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Identification
NameProgesterone
Accession NumberDB00396  (APRD00700)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

The major progestational steroid that is secreted primarily by the corpus luteum and the placenta. Progesterone acts on the uterus, the mammary glands, and the brain. It is required in embryo implantation, pregnancy maintenance, and the development of mammary tissue for milk production. Progesterone, converted from pregnenolone, also serves as an intermediate in the biosynthesis of gonadal steroid hormones and adrenal corticosteroids. [PubChem]

Structure
Thumb
Synonyms
(S)-4-Pregnene-3,20-dione
(S)-Pregn-4-en-3,20-dione
(S)-Progesterone
17alpha-Progesterone
17α-progesterone
4-Pregnene-3,20-dione
Agolutin
Akrolutin
Corpus Luteum Hormone
Crinone
delta(4)-Pregnene-3,20-dione
Gelbkoerperhormon
Luteohormone
Lutogynon
Pregn-4-ene-3,20-dione
Progesteron
Progesterona
Progestérone
Progesterone
Progesteronum
External Identifiers
  • BP 14
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Progesterone Injectionsolution50 mgintramuscularActavis Pharma Company2016-04-13Not applicableCanada
Crinonegel45 mg/1.125gvaginalColumbia Laboratories, Inc.1997-05-13Not applicableUs
Crinonegel90 mg/1.125gvaginalActavis Pharma, Inc.1997-05-13Not applicableUs
Crinonegel90 mg/1.125gvaginalColumbia Laboratories, Inc.1997-05-13Not applicableUs
Crinonegel45 mg/1.125gvaginalActavis Pharma, Inc.1997-05-13Not applicableUs
Crinonegel90 mg/1.125gvaginalActavis Pharma, Inc.1997-05-13Not applicableUs
Crinonegel8 %vaginalEmd Serono A Division Of Emd Inc Canada2000-05-20Not applicableCanada
Crinonegel90 mg/1.125gvaginalColumbia Laboratories, Inc.1997-05-13Not applicableUs
Crinonegel45 mg/1.125gvaginalActavis Pharma, Inc.1997-05-13Not applicableUs
Endometrinvaginal tablet, effervescent100 mgvaginalFerring Inc2009-11-30Not applicableCanada
Endometrininsert100 mg/1vaginalFerring Pharmaceuticals Inc.2007-06-21Not applicableUs
Gesterol In Oil-liq Im 50mg/mlliquid50 mgintramuscularGermiphene Corporation1995-12-311999-04-14Canada
PMS-progesterone Inj 50mg/ml USPliquid50 mgintramuscularPharmascience Inc1989-12-312004-01-21Canada
Prochievegel90 mg/1.125gvaginalColumbia Laboratories1997-05-13Not applicableUs
Prochievegel45 mg/1.125gvaginalColumbia Laboratories1997-05-13Not applicableUs
Progesteronecapsule200 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-30Not applicableUs
Progesteronecapsule200 mg/1oralWatson Laboratories, Inc.2010-07-30Not applicableUs
Progesteronecapsule100 mg/1oralWatson Laboratories, Inc.2010-07-30Not applicableUs
Progesteroneinjection, solution50 mg/mLintramuscularActavis Pharma, Inc.1978-05-11Not applicableUs
Progesterone Inj 50mg/ml USPliquid50 mgintramuscularCytex Pharmaceuticals Inc1992-12-31Not applicableCanada
Prometriumcapsule100 mg/1oralAbb Vie Inc.2010-07-30Not applicableUs
Prometriumcapsule100 mg/1oralAvera Mc Kennan Hospital2015-08-11Not applicableUs
Prometriumcapsule100 mg/1oralPhysicians Total Care, Inc.2003-03-14Not applicableUs
Prometriumcapsule100 mg/1oralbryant ranch prepack2010-07-30Not applicableUs
Prometriumcapsule200 mg/1oralPhysicians Total Care, Inc.2004-11-03Not applicableUs
Prometriumcapsule200 mg/1oralbryant ranch prepack2010-07-30Not applicableUs
