Citations for: Singh, M. M. Centchroman, a Selective Estrogen Receptor Modulator, as a Contraceptive and for the Management of Hormone-Related Clinical Disorders. Med. Res. Rev. 2001, 21 (4), 302–347.

Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
Androgen Receptor Activity
No activity
Ormeloxifene (API)
Pharmacology Data Field
Estrogen Receptor Activity
Competitive partial agonist: has both agonist and antagonist behavior, depending on the tissue it's in.
Ormeloxifene (API)
Physical & Chemical Properties Data Field
Appearance
white crystalline substance
Ormeloxifene (API)
Physical & Chemical Properties Data Field
Melting Point
165-166 °C
Ormeloxifene (API)
Physical & Chemical Properties Data Field
Solubility
Soluble in chloroform, acetone, methanol, and ethanol. Almost insoluble in water, isobutanol, HCl, or NaOH.
Ormeloxifene (API)
Physical & Chemical Properties Data Field
logP
7.41
Ormeloxifene (API)
Metabolites
7-Desmethyl Centchroman
N/A
Metabolites
Ormeloxifene Metabolite 2
N/A
Metabolites
Ormeloxifene Metabolite 3
N/A
Metabolites
Ormeloxifene Metabolite 4
N/A
Metabolites
Ormeloxifene Metabolite 5
N/A
Metabolites
Ormeloxifene Metabolite 6
N/A
Pharmacology Data Field
Elimination Half-Life (t1/2)
Human women: 168 h
Rhesus monkey: 45 h
Rat: 24.1 h
Ormeloxifene (API)
Pharmacology Data Field
Serum Protein Binding
Binds to albumin
Ormeloxifene (API)
Toxicology Data Field
Carcinogenicity
No carcinogenic effects observed in rats and mice
Ormeloxifene (API)
Pharmacology Data Field
Excretion
Primarily through feces. Excreted in milk, but "unlikely to be of much physiological consequence to suckling babies."
Ormeloxifene (API)
Pharmacology Data Field
Cmax
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
Ormeloxifene (API)
Pharmacology Data Field
Tmax
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
Ormeloxifene (API)
Toxicology Data Field
Mutagenicity
Lacks mutagenicity
Ormeloxifene (API)
Toxicology Data Field
Genotoxicity
Lacks genotoxicity
Ormeloxifene (API)
Toxicology Data Field
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
Ormeloxifene (API)