Disposition and metabolism of cetrorelix, a potent luteinizing hormone- releasing hormone antagonist, in rats and dogs

Drug Metabolism and Disposition

Volumn 28, Issue 1, 2000, Pages 10-20

  Schwahn, Martin ^a   Schupke, Hubert ^a   Gasparic, Antje ^a   Krone, Dorothee ^a   Peter, Gernot ^a   Hempel, Roland ^a   Kronbach, Thomas ^a   Locher, Mathias ^a   Jahn, Wolfgang ^a   Engel, Jürgen ^a  

^a ASTA MEDICA AG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

CETRORELIX; GONADORELIN ANTAGONIST; HEPTAPEPTIDE; TETRAPEPTIDE;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; DOG; DRUG ABSORPTION; DRUG DISPOSITION; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG URINE LEVEL; FEMALE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ABSORPTION; ANIMALS; CARBON RADIOISOTOPES; DOGS; FEMALE; GONADOTROPIN-RELEASING HORMONE; HORMONE ANTAGONISTS; INJECTIONS, SUBCUTANEOUS; MALE; RATS; RATS, WISTAR; TISSUE DISTRIBUTION;

ANIMALIA; CANIS FAMILIARIS;

EID: 18544399515     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (24)

1. Bajusz S, Kovacs M, Gazdag M, Bokser L, Karashima T, Csernus VJ, Janaky T, Guoth J and Schally AV (1988) Highly potent antagonists of luteinizing hormone-releasing hormone free of edematogenic effects. Proc Natl Acad Sci USA 85:1637-1641.
2. Barnfield DJ, Barker YK, Knott S, Miles GS and Warrander A (1988) The disposition of zoladex (ICI 118,630) in laboratory animals. Pharm Weekbl Sci 10/1:56.
3. Barnfield DJ and Warrander A (1988) The metabolism of zoladex (ICI 118,630) in laboratory animals. Pharm Weekbl Sci 10/1:56.
4. Berger H, Heinrich N, Albrecht E, Kertscher U, Oehlke J, Bienert M, Schäfer H, Baeger I and Mehlis B (1991) Gonadotropin-releasing hormone (GnRH) analogs: Relationship between their structure, proteolytic inactivation and pharmacokinetics in rats. Regul Pept 33:299-311.
5. Berger H, Sandow J, Heinrich N, Albrecht E, Kertscher U and Oehlke J (1993) Disposition of the 3H-labeled gonadotropin-releasing hormone analog buserelin in rats. Drug Metab Dispos 21:818-822.
6. Chan RL and Chaplin MD (1985) Plasma binding of LHRH and nafarelin, a highly potent LHRH agonist. Biochem Biophys Res Commun 127:673-679.
7. Chan RL, Ho W, Webb AS, LaFargue JA and Nerenberg CA (1988) Disposition of detirelix, a potent luteinising hormone-releasing hormone antagonist, in rats and monkeys. Pharm Res 5:335-340.
8. Chan RL, Hsieh SC, Haroldsen PE, Ho W and Nestor JJ Jr (1991) Disposition of RS-26306, a potent luteinising hormone-releasing hormone antagonist, in monkeys and rats after single intravenous and subcutaneous administration. Drug Metab Dispos 19:858-864.
9. Chu NI, Chan RL, Hama KM and Chaplin MD (1985) Disposition of narfarelin acetate, a potent luteinising hormone-releasing hormone agonist, in rats and rhesus monkeys. Drug Metab Dispos 13:560-565.
10. Csernus VJ, Szende B, Groot K, Redding TW and Schally AV (1990) Development of radioimmunoassay for a potent luteinizing hormone-releasing hormone antagonist. Drug Res 40:111-118.
11. Deger W, Loosz A, Wolf-Heuss E, Engel J and Schally AV (1993) Stability of cetrorelix acetate under the influence of proteolytic enzymes, Presentation at the 2nd Symposion on Chem. Chemistry; 1993 Apr 1-4; Bad Nauheim, Germany.
12. Fekete M, Bajusz S, Groot K, Csernus VJ and Schally AV (1989) Comparison of different agonists and antagonists of luteinizing hormone-releasing hormone for receptor-binding ability to rat pituitary and human breast cancer membranes. Endocrinology 124:946-955.
13. Gibaldi M and Perrier D (1982) Pharmacokinetics, 2nd ed., Marcel Dekker, New York.
14. Gut I, Terelius Y, Frantik E, Linhart I, Soucek P, Filipcova B and Kluckova H (1993) Exposure to various benzene derivatives differently induces cytochromes P450 2B1 and P450 2E1 in rat liver. Arch Toxicol 67:237-243.
15. Hempel R, Schupke H, Gasparic A, Schwahn M, Peter G and Kronbach T (1998) Metabolism of the LH-releasing hormone antagonist cetrorelix in rats and dogs following subcutaneous administration (Abstract). ISSX Proc 13:78.
16. Hsueh AJW and Schaeffer JM (1985) Gonadotropin releasing hormone as a paracrine hormone and neurotransmitter in extrapituitary sites. J Steroid Biochem 23:757-764.
17. Müller A, Busker E, Engel J, Kutscher B, Bernd M and Schally AV (1994) Structural investigation of cetrorelix, a new potent and long-acting LH-RH antagonist. Int J Peptide Protein Res 43:264-270.
18. Pacifici GM and Viani A (1992) Methods of determining plasma and tissue Binding of drugs. Clin Pharmacokinet 23:449-468.
19. Roepstorff R and Fohlman J (1984) Proposal for a common nomenclature for sequence ions in mass spectra of peptides. Biomed Mass Spectrom 11:601.
20. Schwahn M, Romeis P, Peter G, Derendorf H and Herbst M (1997) Absolute bioavailability and dose proportionality of CET, a novel LH-RH antagonist, in male and female rats. Arch Pharmacol 355:R8.
21. 2- and COOH-terminal tripeptides from the luteinizing hormone-releasing hormone. Proc Natl Acad Sci USA 82:1025-1029.
22. Spector WS, ed (1956) Handbook of Biological Data, W B Saunders Company, Philadelphia.
23. Ueno H and Matsuo S (1991) High-performance liquid chromatography followed by radioimmunoassay for the determination of a luteinizing hormone-releasing hormone analogue, leuprorelin, and its metabolite. J Chromatogr 566:57-66.
24. Waynforth HB (1980) Experimental and Surgical Technique in the Rat, Academic Press, London.