Prasterone

Summary

Prasterone (CHEMBL90593) is an approved small-molecule androgen (ATC A14AA07); indicated across 32 conditions including postmenopausal atrophic vaginitis and rheumatoid arthritis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A14AA07 (+1 more)
• Indications: 32 conditions
• Clinical trials: 97
• Chemistry: 288.4 Da · C19H28O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL90593
Name	Prasterone
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5881
ChEBI	CHEBI:28689
ATC	A14AA07, G03XX01
Molecular formula	C19H28O2
Molecular weight	288.4
InChIKey	FMGSKLZLMKYGDP-USOAJAOKSA-N

SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC=C4[C@@]3(CC[C@@H](C4)O)C

IUPAC name: (3S,8R,9S,10R,13S,14S)-3-hydroxy-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-one

ChEBI definition: An androstanoid that is androst-5-ene substituted by a β-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands.

Pharmacological roles (ChEBI): androgen.

Other ChEBI roles (chemical / environmental): human metabolite, mouse metabolite.

Also known as: Biolaif, Dehydroandrosterone, Dehydroepiandrosterone, Dehydroisoandrosterone, Dhea, EM-760, Enzymatic therapy, Isoandrostenolone, Intrarosa, Natrol dhea, NSC-9896, Prasterona

Patent coverage: 7,604 distinct patent families (23,422 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
	Glycine Receptor (All subtypes)	Inhibition

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Prelamin-A/C, Peripheral myelin protein 22, Menin/Histone-lysine N-methyltransferase MLL, Corticosteroid-binding globulin, Beta-glucuronidase, Sex hormone-binding globulin, Cytochrome P450 3A4, Glucose-6-phosphate 1-dehydrogenase, G-protein coupled bile acid receptor 1.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SHBG	7.84	Kd	14.45	nM	CHEMBL_ACT_2155704
GPBAR1	5.48	EC50	3330	nM	CHEMBL_ACT_2117834
G6PD	5.21	Ki	6200	nM	CHEMBL_ACT_2609798
G6PD	5.05	Ki	8900	nM	CHEMBL_ACT_2609797
SERPINA6	5	Ki	10000	nM	CHEMBL_ACT_969296

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

32 indications (6 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
postmenopausal atrophic vaginitis	4	MONDO:0001410	EFO:1001271
rheumatoid arthritis	4	MONDO:0008383	EFO:0000685
osteoarthritis	4	MONDO:0005178	MONDO:0005178
infertility disorder	3	MONDO:0005047	EFO:0000545
malaria	3	MONDO:0005136	EFO:0001068
physiological sexual disorder	3	MONDO:0002134	EFO:0004714
breast neoplasm	3	MONDO:0021100	MONDO:0007254
adrenocortical insufficiency	3	MONDO:0000004	EFO:0009491
female reproductive system neoplasm	3	MONDO:0021148	MONDO:0021148
chronic primary adrenal insufficiency	3	MONDO:0015129	MONDO:0015129
anorexia nervosa	3	MONDO:0005351	MONDO:0005351
systemic lupus erythematosus	3	MONDO:0007915	MONDO:0007915
substance withdrawal syndrome	2	MONDO:0005567	EFO:0005800
Crohn disease	2	MONDO:0005011	EFO:0000384
HIV infectious disease	2	MONDO:0005109	EFO:0000764
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
erectile dysfunction	2	MONDO:0005362	EFO:0004234
primary ovarian failure	2	MONDO:0005387	EFO:0004266
post-traumatic stress disorder	2	MONDO:0005146	EFO:0001358
depressive disorder	2	MONDO:0002050	MONDO:0002050
myotonic dystrophy	2	MONDO:0016107	MONDO:0016107
synovial sarcoma	1	MONDO:0010434	EFO:0001376
type 1 diabetes mellitus	0	MONDO:0005147	MONDO:0005147

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

Clinical trials

Total trials: 97.

