Drospirenone

Summary

Drospirenone (CHEMBL1509) is an approved small-molecule contraceptive drug (ATC G03AC10) targeting NR3C2; indicated across 9 conditions including acne and polycystic ovary syndrome.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G03AC10
• Targets: 1 (NR3C2)
• Indications: 9 conditions
• Clinical trials: 41
• Chemistry: 366.5 Da · C24H30O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1509
Name	Drospirenone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	68873
ChEBI	CHEBI:50838
ATC	G03AC10
Molecular formula	C24H30O3
Molecular weight	366.5
InChIKey	METQSPRSQINEEU-HXCATZOESA-N

SMILES: C[C@]12CCC(=O)C=C1[C@@H]3C[C@@H]3[C@@H]4[C@@H]2CC[C@]5([C@H]4[C@@H]6C[C@@H]6[C@@]57CCC(=O)O7)C

IUPAC name: (1R,2R,4R,10R,11S,14S,15S,16S,18S,19S)-10,14-dimethylspiro[hexacyclo[9.8.0.02,4.05,10.014,19.016,18]nonadec-5-ene-15,5’-oxolane]-2’,7-dione

Pharmacological roles (ChEBI): contraceptive drug, progestin.

Also known as: Drospirenona, Drospirenone, Drospirenone component of angeliq, Drospirenone component of beyaz, Drospirenone component of nextstellis, Drospirenone component of safyral, Drospirenone component of yasmin, Drospirenone component of yaz, NSC-760103, Slynd, ZK 30595, ZK-30595

Patent coverage: 1,657 distinct patent families (5,927 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
NR3C2	Mineralocorticoid receptor	Antagonist		0%	P08235

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: ATP-binding cassette sub-family C member 4, 5-hydroxytryptamine receptor 2B, Androgen receptor, Glucocorticoid receptor, Progesterone receptor, Muscarinic acetylcholine receptor M2, 5-hydroxytryptamine receptor 2A, Androgen receptor, Bile salt export pump.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 10 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PGR	8.21	AC50	6.1	nM	CHEMBL_ACT_25222676
PGR	7.36	IC50	43.3	nM	CHEMBL_ACT_17672103
NR3C1	7.11	AC50	78	nM	CHEMBL_ACT_25175435
P15207	6.82	AC50	150	nM	CHEMBL_ACT_25232642
AR	6.2	IC50	630	nM	CHEMBL_ACT_17672113

Target pathways

Aggregated over 1 target gene(s): NR3C2.

Top Reactome pathways

9 total, by targets touching each:

Pathway	Targets	Genes
Cellular responses to stress	1	NR3C2
SUMOylation	1	NR3C2
SUMO E3 ligases SUMOylate target proteins	1	NR3C2
HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand	1	NR3C2
Nuclear Receptor transcription pathway	1	NR3C2
Metabolism of proteins	1	NR3C2
SUMOylation of intracellular receptors	1	NR3C2
Post-translational protein modification	1	NR3C2
Cellular responses to stimuli	1	NR3C2

Dominant GO biological processes

GO term	Targets
regulation of transcription by RNA polymerase II	1
signal transduction	1
nuclear receptor-mediated steroid hormone signaling pathway	1
positive regulation of non-canonical NF-kappaB signal transduction	1
regulation of DNA-templated transcription	1
cellular response to hormone stimulus	1
response to lipid	1

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
acne	4	MONDO:0011438	EFO:0003894

7 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
polycystic ovary syndrome	3	MONDO:0008487	EFO:0000660
hidradenitis suppurativa	2	MONDO:0006559	EFO:1000710
bulimia nervosa	2	MONDO:0005452	EFO:0005204
binge eating disorder	2	MONDO:0005582	EFO:0005924
depressive disorder	2	MONDO:0002050	MONDO:0002050
premenstrual tension	2	MONDO:0004169	MONDO:0004169
obesity disorder	1	MONDO:0011122	EFO:0001073

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 41.

