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Chemistry

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Also known as: 198481-32-2, Bazedoxifene [inn], Tse-424, Bazedoxifene free base, 1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol, 1h-indol-5-ol, 1-[[4-[2-(hexahydro-1h-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-

Molecular Formula

C₃₀H₃₄N₂O₃

Molecular Weight

470.6 g/mol

InChI Key

UCJGJABZCDBEDK-UHFFFAOYSA-N

FDA UNII

Q16TT9C5BK

Bazedoxifene is an indole derivative and third-generation selective estrogen receptor modulator (SERM) with potential antineoplastic activity. Upon administration, bazedoxifene specifically binds to estrogen receptors in responsive tissues, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it either promotes or suppresses the transcription of estrogen-regulated genes. Bazedoxifene acts as an estrogen antagonist in uterine and breast tissue, thereby blocking the proliferative effects of estrogen-binding to ER-positive cells in these tissues. Bazedoxifene functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In bone, it decreases bone resorption and bone turnover and increases bone mineral density.

Bazedoxifene is an Estrogen Agonist/Antagonist. The mechanism of action of bazedoxifene is as a Selective Estrogen Receptor Modulator.

1 2D Structure

Bazedoxifene

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol

2.1.2 InChI

InChI=1S/C30H34N2O3/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31/h6-15,20,33-34H,2-5,16-19,21H2,1H3

2.1.3 InChI Key

UCJGJABZCDBEDK-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O

2.2 Other Identifiers

2.2.1 UNII

Q16TT9C5BK

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Bazedoxifene Acetate

2. Tse 424

3. Tse-424

4. Tse424

5. Way-140424

2.3.2 Depositor-Supplied Synonyms

1. 198481-32-2

2. Bazedoxifene [inn]

3. Tse-424

4. Bazedoxifene Free Base

5. 1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol

6. 1h-indol-5-ol, 1-[[4-[2-(hexahydro-1h-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-

7. Q16tt9c5bk

8. Chembl46740

9. 198481-32-2 (free Base)

10. 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol

11. Way 140424

12. Bazedoxifeno

13. 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1h-indol-5-ol

14. 1h-indol-5-ol, 1-((4-(2-(hexahydro-1h-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-

15. Unii-q16tt9c5bk

16. Bazedoxifeno [inn-spanish]

17. 1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol

18. Bazedoxifene [mi]

19. Bazedoxifene [vandf]

20. Schembl41935

21. Bazedoxifene [who-dd]

22. Gtpl7355

23. Bazedoxifene [ema Epar]

24. Dtxsid70173593

25. Chebi:135947

26. Ex-a5409

27. Hy-a0031

28. Zinc1895505

29. Bdbm50099585

30. Akos030255808

31. Ak R215 Component Bazedoxifene

32. Ak-r215 Component Bazedoxifene

33. Cs-0932

34. Db06401

35. Sb19326

36. 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-indol-5-ol

37. 1-((4-(2-hexahydro-1h-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol

38. As-78494

39. Us8815934, No. 98

40. A15019

41. D94589

42. Ab01566901_01

43. A879977

44. J-012822

45. Q4875166

46. 1-(p-(2-(hexahydro-1h-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol

2.4 Create Date

2005-08-08

3 Chemical and Physical Properties

Molecular Formula	C₃₀H₃₄N₂O₃
Molecular Weight	470.6 g/mol
XLogP3	6.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Exact Mass	470.25694295 g/mol
Monoisotopic Mass	470.25694295 g/mol
Topological Polar Surface Area	57.9 Å²
Heavy Atom Count	35
Formal Charge	0
Complexity	623
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
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

Indicated for following conditions alone or in combination with conjugated estrogens in women with a uterus: - Treatment of moderate to severe vasomotor symptoms associated with menopause - Prevention of postmenopausal osteoporosis

FDA Label

Conbriza is indicated for the treatment of postmenopausal osteoporosis in women at increased risk of fracture. A significant reduction in the incidence of vertebral fractures has been demonstrated; efficacy on hip fractures has not been established.

When determining the choice of Conbriza or other therapies, including oestrogens, for an individual postmenopausal woman, consideration should be given to menopausal symptoms, effects on uterine and breast tissues, and cardiovascular risks and benefits.

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Selective Estrogen Receptor Modulators

A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) (See all compounds classified as Selective Estrogen Receptor Modulators.)

Bone Density Conservation Agents

Agents that inhibit BONE RESORPTION and/or favor BONE MINERALIZATION and BONE REGENERATION. They are used to heal BONE FRACTURES and to treat METABOLIC BONE DISEASES such as OSTEOPOROSIS. (See all compounds classified as Bone Density Conservation Agents.)

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

BAZEDOXIFENE

5.2.2 FDA UNII

Q16TT9C5BK

5.2.3 Pharmacological Classes

Mechanisms of Action [MoA] - Selective Estrogen Receptor Modulators

5.3 ATC Code

G03XC02

G - Genito urinary system and sex hormones

G03 - Sex hormones and modulators of the genital system

G03X - Other sex hormones and modulators of the genital system

G03XC - Selective estrogen receptor modulators

G03XC02 - Bazedoxifene

5.4 Absorption, Distribution and Excretion

Absorption

Bazedoxifene is rapidly absorbed with a tmax of approximately 2 hours and exhibits a linear increase in plasma concentrations for single doses from 0.5 mg up to 120 mg and multiple daily doses from 1 mg to 80 mg. The absolute bioavailability of bazedoxifene is approximately 6%.

Route of Elimination

The major route of elimination of radio-labelled bazedoxifene is the faeces, and less than 1% of the dose is eliminated in urine.

Volume of Distribution

Following intravenous administration of a 3 mg dose of bazedoxifene, the volume of distribution is 14.7 3.9 l/kg.

Clearance

The apparent oral clearance of bazedoxifene is approximately 4 to 5 l/h/kg.

5.5 Metabolism/Metabolites

Glucuronidation is the major metabolic pathway. After peroral application, bazedoxifene is metabolized by UDP-glucuronosyltransferases (UGTs) to bazedoxifene-4'-glucuronide (M4) and bazedoxifene-5-glucuronide (M5).Little or no cytochrome P450-mediated metabolism is evident. The concentrations of this glucuronide are approximately 10-fold higher than those of unchanged active substance in plasma.

5.6 Biological Half-Life

~30 hours.

5.7 Mechanism of Action

Bazedoxifene belongs to a class of compounds known as selective estrogen receptor modulators (SERMs). Bazedoxifene acts as both an oestrogen-receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifene decreases bone resorption and reduces biochemical markers of bone turnover to the premenopausal range. These effects on bone remodelling lead to an increase in bone mineral density (BMD), which in turn contributes to a reduction in the risk of fractures. Bazedoxifene functions primarily as an oestrogen-receptor antagonist in uterine and breast tissues.

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