MITOTOX

Drug

D0791 | bazedoxifene

Molecular Formula	C30H34N2O3
Molecular Weight	470.6
Structure
State	solid
Clearance	The apparent oral clearance of bazedoxifene is approximately 4 to 5 l/h/kg.
Volume of distribution	Following intravenous administration of a 3 mg dose of bazedoxifene, the volume of distribution is 14.7 ± 3.9 l/kg.
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.
Protein binding	98-99%.
Half life	~30 hours.
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%.

G03XC02 Bazedoxifene

[G03XC] Selective estrogen receptor modulators

[G03X] OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM

[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM

[G] Genitourinary system and reproductive hormones

G03CC07 Conjugated estrogens and bazedoxifene

[G03CC] Estrogens, combinations with other drugs

[G03C] ESTROGENS

[G03] SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM

[G] Genitourinary system and reproductive hormones

Toxicity	Dose	Species	Model	Method	Action	Positive criterion	Reference
MEMBRANE POTENTIAL	11.01±0.75	human	qHTS-HepG2	MMP assay	decrease	IC50	163
MEMBRANE POTENTIAL	15.45	human	HepG2	MMP assay	decrease	IC50	163
MEMBRANE POTENTIAL		rat	hepatocytes	MMP assay	Negative	IC50	163

Pictogram	Signal	Statements	Precautionary Statement Codes
	Danger	The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory. H360 (100%): May damage fertility or the unborn child [Danger Reproductive toxicity]	P201, P202, P281, P308+P313, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Pictogram

Signal

Statements

Precautionary Statement Codes

Danger

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

H360 (100%): May damage fertility or the unborn child [Danger Reproductive toxicity]

P201, P202, P281, P308+P313, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

1-((4-(2-Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol	1-(4-(2-(azepan-1-yl)ethoxy)benzyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol	1-[4-(2-Azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol
1-[[4-[2-(AZEPAN-1-YL)ETHOXY]PHENYL]METHYL]-2-(4-HYDROXYPHENYL)-3-METHYL-INDOL-5-OL	1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol	1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol
198481-32-2	1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-	1H-Indol-5-ol, 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-
3473AH	A15019	AB01566901_01
AKOS030255808	BDBM50099585	Bazedoxifene
Bazedoxifene [INN]	Bazedoxifeno	Bazedoxifeno [INN-Spanish]
C30H34N2O3	CHEBI:135947	CHEMBL46740
CS-0932	CTK4E2538	Conbriza
DB06401	DTXSID70173593	GTPL7355
HY-A0031	J-012822	Q16TT9C5BK
Q4875166;	RT-011426	SB19326
SCHEMBL41935	TSE-424	UCJGJABZCDBEDK-UHFFFAOYSA-N
UNII-Q16TT9C5BK	US8815934, No. 98	W-5320
WAY 140424	ZINC1895505