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    Telapristone Acetate

    ACTIVE PHARMA INGREDIENTS

    DIGITAL CONTENT

    PharmaCompass
    Xls

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    2D Structure
    Also known as: Proellex, 198414-31-2, Telapristone acetate [usan], 1k9eyk92pq, Zpv-200, Ru-44675
    Molecular Formula
    C31H39NO5
    Molecular Weight
    505.6  g/mol
    InChI Key
    JVBGZFRPTRKSBB-MJBQOYBXSA-N
    FDA UNII
    1K9EYK92PQ
    Telapristone Acetate is the acetate form of the 21-substituted-19-nor-progestin telapristone, an orally available selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Upon oral administration, CDB-4124 competitively binds to the progesterone receptor (PR) in progesterone-responsive tissue and inhibits PR-mediated gene expression. This interferes with progesterone activity in the reproductive system. As a result, this agent may suppress ovulation and inhibit proliferation of endometrial tissue. Also, this agent may prevent cell growth and induce apoptosis in estrogen receptor (ER) and PR-positive breast cancer cells through a reduction in progesterone levels, ER downregulation and a suppression of the expression of cyclin-dependent kinases (CDK) 2 and 4, ultimately leading to G1/S cell cycle arrest. Unlike some other SPRMs, this agent does not exert any estrogenic, androgenic, anti-estrogenic, and anti-androgenic activities.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    [(8S,11R,13S,14S,17R)-11-[4-(dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
    2.1.2 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
    2.1.3 InChI Key
    JVBGZFRPTRKSBB-MJBQOYBXSA-N
    2.1.4 Canonical SMILES
    CC(=O)OC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC
    2.1.5 Isomeric SMILES
    CC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H](C3=C4CCC(=O)C=C4CC[C@@H]23)C5=CC=C(C=C5)N(C)C)C)C(=O)COC
    2.2 Other Identifiers
    2.2.1 UNII
    1K9EYK92PQ
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Cdb 4124

    2. Cdb-4124

    3. Cdb4124

    4. Proellex

    2.3.2 Depositor-Supplied Synonyms

    1. Proellex

    2. 198414-31-2

    3. Telapristone Acetate [usan]

    4. 1k9eyk92pq

    5. Zpv-200

    6. Ru-44675

    7. 17alpha-acetoxy-11beta-(4-(dimethylamino)phenyl)-21-methoxy-19-norpregna-4,9-dien-3,20-dione

    8. Telapristone Acetate (usan)

    9. (8s,11r,13s,14s,17r)-11-(4-(dimethylamino)phenyl)-17-(2-methoxyacetyl)-13-methyl-3-oxo-2,3,6,7,8,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl Acetate

    10. [(8s,11r,13s,14s,17r)-11-[4-(dimethylamino)phenyl]-17-(2-methoxyacetyl)-13-methyl-3-oxo-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] Acetate

    11. Unii-1k9eyk92pq

    12. Ccris 9331

    13. Cdb 4124

    14. Schembl374762

    15. Chembl2105694

    16. Cdb4124

    17. Dtxsid60173587

    18. Chebi:188804

    19. Telapristone Acetate [who-dd]

    20. Db05253

    21. D09972

    22. Q7695644

    23. 11.beta.-(4-(dimethylamino)phenyl)-17-acetoxy-21-methoxy- 19-norpregna-4,9-diene-3,20-dione

    24. 19-norpregna-4,9-diene-3,20-dione, 17-(acetyloxy)-11-(4-(dimethylamino)phenyl)-21-methoxy-, (11.beta.)-

    25. 19-norpregna-4,9-diene-3,20-dione, 17-(acetyloxy)-11-(4-(dimethylamino)phenyl)-21-methoxy-, (11beta)-

    2.4 Create Date
    2006-10-25
    3 Chemical and Physical Properties
    Molecular Weight 505.6 g/mol
    Molecular Formula C31H39NO5
    XLogP33.4
    Hydrogen Bond Donor Count0
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count7
    Exact Mass505.28282334 g/mol
    Monoisotopic Mass505.28282334 g/mol
    Topological Polar Surface Area72.9 Ų
    Heavy Atom Count37
    Formal Charge0
    Complexity1020
    Isotope Atom Count0
    Defined Atom Stereocenter Count5
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    For the treatment of uterine fibroids and endometriosis.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

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

    5.2 Absorption, Distribution and Excretion

    Absorption

    Orally-available

    5.3 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.