Identification
NameUlipristal
Accession NumberDB08867  (DB05366)
TypeSmall Molecule
GroupsApproved
Description

Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception (Ella) and for the treatment of uterine fibroids (Fibristal). It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor, however compared to mifepristone (a progesterone receptor antagonist), ulipristal is more tolerable and has lower glucocorticoid activity and better binding affinity.

Ulipristal is currently recommended as first line therapy for emergency contraception, due to improved efficacy and similar side effect profile as compared to the traditional use of levonorgestrel or the Yuzpe regimen. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. A recent systematic review proclaimed that the majority of available evidence demonstrates an inhibitory effect on ovulation rather than a post-fertilization effect on the endometrium, which has been heavily debated due to ethical concerns related to abortion (Rosato et al, 2016).

Structure
Thumb
SynonymsNot Available
External IDs CDB 2914 / CDB-2914 / CDB2914
Product Ingredients
IngredientUNIICASInChI KeyDetails
Ulipristal AcetateYF7V70N02B 126784-99-4OOLLAFOLCSJHRE-ZHAKMVSLSA-NDetails
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EllaTablet30 mgOralLaboratoire HRA Pharma2015-09-01Not applicableCanada
EllaTablet30 mg/1OralAfaxys Inc.2010-08-13Not applicableUs
EllaTablet30 mg/1OralA S Medication Solutions2010-08-132017-06-20Us
EllaoneTablet30 mgOralLaboratoire HRA Pharma2009-05-15Not applicableEu
EsmyaTablet5 mgOralGedeon Richter Ltd.2012-02-23Not applicableEu
EsmyaTablet5 mgOralGedeon Richter Ltd.2012-02-23Not applicableEu
EsmyaTablet5 mgOralGedeon Richter Ltd.2012-02-23Not applicableEu
EsmyaTablet5 mgOralGedeon Richter Ltd.2012-02-23Not applicableEu
EsmyaTablet5 mgOralGedeon Richter Ltd.2012-02-23Not applicableEu
FibristalTablet5 mgOralAllergan Pharma Co.2013-07-04Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EllaOneHRA Pharma
Esmya Preglen UK
Brand mixturesNot Available
Categories
UNII6J5J15Q2X8
CAS number159811-51-5
WeightAverage: 433.592
Monoisotopic: 433.261693991
Chemical FormulaC28H35NO3
InChI KeyHKDLNTKNLJPAIY-WKWWZUSTSA-N
InChI
InChI=1S/C28H35NO3/c1-17(30)28(32)14-13-25-23-11-7-19-15-21(31)10-12-22(19)26(23)24(16-27(25,28)2)18-5-8-20(9-6-18)29(3)4/h5-6,8-9,15,23-25,32H,7,10-14,16H2,1-4H3/t23-,24+,25-,27-,28-/m0/s1
IUPAC Name
(10S,11S,14R,15S,17R)-14-acetyl-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one
SMILES
CN(C)C1=CC=C(C=C1)[[email protected]]1C[[email protected]@]2(C)[[email protected]@H](CC[[email protected]]2(O)C(C)=O)[[email protected]@H]2CCC3=CC(=O)CCC3=C12
Pharmacology
Indication

As the product Ella (available in Canada and the US), ulipristal is indicated for use as emergency contraception after unprotected intercourse or possible contraceptive failure when administered within 120 hours (5 days) after unprotected intercourse or a known or suspected contraceptive failure. As the product Fibristal (available in Canada), ulipristal is indicated for treatment of the signs and symptoms of uterine fibroids in adult women.

Structured Indications
Pharmacodynamics

Ulipristal is a selective, reversible progestin receptor modulator and its tissue targets include the uterus, cervix, ovaries, and hypothalamus. Ulipristal may act as an agonist or antagonist in the presence or absence of progesterone based on the tissue target. If given mid-follicular phase, development of the follicle growth is delayed and estradiol concentrations decrease. If given at the time when luteinizing hormone peaks, follicular rapture is delayed by several days. If given early-luteal phase, a decrease in endometrial thickness can be observed.

