticlopidine.Approved
TioclomarolConjugated estrogens may decrease the anticoagulant activities of Tioclomarol.Experimental
TipranavirConjugated estrogens may increase the dermatologic adverse activities of Tipranavir.Approved, Investigational
TixocortolThe serum concentration of Tixocortol can be increased when it is combined with Conjugated estrogens.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Conjugated estrogens.Approved
TocilizumabThe serum concentration of Conjugated estrogens can be decreased when it is combined with Tocilizumab.Approved
TolcaponeThe metabolism of Conjugated estrogens can be decreased when combined with Tolcapone.Approved, Withdrawn
TopiramateThe serum concentration of Conjugated estrogens can be decreased when it is combined with Topiramate.Approved
TrandolaprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Trandolapril.Approved
Tranexamic AcidConjugated estrogens may increase the thrombogenic activities of Tranexamic Acid.Approved
TretinoinThe therapeutic efficacy of Conjugated estrogens can be decreased when used in combination with Tretinoin.Approved, Investigational, Nutraceutical
TriamcinoloneThe serum concentration of Triamcinolone can be increased when it is combined with Conjugated estrogens.Approved, Vet Approved
TroxerutinConjugated estrogens may decrease the anticoagulant activities of Troxerutin.Investigational
UbenimexThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ubenimex.Experimental, Investigational
UlinastatinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ulinastatin.Investigational
UlobetasolThe serum concentration of Ulobetasol can be increased when it is combined with Conjugated estrogens.Approved
Ursodeoxycholic acidThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Conjugated estrogens.Approved, Investigational
ValdecoxibValdecoxib may increase the thrombogenic activities of Conjugated estrogens.Investigational, Withdrawn
VemurafenibThe serum concentration of Conjugated estrogens can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Conjugated estrogens can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Conjugated estrogens can be decreased when combined with Verapamil.Approved
VildagliptinThe serum concentration of Conjugated estrogens can be decreased when it is combined with Vildagliptin.Approved, Investigational
Vitamin CThe serum concentration of Conjugated estrogens can be increased when it is combined with Vitamin C.Approved, Nutraceutical
VoriconazoleThe metabolism of Conjugated estrogens can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinConjugated estrogens may decrease the anticoagulant activities of Warfarin.Approved
XimelagatranThe serum concentration of Conjugated estrogens can be decreased when it is combined with Ximelagatran.Approved, Investigational, Withdrawn
Z-Val-Ala-Asp fluoromethyl ketoneThe serum concentration of Conjugated estrogens can be decreased when it is combined with Z-Val-Ala-Asp fluoromethyl ketone.Experimental
ZiprasidoneThe metabolism of Conjugated estrogens can be decreased when combined with Ziprasidone.Approved
ZofenoprilThe serum concentration of Conjugated estrogens can be decreased when it is combined with Zofenopril.Experimental
ZucapsaicinThe metabolism of Conjugated estrogens can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

Synthesis Reference

Vallapa Soong, "Process for the preparation of conjugated estrogens from pregnant mare urine." U.S. Patent US20020156303, issued October 24, 2002.

US20020156303
General References
  1. 14. (2015). In Pharmacology for Women’s Health. Jones & Bartlett Publishers.
