Estradiol Valerate

Summary

Estradiol Valerate (CHEMBL1511) is an approved small molecule; indicated across 11 conditions including primary ovarian failure and hypogonadism.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 11 conditions
• Clinical trials: 59
• Chemistry: 356.5 Da · C23H32O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1511
Name	Estradiol Valerate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	13791
Molecular formula	C23H32O3
Molecular weight	356.5
InChIKey	RSEPBGGWRJCQGY-RBRWEJTLSA-N

SMILES: CCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C

IUPAC name: [(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] pentanoate

Also known as: Climaval, Deladumone, Delestrogen, Estradiol valerate, Estradiol valerate component of natazia, Femtab, NSC-17590, Progynon depot, Progynon-depot-10, Progynova, Valerate d’estradiol, Valerato de estradiol

Patent coverage: 2,316 distinct patent families (7,315 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,272 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Microtubule-associated protein tau, Streptokinase A, Nuclear receptor ROR-gamma, Prelamin-A/C, Histone-lysine N-methyltransferase 2A, Androgen receptor, Estrogen receptor, Thromboxane A2 receptor, Progesterone receptor, Muscarinic acetylcholine receptor M1.

Bioactivity

ChEMBL activities: 8 potent at pChembl ≥ 5 of 17 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
AR	7.34	AC50	46	nM	CHEMBL_ACT_25203281
ESR1	7.08	AC50	82.2	nM	CHEMBL_ACT_25138781
PGR	6.63	AC50	234.4	nM	CHEMBL_ACT_25204214
MAPT	5.8	Potency	1585	nM	CHEMBL_ACT_4013154
P10520	5.42	EC50	3834	nM	CHEMBL_ACT_4921641
LMNA	5.25	Potency	5623	nM	CHEMBL_ACT_3635486
ADORA3	5.17	AC50	6738	nM	CHEMBL_ACT_25198656
PTGS1	5.15	AC50	7046	nM	CHEMBL_ACT_25205147

Target pathways

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

Indications & clinical

Indications

11 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
primary ovarian failure	4	MONDO:0005387	HP:0008209
hypogonadism	4	MONDO:0002146	MONDO:0002146
infertility disorder	3	MONDO:0005047	EFO:0000545
postmenopausal atrophic vaginitis	3	MONDO:0001410	EFO:1001271
polycystic ovary syndrome	0	MONDO:0008487	EFO:0000660

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

Clinical trials

Total trials: 59.