Mechanism of action

The exact mechanism of action has been heavily debated, although recent evidence suggests that ulipristal functions primarily through inhibition of ovulation, via prevention of progestin binding to the progesterone receptor. In the treatment of fibroids, ulipristal exerts a direct action on fibroids reducing their size through inhibition of cell proliferation and induction of apoptosis.

TargetKindPharmacological actionActionsOrganismUniProt ID
Progesterone receptorProteinyes
modulator
HumanP06401 details
Glucocorticoid receptorProteinyes
antagonist
HumanP04150 details
Androgen receptorProteinunknownNot AvailableHumanP10275 details
Related Articles
Absorption

Tmax, healthy subjects, single oral dose = 60-90 minutes; Cmax, healthy subjects, single oral dose = 176 ± 89 ng/mL; AUC(0-∞), healthy subjects, single oral dose = 556 ± 260 ng·h/mL;

Volume of distributionNot Available
Protein binding

>94% bound to plasma proteins such as albumin, alpha1-acid glycoprotein, lipoproteins (VLDL, LDL, and HDL- due to its lipophillic nature)

Metabolism

Ulipristal is metabolized by CYP3A4 and to a lesser extent by CYP1A2 into mono-demethylated (active) and di-methylated (inactive) metabolites.

Route of eliminationNot Available
Half life

Mean elimination half-life, single oral dose, healthy subject = 32.4 ± 6.3 hours

Clearance

Mean oral clearance, single oral dose, healthy subject (CL/F) = 76.8 ± 64.0L/h

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Ulipristal can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Ulipristal can be increased when it is combined with Acetaminophen.Approved
AfatinibThe serum concentration of Ulipristal can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Ulipristal can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Ulipristal can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Ulipristal can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Ulipristal can be increased when it is combined with Alfentanil.Approved, Illicit
AllylestrenolThe therapeutic efficacy of Allylestrenol can be decreased when used in combination with Ulipristal.Approved
AltrenogestThe therapeutic efficacy of Altrenogest can be decreased when used in combination with Ulipristal.Vet Approved
AmantadineThe serum concentration of Ulipristal can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Ulipristal can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Ulipristal can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Ulipristal can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Ulipristal can be increased when it is combined with Amlodipine.Approved
AmobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Amobarbital.Approved, Illicit
AmprenavirThe serum concentration of Ulipristal can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Ulipristal can be increased when it is combined with Amsacrine.Approved
AprepitantThe serum concentration of Ulipristal can be increased when it is combined with Aprepitant.Approved, Investigational
AstemizoleThe serum concentration of Ulipristal can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Ulipristal can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Ulipristal can be increased when it is combined with Atenolol.Approved
AtomoxetineThe serum concentration of Ulipristal can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Ulipristal can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Ulipristal can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Ulipristal can be increased when it is combined with Azithromycin.Approved
BarbexacloneThe serum concentration of Ulipristal can be decreased when it is combined with Barbexaclone.Experimental
BarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Barbital.Illicit
BenzocaineThe serum concentration of Ulipristal can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Ulipristal can be increased when it is combined with Bepridil.Approved, Withdrawn
BexaroteneThe serum concentration of Ulipristal can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Ulipristal can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Ulipristal can be increased when it is combined with Boceprevir.Withdrawn
BortezomibThe serum concentration of Ulipristal can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Ulipristal can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Ulipristal can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Ulipristal can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Ulipristal can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Ulipristal can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Ulipristal can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Ulipristal can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Ulipristal can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Ulipristal can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Ulipristal can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Ulipristal can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Ulipristal can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Ulipristal can be increased when it is combined with Caspofungin.Approved
CeritinibThe serum concentration of Ulipristal can be increased when it is combined with Ceritinib.Approved
ChloroquineThe serum concentration of Ulipristal can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Ulipristal can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Ulipristal can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Ulipristal can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Ulipristal can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Ulipristal can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Ulipristal can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Ulipristal can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Ulipristal can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Ulipristal can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Ulipristal can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Ulipristal can be increased when it is combined with Clemastine.Approved