External Links
KEGG Drug
D04070
PubChem Substance
46505680
ChemSpider
9532
ChEBI
8389
ChEMBL
CHEMBL2106240
Therapeutic Targets Database
DNC001150
PharmGKB
PA164754789
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Conjugated_estrogen
ATC Codes
G03CC07 — Conjugated estrogens and bazedoxifeneG03CA57 — Conjugated estrogens
AHFS Codes
  • 68:16.04 — Estrogens
FDA label
Download (5.44 MB)
MSDS
Download (34.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingPreventionMenopause1
1CompletedNot AvailableAtrophic Vaginitis1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedDiagnosticEstrogen Replacement Therapy / Healthy Volunteers1
1CompletedHealth Services ResearchOne to five years postmenopausal1
1CompletedPreventionOne to five years postmenopausal1
1CompletedScreeningOne to five years postmenopausal1
1CompletedTreatmentOne to five years postmenopausal2
2CompletedPreventionCardiovascular Disease (CVD) / Endometrial Hyperplasia / Heart Diseases / Menopausal Complaints / Menopause / Uterine Diseases1
2CompletedTreatmentAmenorrhea / One to five years postmenopausal1
2CompletedTreatmentEndometriosis1
2CompletedTreatmentEpilepsies / Menopause1
2CompletedTreatmentHypertensive / One to five years postmenopausal / Pre-Hypertension1
2CompletedTreatmentMenopausal and Female Climacteric States / Menopausal Hot Flushes1
2CompletedTreatmentParkinson's Disease (PD)1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentShock, Hemorrhagic1
2CompletedTreatmentTraumatic Brain Injury (TBI)1
2CompletedTreatmentOne to five years postmenopausal2
2RecruitingPreventionCancer, Breast1
2RecruitingTreatmentDisseminated Sclerosis / Menopause1
2, 3CompletedHealth Services ResearchCardiovascular Disease (CVD) / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases1
2, 3CompletedTreatmentAnorexia Nervosa (AN)1
3CompletedOtherPostmenopausal Women1
3CompletedPreventionBone destruction / Bone Diseases / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Heart Diseases / Hypercholesterolaemia / Hypertensive / Myocardial Ischemia / One to five years postmenopausal / Thrombosis1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Arteriosclerosis / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia / One to five years postmenopausal1
3CompletedSupportive CareCancer, Breast / Menopausal Hot Flushes / Menopausal Symptoms1
3CompletedTreatmentHormone Replacement Therapy1
3CompletedTreatmentBone destruction / Menopause1
3CompletedTreatmentPelvic Organ Prolapse (POP) / Vulvovaginal Atrophy1
3CompletedTreatmentBone destruction1
3TerminatedTreatmentEndometrial Cancers1
3TerminatedTreatmentSystemic Lupus Erythematosus (SLE)1
4CompletedNot AvailableOne to five years postmenopausal1
4CompletedBasic ScienceMenopause / Pelvic Organ Prolapse (POP)1
4CompletedSupportive CareAtrophic Vaginitis / Endometrial Hyperplasia / Pelvic Organ Prolapse (POP)1
4RecruitingBasic ScienceAtrophic Vaginitis / Menopause / Recurrent Urinary Tract Infections1
4RecruitingPreventionBMI >30 kg/m2 / Glucose Homeostasis / Postmenopausal Syndrome1
4RecruitingTreatmentCystocele / Pelvic Floor Disorders / Pelvic Organ Prolapse (POP) / Urogenital Prolapse / Uterine Prolapse / Vaginal Prolapse / Vaginal Vault Prolapse1
4RecruitingTreatmentEstrogens / General Surgery / Menopause / Pelvic Floor Disorders1
4RecruitingTreatmentIncontinence / Nocturia / Overactive Bladder1
4RecruitingTreatmentMicroscopic Hematuria1
4RecruitingTreatmentOveractive Bladder1
4RecruitingTreatmentSexual Dysfunction, Physiological1
4Unknown StatusPreventionArteriosclerosis / Menopause1
Not AvailableCompletedNot AvailableAbnormal Mammogram / Mammographic Density1
Not AvailableCompletedNot AvailableDementia Syndromes1
Not AvailableCompletedTreatmentOvarian Failure, Premature1
Not AvailableCompletedTreatmentOveractive Bladder1
Not AvailableCompletedTreatmentUnspecified Injury of Brachial Artery, Left Side, Initial Encounter1
Not AvailableEnrolling by InvitationNot AvailablePelvic Organ Prolapse (POP) / Postoperative pain1
Not AvailableRecruitingOtherPelvic Floor Disorders1
Not AvailableRecruitingTreatmentPelvic Organ Prolapse (POP)1
Not AvailableSuspendedTreatmentAtrophic Vaginitis / Menopause1
Not AvailableTerminatedTreatmentMenopausal Hot Flushes1
Not AvailableUnknown StatusPreventionQuality of Life / Urinary Tract Infections (UTIs) / Vaginal Infections1
Not AvailableUnknown StatusSupportive CareBone destruction / Cancer, Breast / Menopausal Hot Flushes / Menopausal Symptoms1

Pharmacoeconomics

Manufacturers
  • Wyeth pharmaceuticals inc
  • Duramed research inc
  • Teva womens health inc