Prometriumcapsule200 mg/1oralAbb Vie Inc.2010-07-30Not applicableUs
Prometriumcapsule100 mgoralMerck Canada Inc1995-12-31Not applicableCanada
Teva-progesteronecapsule100 mgoralTeva Canada Limited2015-04-16Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Progesteroneinjection, solution50 mg/mLintramuscularFresenius Kabi USA, LLC2001-07-19Not applicableUs
Progesteronecapsule100 mg/1oralTeva Pharmaceuticals USA Inc2012-03-01Not applicableUs
Progesteronecapsule200 mg/1oralBanner Life Sciences Llc.2015-10-01Not applicableUs
Progesteronecapsule100 mg/1oralAkorn, Inc.2012-10-04Not applicableUs
Progesteronecapsule200 mg/1oralGolden State Medical Supply, Inc.2014-04-23Not applicableUs
Progesteronecapsule200 mg/1oralBanner Pharmacaps2014-01-01Not applicableUs
Progesteronecapsule100 mg/1oralGolden State Medical Supply, Inc.2014-04-23Not applicableUs
Progesteronecapsule100 mg/1oralBanner Pharmacaps2014-01-01Not applicableUs
Progesteronecapsule200 mg/1oralAv Kare, Inc.2014-09-29Not applicableUs
Progesteroneinjection, solution50 mg/mLintramuscularAmerican Regent, Inc.2010-09-29Not applicableUs
Progesteronecapsule100 mg/1oralAv Kare, Inc.2014-09-29Not applicableUs
Progesteroneinjection50 mg/1intramuscularWest ward Pharmaceutical Corp2010-10-28Not applicableUs
Progesteronecapsule200 mg/1oralAv Kare, Inc.2013-06-042015-12-29Us
Progesteronecapsule100 mg/1oralBanner Life Sciences Llc.2015-10-01Not applicableUs
Progesteronecapsule200 mg/1oralTeva Pharmaceuticals USA Inc2012-03-01Not applicableUs
Progesteronecapsule100 mg/1oralAv Kare, Inc.2013-06-042015-12-29Us
Progesteronecapsule200 mg/1oralAkorn, Inc.2012-10-04Not applicableUs
Progesterone Injection USPinjection, solution50 mg/mLintramuscularPharma Force, Inc.2009-09-04Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AgolutinBiotika
CyclogestActavis
GesterolNot Available
GestoneNordic Pharma
ProgestasertNot Available
ProgestogelBesins
Qi NingAisheng Pharmaceutical
RelantanAversi
SustenSun Pharma
UtrogestanBesins
UtrogestranFaran Laboratories
UtrovinBestochem
VasclorVerisfield
Brand mixtures
NameLabellerIngredients
Estrogel PropakMerck Canada Inc
SaltsNot Available
Categories
UNII4G7DS2Q64Y
CAS number57-83-0
WeightAverage: 314.4617
Monoisotopic: 314.224580204
Chemical FormulaC21H30O2
InChI KeyInChIKey=RJKFOVLPORLFTN-LEKSSAKUSA-N
InChI
InChI=1S/C21H30O2/c1-13(22)17-6-7-18-16-5-4-14-12-15(23)8-10-20(14,2)19(16)9-11-21(17,18)3/h12,16-19H,4-11H2,1-3H3/t16-,17+,18-,19-,20-,21+/m0/s1
IUPAC Name
(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-5-one
SMILES
[H][C@@]12CC[[email protected]](C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassPregnane steroids
Direct ParentGluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
Substituents
  • Progestogin-skeleton
  • 20-oxosteroid
  • Oxosteroid
  • 3-oxosteroid
  • 3-oxo-delta-4-steroid
  • Delta-4-steroid
  • Cyclic ketone
  • Ketone
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) treatment for infertile women with progesterone deficiency and for the treatment of secondary amenorrhea. Also used for the reduction of the incidence of endometrial hyperplasia and the attendant risk of endometrial carcinoma in postmenopausal women receiving estrogen replacement therapy, as well as treatment of abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology such as fibroids or uterine cancer.
