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dienogest 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids, progestogens | 871 | 65928-58-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.140 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.032 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 42.560 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 9.036 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 19.200 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 30.240 | % | High | 1 |
| herg | hERG pIC50 | 4.709 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.133 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 25.293 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 15.430 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,PDK1,PDK2,PDK4,PRKDC,TEK | 17 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,MAP2K6,MAP3K14 | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 5.808 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 32.211 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 17.120 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 15.205 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 31.020 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 40.644 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 64.010 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 18.360 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 289.068 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 23, 2020 | PMDA | Mochida Pharmaceutical Co., Ltd. | |
| May 6, 2010 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Uterine haemorrhage | 51.96 | 30.18 | 12 | 1108 | 4740 | 90622587 |
| Genital haemorrhage | 40.07 | 30.18 | 11 | 1109 | 8691 | 90618636 |
| Intermenstrual bleeding | 34.90 | 30.18 | 10 | 1110 | 9213 | 90618114 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Uterine haemorrhage | 53.75 | 31.17 | 11 | 964 | 3483 | 110584841 |
| Genital haemorrhage | 40.64 | 31.17 | 10 | 965 | 7242 | 110581082 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 | D000080066 | Contraceptive Agents, Hormonal |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D003270 | Contraceptive Agents |
| MeSH PA | D003271 | Contraceptive Agents, Female |
| MeSH PA | D003272 | Contraceptive Agents, Male |
| MeSH PA | D003278 | Contraceptives, Oral, Hormonal |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D012102 | Reproductive Control Agents |
| MeSH PA | D018931 | Antineoplastic Agents, Hormonal |
| FDA EPC | N0000175602 | Progestin |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:49326 | synthetic oral contraceptive |
| CHEBI has role | CHEBI:50779 | appetite enhancer |
| CHEBI has role | CHEBI:59826 | progestin |
| CHEBI has role | CHEBI:70709 | progesterone receptor agonist |
Related Drugs by ATC class:
G03AA Progestogens and estrogens, fixed combinations 17 drugs
G03AB Progestogens and estrogens, sequential preparations 10 drugs
G03DB Pregnadien derivatives 7 drugs
G03FA Progestogens and estrogens, fixed combinations 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Progesterone receptor | Nuclear hormone receptor | AGONIST | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 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 |
| 46M3EV8HHE | INXIGHT DRUGS |
Pharmaceutical products:
None