BIOMAT Database Logo BIOMAT Database Logo

Metabolism of levormeloxifene, a selective oestrogen receptor modulator, in the Sprague-Dawley rat, Cynomolgus monkey and postmenopausal woman. 2000

R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
F. Hoffman-La Roche Ltd, Pharmaceutical Division, Basel, Switzerland. richard.mountfield@roche.com

1. The metabolic fate of levormeloxifene in the Sprague-Dawley rat, Cynomolgus monkey and postmenopausal volunteer has been investigated. 2. Two doses of [14C]levormeloxifene, 0.7 and 50 mg/kg, were given to the male and female rat and monkey, and a single 20-mg dose to the postmenopausal volunteer. 3. The primary route of excretion in all three species was the faeces. Metabolism was similar in all three species, with demethylation forming the major metabolite in the rat and postmenopausal volunteer. One of the major metabolites in the monkey involved an oxidative ring opening of a pyrrole ring. 4. The main site of metabolism of levormeloxifene is the liver and the majority of the drug and its metabolites is excreted via the faecal route. Metabolic pathways appear to be similar in the three species studied.

UI MeSH Term Description Entries
D008297 Male Males
D011759 Pyrrolidines Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH. Tetrahydropyridine,Tetrahydropyridines
D011946 Receptors, Antigen Molecules on the surface of B- and T-lymphocytes that recognize and combine with specific antigens. Antigen Receptors,Antigen Receptor,Receptor, Antigen
D002250 Carbon Radioisotopes Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes. Radioisotopes, Carbon
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D005243 Feces Excrement from the INTESTINES, containing unabsorbed solids, waste products, secretions, and BACTERIA of the DIGESTIVE SYSTEM.
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Pharmacokinetics and allometric scaling of levormeloxifene, a selective oestrogen receptor modulator.
April 2003, Biopharmaceutics & drug disposition,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Metabolism, disposition, excretion, and pharmacokinetics of levormeloxifene, a selective estrogen receptor modulator, in the rat.
May 2000, Drug metabolism and disposition: the biological fate of chemicals,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Levormeloxifene: safety, pharmacodynamics and pharmacokinetics in healthy postmenopausal women following single and multiple doses of a new selective oestrogen receptor modulator.
March 2002, British journal of clinical pharmacology,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues.
September 2013, Regulatory peptides,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Differences in chlorzoxazone metabolism in full mature male and female Sprague-Dawley rat, Beagle dog and Cynomolgus monkey liver.
February 2000, Human & experimental toxicology,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Safety Evaluation of Lipid Nanoparticle-Formulated Modified mRNA in the Sprague-Dawley Rat and Cynomolgus Monkey.
March 2018, Veterinary pathology,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Protein binding of tirilazad (U-74006) in human, Sprague-Dawley rat, beagle dog and cynomolgus monkey serum.
April 1994, The Journal of pharmacology and experimental therapeutics,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Serum domoic acid clearance and clinical observations in the cynomolgus monkey and Sprague-Dawley rat following a single i.v. dose.
April 1994, Bulletin of environmental contamination and toxicology,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Pre- and postnatal development studies of lasofoxifene, a selective estrogen receptor modulator (SERM), in Sprague-Dawley rats.
June 2004, Birth defects research. Part B, Developmental and reproductive toxicology,
R J Mountfield, and A M Panduro, and O Wassmann, and M Thompson, and B John, and N van der Merbel
Assay for levormeloxifene, a selective estrogen receptor modulator, in human and monkey plasma employing high-performance liquid chromatography and solid-phase extraction.
June 1999, Journal of chromatography. B, Biomedical sciences and applications,
Copied contents to your clipboard!