PharmacodynamicsProgesterone is a naturally occuring progestin or a synthetic form of the naturally occurring female sex hormone, progesterone. In a woman's normal menstrual cycle, an egg matures and is released from the ovaries (ovulation). The ovary then produces progesterone, preventing the release of further eggs and priming the lining of the womb for a possible pregnancy. If pregnancy occurs, progesterone levels in the body remain high, maintaining the womb lining. If pregnancy does not occur, progesterone levels in the body fall, resulting in a menstrual period. Progesterone tricks the body processes into thinking that ovulation has already occurred by maintaining high levels of the synthetic progesterone. This prevents the release of eggs from the ovaries.
Mechanism of actionProgesterone shares the pharmacological actions of the progestins. Progesterone binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Progesterone will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. In women who have adequate endogenous estrogen, progesterone transforms a proliferative endometrium into a secretory one. Progesterone is essential for the development of decidual tissue and is necessary to increase endometrial receptivity for implantation of an embryo. Once an embryo has been implanted, progesterone acts to maintain the pregnancy. Progesterone also stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has little estrogenic and androgenic activity.
Related Articles
AbsorptionProgesterone absorption is prolonged with an absorption half-life of approximately 25-50 hours.
Volume of distributionNot Available
Protein binding96%-99%
Metabolism

Progesterone is metabolized primarily by the liver largely to pregnanediols and pregnanolones.

SubstrateEnzymesProduct
Progesterone
6β-HydroxyprogesteroneDetails
Progesterone
2β-HydroxyprogesteroneDetails
Progesterone
21-HydroxyprogesteroneDetails
Progesterone
17β-HydroxyprogesteroneDetails
17β-Hydroxyprogesterone
17β,21-HydroxyprogesteroneDetails
Progesterone
16β-HydroxyprogesteroneDetails
Progesterone
16β-HydroxyprogesteroneDetails
Progesterone
Not Available
15β-HydroxyprogesteroneDetails
Progesterone
Not Available
7β-HydroxyprogesteroneDetails
Route of eliminationThe glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces. Progesterone metabolites are excreted mainly by the kidneys.
Half life34.8-55.13 hours
Clearance
  • 2510 +/- 135 L/day [cycling women]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
17-alpha-hydroxylase deficiency (CYP17)DiseaseSMP00566
Corticosterone methyl oxidase I deficiency (CMO I)DiseaseSMP00577
SteroidogenesisMetabolicSMP00130
Adrenal Hyperplasia Type 3 or Congenital Adrenal Hyperplasia due to 21-hydroxylase DeficiencyDiseaseSMP00373
Congenital Lipoid Adrenal Hyperplasia (CLAH) or Lipoid CAHDiseaseSMP00371
Adrenal Hyperplasia Type 5 or Congenital Adrenal Hyperplasia due to 17 Alpha-hydroxylase DeficiencyDiseaseSMP00372
11-beta-hydroxylase deficiency (CYP11B1)DiseaseSMP00575
Corticosterone methyl oxidase II deficiency - CMO IIDiseaseSMP00578
21-hydroxylase deficiency (CYP21)DiseaseSMP00576
Apparent mineralocorticoid excess syndromeDiseaseSMP00717
3-Beta-Hydroxysteroid Dehydrogenase DeficiencyDiseaseSMP00718
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.982
Caco-2 permeable+0.7724
P-glycoprotein substrateSubstrate0.5449
P-glycoprotein inhibitor IInhibitor0.8841
P-glycoprotein inhibitor IIInhibitor0.6043
Renal organic cation transporterNon-inhibitor0.6931
CYP450 2C9 substrateNon-substrate0.847
CYP450 2D6 substrateNon-substrate0.8795
CYP450 3A4 substrateSubstrate0.7408
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9533
CYP450 2C19 inhibitorNon-inhibitor0.6514