  • Roche palo alto llc
Packagers
Dosage forms
FormRouteStrength
TabletOral0.3 mg
TabletOral0.625 mg
TabletOral1.25 mg
TabletOral2.5 mg
Tablet, film coatedOral
Tablet, multilayer, extended releaseOral
TabletOral
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous25 mg/5mL
Tablet, extended releaseOral0.3 mg
Tablet, extended releaseOral0.625 mg
Tablet, extended releaseOral1.25 mg
Tablet, film coatedOral.3 mg/1
Tablet, film coatedOral.45 mg/1
Tablet, film coatedOral.625 mg/1
Tablet, film coatedOral.9 mg/1
Tablet, film coatedOral1.25 mg/1
CreamTopical; Vaginal.625 mg
Powder, for solutionIntramuscular; Intravenous25 mg
TabletOral0.9 mg
CreamVaginal.625 mg/g
CreamVaginal0.625 mg
Kit
Kit; tabletOral
Tablet, sugar coatedOral
Prices
Unit descriptionCostUnit
Premarin 0.625 mg/gm Cream 42.5 gm Tube134.05USD tube
Premarin 25 mg vial107.54USD vial
Premphase 28 0.625-5 mg tablet Disp Pack69.99USD disp
Premarin vaginal cream-appl3.07USD g
Prempro 0.3 mg-1.5 mg tablet2.34USD tablet
Prempro 0.45-1.5 mg tablet2.34USD tablet
Prempro 0.625-2.5 mg tablet2.34USD tablet
Prempro 0.625-5 mg tablet2.34USD tablet
Premarin 0.45 mg tablet1.97USD tablet
Premarin 0.9 mg tablet1.97USD tablet
Premarin 2.5 mg tablet1.83USD tablet
Premarin 2.5 mg Tabs1.82USD tablet
Premarin 0.3 mg tablet1.42USD tablet
Premarin 0.625 mg tablet1.42USD tablet
Premarin 1.25 mg tablet1.42USD tablet
Premarin 0.625 mg/g Cream0.69USD g
C.E.S. 0.625 mg Tablet0.11USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5908638No1995-07-262015-07-26Us
US5547948No1995-01-172015-01-17Us
US5998402No1997-04-042017-04-04Us
US6479535No1999-05-062019-05-06Us
US7138392No1997-04-042017-04-04Us
US7683051No2007-03-102027-03-10Us
US8815934No1999-05-062019-05-06Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)173 °CNot Available
water solubility0.0036 mg/mlNot Available
Predicted Properties
Not Available
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.997
Blood Brain Barrier+0.9486
Caco-2 permeable-0.8738
P-glycoprotein substrateNon-substrate0.5295
P-glycoprotein inhibitor INon-inhibitor0.5198
P-glycoprotein inhibitor IINon-inhibitor0.9431
Renal organic cation transporterNon-inhibitor0.8313
CYP450 2C9 substrateNon-substrate0.7886
CYP450 2D6 substrateNon-substrate0.8125
CYP450 3A4 substrateSubstrate0.6454
CYP450 1A2 substrateNon-inhibitor0.8152
CYP450 2C9 inhibitorNon-inhibitor0.8454
CYP450 2D6 inhibitorNon-inhibitor0.9026
CYP450 2C19 inhibitorNon-inhibitor0.8017
CYP450 3A4 inhibitorNon-inhibitor0.9204
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8461
Ames testNon AMES toxic0.5177
CarcinogenicityNon-carcinogens0.5338
BiodegradationNot ready biodegradable0.6303
Rat acute toxicity2.3418 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6053
hERG inhibition (predictor II)Inhibitor0.7941
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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. Ropero AB, Eghbali M, Minosyan TY, Tang G, Toro L, Stefani E: Heart estrogen receptor alpha: distinct membrane and nuclear distribution patterns and regulation by estrogen. J Mol Cell Cardiol. 2006 Sep;41(3):496-510. Epub 2006 Jul 28. [PubMed:16876190]
  2. Stroud FC, Appt SE, Wilson ME, Franke AA, Adams MR, Kaplan JR: Concentrations of isoflavones in macaques consuming standard laboratory monkey diet. J Am Assoc Lab Anim Sci. 2006 Jul;45(4):20-3. [PubMed:16884174]
  3. Hou NN, Zhu YM, Huang HF: [The expression of estrogen receptor alpha and beta in the intervention of different estrogens in rat bone metabolism]. Fen Zi Xi Bao Sheng Wu Xue Bao. 2006 Aug;39(4):289-96. [PubMed:16955786]
  4. Gouva L, Tsatsoulis A: The role of estrogens in cardiovascular disease in the aftermath of clinical trials. Hormones (Athens). 2004 Jul-Sep;3(3):171-83. [PubMed:16982590]
  5. Smith MR: Selective estrogen receptor modulators to prevent treatment-related osteoporosis. Rev Urol. 2005;7 Suppl 3:S30-5. [PubMed:16985877]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
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. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M: Substrate inhibition kinetics for cytochrome P450-catalyzed reactions. Drug Metab Dispos. 2001 Apr;29(4 Pt 1):368-74. [PubMed:11259318]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 Da
References
  1. Zhu BT, Wu KY, Wang P, Cai MX, Conney AH: O-methylation of catechol estrogens by human placental catechol-o-methyltransferase: interindividual differences in sensitivity to heat inactivation and to inhibition by dietary polyphenols. Drug Metab Dispos. 2010 Oct;38(10):1892-9. doi: 10.1124/dmd.110.033548. Epub 2010 Jul 6. [PubMed:20606002]
