Drospirenone

Progestin — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Drospirenone is an ofp drug in the Progestin class catalogued in DrugCentral. It was first approved by the PMDA in 2010. DrugCentral lists 3 molecular targets, including NR3C2, PGR and AR. Recorded indications include Acne vulgaris, Atrophic vaginitis, Atrophic vulva and Contraception.

• Approval status: ofp (first approved 2010 by the PMDA).
• Drug class: Progestin.
• Molecular targets: NR3C2, PGR and AR (3 listed in DrugCentral).
• Indications: Acne vulgaris, Atrophic vaginitis, Atrophic vulva, Contraception and Controlled ovarian stimulation and others.
• ATC code: G03AA12 (Progestogens and estrogens, fixed combinations).
• Molecular formula: C24H30O3; molecular weight 366.50 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (8)

• Acne vulgaris
• Atrophic vaginitis
• Atrophic vulva
• Contraception
• Controlled ovarian stimulation
• Dysmenorrhea
• Menopausal flushing
• Premenstrual dysphoric disorder

Off-label uses (1)

• Polycystic ovaries

Contraindications (57)

• Acute nephropathy
• Adrenal cortical hypofunction
• Asthma
• Bed-ridden
• Body fluid retention
• Breast lump
• Carcinoma of female breast
• Cardiovascular event risk
• Cerebrovascular accident
• Chloasma
• Chorea
• Chronic heart failure
• Deep venous thrombosis
• Dementia
• Depressive disorder
• Diabetes mellitus
• Diplopia
• Disease of liver
• Disorder of coronary artery
• Disorder of gallbladder
• Endometrial carcinoma
• Endometriosis
• Epilepsy
• Estrogen receptor positive tumor
• Family history of malignant neoplasm of breast
• Functional visual loss
• Hepatic porphyria
• Humoral hypercalcemia of malignancy
• Hypercholesterolemia
• Hyperkalemia
• + 27 more

Mechanism & targets

• Established pharmacologic class: Progestin

Molecular targets (3)

Target	Gene	Action	Activity
Mineralocorticoid receptor	NR3C2	antagonist	IC50 10.50
Progesterone receptor	PGR	agonist	EC50 10.50
Androgen receptor	AR	unknown	IC50 8.50

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2021-05-19	EMA	—	Gedeon Richter Plc; Estetra SPRL
2019-05-23	FDA	—	EXELTIS USA INC
2010-07-23	PMDA	—	Bayer Yakuhin, Ltd.

ATC classification

ATC code	Therapeutic hierarchy
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
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
G03AC10	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE › Progestogens
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

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Pregnancy on oral contraceptive	306.4
Intermenstrual bleeding	200.3
Heavy menstrual bleeding	83.2
Pulmonary embolism	80.6
Deep vein thrombosis	61.1
Food allergy	44.0
Meningioma	43.8
Depressive symptom	43.8
Idiopathic intracranial hypertension	43.3
Abortion spontaneous	39.8
Allergic reaction to excipient	34.9
Polymenorrhoea	32.8

Chemical structure

• Molecular formula: C₂₄H₃₀O₃
• Molecular weight: 366.50 g/mol
• CAS number: —
• InChIKey: METQSPRSQINEEU-HXCATZOESA-N
• PubChem CID: 68873

C[C@]12CC[C@H]3[C@@H]([C@H]4C[C@H]4C4=CC(=O)CC[C@]34C)[C@@H]1[C@@H]1C[C@@H]1[C@@]21CCC(=O)O1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Drospirenone used for?

DrugCentral lists the following indications for Drospirenone: Acne vulgaris, Atrophic vaginitis, Atrophic vulva, Contraception, Controlled ovarian stimulation, Dysmenorrhea, Menopausal flushing and Premenstrual dysphoric disorder.

How does Drospirenone work?

Its molecular targets in DrugCentral include NR3C2 (antagonist), PGR (agonist) and AR.

When was Drospirenone first approved?

Drospirenone was first approved by the PMDA in 2010.

What drug class does Drospirenone belong to?

Drospirenone is in the Progestin class.

What is the chemical formula of Drospirenone?

Drospirenone has the molecular formula C24H30O3 and a molecular weight of 366.50 g/mol.

Sources

• DrugCentral drug card 968 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1509 — compound record and bioactivity
• PubChem CID 68873 — chemical identifiers
• DrugBank DB01395 — drug record
• FDA UNII N295J34A25 — substance identity
• DailyMed: FDA labels for Drospirenone — current prescribing information (label search)
• UniProt P08235 (NR3C2) — target protein
• UniProt P06401 (PGR) — target protein
• UniProt P10275 (AR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.