ClofazimineThe serum concentration of Ulipristal can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Ulipristal can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of Ulipristal can be increased when it is combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Ulipristal can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Ulipristal can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Ulipristal can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Ulipristal can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe serum concentration of Ulipristal can be increased when it is combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Ulipristal can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Ulipristal can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Ulipristal can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Ulipristal can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Ulipristal can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Ulipristal can be increased when it is combined with Dactinomycin.Approved
DarunavirThe serum concentration of Ulipristal can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Ulipristal can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Ulipristal can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Ulipristal can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe serum concentration of Ulipristal can be increased when it is combined with Delavirdine.Approved
DesipramineThe serum concentration of Ulipristal can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Ulipristal can be increased when it is combined with Desloratadine.Approved, Investigational
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Ulipristal.Approved
DexamethasoneThe serum concentration of Ulipristal can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Ulipristal can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Ulipristal can be increased when it is combined with Diclofenac.Approved, Vet Approved
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Ulipristal.Approved
DigoxinThe serum concentration of Ulipristal can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe serum concentration of Ulipristal can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Ulipristal can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Ulipristal can be increased when it is combined with Dipyridamole.Approved
DoxazosinThe serum concentration of Ulipristal can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Ulipristal can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Ulipristal can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe serum concentration of Ulipristal can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Ulipristal can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Ulipristal can be increased when it is combined with Dronedarone.Approved
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Ulipristal.Approved
DydrogesteroneThe therapeutic efficacy of Dydrogesterone can be decreased when used in combination with Ulipristal.Approved, Withdrawn
EfavirenzThe serum concentration of Ulipristal can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Ulipristal can be increased when it is combined with Elbasvir.Approved
EnalaprilThe serum concentration of Ulipristal can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Ulipristal can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Ulipristal can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Ulipristal can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Ulipristal can be increased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Ulipristal can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Ulipristal can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Ulipristal can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Ulipristal can be decreased when it is combined with Estrone.Approved
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol diacetate can be decreased when used in combination with Ulipristal.Approved
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Ulipristal.Approved, Investigational
EtoposideThe serum concentration of Ulipristal can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Ulipristal can be decreased when it is combined with Etravirine.Approved
FelbamateThe serum concentration of Ulipristal can be decreased when it is combined with Felbamate.Approved
FelodipineThe serum concentration of Ulipristal can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Ulipristal can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Ulipristal can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Ulipristal can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe serum concentration of Ulipristal can be increased when it is combined with Fluconazole.Approved
FluoxetineThe serum concentration of Ulipristal can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Ulipristal can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Ulipristal can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Ulipristal can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe serum concentration of Ulipristal can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Ulipristal can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Ulipristal can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Ulipristal can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Ulipristal can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Ulipristal can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Ulipristal can be increased when it is combined with Genistein.Investigational
