dienogest 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
steroids, progestogens 871 65928-58-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dienogest
  • dienogestril
  • dinagest
  • STS 557
  • Molecular weight: 311.43
  • Formula: C20H25NO2
  • CLOGP: 2.16
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 61.09
  • ALOGS: -3.61
  • ROTB: 1

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
2 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 94 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.29 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.10 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 11 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 6, 2010 FDA
Jan. 23, 2020 PMDA Mochida Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

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
Intermenstrual bleeding 36.67 32.62 10 755 7916 63480341

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Coeliac disease 37.33 34.96 10 619 11341 79732418

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC G03AA16 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens and estrogens, fixed combinations
ATC G03AB08 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens and estrogens, sequential preparations
ATC G03DB08 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS
Pregnadien derivatives
ATC G03FA15 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
PROGESTOGENS AND ESTROGENS IN COMBINATION
Progestogens and estrogens, fixed combinations
FDA CS M0447349 Progesterone Congeners
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D003270 Contraceptive Agents
MeSH PA D003271 Contraceptive Agents, Female
MeSH PA D000080066 Contraceptive Agents, Hormonal
MeSH PA D003272 Contraceptive Agents, Male
MeSH PA D003278 Contraceptives, Oral, Hormonal
MeSH PA D006727 Hormone Antagonists
MeSH PA D012102 Reproductive Control Agents
FDA EPC N0000175602 Progestin
CHEBI has role CHEBI:49326 synthetic oral contraceptives
CHEBI has role CHEBI:59826 progestins
CHEBI has role CHEBI:70709 progesterone receptor agonists

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Contraception indication 13197004
Dysmenorrhea indication 266599000
Polycystic ovaries off-label use 69878008
Hyperlipoproteinemia contraindication 3744001 DOID:1168
Hypocalcemia contraindication 5291005
Hypercholesterolemia contraindication 13644009
Myocardial infarction contraindication 22298006 DOID:5844
Diplopia contraindication 24982008
Retinal hemorrhage contraindication 28998008
Depressive disorder contraindication 35489007
Chloasma contraindication 36209000
Migraine contraindication 37796009 DOID:6364
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Body fluid retention contraindication 43498006
Thrombosis of retinal vein contraindication 46085004
Humoral hypercalcemia of malignancy contraindication 47709007
Chronic heart failure contraindication 48447003
Dementia contraindication 52448006
Hepatic porphyria contraindication 55056006 DOID:3133
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Hyperlipidemia contraindication 55822004 DOID:1168
Thrombophlebitis contraindication 64156001 DOID:3875
Intermenstrual bleeding - irregular contraindication 64996003
Diabetes mellitus contraindication 73211009 DOID:9351
Epilepsy contraindication 84757009 DOID:1826
Breast lump contraindication 89164003
Kidney disease contraindication 90708001 DOID:557
Uterine leiomyoma contraindication 95315005 DOID:13223
Deep venous thrombosis contraindication 128053003
Seizure disorder contraindication 128613002
Endometriosis contraindication 129103003
Bed-ridden contraindication 160685001
Mammography abnormal contraindication 168750009
Asthma contraindication 195967001 DOID:2841
Cerebrovascular accident contraindication 230690007
Pulmonary thromboembolism contraindication 233935004
Thrombophilia contraindication 234467004 DOID:2452
Disease of liver contraindication 235856003 DOID:409
Endometrial carcinoma contraindication 254878006 DOID:2871
Chorea contraindication 271700006
Pregnancy, function contraindication 289908002
Hypertriglyceridemia contraindication 302870006
Functional visual loss contraindication 313165001
Malignant tumor of ovary contraindication 363443007 DOID:2394
Thromboembolic disorder contraindication 371039008
Cardiovascular event risk contraindication 395112001
Disorder of coronary artery contraindication 414024009
Obesity contraindication 414916001 DOID:9970
Estrogen receptor positive tumor contraindication 416053008
Porphyria contraindication 418470004
Optic disc edema contraindication 423341008 DOID:146
Family history of malignant neoplasm of breast contraindication 429740004
Hypertensive urgency contraindication 443482000
Carcinoma of female breast contraindication 447782002
Smokes tobacco daily contraindication 449868002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
N/A,2MG,3MG,N/A,N/A;3MG,2MG,2MG,1MG,N/A NATAZIA BAYER HLTHCARE N022252 May 6, 2010 RX TABLET ORAL 8071577 May 13, 2026 PREVENTION OF PREGNANCY
N/A,2MG,3MG,N/A,N/A;3MG,2MG,2MG,1MG,N/A NATAZIA BAYER HLTHCARE N022252 May 6, 2010 RX TABLET ORAL 8153616 Jan. 30, 2028 TREATMENT OF HEAVY MENSTRUAL BLEEDING IN WOMEN WITHOUT ORGANIC PATHOLOGY WHO CHOOSE TO USE AN ORAL CONTRACEPTIVE AS THEIR METHOD OF CONTRACEPTION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Progesterone receptor Nuclear hormone receptor AGONIST DRUG LABEL DRUG LABEL

External reference:

IDSource
4029967 VUID
N0000181307 NUI
D03799 KEGG_DRUG
22968 RXNORM
4029967 VANDF
C0057916 UMLSCUI
CHEBI:70708 CHEBI
CHEMBL1201864 ChEMBL_ID
DB09123 DRUGBANK_ID
C023635 MESH_SUPPLEMENTAL_RECORD_UI
68861 PUBCHEM_CID
7654 IUPHAR_LIGAND_ID
5286 INN_ID
46M3EV8HHE UNII
22992 MMSL
d06271 MMSL
006572 NDDF
703097002 SNOMEDCT_US
703726009 SNOMEDCT_US

Pharmaceutical products:

None