Ormeloxifene

Names

Centchroman

CASRN

78994-24-8

PubChem CID

154413

UNII

44AXY5VE90

KEGG Entry Number

D08301

Wikipedia Entry Name

Ormeloxifene

ATC Code(s)

• G03XC04

Appearance

white crystalline substance

Melting Point

165-166 °C

Solubility

Soluble in chloroform, acetone, methanol, and ethanol. Almost insoluble in water, isobutanol, HCl, or NaOH.

logP

7.41

Side Effects

Nausea, headache, weight gain, delayed or prolonged menstrual period.

Carcinogenicity

No carcinogenic effects observed in rats and mice

Mutagenicity

Lacks mutagenicity

Genotoxicity

Lacks genotoxicity

LD₅₀

Mouse, oral, both D and L enantiomers: >1600 mg/kg
Mouse, intraperitoneal, both D and L enantiomers: 400 mg/kg
Mouse, intraperitoneal, L enantiomer: 316 mg/kg
Mouse, intraperitoneal, D enantiomer: 383 mg/kg
Rat, oral, both D and L enantiomers: >2000 mg/kg
Rhesus monkey, intraperitoneal, both D and L enantiomers: 216 mg/kg

Androgen Receptor Activity

No activity

Estrogen Receptor Activity

Competitive partial agonist: has both agonist and antagonist behavior, depending on the tissue it's in.

Elimination Half-Life (t_1/2)

Human women: 168 h
Rhesus monkey: 45 h
Rat: 24.1 h

Serum Protein Binding

Binds to albumin

Excretion

Primarily through feces. Excreted in milk, but "unlikely to be of much physiological consequence to suckling babies."

C_max

122.57 +/- 6.25 ng/mL from single 60 mg oral dose
55.25 +/1 15.45 ng/mL from single 30 mg oral dose
67.55 +/- 6.84 ng/mL from single 30 mg dose of Saheli product
69.44 +/- 9.38 ng/mL from single 30 mg dose of Centron product
54.98 +/- 14.19 ng/mL from 30 mg dose twice a week for 12 weeks

T_max

4 h from single 60 mg oral dose
5.18 +/- 1.78 h from single 30 mg oral dose
5.33 +/- 0.84 h from single 30 mg oral dose of Saheli product
4.33 +/- 0.67 h from single 30 mg oral dose of Centron product
6.637 +/- 1.15 h from 30 mg oral dose twice a week for 12 weeks

Indications

Oral contraception, dysfunctional uterine bleeding, advanced breast cancer.