Phase distribution

Phase	Trials
PHASE1	14
PHASE4	9
Not specified	9
PHASE3	4
PHASE2	3
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05837624	PHASE4	RECRUITING	Estetrol/Drospirenone to Reduce the Average Size of Endometriomas
NCT07293728	PHASE4	NOT_YET_RECRUITING	A Randomized Feasibility Trial Comparing Drospirenone and Norethindrone for Postpartum Hypertension Management in Preeclampsia
NCT00640224	PHASE4	COMPLETED	Insulin Resistance, Polycystic Ovary Syndrome, and Bone Research Study
NCT01109979	PHASE4	COMPLETED	Effect of Estradiol+Drospirenone Versus Estradiol+MPA on Endothelial Function
NCT01608698	PHASE4	UNKNOWN	Comparison of Body Weight Change During Contraception With Belara and Yasmin
NCT02027337	PHASE4	UNKNOWN	Hemocoagulation and Lipoperoxidation in Women Using Combined Oral Contraceptives, Correction by Antioxidants
NCT03124524	PHASE4	COMPLETED	Treatment Choice in Primary Dysmenorrhea
NCT06316180	PHASE4	COMPLETED	The Use of Drospirenone/Estetrol in Random Start Rapid Endometrial Preparation
NCT06324851	PHASE4	COMPLETED	The Use of Drospirenone/Estetrol, Nomegestrol Acetate/Estradiol and Ethinylestradiol/Dienogest in Random Start Rapid Endometrial Preparation
NCT00367276	PHASE3	COMPLETED	Study to Evaluate the Effect of Six Cycles of Treatment With a Combined Oral Contraceptive (EE 0.30 mg/DRSP 3 mg) on Quality of Life.
NCT00468481	PHASE3	COMPLETED	Efficacy and Safety Study for an Oral Contraceptive Containing Folate
NCT00722761	PHASE3	COMPLETED	Safety and Efficacy Of Drospirenone and Ethinyl Estradiol vs Placebo in the Treatment of Truncal Acne
NCT05461573	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of LPRI-CF113 as an Oral Contraceptive in Females
NCT06345560	PHASE1/PHASE2	RECRUITING	Pharmacokinetics of Drospirenone Only Pills: A Pre- and Post-Bariatric Surgery Study
NCT00089414	PHASE2	TERMINATED	Treatment of Menstrually Related Disorders With Continuous v. Interrupted Oral Contraceptives
NCT00420342	PHASE2	COMPLETED	Effects of Angeliq and Prempro on Blood Pressure and Sodium Sensitivity in Postmenopausal Women With Prehypertension
NCT00722800	PHASE2	TERMINATED	A Study to Examine the Safety and Efficacy of Drospirenone and Ethinyl Estradiol (YAZ) Versus Placebo In HS
NCT06608186	PHASE1/PHASE2	COMPLETED	Can Drospirenone be Used to Prevent LH Surge in Controlled Ovarian Stimulation in PCOS?!
NCT07340190	PHASE1	NOT_YET_RECRUITING	A Drug-drug Interaction Study to Evaluate the Effects of Pelabresib on the Pharmacokinetics of Repaglinide, Midazolam, and Combined Oral Contraceptive in Patients With Advanced Malignancies
NCT01182194	PHASE1	COMPLETED	Drospirenone/Ethinyl Estradiol (3 mg/0.02 mg) Tablets Under Fasting Conditions.
NCT01182207	PHASE1	COMPLETED	Drospirenone/Ethinyl Estradiol (3 mg/0.02 mg) Tablets Under Non-Fasting Conditions
NCT02885454	PHASE1	COMPLETED	To Evaluate the Effects of Odalasvir and AL-335 With Simeprevir on the Single-Dose Pharmacokinetics of Ethinylestradiol and Drospirenone in Healthy Female Participants
NCT03111511	PHASE1	COMPLETED	A Study in Healthy Female Participants to Investigate the Effect of JNJ-56136379 at Steady-state on the Single-dose Pharmacokinetics of Ethinylestradiol and Drospirenone (Oral Contraceptive) and on the Single-dose Pharmacokinetics of Midazolam (Probe Substrate for Cytochrome P450 3A4)
NCT03126097	PHASE1	TERMINATED	A Study to Investigate the Interaction Between JNJ-64155806 and Ethinylestradiol/Drospirenone in Healthy Females
NCT03890341	PHASE1	WITHDRAWN	Study in Women on the Effect of JNJ-64530440 on Oral Contraceptive and Midazolam, and the Effect of a High-fat Meal on JNJ-64530440
NCT05706753	PHASE1	COMPLETED	A Study of Milvexian in Healthy Adult Females
NCT05985590	PHASE1	COMPLETED	A Study to Investigate the Effects of BMS-986278 on Drospirenone and Ethinyl Estradiol Drug Levels in Healthy Female Participants
NCT06039826	PHASE1	COMPLETED	A Study of LY3437943 in Postmenopausal Female Participants Who Are Overweight or Obese
NCT06233058	PHASE1	UNKNOWN	Drospirenone (3 mg) + Ethinyl Estradiol (0.03 mg) Tablets Relative to Yasmin®
NCT06233071	PHASE1	UNKNOWN	Drospirenone (3 mg) + Ethinyl Estradiol (0.02 mg) Tablets Relative to Yaz®
NCT06250205	PHASE1	COMPLETED	Evaluate the Pharmacokinetics of a Combined Oral Contraceptive (COC) With and Without Obicetrapib
NCT07181343	PHASE1	COMPLETED	A Drug-Drug Interaction Study Between HS-10374 Tablets and Drospirenone and Ethinyl Estradiol Tablets(Yasmin®)
NCT06345586	Not specified	RECRUITING	Drospirenone Only Pills and Cervical Mucus Changes: A Pre- and Post-Bariatric Surgery Study
NCT07061093	Not specified	RECRUITING	Prospective Evaluation on the Role Exerted by Hormonal Contraceptives on 24-h Blood Pressure. A Prospective Observational Study
NCT00302848	Not specified	COMPLETED	European Active Surveillance Study (EURAS)
NCT00633360	Not specified	COMPLETED	The Oral Contraceptive Pill for Premenstrual Worsening of Depression
NCT01432028	Not specified	COMPLETED	Pharmacogenetic Study of Different Hormone Therapies in Recent Menopause Women
NCT01519401	Not specified	COMPLETED	Effect of Two Different Dosages of Ethinyl-estradiol in Association With Drospirenone in Women With Polycystic Ovary Syndrome.
NCT02757469	Not specified	UNKNOWN	Oral Contraceptives as Infertility Treatments for Premature Ovarian Failure
NCT05872425	Not specified	COMPLETED	Efficacy and Safety of Dingkundan Combined With Combination Oral Contraceptives in the Treatment of PCOS
NCT06174792	Not specified	UNKNOWN	Evaluation of the Efficacy and Safety of Drospirenone in the Treatment of Adenomyosis

