List of API Suppliers of Estetrol API listed on PharmaCompass.com

Estetrol

EUROAPI, the leading small molecules API player, provides both API sales & CDMO services.

ACCESS ALL DATA
Browse all information
CHEMISTRY
Discover Molecule Insights

ACTIVE PHARMA INGREDIENTS

3 API Suppliers, 2 USDMF, 1 JDMF, 1 NDC API, 1 Listed Suppliers

3 API Suppliers
2 USDMF
1 JDMF
1 NDC API
1 Listed Suppliers

DEVELOPMENTS

19 Drugs in Development

19 Drugs in Development

INTERMEDIATES

1 Intermediates Suppliers

1 Intermediates Suppliers

FINISHED DOSAGE FORMULATIONS

2 FDF Dossiers, 1 FDA Orange Book, 1 Canada

2 FDF Dossiers
1 FDA Orange Book
1 Canada

DIGITAL CONTENT

1 DATA COMPILATION #PharmaFlow, 4 NEWS #PharmaBuzz

media
1 DATA COMPILATION #PharmaFlow
4 NEWS #PharmaBuzz

MARKET PLACE

8 APIs

marketPlace
8 APIs

PATENTS & EXCLUSIVITIES

4 US Patents, 1 US Exclusivities

patents
4 US Patents
1 US Exclusivities

Synopsis

ACTIVE PHARMA INGREDIENTS

API Suppliers

USDMF

CEP/COS

JDMF

EU WC

KDMF

NDC API

VMF

Listed Suppliers

API REF. PRICE (USD/KG)

$ 0

MARKET PLACE

API

FDF

FINISHED DOSAGE FORMULATIONS

FDF Dossiers

FDA Orange Book

Europe

Canada

Australia

South Africa

Listed Dossiers

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

EDQM

USP

Others

PATENTS & EXCLUSIVITIES

US Patents

US Exclusivities

Health Canada Patents

DIGITAL CONTENT

Data Compilation #PharmaFlow

Stock Recap #PipelineProspector

Weekly News Recap #Phispers

News #PharmaBuzz

GLOBAL SALES INFORMATION

US Medicaid (USD)

Annual Reports (USD Million)

Finished Drug Prices

0RELATED EXCIPIENT COMPANIES

0EXCIPIENTS BY APPLICATIONS

Chemistry

Click the arrow to open the dropdown

Click the button for full data set

Also known as: 15183-37-6, Estetrol anhydrous, 15.alpha.-hydroxyestriol, Enb39r14vf, (8r,9s,13s,14s,15r,16r,17r)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,15,16,17-tetrol, Estetrol (usan)

Molecular Formula

C₁₈H₂₄O₄

Molecular Weight

304.4 g/mol

InChI Key

AJIPIJNNOJSSQC-NYLIRDPKSA-N

FDA UNII

ENB39R14VF

A metabolite of ESTRIOL with a 15-alpha-hydroxyl group. Estetrol can be converted from estriol sulfate or DEHYDROEPIANDROSTERONE SULFATE by the fetal-placental unit.

Estetrol anhydrous is an Estrogen. The mechanism of action of estetrol anhydrous is as an Estrogen Receptor Agonist.

1 2D Structure

Estetrol

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(8R,9S,13S,14S,15R,16R,17R)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,15,16,17-tetrol

2.1.2 InChI

InChI=1S/C18H24O4/c1-18-7-6-12-11-5-3-10(19)8-9(11)2-4-13(12)14(18)15(20)16(21)17(18)22/h3,5,8,12-17,19-22H,2,4,6-7H2,1H3/t12-,13-,14-,15-,16-,17+,18+/m1/s1

2.1.3 InChI Key

AJIPIJNNOJSSQC-NYLIRDPKSA-N

2.1.4 Canonical SMILES

CC12CCC3C(C1C(C(C2O)O)O)CCC4=C3C=CC(=C4)O

2.1.5 Isomeric SMILES

C[C@]12CC[C@H]3[C@H]([C@@H]1[C@H]([C@H]([C@@H]2O)O)O)CCC4=C3C=CC(=C4)O

2.2 Other Identifiers

2.2.1 UNII

ENB39R14VF

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 15 Alpha Hydroxy Estriol

2. 15 Alpha Hydroxyestriol

3. 15 Alpha-hydroxyestriol

4. 15-alpha-hydroxy-estriol

2.3.2 Depositor-Supplied Synonyms

1. 15183-37-6

2. Estetrol Anhydrous

3. 15.alpha.-hydroxyestriol

4. Enb39r14vf

5. (8r,9s,13s,14s,15r,16r,17r)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,15,16,17-tetrol

6. Estetrol (usan)

7. Estetrol [usan]

8. (8r,9s,13s,14s,15r,16r,17r)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6h-cyclopenta[a]phenanthrene-3,15,16,17-tetraol

