ulipristal indications/contra

Stem definitionDrug idCAS RN
steroidal compounds acting on progesterone receptors 4166 126784-99-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • CDB-2914
  • ulipristal acetate
  • ella
  • EllaOne
  • esmya
  • ulipristal
Ulipristal acetate is a selective progesterone receptor modulator with antagonistic and partial agonistic effects (a progesterone agonist/antagonist) at the progesterone receptor. It binds the human progesterone receptor and prevents progesterone from occupying its receptor. The likely primary mechanism of action of ulipristal acetate for emergency contraception is inhibition or delay of ovulation.
  • Molecular weight: 475.63
  • Formula: C30H37NO4
  • CLOGP: 4.51
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 0
  • TPSA: 63.68
  • ALOGS: -5.14
  • ROTB: 5

Drug dosage:

DoseUnitRoute
30 mg O
5 mg O

Approvals:

DateAgencyCompanyOrphan
May 15, 2009 EMA
Aug. 13, 2010 FDA LAB HRA PHARMA

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Unintended pregnancy 242.78 110.79 37 122 3086 3382614
Pregnancy after post coital contraception 119.91 110.79 12 147 18 3385682

Pharmacologic Action:

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SourceCodeDescription
ATC G03AD02 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Emergency contraceptives
ATC G03XB02 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
Progesterone receptor modulators
FDA EPC N0000191263 Progesterone Agonist/Antagonist
FDA MoA N0000191262 Selective Progesterone Receptor Modulators
MeSH PA D003270 Contraceptive Agents
MeSH PA D003271 Contraceptive Agents, Female
MeSH PA D012102 Reproductive Control Agents
CHEBI has role CHEBI:49323 contraceptive drug
CHEBI has role CHEBI:71027 progesterone receptor modulator

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Uterine leiomyoma indication 95315005 DOID:13223
Postcoital contraception indication 268463003
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.7 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
30MG ELLA LAB HRA PHARMA N022474 Aug. 13, 2010 RX TABLET ORAL 9283233 April 13, 2030 METHOD FOR CONTRACEPTION TO A WOMAN COMPRISING ADMINISTERING TO THE WOMAN 30MG OF ULIPRISTAL ACETATE MORE THAN 72 HOURS AND UP TO 120 HOURS AFTER AN UNPROTECTED INTERCOURSE
30MG ELLA LAB HRA PHARMA N022474 Aug. 13, 2010 RX TABLET ORAL 8426392 June 12, 2030 ELLA IS A PROGESTERONE AGONIST/ANTAGONIST EMERGENCY CONTRACEPTION INDICATED FOR THE PREVENTION OF PREGNANCY FOLLOWING UNPROTECTED INTERCOURSE OR A KNOWN OR SUSPECTED CONTRACEPTIVE FAILURE. ELLA CAN BE TAKEN WITH OR WITHOUT FOOD
30MG ELLA LAB HRA PHARMA N022474 Aug. 13, 2010 RX TABLET ORAL 8962603 June 12, 2030 METHOD FOR PROVIDING POST COITAL CONTRACEPTION TO A WOMAN BY ADMINISTERING ABOUT 30 MG OF ULIPRISTAL ACETATE WITHIN ABOUT 120 HOURS AFTER INTERCOURSE, WHEREIN THE WOMAN IS OVERWEIGHT HAVING A BMI OF 25 TO 29.99

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Progesterone receptor Nuclear hormone receptor ANTAGONIST IC50 9.70 IUPHAR IUPHAR

External reference:

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IDSource
7460 IUPHAR_LIGAND_ID
4030133 VUID
N0000181720 NUI
C2723461 UMLSCUI
D09567 KEGG_DRUG
6J5J15Q2X8 UNII
8367 INN_ID
159811-51-5 SECONDARY_CAS_RN
1005921 RXNORM
d07495 MMSL
4030140 VANDF
N0000181724 NDFRT
013245 NDDF
703249005 SNOMEDCT_US
703737005 SNOMEDCT_US
CHEMBL260538 ChEMBL_ID
C094854 MESH_SUPPLEMENTAL_RECORD_UI
DB08867 DRUGBANK_ID
CHEMBL2103846 ChEMBL_ID
13559281 PUBCHEM_CID
C555622 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:71025 CHEBI
2S0 PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
ella HUMAN PRESCRIPTION DRUG LABEL 1 50102-911 TABLET 30 mg ORAL NDA 18 sections