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

26 molecules share ≥1 primary target. Top 26 by shared-target count:

Molecule	Source	Status	Shared targets
EPLERENONE	ChEMBL + PubChem	Phase 4 (approved)	NR3C2
BUDESONIDE	ChEMBL	Phase 4 (approved)	NR3C2
DEXAMETHASONE	ChEMBL	Phase 4 (approved)	NR3C2
FINERENONE	ChEMBL	Phase 4 (approved)	NR3C2
FLUTICASONE FUROATE	ChEMBL	Phase 4 (approved)	NR3C2
FLUTICASONE PROPIONATE	ChEMBL	Phase 4 (approved)	NR3C2
HYDROCORTISONE	ChEMBL	Phase 4 (approved)	NR3C2
HYDROCORTISONE BUTYRATE	ChEMBL	Phase 4 (approved)	NR3C2
MEDROXYPROGESTERONE	ChEMBL	Phase 4 (approved)	NR3C2
MIFEPRISTONE	ChEMBL	Phase 4 (approved)	NR3C2
PREDNISOLONE	ChEMBL	Phase 4 (approved)	NR3C2
PROGESTERONE	ChEMBL	Phase 4 (approved)	NR3C2
SPIRONOLACTONE	ChEMBL	Phase 4 (approved)	NR3C2
ASOPRISNIL	ChEMBL	Phase 3	NR3C2
BALCINRENONE	ChEMBL	Phase 3	NR3C2
CORTICOSTERONE	ChEMBL	Phase 3	NR3C2
ALDOSTERONE	ChEMBL	Phase 2	NR3C2
LY2623091	ChEMBL	Phase 2	NR3C2
METRIBOLONE	ChEMBL	Phase 2	NR3C2
MT-3995	ChEMBL	Phase 2	NR3C2
ONAPRISTONE	ChEMBL	Phase 2	NR3C2
STANOLONE	ChEMBL	Phase 2	NR3C2
TUROFEXORATE ISOPROPYL	ChEMBL	Phase 2	NR3C2
Enzalutamide	PubChem	Approved	NR3C2
Fludrocortisone	PubChem	Approved	NR3C2
ursodiol	PubChem	Approved	NR3C2