NAV

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
3D
Similar Structures
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
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Pharmacology

Indication

For the treatment of uterine fibroids and endometriosis.

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Contraindications & Blackbox Warnings
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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.

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
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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

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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
PubChem Substance
347910049
ChemSpider
7981950
ChEMBL
CHEMBL2105694
Wikipedia
Proellex

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentAnemia / Uterine Fibroids (Leiomyomas)2
3TerminatedTreatmentUterine Fibroids (Leiomyomas)4
3WithdrawnTreatmentUterine Fibroids (Leiomyomas)1
2CompletedPreventionBrca1 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 Cancer1
2CompletedTreatmentEndometriosis1

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
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4i-0000940000-a6bee635b3daef27e83b
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-006x-9000510000-cf6a407b53b30d02f847
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0233-0119600000-5648761794959c44704e
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0zfu-9000700000-45e959fba2541e38b088
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-052f-9000110000-b59092e407c0e49f0b7e
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-001j-1954310000-75810e3d481583f5c56f
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-239.9765848
predicted
DarkChem Lite v0.1.0
[M+H]+240.3589848
predicted
DarkChem Lite v0.1.0
[M+Na]+239.9281848
predicted
DarkChem Lite v0.1.0

Targets

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Details1. Progesterone receptor
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