Telapristone acetate
Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- Telapristone acetate
- DrugBank Accession Number
- DB05253
- Background
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
- 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
- Indication
For the treatment of uterine fibroids and endometriosis.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- 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.
Target Actions Organism UProgesterone receptor Not Available Humans - 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- 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
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Proellex
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
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
- External Links
- PubChem Substance
- 347910049
- ChemSpider
- 7981950
- ChEMBL
- CHEMBL2105694
- Wikipedia
- Proellex
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample data3 Terminated Treatment Anemia / Uterine Fibroids (Leiomyomas) 2 somestatus stop reason just information to hide 3 Terminated Treatment Uterine Fibroids (Leiomyomas) 4 somestatus stop reason just information to hide 3 Withdrawn Treatment Uterine Fibroids (Leiomyomas) 1 somestatus stop reason just information to hide 2 Completed Prevention Brca1 Mutation Carrier / Brca2 Mutation Carrier / Breast Cancer, Stage IA / Breast Cancer, Stage IB / Ductal Breast Carcinoma In Situ / Lobular Breast Carcinoma In Situ / Stage 0 Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer 1 somestatus stop reason just information to hide 2 Completed Treatment Endometriosis 1 somestatus stop reason just information to hide
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
Property Value Source Water Solubility 0.00556 mg/mL ALOGPS logP 4.63 ALOGPS logP 4.45 Chemaxon logS -5 ALOGPS pKa (Strongest Acidic) 18.42 Chemaxon pKa (Strongest Basic) 4.89 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 72.91 Å2 Chemaxon Rotatable Bond Count 7 Chemaxon Refractivity 144.89 m3·mol-1 Chemaxon Polarizability 56.9 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 239.9765848 predictedDarkChem Lite v0.1.0 [M+H]+ 240.3589848 predictedDarkChem Lite v0.1.0 [M+Na]+ 239.9281848 predictedDarkChem Lite v0.1.0
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General 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. Depending on the isoform, progesterone receptor functions as a transcriptional activator or repressor
- Specific Function
- ATPase binding
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
Drug created at November 18, 2007 18:09 / Updated at February 21, 2021 18:51