GestodeneThe therapeutic efficacy of Gestodene can be decreased when used in combination with Ulipristal.Approved
GestrinoneThe therapeutic efficacy of Gestrinone can be decreased when used in combination with Ulipristal.Approved
GlyburideThe serum concentration of Ulipristal can be increased when it is combined with Glyburide.Approved
Gramicidin DThe serum concentration of Ulipristal can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Ulipristal can be increased when it is combined with Grepafloxacin.Withdrawn
GriseofulvinThe serum concentration of Ulipristal can be decreased when it is combined with Griseofulvin.Approved, Vet Approved
HaloperidolThe serum concentration of Ulipristal can be increased when it is combined with Haloperidol.Approved
HexobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Hexobarbital.Approved
HydrocortisoneThe serum concentration of Ulipristal can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
Hydroxyprogesterone caproateThe therapeutic efficacy of Hydroxyprogesterone caproate can be decreased when used in combination with Ulipristal.Approved
IdelalisibThe serum concentration of Ulipristal can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Ulipristal can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Ulipristal can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Ulipristal can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Ulipristal can be increased when it is combined with Indomethacin.Approved, Investigational
IsavuconazoniumThe serum concentration of Ulipristal can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsradipineThe serum concentration of Ulipristal can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Ulipristal can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Ulipristal can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ulipristal can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Ulipristal can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Ulipristal can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Ulipristal can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Ulipristal can be increased when it is combined with Lapatinib.Approved, Investigational
LevofloxacinThe serum concentration of Ulipristal can be increased when it is combined with Levofloxacin.Approved, Investigational
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Ulipristal.Approved, Investigational
LevothyroxineThe serum concentration of Ulipristal can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Ulipristal can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Ulipristal can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Ulipristal can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Ulipristal can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Ulipristal can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Ulipristal can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Ulipristal can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Ulipristal can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Ulipristal can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Ulipristal can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Ulipristal can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Ulipristal can be decreased when it is combined with Lumacaftor.Approved
LynestrenolThe therapeutic efficacy of Lynestrenol can be decreased when used in combination with Ulipristal.Investigational
MaprotilineThe serum concentration of Ulipristal can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Ulipristal can be increased when it is combined with Mebendazole.Approved, Vet Approved
MedrogestoneThe therapeutic efficacy of Medrogestone can be decreased when used in combination with Ulipristal.Approved
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone acetate can be decreased when used in combination with Ulipristal.Approved, Investigational
MefloquineThe serum concentration of Ulipristal can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Ulipristal.Approved, Vet Approved
MeprobamateThe serum concentration of Ulipristal can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Ulipristal can be increased when it is combined with Methadone.Approved
MethohexitalThe serum concentration of Ulipristal can be decreased when it is combined with Methohexital.Approved
MethylphenobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Methylphenobarbital.Approved
MetoprololThe serum concentration of Ulipristal can be increased when it is combined with Metoprolol.Approved, Investigational
MexiletineThe metabolism of Ulipristal can be decreased when combined with Mexiletine.Approved
MibefradilThe serum concentration of Ulipristal can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Ulipristal can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Ulipristal can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Ulipristal can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Ulipristal can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Ulipristal can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Ulipristal can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Ulipristal can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Ulipristal can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Ulipristal can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Ulipristal can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Ulipristal can be increased when it is combined with Naringenin.Experimental