  2. Jobe SO, Ramadoss J, Koch JM, Jiang Y, Zheng J, Magness RR: Estradiol-17beta and its cytochrome P450- and catechol-O-methyltransferase-derived metabolites stimulate proliferation in uterine artery endothelial cells: role of estrogen receptor-alpha versus estrogen receptor-beta. Hypertension. 2010 Apr;55(4):1005-11. doi: 10.1161/HYPERTENSIONAHA.109.146399. Epub 2010 Mar 8. [PubMed:20212268]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Organic anion transmembrane transporter activity
Specific Function
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
Gene Name
ABCC3
Uniprot ID
O15438
Uniprot Name
Canalicular multispecific organic anion transporter 2
Molecular Weight
169341.14 Da
References
  1. Hirohashi T, Suzuki H, Sugiyama Y: Characterization of the transport properties of cloned rat multidrug resistance-associated protein 3 (MRP3). J Biol Chem. 1999 May 21;274(21):15181-5. [PubMed:10329726]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. Zelcer N, Reid G, Wielinga P, Kuil A, van der Heijden I, Schuetz JD, Borst P: Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7. [PubMed:12523936]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transporter activity
Specific Function
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
Molecular Weight
171589.5 Da
References
  1. Qian YM, Song WC, Cui H, Cole SP, Deeley RG: Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1. J Biol Chem. 2001 Mar 2;276(9):6404-11. Epub 2000 Dec 1. [PubMed:11102445]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [PubMed:10871297]
  2. Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. [PubMed:9539145]
  3. 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]
  4. 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]
  5. Kontaxi M, Echkardt U, Hagenbuch B, Stieger B, Meier PJ, Petzinger E: Uptake of the mycotoxin ochratoxin A in liver cells occurs via the cloned organic anion transporting polypeptide. J Pharmacol Exp Ther. 1996 Dec;279(3):1507-13. [PubMed:8968376]
  6. Pang KS, Wang PJ, Chung AY, Wolkoff AW: The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein. Hepatology. 1998 Nov;28(5):1341-6. [PubMed:9794920]
  7. Bossuyt X, Muller M, Meier PJ: Multispecific amphipathic substrate transport by an organic anion transporter of human liver. J Hepatol. 1996 Nov;25(5):733-8. [PubMed:8938553]
  8. Hagenbuch B, Adler ID, Schmid TE: Molecular cloning and functional characterization of the mouse organic-anion-transporting polypeptide 1 (Oatp1) and mapping of the gene to chromosome X. Biochem J. 2000 Jan 1;345 Pt 1:115-20. [PubMed:10600646]
  9. Lee TK, Koh AS, Cui Z, Pierce RH, Ballatori N: N-glycosylation controls functional activity of Oatp1, an organic anion transporter. Am J Physiol Gastrointest Liver Physiol. 2003 Aug;285(2):G371-81. Epub 2003 Apr 17. [PubMed:12702494]
  10. Kouzuki H, Suzuki H, Ito K, Ohashi R, Sugiyama Y: Contribution of organic anion transporting polypeptide to uptake of its possible substrates into rat hepatocytes. J Pharmacol Exp Ther. 1999 Feb;288(2):627-34. [PubMed:9918568]
  11. Eckhardt U, Schroeder A, Stieger B, Hochli M, Landmann L, Tynes R, Meier PJ, Hagenbuch B: Polyspecific substrate uptake by the hepatic organic anion transporter Oatp1 in stably transfected CHO cells. Am J Physiol. 1999 Apr;276(4 Pt 1):G1037-42. [PubMed:10198348]
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
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Not Available
Gene Name
SLC22A10
Uniprot ID
Q63ZE4
Uniprot Name
Solute carrier family 22 member 10
Molecular Weight
60256.57 Da
References
  1. Youngblood GL, Sweet DH: Identification and functional assessment of the novel murine organic anion transporter Oat5 (Slc22a19) expressed in kidney. Am J Physiol Renal Physiol. 2004 Aug;287(2):F236-44. Epub 2004 Apr 6. [PubMed:15068970]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. [PubMed:14762099]
  2. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. [PubMed:12679720]
  3. Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol. 2002 May;61(5):982-8. [PubMed:11961115]
  4. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [PubMed:11306713]
  5. Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [PubMed:12011098]
  6. Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. [PubMed:15100168]
  7. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. [PubMed:10224140]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Thyroid hormone transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-gluc...
