Telapristone acetate

Identification

Name
Telapristone acetate
Accession Number
DB05253
Description

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

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 505.655
Monoisotopic: 505.28282336
Chemical Formula
C31H39NO5
Synonyms
  • 17alpha-Acetoxy-11beta-(4-(dimethylamino)phenyl)-21-methoxy-19-norpregna-4,9-dien-3,20-dione
  • Telapristone acetate
External IDs
  • CDB 4124
  • CDB-4124
  • RU 44675

Pharmacology

Pharmacology
Accelerate your drug discovery research with the industry’s only fully connected ADMET dataset, ideal for:
Machine Learning
Data Science
Drug Discovery
Accelerate your drug discovery research with our fully connected ADMET dataset
Learn more
Indication

For the treatment of uterine fibroids and endometriosis.

Contraindications & Blackbox Warnings
Contraindications
Contraindications & Blackbox Warnings
With our commercial data, access important information on dangerous risks, contraindications, and adverse effects.
Learn more
Our Blackbox Warnings cover Risks, Contraindications, and Adverse Effects
Learn more
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
Adverse Effects
Medicalerrors
Reduce medical errors
and improve treatment outcomes with our comprehensive & structured data on drug adverse effects.
Learn more
Reduce medical errors & improve treatment outcomes with our adverse effects data
Learn more
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

Products

Products
Comprehensive & structured drug product info
From application numbers to product codes, connect different identifiers through our commercial datasets.
Learn more
Easily connect various identifiers back to our datasets
Learn more
International/Other Brands
Proellex

Categories

Drug Categories
Classification
Not classified

Chemical Identifiers

UNII
1K9EYK92PQ
CAS number
198414-31-2
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
(1R,3aS,3bS,10R,11aS)-10-[4-(dimethylamino)phenyl]-1-(2-methoxyacetyl)-11a-methyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl acetate
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]

References

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

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentAnemia / Uterine Leiomyomas2
3TerminatedTreatmentUterine Leiomyomas4
3WithdrawnTreatmentUterine Leiomyomas1
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

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
Water Solubility0.00556 mg/mLALOGPS
logP4.63ALOGPS
logP4.45ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)18.42ChemAxon
pKa (Strongest Basic)4.89ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area72.91 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity144.89 m3·mol-1ChemAxon
Polarizability56.9 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

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 18:09 / Updated on February 21, 2021 18:51