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8203
Ames testNon AMES toxic0.9626
CarcinogenicityNon-carcinogens0.9151
BiodegradationNot ready biodegradable0.9575
Rat acute toxicity1.8041 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7451
hERG inhibition (predictor II)Non-inhibitor0.7454
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bristol myers squibb
  • Amarin pharmaceuticals inc
  • Solvay pharmaceuticals
  • Esi pharmacal
  • Unimed pharmaceuticals llc
  • Watson laboratories inc
  • App pharmaceuticals llc
  • Eli lilly and co
  • Pharmaforce inc
  • Alza corp
  • Ferring pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Solutionintramuscular50 mg
Gelvaginal45 mg/1.125g
Gelvaginal8 %
Gelvaginal90 mg/1.125g
Insertvaginal100 mg/1
Vaginal tablet, effervescentvaginal100 mg
Metered-dose pump; capsuleoral; transdermal
Injectionintramuscular50 mg/1
Injection, solutionintramuscular50 mg/mL
Liquidintramuscular50 mg
Capsuleoral100 mg/1
Capsuleoral100 mg
Capsuleoral200 mg/1
Prices
Unit descriptionCostUnit
Prochieve 4% Gel (18 Applicators Per Box)160.18USD tube
Crinone 8% Gel (1 Box = 6 Applications)84.26USD box
Prochieve 8% Gel 1.45 gm Tube14.83USD tube
Crinone 8% gel13.61USD g
Prochieve 8% gel12.0USD g
Prochieve 4% gel8.56USD g
Progesterone 50 mg/ml6.6USD ml
Progesterone oil 50 mg/ml vial3.88USD ml
Prometrium 200 mg capsule3.84USD capsule
First-progesterone vgs 400 susuppositoryp3.33USD each
First-progesterone vgs 200 suppository3.15USD each
First-progesterone vgs 100 suppository3.0USD each
First-progesterone vgs 50 suppository2.93USD each
First-progesterone vgs 25 suppository2.88USD each
Prometrium 100 mg capsule1.69USD capsule
Progesterone powder micronized0.74USD g
Progesterone powder milled0.73USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5543150 No1993-09-152013-09-15Us
US7300664 No1999-11-172019-11-17Us
US7320800 No1999-11-172019-11-17Us
US7393543 No1999-11-172019-11-17Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point121 °CPhysProp
water solubility8.81 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP3.87HANSCH,C ET AL. (1995)
logS-4.43ADME Research, USCD
Caco2 permeability-4.37ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00546 mg/mLALOGPS
logP3.58ALOGPS
logP4.15ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)18.92ChemAxon
pKa (Strongest Basic)-4.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area34.14 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity92.71 m3·mol-1ChemAxon
Polarizability37.15 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (11.5 KB)
Spectra
Spectrum TypeDescriptionSplash Key
GC-MSGC-MS Spectrum - GC-MSsplash10-0fbc-5910000000-422e38df6de7e8b0a4b7View in MoNA
GC-MSGC-MS Spectrum - GC-MSsplash10-0fbc-5910000000-385f45345742235da8e0View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)splash10-014i-1009000000-0f8b7c3e6c2265c3889fView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)splash10-052b-8900000000-0b0167121b798e7e7534View in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)splash10-052b-9400000000-881510cbcecd9cb61f4fView in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (JEOL JMS-01-SG-2) , Positivesplash10-024l-6923000000-639c7405f69825de7f90View in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (HITACHI M-52) , Positivesplash10-0229-2941000000-1e075d8489b79cf4e34aView in MoNA
MSMass Spectrum (Electron Ionization)splash10-006x-7931000000-f6ad83adccd7e016fa29View in MoNA
1D NMR1H NMR SpectrumNot Available
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Nejib M. Nasraoui, Alain Piasco, “Derivatives of 19-nor progesterone; process for producing them and the pharmaceutical compositions incorporating them.” U.S. Patent US5223492, issued May, 1971.

