Metabolism of toremifene in the rat

Sipilä, Hannu; Kangas, Lauri; Vuorilehto, Lauri; Kalapudas, Arm; Eloranta, Maire; Södervall, Marja; Toivola, Reijo; Anttila, Markku

doi:10.1016/0022-4731(90)90007-f

Cited by 29 publications

(32 citation statements)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…However, no information regarding the absolute bioavailability of tamoxifen in laboratory animals was available. The same holds true for toremifene, which was also almost completely absorbed after oral administration to rats, as indicated by similar amounts of radiolabeled compounds excreted renally after intravenous and oral administration (SIPILA et al 1990).…”

Section: Pharmacokinetics In Animals 1 Absorptionmentioning

confidence: 76%

“…The mean apparent Vz/f ranged between 4571 and 9581 in healthy subjects and increased with age. The mean oral CLif was 2.7-5.1I/h (ANTTILA et al 1990;SOTANIEMI and ANTTILA 1997). These values, however, should be judged with caution, since the absolute bioavailability of toremifene after oral administration is not known.…”

Section: Distributionmentioning

confidence: 91%

“…After single and mUltiple oral administration, postmaximum serum concentrations of toremifene decreased biphasically with mean half-lives of 4h and 4-6days (ANTTILA et al 1990(ANTTILA et al , 1995SOTANIEMI and ANTTILA 1997). The mean apparent Vz/f ranged between 4571 and 9581 in healthy subjects and increased with age.…”

Section: Distributionmentioning

confidence: 94%

“…It was shown that the chlorine atom was still present in all identified metabolites of toremifene, which indicates its metabolic stability. It was proposed that the presence of the chlorine atom may inhibit the formation of DNA-reactive metabolites (SIPILA et al 1990); however, low levels of DNA adducts were detected in rat liver after toremifene treatment (WISEMAN and GOA 1997).…”

Section: Metabolismmentioning

confidence: 98%

“…Additionally, a TLC method was described for the determination of the parent compound and two of its metabolites also using the UV light-mediated conversion to phenanthrene derivatives (ANTTILA et al 1990). Recently, a liquid chromatography-mass spectrometry (LC-MS) method was published for the analysis of toremifene and five of its metabolites with a lower limit of quantification for toremifene of 10ng/ml (MARTINSEN and GYNTHER 1996).…”

mentioning

confidence: 99%

See 4 more Smart Citations

Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens

Kuhnz¹,

Blode²,

Zimmermann³

1993

Handbook of Experimental Pharmacology

View full text Add to dashboard Cite

Section: Pharmacokinetics In Animals 1 Absorptionmentioning

confidence: 76%

Section: Distributionmentioning

confidence: 91%

Section: Distributionmentioning

confidence: 94%

Section: Metabolismmentioning

confidence: 98%

mentioning

confidence: 99%

See 3 more Smart Citations

Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens

Kuhnz¹,

Blode²,

Zimmermann³

1993

Handbook of Experimental Pharmacology

View full text Add to dashboard Cite

Female Sex Hormones, Contraceptives, And Fertility Drugs

Ruenitz

2010

Burger's Medicinal Chemistry and Drug Discovery

View full text Add to dashboard Cite

Substances that interact with estrogen or progesterone receptors have clinical applications in hormone replacement therapy, birth control, prevention and treatment of hormone‐dependent cancer, and in stimulation of fertility. This chapter describes the specific drugs in each of these categories, and their counterparts now in clinical trials or in use experimentally, with respect to mechanism of pharmacologic action, noteworthy routes of biotransformation, structure–activity relationships, and current and future prospects for therapeutic uses. The history of discovery and current understanding of the molecular endocrinologic basis of selective estrogen receptor modulators are covered, as are mechanistic, structural, and clinical aspects of drugs that interfere with estrogen biosynthesis (aromatase inhibitors). Structural and pharmacologic aspects of environmental/dietary estrogens and progestins are also included.

show abstract

Cone voltage and collision cell collision‐induced dissociation study of triphenylethylenes of pharmaceutical interest

Makowiecki

Tolonen

Uusitalo

et al. 2001

Rapid Comm Mass Spectrometry

View full text Add to dashboard Cite

Fragmentations of three triphenylethylene compounds (toremifene and its two metabolites) with different functional side-chain groups (alcohol, acid and amine) were studied. The compounds were dissociated by collision-induced dissociation (CID) in the interface region of an electrospray ionization source (ESI(+)) and in the collision cell of a triple quadrupole mass spectrometer. Fragmentation pathways for these molecules are proposed, based on accurate mass measurements of in-source fragment ions and MS/MS experiments using product and precursor ion scanning. The side-chain functional groups were found to strongly affect the fragmentations of the molecular ions. The fragmentation pathways of the protonated molecule and sodium ion adduct were quite similar, but the subsequent stabilities of certain common fragments were surprisingly different.

show abstract

Metabolism of toremifene in the rat

Cited by 29 publications

References 3 publications

Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens

Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens

Female Sex Hormones, Contraceptives, And Fertility Drugs

Cone voltage and collision cell collision‐induced dissociation study of triphenylethylenes of pharmaceutical interest

Contact Info

Product

Resources

About