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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
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 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.


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ABOUT THIS PAGE

Telapristone Acetate Manufacturers

A Telapristone Acetate manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Telapristone Acetate, including repackagers and relabelers. The FDA regulates Telapristone Acetate manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Telapristone Acetate API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

Telapristone Acetate Suppliers

A Telapristone Acetate supplier is an individual or a company that provides Telapristone Acetate active pharmaceutical ingredient (API) or Telapristone Acetate finished formulations upon request. The Telapristone Acetate suppliers may include Telapristone Acetate API manufacturers, exporters, distributors and traders.

click here to find a list of Telapristone Acetate suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.

Telapristone Acetate USDMF

A Telapristone Acetate DMF (Drug Master File) is a document detailing the whole manufacturing process of Telapristone Acetate active pharmaceutical ingredient (API) in detail. Different forms of Telapristone Acetate DMFs exist exist since differing nations have different regulations, such as Telapristone Acetate USDMF, ASMF (EDMF), JDMF, CDMF, etc.

A Telapristone Acetate DMF submitted to regulatory agencies in the US is known as a USDMF. Telapristone Acetate USDMF includes data on Telapristone Acetate's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Telapristone Acetate USDMF is kept confidential to protect the manufacturer’s intellectual property.

click here to find a list of Telapristone Acetate suppliers with USDMF on PharmaCompass.

Telapristone Acetate GMP

Telapristone Acetate Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Telapristone Acetate GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Telapristone Acetate GMP manufacturer or Telapristone Acetate GMP API supplier for your needs.

Telapristone Acetate CoA

A Telapristone Acetate CoA (Certificate of Analysis) is a formal document that attests to Telapristone Acetate's compliance with Telapristone Acetate specifications and serves as a tool for batch-level quality control.

Telapristone Acetate CoA mostly includes findings from lab analyses of a specific batch. For each Telapristone Acetate CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Telapristone Acetate may be tested according to a variety of international standards, such as European Pharmacopoeia (Telapristone Acetate EP), Telapristone Acetate JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Telapristone Acetate USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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