Integrated pharmacometrics and systems pharmacology model-based analyses to guide GnRH receptor modulator development for management of endometriosis

CPT: Pharmacometrics and Systems Pharmacology

Volumn 1, Issue 1, 2012, Pages

  Riggs, M M ^a   Bennetts, M ^b   Van Der Graaf, P H ^b   Martin, S W ^c  

^a Metrum Research Group LLC   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^c PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALKALINE PHOSPHATASE BONE ISOENZYME; ANTIESTROGEN; ELAGOLIX; ESTRADIOL; ESTROGEN; FOLLITROPIN; GONADORELIN; GONADORELIN AGONIST; GONADORELIN ANTAGONIST; LEUPRORELIN; LUTEINIZING HORMONE; PARATHYROID HORMONE; PROGESTERONE; PROMEGESTONE; TRIPTORELIN;

ARTICLE; BONE DENSITY; CALCIUM URINE LEVEL; DRUG EFFICACY; DYSMENORRHEA; DYSPAREUNIA; ENDOMETRIOSIS; ESTRADIOL BLOOD LEVEL; FEMALE; HUMAN; LUMBAR SPINE; MENOPAUSE; OSTEOBLAST; PELVIS PAIN SYNDROME; POSTMENOPAUSE; PRIORITY JOURNAL;

EID: 84875417302     PISSN: None     EISSN: 21638306     Source Type: Journal    
DOI: 10.1038/psp.2012.10     Document Type: Article

References (48)