US5223492
General References
  1. Allen WM: THE ISOLATION OF CRYSTALLINE PROGESTIN. Science. 1935 Aug 2;82(2118):89-93. [PubMed:17747122 ]
  2. Allen WM: Progesterone: how did the name originate? South Med J. 1970 Oct;63(10):1151-5. [PubMed:4922128 ]
  3. Schumacher M, Guennoun R, Robert F, Carelli C, Gago N, Ghoumari A, Gonzalez Deniselle MC, Gonzalez SL, Ibanez C, Labombarda F, Coirini H, Baulieu EE, De Nicola AF: Local synthesis and dual actions of progesterone in the nervous system: neuroprotection and myelination. Growth Horm IGF Res. 2004 Jun;14 Suppl A:S18-33. [PubMed:15135772 ]
  4. Hould FS, Fried GM, Fazekas AG, Tremblay S, Mersereau WA: Progesterone receptors regulate gallbladder motility. J Surg Res. 1988 Dec;45(6):505-12. [PubMed:3184927 ]
External Links
ATC CodesG03DA04G03FA04
AHFS Codes
  • 68:32.00
PDB EntriesNot Available
FDA labelDownload (86.6 KB)
MSDSDownload (74.2 KB)
Interactions
Drug Interactions
Drug
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Progesterone.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Progesterone.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Progesterone.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Progesterone.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Progesterone.
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Progesterone.
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Progesterone.
BexaroteneThe serum concentration of Progesterone can be decreased when it is combined with Bexarotene.
BivalirudinThe therapeutic efficacy of Bivalirudin can be decreased when used in combination with Progesterone.
BosentanThe serum concentration of Progesterone can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Progesterone.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Progesterone.
ButoconazoleThe therapeutic efficacy of Progesterone can be decreased when used in combination with Butoconazole.
C1 Esterase Inhibitor (Human)Progesterone may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Progesterone.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Progesterone.
Citric AcidThe therapeutic efficacy of Citric Acid can be decreased when used in combination with Progesterone.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Progesterone.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Progesterone.
DabrafenibThe serum concentration of Progesterone can be decreased when it is combined with Dabrafenib.
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Progesterone.
DanaparoidThe therapeutic efficacy of Danaparoid can be decreased when used in combination with Progesterone.
DeferasiroxThe serum concentration of Progesterone can be decreased when it is combined with Deferasirox.
DesirudinThe therapeutic efficacy of Desirudin can be decreased when used in combination with Progesterone.
DicoumarolThe therapeutic efficacy of Dicoumarol can be decreased when used in combination with Progesterone.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Progesterone.
Edetic AcidThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Progesterone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Progesterone.
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Progesterone.
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Progesterone.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Progesterone.
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Progesterone.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Progesterone.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Progesterone.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Progesterone.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Progesterone.
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Progesterone.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Progesterone.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Progesterone.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Progesterone.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Progesterone.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Progesterone.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Progesterone.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Progesterone.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Progesterone.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Progesterone.
MitotaneThe serum concentration of Progesterone can be decreased when it is combined with Mitotane.
NadroparinThe therapeutic efficacy of Nadroparin can be decreased when used in combination with Progesterone.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Progesterone.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Progesterone.
PhenindioneThe therapeutic efficacy of Phenindione can be decreased when used in combination with Progesterone.
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Progesterone.
PhenytoinThe metabolism of Progesterone can be increased when combined with Phenytoin.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Progesterone.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Progesterone.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Progesterone.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Progesterone.
