Telapristone acetate

Identification

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Name
Telapristone acetate
Accession Number
DB05253
Type
Small Molecule
Groups
Investigational
Description

Telapristone acetate, an orally-available, selective progesterone receptor modulator, is in development to alleviate symptoms associated with both uterine fibroids and endometriosis.

Structure
Thumb
Synonyms
  • 17alpha-Acetoxy-11beta-(4-(dimethylamino)phenyl)-21-methoxy-19-norpregna-4,9-dien-3,20-dione
External IDs
CDB 4124 / CDB-4124 / RU 44675
International/Other Brands
Proellex
Categories
UNII
1K9EYK92PQ
CAS number
198414-31-2
Weight
Average: 505.655
Monoisotopic: 505.28282336
Chemical Formula
C31H39NO5
InChI Key
JVBGZFRPTRKSBB-MJBQOYBXSA-N
InChI
InChI=1S/C31H39NO5/c1-19(33)37-31(28(35)18-36-5)15-14-27-25-12-8-21-16-23(34)11-13-24(21)29(25)26(17-30(27,31)2)20-6-9-22(10-7-20)32(3)4/h6-7,9-10,16,25-27H,8,11-15,17-18H2,1-5H3/t25-,26+,27-,30-,31-/m0/s1
IUPAC Name
SMILES
[H][C@@]12CC[C@](OC(C)=O)(C(=O)COC)[C@@]1(C)C[C@H](C1=CC=C(C=C1)N(C)C)C1=C3CCC(=O)C=C3CC[C@@]21[H]

Pharmacology

Indication

For the treatment of uterine fibroids and endometriosis.

Pharmacodynamics

Patients receiving Proellex saw improvements in key symptoms associated with uterine fibroids, namely reduced pain and bleeding, as well as effects on bone retention.

Mechanism of action

Proellex selectively blocks the progesterone receptor thus avoiding the adverse effects of GnRH agonists associated with the induction of a low estrogen, menopausal-like state in women.

TargetActionsOrganism
UProgesterone receptorNot AvailableHumans
Absorption

Orally-available

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

References

General References
Not Available
External Links
PubChem Substance
347910049
ChemSpider
7981950
ChEMBL
CHEMBL2105694
Wikipedia
Proellex

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAbsorption / Excretion / Metabolism1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableImpaired Hepatic Function1
1CompletedBasic ScienceComparison of 2 Different Formulations of 12 mg Proellex Vaginal Capsules1
1CompletedBasic SciencePharmacokinetics1
1CompletedTreatmentDrug Drug Interaction (DDI)1
1CompletedTreatmentHealthy Volunteers3
1TerminatedTreatmentAmenorrhea1
1, 2CompletedTreatmentAmenorrhea1
1, 2CompletedTreatmentUterine Leiomyomata1
1, 2TerminatedNot AvailableImpaired Renal Function1
2Active Not RecruitingPreventionBrca1 Mutation Carrier / Brca2 Mutation Carrier / Ductal Breast Carcinoma In Situ / Lobular Breast Carcinoma In Situ / Stage 0 Breast Cancer / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer1
2Active Not RecruitingTreatmentStage IA Breast Cancer / Stage IB Breast Cancer / Stage II Breast Cancer1
2CompletedTreatmentEndometriosis1
2CompletedTreatmentUterine Leiomyomas7
2TerminatedPreventionUterine Leiomyomas1
2TerminatedTreatmentEndometriosis2
2TerminatedTreatmentUterine Leiomyomas2
2WithdrawnTreatmentEndometriosis1
3TerminatedTreatmentAnemias / Uterine Leiomyomas2
3TerminatedTreatmentUterine Leiomyomas4
3WithdrawnTreatmentUterine Leiomyomas1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name
PGR
Uniprot ID
P06401
Uniprot Name
Progesterone receptor
Molecular Weight
98979.96 Da

Drug created on November 18, 2007 11:09 / Updated on September 02, 2019 18:10