9. E4

10. (14beta,15alpha,16alpha,17alpha)-estra-1,3,5(10)-triene-3,15,16,17-tetrol

11. E-4

12. Unii-enb39r14vf

13. Estell

14. Estetrolum

15. Oestetrol

16. Donesta

17. Estetrol (anhydrous)

18. 15alpha-hydroxyestriol

19. 15 Alpha-hydroxyestriol

20. Estetrol [inn]

21. Estetrol [who-dd]

22. Mls006010253

23. Schembl145580

24. Estetrol, >=98% (hplc)

25. Chembl1230314

26. Gtpl11591

27. Dtxsid50164888

28. Chebi:142773

29. Bdbm158505

30. Zinc5764481

31. Estetrol (anhydrous) [usan]

32. Who 10439

33. Akos030254521

34. At27982

35. Db12235

36. Ncgc00345819-03

37. Hy-15731

38. Smr004701329

39. Us9034854, E4

40. Cs-0008552

41. D11513

42. J-008852

43. Q5401078

44. Drovelis (ema); ; Estetrol Monohydrate + Drospirenone

45. Lydisilka (ema); ; Estetrol Monohydrate + Drospirenone

46. Nextstellis (us); Estetrol Monohydrate + Drospirenone

47. 1,3,5(10)-estratrien-3,15alpha,16alpha,17beta-tetrol

48. Estra-1(10),2,4-triene-3,15alpha,16alpha,17beta-tetrol

49. Estra-1,3,5(10)-triene-3,15alpha,16alpha,17beta-tetrol

50. 3,15alpha,16alpha,17beta-tetrahydroxyestra-1,3,5(10)-triene

51. Estra-1,3,5(10)-triene-3,15 Alpha,16alpha,17beta-tetrol

52. (15alpha,16alpha,17beta)-estra-1(10),2,4-triene-3,15,16,17-tetrol

53. Estra-1,3,5(10)-triene-3,15,16,17-tetrol, (15alpha,16alpha,17beta)-

54. Estra-1,3,5(10)-triene-3,15.alpha.,16.alpha.,17.beta.-tetrol

55. Estra-1,3,5(10)-triene-3,15,16,17-tetrol, (15.alpha.,16.alpha.,17.beta.)-

56. 4oh

2.4 Create Date

2005-08-08

3 Chemical and Physical Properties

Molecular Formula	C₁₈H₂₄O₄
Molecular Weight	304.4 g/mol
XLogP3	1.5
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	0
Exact Mass	304.16745924 g/mol
Monoisotopic Mass	304.16745924 g/mol
Topological Polar Surface Area	80.9 Å²
Heavy Atom Count	22
Formal Charge	0
Complexity	441
Isotope Atom Count	0
Defined Atom Stereocenter Count	7
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

Estetrol is indicated in combination with drospirenone for the prevention of pregnancy.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Estetrol prevents pregnancy by suppressing ovulation.

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

ESTETROL ANHYDROUS

5.2.2 FDA UNII

ENB39R14VF

5.2.3 Pharmacological Classes

Mechanisms of Action [MoA] - Estrogen Receptor Agonists

5.3 Absorption, Distribution and Excretion

Absorption

Estetrol is rapidly absorbed from the gastrointestinal tract. The Cmax of estetrol is 18 ng/mL according to the results of a pharmacokinetic study, with an AUC of 36.4 ngh/mL. When estetrol and drospirenone are taken in a single product, maximum serum concentrations of approximately 48.7 ng/mL are achieved within 1-3 h. Bioavailability of the combination ranges between 76 and 85%. The Tmax can range from 0.5 to 2 hours and time to steady state is approximately 4 days, according to the results of one clinical study.

Route of Elimination

Estrogens are generally excreted as sulfated and glucuronidated derivatives. Approximately 69% of a dose of estetrol is excreted in the urine, and about 22% is excreted in the feces as unchanged drug.

Volume of Distribution

Limited distribution of estetrol into red blood cells has been demonstrated.

5.4 Metabolism/Metabolites

Estretol is heavily metabolized after oral administration. Phase 2 metabolism of estrogen forms glucuronide and sulfate conjugates with negligible in-vitro estrogenic activity. In vitro metabolism studies demonstrate that UGT2B7 catalyzes the formation of E4-16-glucuronide. Estetrol is combined with [drospirenone] in a product. The hepatic cytochrome enzyme CYP3A4 metabolizes drospirenone to two primary metabolites: the acid form of drospirenone through the opening of the lactone ring and the 4,5 dihydrodrospirenone formed by reduction, followed by sulfation. Both metabolites are pharmacologically inactive.

5.5 Biological Half-Life

The elimination half-life of estetrol is approximately 27 hours. Half-life may range between 19-40 hours.

5.6 Mechanism of Action

Estetrol is a synthetic analogue of a naturally occurring estrogen present during pregnancy, demonstrating selectivity for both estrogen receptor- (ER-) and ER- and suppressing ovulation. Estetrol binds with a low to moderate affinity human estrogen receptor alpha (ER alpha) and ER beta with a preference for ER alpha. Estetrol demonstrates a unique mechanism of action via tissue selective activity, showing estrogen receptor agonist activity on the vagina, the uterus and the endometrium, and negative estrogenic activity on breast tissue.

API SUPPLIERS