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Progesterone.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Progesterone.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Progesterone.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Progesterone.
SiltuximabThe serum concentration of Progesterone can be decreased when it is combined with Siltuximab.
St. John's WortThe serum concentration of Progesterone can be decreased when it is combined with St. John's Wort.
SulfanilamideThe therapeutic efficacy of Progesterone can be decreased when used in combination with Sulfanilamide.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Progesterone.
TerconazoleThe therapeutic efficacy of Progesterone can be decreased when used in combination with Terconazole.
TinzaparinThe therapeutic efficacy of Tinzaparin can be decreased when used in combination with Progesterone.
TioconazoleThe therapeutic efficacy of Progesterone can be decreased when used in combination with Tioconazole.
TocilizumabThe serum concentration of Progesterone can be decreased when it is combined with Tocilizumab.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Progesterone.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Progesterone.
TreprostinilThe therapeutic efficacy of Treprostinil can be decreased when used in combination with Progesterone.
UlipristalThe therapeutic efficacy of Progesterone can be decreased when used in combination with Ulipristal.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Progesterone.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Progesterone.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Progesterone.
WarfarinThe therapeutic efficacy of Warfarin can be decreased when used in combination with Progesterone.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Increase dietary intake of magnesium, folate, vitamin B6, B12, and/or consider taking a multivitamin.
  • Take at the same time everyday.
  • Take with food.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.Isoform A: inactive in stimulating c-Src/MAPK signaling on hormone stimulation.Isoform 4: Increases mitochondrial ...
Gene Name:
PGR
Uniprot ID:
P06401
Molecular Weight:
98979.96 Da
References
  1. Madauss KP, Stewart EL, Williams SP: The evolution of progesterone receptor ligands. Med Res Rev. 2007 May;27(3):374-400. [PubMed:17013809 ]
  2. Gizard F, Robillard R, Gross B, Barbier O, Revillion F, Peyrat JP, Torpier G, Hum DW, Staels B: TReP-132 is a novel progesterone receptor coactivator required for the inhibition of breast cancer cell growth and enhancement of differentiation by progesterone. Mol Cell Biol. 2006 Oct;26(20):7632-44. [PubMed:17015480 ]
  3. Wu HB, Fabian S, Jenab S, Quinones-Jenab V: Progesterone receptors activation after acute cocaine administration. Brain Res. 2006 Dec 18;1126(1):188-92. Epub 2006 Nov 15. [PubMed:17109827 ]
  4. Boonyaratanakornkit V, McGowan E, Sherman L, Mancini MA, Cheskis BJ, Edwards DP: The role of extranuclear signaling actions of progesterone receptor in mediating progesterone regulation of gene expression and the cell cycle. Mol Endocrinol. 2007 Feb;21(2):359-75. Epub 2006 Nov 30. [PubMed:17138644 ]
  5. Tranguch S, Smith DF, Dey SK: Progesterone receptor requires a co-chaperone for signalling in uterine biology and implantation. Reprod Biomed Online. 2006 Nov;13(5):651-60. [PubMed:17169175 ]
  6. Luconi M, Bonaccorsi L, Maggi M, Pecchioli P, Krausz C, Forti G, Baldi E: Identification and characterization of functional nongenomic progesterone receptors on human sperm membrane. J Clin Endocrinol Metab. 1998 Mar;83(3):877-85. [PubMed:9506743 ]
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 tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Molecular Weight:
66215.45 Da
References
  1. Kumar AS, Cureton E, Shim V, Sakata T, Moore DH, Benz CC, Esserman LJ, Hwang ES: Type and duration of exogenous hormone use affects breast cancer histology. Ann Surg Oncol. 2007 Feb;14(2):695-703. Epub 2006 Nov 14. [PubMed:17103262 ]
  2. Lessey BA, Palomino WA, Apparao KB, Young SL, Lininger RA: Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women. Reprod Biol Endocrinol. 2006;4 Suppl 1:S9. [PubMed:17118173 ]
