The dosing solution influence on the pharmacokinetics of degarelix, a new GnRH0 antagonist, after s.c. administration to beagle dogs

European Journal of Pharmaceutical Sciences

Volumn 20, Issue 3, 2003, Pages 335-340

  Agersø, Henrik ^a   Koechling, Wolfgang ^a   Knutsson, Magnus ^a   Hjortkjær, Rolf ^a   Karlsson, Mats O ^b  

^a Ferring Pharmaceuticals AS   (Denmark)

^b UPPSALA UNIVERSITY   (Sweden)

Author keywords

Degarelix; FE200486; Non linear mixed effects; NONMEM; Pharmacokinetics; Prostate cancer

Indexed keywords

ABSORPTION; COMPUTER SIMULATION; PHARMACOKINETICS; TUMORS;

PLASMA CONCENTRATIONS;

DRUG DOSAGE;

DEGARELIX; FE 200486; GONADORELIN ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; COMPARTMENT MODEL; CONTROLLED STUDY; DATA ANALYSIS; DOG; DOSE CALCULATION; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG DOSE REGIMEN; DRUG HALF LIFE; MALE; NONHUMAN; NONLINEAR SYSTEM; PRIORITY JOURNAL;

EID: 0242334085     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejps.2003.08.001     Document Type: Article

References (13)

1. Beal, S.L., Sheiner, L.B., 2000. NONMEM users guide. NONMEM Project Group: University of California San Francisco: San Francisco.
2. Broqua P., Riviere P.J., Conn P.M., Rivier J.E., Aubert M.L., Junien J.L. Pharmacological profile of a new, potent, and long-acting gonadotropin- releasing hormone antagonist: degarelix. J. Pharmacol. Exp. Ther. 301:2002;95-102.
3. Cook T., Sheridan W.P. Development of GnRH antagonists for prostate cancer: new approaches to treatment. Oncologist. 5:2000;162-168.
4. de Pinieux G., Legrier M.E., Poirson-Bichat F., Courty Y., Bras-Goncalves R., Dutrillaux A.M., Nemati F., Oudard S., Lidereau R., Broqua P., Junien J.L., Dutrillaux B., Poupon M.F. Clinical and experimental progression of a new model of human prostate cancer and therapeutic approach. Am. J. Pathol. 159:2001;753-764.
5. Giberti C., Barreca T., Martorana G., Truini M., Franceschini R., Rolandi E., Giuliani L. Hormonal pattern and testicular histology in patients with prostatic cancer after long-term treatment with a gonadotropin-releasing hormone agonist analogue. Eur. Urol. 15:1988;125-127.
6. Gonzalez-Barcena D., Vadillo-Buenfil M., Gomez-Orta F., Fuentes G.M., Cardenas-Cornejo I., Graef-Sanchez A., Comaru-Schally A.M., Schally A.V. Responses to the antagonistic analog of LH-RH (SB-75, Cetrorelix) in patients with benign prostatic hyperplasia and prostatic cancer. Prostate. 24:1994;84-92.
7. Jiang G., Stalewski J., Galyean R., Dykert J., Schteingart C., Broqua P., Aebi A., Aubert M.L., Semple G., Robson P., Akinsanya K., Haigh R., Riviere P., Trojnar J., Junien J.L., Rivier J.E. GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J. Med. Chem. 44:2001;453-467.
8. Jonsson E.N., Karlsson M.O. Xpose - an S-PLUS based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput. Methods Programs Biomed. 58:1999;51-64.
9. Korkut E., Bokser L., Comaru-Schally A.M., Groot K., Schally A.V. Inhibition of growth of experimental prostate cancer with sustained delivery systems (microcapsules and microgranules) of the luteinizing hormone-releasing hormone antagonist SB-75. Proc. Natl. Acad. Sci. U.S.A. 88:1991;844-848.
10. Kuhn J.M., Abourachid H., Brucher P., Doutres J.C., Fretin J., Jaupitre A., Jorest R., Lambert D., Petit J., Pin J., Blumberg J., Dufour-Esquerre F. A randomized comparison of the clinical and hormonal effects of two GnRH agonists in patients with prostate cancer. Eur. Urol. 32:1997;397-403.
11. Redding T.W., Schally A.V., Radulovic S., Milovanovic S., Szepeshazi K., Isaacs J.T. Sustained release formulations of luteinizing hormone-releasing hormone antagonist SB-75 inhibit proliferation and enhance apoptotic cell death of human prostate carcinoma (PC-82) in male nude mice. Cancer Res. 52:1992;2538-2544.
12. Reissmann T., Schally A.V., Bouchard P., Riethmiiller H., Engel J. The LHRH antagonist cetrorelix: a review. Hum. Reprod. Update. 6:2000;322-331.
13. Sheiner L.B., Grasela T.H. An introduction to mixed effect modelling: concepts, definitions, and justification. J. Pharmacokinet. Biopharm. 19:1991;11-24.