Phase distribution

Phase	Trials
Not specified	25
PHASE4	21
PHASE3	8
PHASE1	3
PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT07499804	PHASE4	RECRUITING	Effect of Tadalafil on Endometrial Thickness and Frozen Embryo Transfer Outcomes
NCT00755963	PHASE4	COMPLETED	Effects of Hormone Replacement Therapy on the Serotonergic System and Mood in Postmenopausal Women
NCT00860964	PHASE4	COMPLETED	A Study of Prevention and Treatment of Postmenopausal Osteoporosis in Chinese Women
NCT01052623	PHASE4	UNKNOWN	Status of Growth Hormone/ Insulin-like Growth Factor-1 (GH/IGF-1) Axis and Growth Failure in Ataxia Telangiectasia (AT)
NCT01218386	PHASE4	COMPLETED	Pretreatment With Estradiol Valerate
NCT01419353	PHASE4	COMPLETED	Programming by Estrogen Treatment in Gonadotropin Releasing Hormone Antagonist Protocol
NCT01500863	PHASE4	COMPLETED	Endometrial Receptivity After GnRH Agonist Triggering
NCT01501448	PHASE4	COMPLETED	Oral Estradiol Valerate Versus Oral Contraceptive Pill in Invitro Fertilization Patients
NCT02330757	PHASE4	UNKNOWN	HRT Versus MOS for Endometrial Preparation Prior to FET in Non PCOS Patients
NCT02352090	PHASE4	COMPLETED	Synthetic vs Natural Estrogen in Combined Oral Contraception
NCT02352597	PHASE4	COMPLETED	Phytoestrogens as an Alternative to Estradiol in Ovulation Induction in PCOS
NCT03060304	PHASE4	UNKNOWN	The Effect of Tamoxifen on Clinical Outcome in Women With Thin Endometrium Undergoing Frozen Thawed Cycle.
NCT03124524	PHASE4	COMPLETED	Treatment Choice in Primary Dysmenorrhea
NCT03620929	PHASE4	UNKNOWN	Estrogen in the Prevention of Adhesion Reformation
NCT03642665	PHASE4	COMPLETED	Natural Versus Artificial Cycle for Frozen-Thawed Embryo Transfer
NCT03789123	PHASE4	UNKNOWN	Effects of Dienogest and Dienogest Plus Estradiol Valerate in Ovarian Endometrioma
NCT03976544	PHASE4	TERMINATED	Natural Cycle Versus Hormone Replacement Therapy Cycle for a Frozen-thawed Embryo Transfer in PGT Patients
NCT04002635	PHASE4	WITHDRAWN	Letrozole for Frozen Embryo Transfer (FET) in Patients With Polycystic Ovary Syndrome (PCOS)
NCT04507022	PHASE4	COMPLETED	The Outcome of Two Protocols Used to Prepare Endometrium for Frozen Embryo Transfer
NCT05197374	PHASE4	COMPLETED	Effect of Estradiol Pretreatment on Antagonist ICSI Cycles
NCT06181305	PHASE4	UNKNOWN	Endometrial Preparation in Frozen Embryo Transfer Cycles
NCT00293059	PHASE3	COMPLETED	Efficacy and Safety Study for the Treatment of Dysfunctional Uterine Bleeding
NCT00307801	PHASE3	COMPLETED	Efficacy and Safety Study for the Treatment of Dysfunctional Uterine Bleeding
NCT00754065	PHASE3	COMPLETED	To Compare SH T00658ID Over Ortho Tri-Cyclen Lo (US/Canada)
NCT00816556	PHASE3	TERMINATED	A Trial to Evaluate the Efficacy of Low Dose Vaginal Estrogens in the Treatment of Atrophic Vaginitis
NCT00909857	PHASE3	COMPLETED	Effect on Primary Dysmenorrhea
NCT02251925	PHASE3	UNKNOWN	Frozen Embryo Transfer in Natural and Hormonal Replacement Cycles
NCT03788681	PHASE3	UNKNOWN	Luteal Phase Support With Estradiol In Poor Responders Undergoing In Vitro Fertilization
NCT03832894	PHASE3	UNKNOWN	Oestradiol Supplementation in Luteal Long Agonist Fresh In Vitro Fertilization/Intra Cytoplasmic Sperm Injection ( IVF/ICSI) Cycle .
NCT07041814	PHASE2	NOT_YET_RECRUITING	A Study Comparing Different Treatment Approaches for the Initiation of Puberty in Girls With Turner Syndrome Using a TRIFECTA-DARED Approach for Rare Diseases
NCT02845388	PHASE2	COMPLETED	Sildenafil Citrate in Frozen Embryo Transfer
NCT05980091	PHASE1	RECRUITING	Optimal Timing of Euploid Day 6 Blastocyst Transfer in Frozen HRT Cycles, Day 6 or Day 7 of Progesterone Administration.
NCT00490308	PHASE1	UNKNOWN	The Influence of Estradiol Supplementation During the Luteal in Patients Undergoing IVF Treatment
NCT04283435	PHASE1	UNKNOWN	Endometrial Effects of Sildenafil in Frozen-Thawed Cycles in Women With Thin Endometrium
NCT04590417	Not specified	ACTIVE_NOT_RECRUITING	Assessment of Drug-drug Interactions Between Feminizing Hormone Therapy and Emtricitabine/Tenofovir Alafenamide Concomitantly for Pre-exposure Prophylaxis Among Transgender Women
NCT05280028	Not specified	RECRUITING	HRT on Overactive Bladder Symptoms, Sexual Function, Depressive Symptoms, Autonomic Function, and Arterial Stiffness
NCT05473273	Not specified	RECRUITING	Descriptive Analysis of Serum Immunological Markers During an Euploid Frozen Embryo Transfer in a Natural Cycle.
NCT07361263	Not specified	RECRUITING	Plasma Oxytocin Response to Oral Estrogens in Healthy Controls and AVP-Deficiency
NCT07379502	Not specified	NOT_YET_RECRUITING	Endometrial Response in Polycystic Ovarian Syndrome Treated With Letrozole Alone or With Added Estradiol Valerate
NCT07419594	Not specified	RECRUITING	Estradiol and Intrusive Memories

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).