NefazodoneThe serum concentration of Ulipristal can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Ulipristal can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Ulipristal can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Ulipristal can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Ulipristal can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Ulipristal can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Ulipristal can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Ulipristal can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Ulipristal can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Ulipristal can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Ulipristal can be increased when it is combined with Nitrendipine.Approved
NomegestrolThe therapeutic efficacy of Nomegestrol can be decreased when used in combination with Ulipristal.Approved
NorethisteroneThe therapeutic efficacy of Norethisterone can be decreased when used in combination with Ulipristal.Approved
OlaparibThe serum concentration of Ulipristal can be increased when it is combined with Olaparib.Approved
OmeprazoleThe serum concentration of Ulipristal can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Ulipristal can be increased when it is combined with Osimertinib.Approved
OxcarbazepineThe serum concentration of Ulipristal can be decreased when it is combined with Oxcarbazepine.Approved
P-NitrophenolThe serum concentration of Ulipristal can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Ulipristal can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Ulipristal can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Ulipristal can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Ulipristal can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Ulipristal can be increased when it is combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Ulipristal can be increased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Ulipristal can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Ulipristal can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Ulipristal can be increased when it is combined with Pimozide.Approved
Platelet Activating FactorThe serum concentration of Ulipristal can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Ulipristal can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Ulipristal can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Ulipristal can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Ulipristal can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Ulipristal can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Ulipristal can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Ulipristal can be increased when it is combined with Probenecid.Approved
ProgesteroneThe therapeutic efficacy of Progesterone can be decreased when used in combination with Ulipristal.Approved, Vet Approved
PromethazineThe serum concentration of Ulipristal can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Ulipristal can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Ulipristal can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Ulipristal can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Ulipristal can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Ulipristal can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Ulipristal can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Ulipristal can be increased when it is combined with Quinine.Approved
RanitidineThe serum concentration of Ulipristal can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ulipristal can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Ulipristal can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Ulipristal can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Ulipristal can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Ulipristal can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Ulipristal can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Ulipristal can be decreased when it is combined with Rifapentine.Approved
RilpivirineThe serum concentration of Ulipristal can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Ulipristal can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Ulipristal can be increased when it is combined with Rolapitant.Approved
RopiniroleThe metabolism of Ulipristal can be decreased when combined with Ropinirole.Approved, Investigational
SaquinavirThe serum concentration of Ulipristal can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Ulipristal can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe serum concentration of Ulipristal can be decreased when it is combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Ulipristal can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Ulipristal can be increased when it is combined with Sertraline.Approved
SildenafilThe serum concentration of Ulipristal can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Ulipristal can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Ulipristal can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Ulipristal can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Ulipristal can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Ulipristal can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Ulipristal can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Ulipristal can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Ulipristal can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Ulipristal can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Ulipristal can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Ulipristal can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe serum concentration of Ulipristal can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Ulipristal can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Ulipristal can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Ulipristal can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Ulipristal can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Ulipristal can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Ulipristal can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of Ulipristal can be increased when it is combined with Telaprevir.Withdrawn
