Telapristone Acetate

Summary

Telapristone Acetate (CHEMBL2105694) is a phase-3 clinical-stage small molecule; indicated across 6 conditions including uterine corpus leiomyoma and endometriosis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 6 conditions
• Clinical trials: 30
• Chemistry: 505.6 Da · C31H39NO5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105694
Name	Telapristone Acetate
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	9806190
Molecular formula	C31H39NO5
Molecular weight	505.6
InChIKey	JVBGZFRPTRKSBB-MJBQOYBXSA-N

SMILES: CC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC

IUPAC name: [(8S,11R,13S,14S,17R)-11-[4-(dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate

Also known as: CDB-4124, Proellextm, Proellex, Progenta, RU 44675, RU-44675, Telapristone acetate, ZPV-200, TELAPRISTONE ACETATE

Patent coverage: 82 distinct patent families (236 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

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

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

Indications & clinical

Indications

6 indications (0 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
uterine corpus leiomyoma	3	MONDO:0007886	EFO:0000731
endometriosis	2	MONDO:0005133	EFO:0001065
breast neoplasm	2	MONDO:0021100	MONDO:0007254
liver disorder	1	MONDO:0005154	EFO:0001421
kidney disorder	1	MONDO:0005240	EFO:0003086
amenorrhea	1	MONDO:0001836	MONDO:0001836

Clinical trials

Total trials: 30.

Phase distribution

Phase	Trials
PHASE2	13
PHASE3	7
PHASE1	7
PHASE1/PHASE2	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00702702	PHASE3	TERMINATED	Safety and Efficacy of Proellex in Pre-menopausal Anemic Women With Symptomatic Uterine Fibroids
NCT00735553	PHASE3	TERMINATED	Evaluating the Safety and Efficacy of Proellex® (CDB-4124) in Premenopausal Women With Symptomatic Uterine Fibroids
NCT00737282	PHASE3	TERMINATED	Multicenter Study Evaluating the Safety of Proellex® in Premenopausal Women With Uterine Fibroids
NCT00785356	PHASE3	TERMINATED	Safety and Efficacy of Proellex in Pre-Menopausal Anemic Women With Symptomatic Uterine Fibroids
NCT00853567	PHASE3	TERMINATED	Evaluating the Safety and Efficacy of Proellex® in Premenopausal Women With Symptomatic Uterine Fibroids
NCT00874302	PHASE3	WITHDRAWN	Safety and Efficacy of 25 and 50 mg Doses of Proellex® in Treating the Recurrence of Uterine Fibroid Symptoms
NCT01069120	PHASE3	TERMINATED	Safety of 25 and 50 mg Proellex® in the Treatment of Women With Symptomatic Uterine Fibroids
NCT00556075	PHASE2	TERMINATED	Safety and Efficacy Study to Evaluate Proellex in the Treatment of Premenopausal Women With Symptomatic Endometriosis
NCT00683917	PHASE2	TERMINATED	Pharmacokinetics, Safety and Efficacy Study of Proellex in Pre-menopausal Women With Symptomatic Uterine Fibroids
NCT00787618	PHASE1/PHASE2	TERMINATED	Evaluate PK and Safety of Proellex® in Females With Various Stages of Impaired Renal Function and Healthy Females
NCT00882258	PHASE2	COMPLETED	Study of Proellex in Pre-menopausal Women With Symptomatic Uterine Fibroids
NCT00958893	PHASE2	TERMINATED	An Extension Study Evaluating Safety and Efficacy of Proellex® In Women Who Have Previously Completed ZPU 003 Ext
NCT01069094	PHASE1/PHASE2	COMPLETED	A Study of Progenta (CDB-4124) in Pre-menopausal Women With Symptomatic Leiomyomata
NCT01187043	PHASE1/PHASE2	COMPLETED	Determination of the Lowest, Safe and Effective Dose of Proellex
NCT01451424	PHASE2	COMPLETED	Evaluation of Safety, Pharmacokinetics, and Efficacy of Proellex Administered Vaginally in Women With Uterine Fibroids
NCT01728454	PHASE2	COMPLETED	Safety and Efficacy of Telapristone Acetate (Proellex®) in the Treatment of Pre-Menopausal Women With Confirmed, Symptomatic Endometriosis
NCT01739621	PHASE2	COMPLETED	Safety, Pharmacokinetics and Efficacy of Proellex® (Telapristone Acetate) Administered Vaginally in the Treatment of Premenopausal Women With Uterine Fibroids Who Have Completed ZPV-200
NCT01800422	PHASE2	UNKNOWN	Oral CDB-4124 vs. Placebo in Stage I-II Primary Breast Cancer
NCT01961908	PHASE2	WITHDRAWN	Open-Label Extension Study to ZPE-202
NCT02301897	PHASE2	COMPLETED	A Multi-Center, Parallel Design, Randomized, Double-Blind Study to Evaluate the Safety and Efficacy of 6 and 12 mg Proellex® (Telapristone Acetate) Administered Orally in the Treatment of Premenopausal Women With Confirmed Symptomatic Uterine Fibroids
NCT02314156	PHASE2	COMPLETED	Transdermal or Oral Telapristone Acetate in Treating Patients Undergoing Mastectomy
NCT02323646	PHASE2	COMPLETED	Safety and Efficacy of Telapristone Acetate (Proellex®) Administered Vaginally for the Treatment of Uterine Fibroids
NCT02811159	PHASE2	TERMINATED	An Extension Study of 12 mg Proellex® (Telapristone Acetate) Administered Orally in the Treatment of Premenopausal Women With Confirmed Symptomatic Uterine Fibroids
NCT00619385	PHASE1	COMPLETED	A Safety and Pharmacokinetic Study of Proellex®
NCT00741273	PHASE1	COMPLETED	Evaluate the Safety and PK of Proellex® in Female Patients With Impaired Hepatic Function and Healthy Adults
NCT00741468	PHASE1	COMPLETED	Open-Label, Multiple-Dose, Non-Randomized Study to Assess Drug-Drug Interactions of Proellex® in Female Subjects
NCT00749879	PHASE1	COMPLETED	Crossover Study of the Safety and PK Properties of Proellex®
NCT00881062	PHASE1	COMPLETED	Investigate Absorption, Metabolism and Excretion of [14C}-Proellex Following Single Oral Dose in Healthy Females
NCT00881608	PHASE1	TERMINATED	Study to Evaluate Menses Induction in Women Administered Proellex
NCT01067807	PHASE1	COMPLETED	Proellex Pharmacokinetics Bridging Study

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

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