drospirenone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| mineralocorticoid receptor (MR, MCR, aldosterone receptor) antagonists | 968 | 67392-87-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source. It is used in combination with estetrol (nextstellis) as oral contraceptive.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.10 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.12 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 76 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 19, 2021 | EMA | Gedeon Richter Plc; Estetra SPRL | |
| May 23, 2019 | FDA | EXELTIS USA INC | |
| July 23, 2010 | PMDA | Bayer Yakuhin, Ltd. |
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 |
|---|---|---|---|---|---|---|
| Pregnancy on oral contraceptive | 67.17 | 30.39 | 12 | 997 | 1025 | 63486988 |
| Pulmonary embolism | 39.55 | 30.39 | 24 | 985 | 116660 | 63371353 |
| Intermenstrual bleeding | 38.35 | 30.39 | 11 | 998 | 7915 | 63480098 |
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 |
|---|---|---|---|---|---|---|
| Pregnancy on oral contraceptive | 46.57 | 35.66 | 8 | 820 | 837 | 79742723 |
| Pulmonary embolism | 40.49 | 35.66 | 24 | 804 | 171630 | 79571930 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G03AA12 | 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 | G03AA18 | 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 | G03AC10 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens |
| ATC | G03FA17 | 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 | D004232 | Diuretics |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D000451 | Mineralocorticoid Receptor Antagonists |
| MeSH PA | D045283 | Natriuretic Agents |
| FDA EPC | N0000175602 | Progestin |
| CHEBI has role | CHEBI:49323 | contraceptive drugs |
| CHEBI has role | CHEBI:59826 | progestins |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Premenstrual dysphoric disorder | indication | 596004 | |
| Contraception | indication | 13197004 | |
| Atrophic vaginitis | indication | 52441000 | |
| Acne vulgaris | indication | 88616000 | |
| Menopausal flushing | indication | 198436008 | |
| Atrophic vulva | indication | 248861000 | DOID:14275 |
| Dysmenorrhea | indication | 266599000 | |
| Controlled ovarian stimulation | indication | 732970000 | |
| Polycystic ovaries | off-label use | 69878008 | |
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Hyperkalemia | contraindication | 14140009 | |
| 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 |
| Acute nephropathy | contraindication | 58574008 | |
| 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 | |
| Adrenal cortical hypofunction | contraindication | 386584007 | DOID:10493 |
| 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 3MG;14.2MG | NEXTSTELLIS | MAYNE PHARMA | N214154 | April 15, 2021 | RX | TABLET | ORAL | 7732430 | March 2, 2025 | USE BY FEMALES OF REPRODUCTIVE POTENTIAL TO PREVENT PREGNANCY |
| 3MG,N/A;0.02MG,N/A;0.451MG,0.451MG | BEYAZ | BAYER HLTHCARE | N022532 | Sept. 24, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | PREVENTION OF PREGNANCY |
| 3MG,N/A;0.02MG,N/A;0.451MG,0.451MG | BEYAZ | BAYER HLTHCARE | N022532 | Sept. 24, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | RAISE FOLATE LEVELS IN WOMEN WHO CHOOSE TO USE AN ORAL CONTRACEPTIVE AS THEIR METHOD OF CONTRACEPTION FOR THE PURPOSE OF REDUCING THE RISK OF A NEURAL TUBE DEFECT IN A PREGNANCY |
| 3MG,N/A;0.02MG,N/A;0.451MG,0.451MG | BEYAZ | BAYER HLTHCARE | N022532 | Sept. 24, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | TREATMENT OF MODERATE ACNE VULGARIS IN WOMEN AT LEAST 14 YEARS OF AGE IF THE PATIENT DESIRES AN ORAL CONTRACEPTIVE FOR BIRTH CONTROL |
| 3MG,N/A;0.02MG,N/A;0.451MG,0.451MG | BEYAZ | BAYER HLTHCARE | N022532 | Sept. 24, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | TREATMENT OF MOOD CHANGES AND/OR ANXIETY AS SYMPTOMS OF PREMENSTRUAL DYSPHORIC DISORDER (PMDD) IN WOMEN WHO CHOOSE TO USE AN ORAL CONTRACEPTIVE AS THEIR METHOD OF CONTRACEPTION |
| 3MG,N/A;0.03MG,N/A;0.451MG,0.451MG | SAFYRAL | BAYER HLTHCARE | N022574 | Dec. 16, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | PREVENTION OF PREGNANCY |
| 3MG,N/A;0.03MG,N/A;0.451MG,0.451MG | SAFYRAL | BAYER HLTHCARE | N022574 | Dec. 16, 2010 | RX | TABLET | ORAL | 11617751 | July 17, 2030 | RAISE FOLATE LEVELS IN WOMEN WHO CHOOSE TO USE AN ORAL CONTRACEPTIVE AS THEIR METHOD OF CONTRACEPTION FOR THE PURPOSE OF REDUCING THE RISK OF A NEURAL TUBE DEFECT IN A PREGNANCY |
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | 10179140 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | 10603281 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | 10849857 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | 11413249 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 4MG | SLYND | EXELTIS USA INC | N211367 | May 23, 2019 | RX | TABLET | ORAL | 9603860 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | 10179140 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | 10603281 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | 10849857 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | 11413249 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | 9603860 | June 28, 2031 | PREVENTION OF PREGNANCY IN FEMALES OF REPRODUCTIVE AGE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 3.5MG | DROSPIRENONE | EXELTIS USA INC | N216285 | June 29, 2022 | DISCN | TABLET, CHEWABLE | ORAL | June 29, 2025 | NEW PRODUCT |
| 3MG;14.2MG | NEXTSTELLIS | MAYNE PHARMA | N214154 | April 15, 2021 | RX | TABLET | ORAL | April 15, 2026 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mineralocorticoid receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 10.50 | WOMBAT-PK | CHEMBL | |||
| Progesterone receptor | Nuclear hormone receptor | AGONIST | EC50 | 10.50 | WOMBAT-PK | CHEMBL | |||
| Androgen receptor | Nuclear hormone receptor | IC50 | 8.50 | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4021271 | VUID |
| N0000179010 | NUI |
| D03917 | KEGG_DRUG |
| 4021271 | VANDF |
| C0043822 | UMLSCUI |
| CHEBI:50838 | CHEBI |
| CHEMBL1509 | ChEMBL_ID |
| DB01395 | DRUGBANK_ID |
| C035144 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68873 | PUBCHEM_CID |
| 2874 | IUPHAR_LIGAND_ID |
| 6519 | INN_ID |
| N295J34A25 | UNII |
| 11636 | RXNORM |
| 16073 | MMSL |
| d04759 | MMSL |
| 009133 | NDDF |
| 395275003 | SNOMEDCT_US |
| 410919000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SLYND | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0642-7470 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 30 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-482 | TABLET, FILM COATED | 0.25 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-482 | TABLET, FILM COATED | 0.25 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-482 | TABLET, FILM COATED | 0.25 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-483 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-483 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 50419-483 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 28 sections |
| Angeliq | HUMAN PRESCRIPTION DRUG LABEL | 2 | 54868-6184 | TABLET, FILM COATED | 0.50 mg | ORAL | NDA | 24 sections |