TelithromycinThe serum concentration of Ulipristal can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Ulipristal can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Ulipristal can be increased when it is combined with Temsirolimus.Approved
Tenofovir disoproxilThe metabolism of Ulipristal can be decreased when combined with Tenofovir.Approved, Investigational
TerazosinThe serum concentration of Ulipristal can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Ulipristal can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Ulipristal can be decreased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Ulipristal can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Ulipristal can be increased when it is combined with Testosterone.Approved, Investigational
TheophyllineThe metabolism of Ulipristal can be decreased when combined with Theophylline.Approved
ThiamylalThe serum concentration of Ulipristal can be decreased when it is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe serum concentration of Ulipristal can be decreased when it is combined with Thiopental.Approved, Vet Approved
TicagrelorThe serum concentration of Ulipristal can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe serum concentration of Ulipristal can be increased when it is combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Ulipristal can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Ulipristal can be increased when it is combined with Tolvaptan.Approved
TopiramateThe serum concentration of Ulipristal can be decreased when it is combined with Topiramate.Approved
TrazodoneThe serum concentration of Ulipristal can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Ulipristal can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Ulipristal can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Ulipristal can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Ulipristal can be increased when it is combined with Trimipramine.Approved
VemurafenibThe serum concentration of Ulipristal can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Ulipristal can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Ulipristal can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Ulipristal can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Ulipristal can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Ulipristal can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of Ulipristal can be increased when it is combined with Voriconazole.Approved, Investigational
ZimelidineThe serum concentration of Ulipristal can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe serum concentration of Ulipristal can be increased when it is combined with Ziprasidone.Approved
Food Interactions
  • A high fat meal may lower mean Cmax and increase mean AUC(0-∞) but these changes are not clinically significant. Take without regards to meals.
References
Synthesis ReferenceNot Available
General References
  1. Pohl O, Osterloh I, Gotteland JP: Ulipristal acetate - safety and pharmacokinetics following multiple doses of 10-50 mg per day. J Clin Pharm Ther. 2013 Aug;38(4):314-20. doi: 10.1111/jcpt.12065. Epub 2013 Apr 3. [PubMed:23550906 ]
  2. Melis GB, Piras B, Marotto MF, Orru' MM, Maricosu G, Pilloni M, Guerriero S, Angiolucci M, Lello S, Paoletti AM: Pharmacokinetic evaluation of ulipristal acetate for uterine leiomyoma treatment. Expert Opin Drug Metab Toxicol. 2012 Jul;8(7):901-8. doi: 10.1517/17425255.2012.695775. Epub 2012 Jun 10. [PubMed:22681335 ]
  3. Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [PubMed:23437846 ]
  4. Martinez AM, Thomas MA: Ulipristal acetate as an emergency contraceptive agent. Expert Opin Pharmacother. 2012 Sep;13(13):1937-42. doi: 10.1517/14656566.2012.705832. Epub 2012 Jul 7. [PubMed:22770536 ]
  5. Maruo T, Ohara N, Matsuo H, Xu Q, Chen W, Sitruk-Ware R, Johansson ED: Effects of levonorgestrel-releasing IUS and progesterone receptor modulator PRM CDB-2914 on uterine leiomyomas. Contraception. 2007 Jun;75(6 Suppl):S99-103. Epub 2007 Mar 21. [PubMed:17531625 ]
  6. Creinin MD, Schlaff W, Archer DF, Wan L, Frezieres R, Thomas M, Rosenberg M, Higgins J: Progesterone receptor modulator for emergency contraception: a randomized controlled trial. Obstet Gynecol. 2006 Nov;108(5):1089-97. [PubMed:17077229 ]
  7. Blithe DL, Nieman LK, Blye RP, Stratton P, Passaro M: Development of the selective progesterone receptor modulator CDB-2914 for clinical indications. Steroids. 2003 Nov;68(10-13):1013-7. [PubMed:14667994 ]
  8. Attardi BJ, Burgenson J, Hild SA, Reel JR: In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88. [PubMed:15120421 ]
  9. Rosato E, Farris M, Bastianelli C: Mechanism of Action of Ulipristal Acetate for Emergency Contraception: A Systematic Review. Front Pharmacol. 2016 Jan 12;6:315. doi: 10.3389/fphar.2015.00315. eCollection 2015. [PubMed:26793107 ]
External Links
ATC CodesG03AD02 — UlipristalG03XB02 — Ulipristal
AHFS Codes
  • 68:12
PDB EntriesNot Available
FDA labelDownload (309 KB)
MSDSDownload (479 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0WithdrawnTreatmentUrogenital Abnormalities1
1CompletedTreatmentHealthy Volunteers1
1Not Yet RecruitingTreatmentHeavy Menstrual Bleeding1
1RecruitingBasic ScienceRenal Function1
1RecruitingPreventionContraception1
1, 2RecruitingTreatmentOvulation Inhibition1
2CompletedNot AvailableContraception1
2CompletedPreventionFocus: Estrogen-free Oral Contraception1
2CompletedTreatmentContraception1
2CompletedTreatmentLeiomyomas3
