Telapristone acetate
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.
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- 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
Phase Status Purpose Conditions Count 3 Terminated Treatment Anemia / Uterine Fibroids (Leiomyomas) 2 3 Terminated Treatment Uterine Fibroids (Leiomyomas) 4 3 Withdrawn Treatment Uterine Fibroids (Leiomyomas) 1 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 2 Completed Treatment Endometriosis 1
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
- 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 at November 18, 2007 18:09 / Updated at February 21, 2021 18:51