  3. Yuri T, Tsukamoto R, Uehara N, Matsuoka Y, Tsubura A: Effects of different durations of estrogen and progesterone treatment on development of N-methyl-N-nitrosourea-induced mammary carcinomas in female Lewis rats. In Vivo. 2006 Nov-Dec;20(6B):829-36. [PubMed:17203775 ]
  4. Montero Girard G, Vanzulli SI, Cerliani JP, Bottino MC, Bolado J, Vela J, Becu-Villalobos D, Benavides F, Gutkind S, Patel V, Molinolo A, Lanari C: Association of estrogen receptor-alpha and progesterone receptor A expression with hormonal mammary carcinogenesis: role of the host microenvironment. Breast Cancer Res. 2007;9(2):R22. [PubMed:17341305 ]
  5. Ghebeh H, Tulbah A, Mohammed S, Elkum N, Bin Amer SM, Al-Tweigeri T, Dermime S: Expression of B7-H1 in breast cancer patients is strongly associated with high proliferative Ki-67-expressing tumor cells. Int J Cancer. 2007 Aug 15;121(4):751-8. [PubMed:17415709 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels.
Gene Name:
NR3C2
Uniprot ID:
P08235
Molecular Weight:
107066.575 Da
References
  1. Rupprecht R, Reul JM, van Steensel B, Spengler D, Soder M, Berning B, Holsboer F, Damm K: Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands. Eur J Pharmacol. 1993 Oct 15;247(2):145-54. [PubMed:8282004 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 17-alpha-monooxygenase activity
Specific Function:
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty.
Gene Name:
CYP17A1
Uniprot ID:
P05093
Molecular Weight:
57369.995 Da
References
  1. Haidar S, Hartmann RW: C16 and C17 substituted derivatives of pregnenolone and progesterone as inhibitors of 17alpha-hydroxylase-C17, 20-lyase: synthesis and biological evaluation. Arch Pharm (Weinheim). 2002;335(11-12):526-34. [PubMed:12596217 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
activator
General Function:
Opioid receptor activity
Specific Function:
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
Molecular Weight:
42644.665 Da
References
  1. Dawson-Basoa ME, Gintzler AR: Estrogen and progesterone activate spinal kappa-opiate receptor analgesic mechanisms. Pain. 1996 Jan;64(1):169-77. [PubMed:8867260 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. 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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid 17-alpha-monooxygenase activity
Specific Function:
Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty.
Gene Name:
CYP17A1
Uniprot ID:
P05093
Molecular Weight:
57369.995 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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
Molecular Weight:
141477.255 Da
References
  1. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. [PubMed:12387747 ]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514 ]
  3. Leonessa F, Kim JH, Ghiorghis A, Kulawiec RJ, Hammer C, Talebian A, Clarke R: C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump. J Med Chem. 2002 Jan 17;45(2):390-8. [PubMed:11784143 ]
  4. Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, Komano T, Hori R: Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone. J Biol Chem. 1992 Dec 5;267(34):24248-52. [PubMed:1360010 ]
  5. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
  6. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M, Lin JH: In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther. 2001 Mar;296(3):723-35. [PubMed:11181899 ]
  7. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
  8. Borgnia MJ, Eytan GD, Assaraf YG: Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J Biol Chem. 1996 Feb 9;271(6):3163-71. [PubMed:8621716 ]
  9. Kim WY, Benet LZ: P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93. [PubMed:15290871 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Molecular Weight:
146405.83 Da
References
  1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759 ]
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, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: Reversal of MRP-mediated multidrug resistance in human lung cancer cells by the antiprogestatin drug RU486. Biochem Biophys Res Commun. 1999 May 19;258(3):513-8. [PubMed:10329417 ]
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 presence of sodium.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
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 ]
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Drug created on June 13, 2005 07:24 / Updated on July 24, 2016 01:51