2CompletedTreatmentOne to five years postmenopausal1
2Not Yet RecruitingPreventionCancer, Breast1
2RecruitingTreatmentCMT1A1
2RecruitingTreatmentEndometriosis of Uterus1
2TerminatedTreatmentDepressive State / PMDD / Premenstrual Dysphoric Disorder / Premenstrual Syndrome1
2, 3CompletedTreatmentPost coital contraception1
3CompletedTreatmentContraception1
3CompletedTreatmentIntramural Fibroids / Uterine Leiomyomas1
3CompletedTreatmentPost coital contraception1
3CompletedTreatmentUterine Bleeding in Women With Leiomyomas2
3CompletedTreatmentUterine Leiomyomas6
3RecruitingOtherPost coital contraception1
3RecruitingTreatmentContraception / Haemorrhage1
3RecruitingTreatmentUterine Leiomyomas1
3WithdrawnTreatmentLeiomyomas1
4Active Not RecruitingBasic ScienceContraception1
4Active Not RecruitingTreatmentEndometriosis1
4Not Yet RecruitingTreatmentUterine Leiomyomas1
4Not Yet RecruitingTreatmentWomen With Leiomyoma After at Least One Unsuccessful IVF Treatment1
4RecruitingBasic ScienceContraception1
4RecruitingTreatmentAbnormal Bleeding / Heavy Menstrual Bleeding1
4RecruitingTreatmentBMI >30 kg/m2 / Contraception1
4RecruitingTreatmentInfertilities1
4RecruitingTreatmentLeiomyomas5
Not AvailableCompletedNot AvailableContraception2
Not AvailableRecruitingNot AvailablePost coital contraception1
Not AvailableRecruitingPreventionPregnancy; Accident / Unplanned Pregnancy1
Not AvailableUnknown StatusNot AvailableInfertilities1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral30 mg
TabletOral30 mg/1
TabletOral5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8426392 No2010-06-122030-06-12Us
US8962603 No2010-06-122030-06-12Us
US9283233 No2010-04-132030-04-13Us
US8735380 No2009-02-202029-02-20Us
US8512745 No2010-06-022030-06-02Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00943 mg/mLALOGPS
logP4.45ALOGPS
logP4.18ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)12.7ChemAxon
pKa (Strongest Basic)4.89ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area57.61 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity129.29 m3·mol-1ChemAxon
Polarizability49.66 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9964
Blood Brain Barrier+0.6396
Caco-2 permeable+0.577
P-glycoprotein substrateSubstrate0.6286
P-glycoprotein inhibitor IInhibitor0.9708
P-glycoprotein inhibitor IIInhibitor0.9321
Renal organic cation transporterNon-inhibitor0.799
CYP450 2C9 substrateNon-substrate0.8337
CYP450 2D6 substrateNon-substrate0.8848
CYP450 3A4 substrateSubstrate0.8312
CYP450 1A2 substrateNon-inhibitor0.5677
CYP450 2C9 inhibitorNon-inhibitor0.7078
CYP450 2D6 inhibitorNon-inhibitor0.7827
CYP450 2C19 inhibitorNon-inhibitor0.6021
CYP450 3A4 inhibitorInhibitor0.7866
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6633
Ames testNon AMES toxic0.8603
CarcinogenicityNon-carcinogens0.7916
BiodegradationNot ready biodegradable0.9933
Rat acute toxicity2.6728 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9538
hERG inhibition (predictor II)Non-inhibitor0.686
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 20-oxosteroids. These are steroid derivatives carrying a C=O group at the 20-position of the steroid skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassOxosteroids
Direct Parent20-oxosteroids
Alternative Parents3-oxosteroids / 17-hydroxysteroids / Dialkylarylamines / Aniline and substituted anilines / Cyclohexenones / Tertiary alcohols / Alpha-hydroxy ketones / Cyclic alcohols and derivatives / Organic oxides / Hydrocarbon derivatives
Substituents20-oxosteroid / 3-oxosteroid / Hydroxysteroid / 17-hydroxysteroid / Aniline or substituted anilines / Dialkylarylamine / Tertiary aliphatic/aromatic amine / Cyclohexenone / Monocyclic benzene moiety / Benzenoid
Molecular FrameworkAromatic homopolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
modulator
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
Uniprot Name:
Progesterone receptor
Molecular Weight:
98979.96 Da
References
  1. Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [PubMed:23437846 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...
Gene Name:
NR3C1
Uniprot ID:
P04150
Uniprot Name:
Glucocorticoid receptor
Molecular Weight:
85658.57 Da
References
  1. Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [PubMed:23437846 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Zinc ion binding
Specific Function:
Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription factor activity is modulated by bound coactivator and corepressor proteins. Transcription activation is down-regulated by NR0B2. Activated, but not phosphorylated, by HIPK3 and ZIPK/DAPK3.
Gene Name:
AR
Uniprot ID:
P10275
Uniprot Name:
Androgen receptor
Molecular Weight:
98987.9 Da
References
  1. Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [PubMed:23437846 ]

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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da
References
  1. Gemzell-Danielsson K, Rabe T, Cheng L: Emergency contraception. Gynecol Endocrinol. 2013 Mar;29 Suppl 1:1-14. doi: 10.3109/09513590.2013.774591. [PubMed:23437846 ]
Kind
Protein
Organism
Human
Pharmacological action
no
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
Uniprot Name:
Cytochrome P450 1A2
Molecular Weight:
58293.76 Da
References
  1. Martinez AM, Thomas MA: Ulipristal acetate as an emergency contraceptive agent. Expert Opin Pharmacother. 2012 Sep;13(13):1937-42. doi: 10.1517/14656566.2012.705832. Epub 2012 Jul 7. [PubMed:22770536 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Uniprot Name:
Serum albumin
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Uniprot Name:
Alpha-1-acid glycoprotein 1
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
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
Drug created on April 26, 2013 23:33 / Updated on September 01, 2017 11:59