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ACTIVE PHARMA INGREDIENTS

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Chemistry

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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

Telapristone Acetate

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 Formula	C₃₁H₃₉NO₅
Molecular Weight	505.6 g/mol
XLogP3	3.4
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	7
Exact Mass	505.28282334 g/mol
Monoisotopic Mass	505.28282334 g/mol
Topological Polar Surface Area	72.9 Å²
Heavy Atom Count	37
Formal Charge	0
Complexity	1020
Isotope Atom Count	0
Defined Atom Stereocenter Count	5
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

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.

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