Phase distribution

Phase	Trials
PHASE3	30
Not specified	19
PHASE2	17
PHASE2/PHASE3	11
PHASE4	7
PHASE1	7
EARLY_PHASE1	4
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05562518	PHASE4	ACTIVE_NOT_RECRUITING	GRACE-trial: a Randomized Active-controlled Trial for vulvovaGinal atRophy in breAst Cancer Patients on Endocrine Therapy.
NCT00543166	PHASE4	UNKNOWN	Sex Steroids in Sjögren’s Syndrome: Effect of Substitution Treatment on Fatigue
NCT00664053	PHASE4	COMPLETED	Effects of DHEA/Exercise on Bone, Muscle and Balance
NCT02766764	PHASE4	UNKNOWN	Combined Dehydropeiandrosterone and Growth Hormone in Women With Expected Poor Ovarian Response Undergoing ICSI
NCT02866253	PHASE4	COMPLETED	Dehydroepiandrosterone (DHEA)Supplementation Pre-IVF(In Vitro Fertilization) Cycles
NCT03418363	PHASE4	COMPLETED	How DHEA Supplements Affect Coagulation in Women Using Birth Control Pills
NCT03568604	PHASE4	COMPLETED	Changes to Vulva, Vestibule, Urethral Meatus and Vagina 20 Weeks Post Daily Prasterone in Women With Dyspareunia
NCT06611514	PHASE3	NOT_YET_RECRUITING	Effect of Intravaginal Prasterone on Symptoms of Genitourinary Syndrome of Menopause (GSM) in Women in Menopause With Previous Breast Cancer
NCT00004313	PHASE3	COMPLETED	Phase III Randomized, Double-Blind, Placebo-Controlled Study of Dehydroepiandrosterone Replacement for Primary Adrenal Insufficiency
NCT00004662	PHASE3	COMPLETED	Phase III Randomized, Double-Blind, Placebo-Controlled Study of Dehydroepiandrosterone in Women With Active Systemic Lupus Erythematosus
NCT00004795	PHASE2/PHASE3	COMPLETED	Phase II/III Randomized, Double-Blind, Placebo-Controlled Study of Dehydroepiandrosterone in Women With Mild to Moderate Systemic Lupus Erythematosus
NCT00053560	PHASE3	UNKNOWN	To Assess Prevention of Bone Loss in Women With Lupus Receiving Treatment With Glucocorticoids
NCT00082511	PHASE3	COMPLETED	GL701 (Prestara™) in Women With Systemic Lupus Erythematosus Receiving Treatment With Glucocorticoids
NCT00167609	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of DHEA for Myotonic Dystrophy
NCT00182975	PHASE3	COMPLETED	Effects of Dehydroepiandrosterone (DHEA) in Humans
NCT00189124	PHASE2/PHASE3	COMPLETED	Dehydroepiandrosterone (DHEA) in Systemic Lupus Erythematosus (SLE) for Coronary Artery Disease (CAD) Prevention
NCT00205686	PHASE3	COMPLETED	Effects of DHEA and Exercise in the Elderly
NCT00248989	PHASE3	COMPLETED	Effect of DHEA on Skin Aging in Postmenopausal Women
NCT00289926	PHASE3	COMPLETED	Efficacy and Safety of Oral DHEA Therapy for Postmenopausal Women on Sexual Function, Wellbeing and Vasomotor Symptoms
NCT00310791	PHASE2/PHASE3	COMPLETED	Adrenal and Gonadal Hormone Replacement in Anorexia Nervosa
NCT00317148	PHASE2/PHASE3	COMPLETED	Effect of Dehydroepiandrosterone (DHEA) on Hot Flashes in Postmenopausal Women
NCT00419913	PHASE2/PHASE3	TERMINATED	A Trial of Dehydroepiandrosterone (DHEA) Treatment for in Vitro Fertilization (IVF)
NCT00575341	PHASE3	COMPLETED	Dehydroepiandrosterone Substitution in Adolescent and Young Women With Central Adrenal Insufficiency
NCT00581087	PHASE3	UNKNOWN	Study of Dehydroepiandrosterone (DHEA) in Respiratory Pulmonary Hypertension in Adults
NCT00650754	PHASE2/PHASE3	TERMINATED	Study of Oral Dehydroepiandrosterone(DHEA) to Treat Previously Unexplained Infertility
NCT00948857	PHASE2/PHASE3	TERMINATED	Dehydroepiandrosterone (DHEA) Treatment and Premature Ovarian Failure (POF)
NCT01256671	PHASE3	COMPLETED	DHEA Against Vaginal Atrophy - Safety Study of 12 Months
NCT01256684	PHASE3	COMPLETED	DHEA Against Vaginal Atrophy - 3-Month Efficacy Study
NCT01358760	PHASE3	COMPLETED	Dehydroepiandrosterone (DHEA) Against Vaginal Atrophy
NCT01376349	PHASE3	COMPLETED	Prasterone (Dehydroepiandrosterone) in Treating Postmenopausal Cancer Survivors With Vaginal Symptoms
NCT01452373	PHASE3	COMPLETED	Dehydroepiandrosterone (DHEA) + Acolbifene Against Vasomotor Symptoms (Hot Flushes) in Postmenopausal Women
NCT01535872	PHASE3	COMPLETED	Study of Dehydroepiandrosterone Treatment for Poor Responders in In Vitro Fertilization Patients
NCT01572025	PHASE3	COMPLETED	Dehydroepiandrosterone (DHEA) Intervention To Treat Ovarian Aging
NCT01724242	PHASE2/PHASE3	WITHDRAWN	Vaginal DHEA for Women After Breast Cancer
NCT01846442	PHASE3	COMPLETED	Topical DHEA Against Vaginal Atrophy
NCT02013544	PHASE3	COMPLETED	Intravaginal Prasterone (DHEA) Against Vulvovaginal Atrophy Associated With Menopause
NCT02150330	PHASE3	COMPLETED	Effects of Dehydroepiandrosterone Supplementation on Cumulus Cells Gene Expression Under Controlled Ovarian Hyper-stimulation in Patients With Diminished Ovarian Reserve
NCT02151006	PHASE3	COMPLETED	Does Dehydro Epiandrosterone (DHEA) Improve Pregnancy Rate in Women Undergoing IVF/ICSI With Expected Poor Ovarian Response?
NCT02561793	PHASE3	UNKNOWN	DHEA Versus Placebo in Women With Poor Ovarian Response
NCT02736591	PHASE3	UNKNOWN	Dehydroepiandrosterone Versus Growth Hormone in Women Undergoing ICSI With Expected Poor Ovarian Response

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).