Gene Name
SLCO1C1
Uniprot ID
Q9NYB5
Uniprot Name
Solute carrier organic anion transporter family member 1C1
Molecular Weight
78695.625 Da
References
  1. Tohyama K, Kusuhara H, Sugiyama Y: Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier. Endocrinology. 2004 Sep;145(9):4384-91. Epub 2004 May 27. [PubMed:15166123]
  2. Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238]
  2. Nozawa T, Tamai I, Sai Y, Nezu J, Tsuji A: Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin. J Pharm Pharmacol. 2003 Jul;55(7):1013-20. [PubMed:12906759]
  3. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001]
  4. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445]
  5. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862]
  6. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
  7. van Montfoort JE, Schmid TE, Adler ID, Meier PJ, Hagenbuch B: Functional characterization of the mouse organic-anion-transporting polypeptide 2. Biochim Biophys Acta. 2002 Aug 19;1564(1):183-8. [PubMed:12101011]
  8. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name
SLCO2B1
Uniprot ID
O94956
Uniprot Name
Solute carrier organic anion transporter family member 2B1
Molecular Weight
76709.98 Da
References
  1. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
  2. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238]
  3. Kobayashi D, Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther. 2003 Aug;306(2):703-8. Epub 2003 Apr 30. [PubMed:12724351]
  4. Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45. Epub 2003 Nov 10. [PubMed:14610227]
  5. Satoh H, Yamashita F, Tsujimoto M, Murakami H, Koyabu N, Ohtani H, Sawada Y: Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos. 2005 Apr;33(4):518-23. Epub 2005 Jan 7. [PubMed:15640378]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
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. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [PubMed:12011098]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Transporter activity
Specific Function
Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
Gene Name
SLC51A
Uniprot ID
Q86UW1
Uniprot Name
Organic solute transporter subunit alpha
Molecular Weight
37734.575 Da
References
  1. Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Transporter activity
Specific Function
Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
Gene Name
SLC51B
Uniprot ID
Q86UW2
Uniprot Name
Organic solute transporter subunit beta
Molecular Weight
14346.195 Da
References
  1. Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Spears KJ, Ross J, Stenhouse A, Ward CJ, Goh LB, Wolf CR, Morgan P, Ayrton A, Friedberg TH: Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochem Pharmacol. 2005 Feb 1;69(3):415-23. Epub 2004 Dec 22. [PubMed:15652233]
  2. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Thyroid hormone transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name
SLCO4A1
Uniprot ID
Q96BD0
Uniprot Name
Solute carrier organic anion transporter family member 4A1
Molecular Weight
77192.505 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Purine nucleotide transmembrane transporter activity
Specific Function
Participates in physiological processes involving bile acids, conjugated steroids and cyclic nucleotides. Enhances the cellular extrusion of cAMP and cGMP. Stimulates the ATP-dependent uptake of a ...
Gene Name
ABCC11
Uniprot ID
Q96J66
Uniprot Name
ATP-binding cassette sub-family C member 11
Molecular Weight
154299.625 Da
References
  1. Chen ZS, Guo Y, Belinsky MG, Kotova E, Kruh GD: Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). Mol Pharmacol. 2005 Feb;67(2):545-57. Epub 2004 Nov 10. [PubMed:15537867]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
  3. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445]
  4. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name
SLC22A11
Uniprot ID
Q9NSA0
Uniprot Name
Solute carrier family 22 member 11
Molecular Weight
59970.945 Da
References
  1. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [PubMed:10660625]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as estrone-3-sulfate (PubMed:10873595). Mediates transport of prostaglandins (PG) E1 and E2, thyroxine (T4), deltorphin II, BQ-123 an...
Gene Name
SLCO3A1
Uniprot ID
Q9UIG8
Uniprot Name
Solute carrier organic anion transporter family member 3A1
Molecular Weight
76552.135 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]
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. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
  2. Suzuki M, Suzuki H, Sugimoto Y, Sugiyama Y: ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9. Epub 2003 Apr 7. [PubMed:12682043]
  3. Imai Y, Asada S, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Breast cancer resistance protein exports sulfated estrogens but not free estrogens. Mol Pharmacol. 2003 Sep;64(3):610-8. [PubMed:12920197]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34