1. Mahmood, T.A. & Templeton, A. Prevalence and genesis of endometriosis. Hum. Reprod. 6, 544-549 (1991
2. Surrey, E.S. & Hornstein, M.D. Prolonged GnRH agonist and add-back therapy for symptomatic endometriosis: long-term follow-up. Obstet. Gynecol. 99, 709-719 (2002
3. Pierce, S.J., Gazvani, M.R. & Farquharson, R.G. Long-term use of gonadotropin-releasing hormone analogs and hormone replacement therapy in the management of endometriosis: A randomized trial with a 6-year follow-up. Fertil. Steril. 74, 964-968 (2000
4. Hornstein, M.D., Surrey, E.S., Weisberg, G.W. & Casino, L.A. Leuprolide acetate depot and hormonal add-back in endometriosis: A 12-month study. Lupron Add-Back Study Group. Obstet. Gynecol. 91, 16-24 (1998
5. Franke, H.R., van de Weijer, P.H., Pennings, T.M. & van der Mooren, M.J. Gonadotropinreleasing hormone agonist plus "add-back" hormone replacement therapy for treatment of endometriosis: A prospective, randomized, placebo-controlled, double-blind trial. Fertil. Steril. 74, 534-539 (2000
6. Fernandez, H., Lucas, C., Hédon, B., Meyer, J.L., Mayenga, J.M. & Roux, C. One year comparison between two add-back therapies in patients treated with a GnRH agonist for symptomatic endometriosis: A randomized double-blind trial. Hum. Reprod. 19, 1465-1471 (2004
7. Biberoglu, K.O. & Behrman, S.J. Dosage aspects of danazol therapy in endometriosis: Short-term and long-term effectiveness. Am. J. Obstet. Gynecol. 139, 645-654 (1981
8. Riggs, M.M. Multiscale systems models as a knowledge bridge between biology, physiology, and pharmacology. AAPS Newsmagazine 17-21 (2011
9. Peterson, M.C. & Riggs, M.M. A physiologically based mathematical model of integrated calcium homeostasis and bone remodeling. Bone 46, 49-63 (2010
10. Spelsberg, T.C., Subramaniam, M., Riggs, B.L. & Khosla, S. The actions and interactions of sex steroids and growth factors/cytokines on the skeleton. Mol. Endocrinol. 13, 819-828 (1999
11. Yang, N.N. et al. Estrogen and raloxifene stimulate transforming growth factor-β3 gene expression in rat bone: A potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology 137, 2075-2084 (1996
12. McCarthy, T.L., Chang, W.Z., Liu, Y. & Centrella, M. Runx2 integrates estrogen activity in osteoblasts. J. Biol. Chem. 278, 43121-43129 (2003
13. Khosla, S. Estrogen and the death of osteoclasts: A fascinating story. BoneKey Osteovision 4, 267-272 (2007
14. Hawse, J.R., Subramaniam, M., Ingle, J.N., Oursler, M.J., Rajamannan, N.M. & Spelsberg, T.C. Estrogen-TGF-βcross-talk in bone and other cell types: Role of TIEG, Runx2, and other transcription factors. J. Cell. Biochem. 103, 383-392 (2008
15. Nordin, B.E. et al. A longitudinal study of bone-related biochemical changes at the menopause. Clin. Endocrinol. (Oxf) 61, 123-130 (2004
16. Dick, I.M., Devine, A., Beilby, J. & Prince, R.L. Effects of endogenous estrogen on renal calcium and phosphate handling in elderly women. Am. J. Physiol. Endocrinol. Metab. 288, E430-E435 (2005
17. Lalonde, R.L. et al. Model-based drug development. Clin. Pharmacol. Ther. 82, 21-32 (2007
18. Bies, R.R., Gastonguay, M.R. & Schwartz, S.L. Mathematics for understanding disease. Clin. Pharmacol. Ther. 83, 904-908 (2008
19. Goldberger, M.J. et al. ASCPT Task Force for advancing pharmacometrics and integration into drug development. Clin. Pharmacol. Ther. 88, 158-161 (2010
20. Sorger P.K. et al. Quantitative and systems pharmacology in the post-genomic era: New approaches to discovering drugs and understanding therapeutic mechanisms. (White paper, QSP Workshop Group, 2011
21. Berg, J.M., Rogers, M.E. & Lyster, P.M. Systems biology and pharmacology. Clin. Pharmacol. Ther. 88, 17-19 (2010
22. Sowers, M.R., Zheng, H., McConnell, D., Nan, B., Harlow, S.D. & Randolph, J.F. Jr. Estradiol rates of change in relation to the final menstrual period in a population-based cohort of women. J. Clin. Endocrinol. Metab. 93, 3847-3852 (2008
23. Garnero, P., Sornay-Rendu, E., Chapuy, M.C. & Delmas, P.D. Increased bone turnover in late postmenopausal women is a major determinant of osteoporosis. J. Bone Miner. Res. 11, 337-349 (1996
24. Bone, H.G. et al. Alendronate and estrogen effects in postmenopausal women with low bone mineral density. Alendronate/estrogen study group. J. Clin. Endocrinol. Metab. 85, 720-726 (2000
25. Abbott. Efficacy and safety study of NBI-56418 sodium in subjects with endometriosis. (2012
26. Matsuo, H. Prediction of the change in bone mineral density induced by gonadotropinreleasing hormone agonist treatment for endometriosis. Fertil. Steril. 81, 149-153 (2004
27. Borderie, D., Cherruau, B., Dougados, M., Ekindjian, O.G. & Roux, C. Biochemical markers as predictors of bone mineral density changes after GnRH agonist treatment. Calcif. Tissue Int. 62, 21-25 (1998
28. Agarwal, S.K., Hamrang, C., Henzl, M.R. & Judd, H.L. Nafarelin vs. leuprolide acetate depot for endometriosis. Changes in bone mineral density and vasomotor symptoms. Nafarelin Study Group. J. Reprod. Med. 42, 413-423 (1997
29. Tahara, M., Matsuoka, T., Yokoi, T., Tasaka, K., Kurachi, H. & Murata, Y. Treatment of endometriosis with a decreasing dosage of a gonadotropin-releasing hormone agonist (nafarelin): A pilot study with low-dose agonist therapy ("draw-back" therapy). Fertil. Steril. 73, 799-804 (2000
30. Hornstein, M.D., Yuzpe, A.A., Burry, K.A., Heinrichs, L.R., Buttram, V.L. Jr & Orwoll, E.S. Prospective randomized double-blind trial of 3 versus 6 months of nafarelin therapy for endometriosis associated pelvic pain. Fertil. Steril. 63, 955-962 (1995
31. Surrey, E.S. & Judd, H.L. Reduction of vasomotor symptoms and bone mineral density loss with combined norethindrone and long-acting gonadotropin-releasing hormone agonist therapy of symptomatic endometriosis: A prospective randomized trial. J. Clin. Endocrinol. Metab. 75, 558-563 (1992
32. Soysal, S., Soysal, M.E., Ozer, S., Gul, N. & Gezgin, T. The effects of post-surgical administration of goserelin plus anastrozole compared to goserelin alone in patients with severe endometriosis: A prospective randomized trial. Hum. Reprod. 19, 160-167 (2004
33. Neurocrine Biosciences. Safety and efficacy study of NBI-56418 in endometriosis (PETAL). (2009
34. The Nafarelin European Endometriosis Trial Group (NEET). Nafarelin for endometriosis: A large-scale, danazol-controlled trial of efficacy and safety, with 1-year follow-up. Fertil. Steril. 57, 514-522 (1992
35. Adamson, G.D., Kwei, L. & Edgren, R.A. Pain of endometriosis: Effects of nafarelin and danazol therapy. Int. J. Fertil. Menopausal Stud. 39, 215-217 (1994
36. Burger, H.G. et al. Prospectively measured levels of serum follicle-stimulating hormone, estradiol, and the dimeric inhibins during the menopausal transition in a population-based cohort of women. J. Clin. Endocrinol. Metab. 84, 4025-4030 (1999
37. Riggs, M.M., Peterson, M.C. & Gastonguay, M.R. Multiscale physiology-based modeling of mineral bone disorder in patients with impaired kidney function. J. Clin. Pharmacol. 52, 45S-53S (2012
38. Pouilles, J.M., Tremollieres, F. & Ribot, C. The effects of menopause on longitudinal bone loss from the spine. Calcif. Tissue Int. 52, 340-343 (1993
39. Amama, E.A., Taga, M. & Minaguchi, H. The effect of gonadotropin-releasing hormone agonist on type I collagen C-telopeptide and N-telopeptide: The predictive value of biochemical markers of bone turnover. J. Clin. Endocrinol. Metab. 83, 333-338 (1998
40. McClung, M.R. et al.; AMG 162 Bone Loss Study Group. Denosumab in postmenopausal women with low bone mineral density. N. Engl. J. Med. 354, 821-831 (2006
41. Raposo, J.F., Sobrinho, L.G. & Ferreira, H.G. A minimal mathematical model of calcium homeostasis. J. Clin. Endocrinol. Metab. 87, 4330-4340 (2002
42. Lemaire, V., Tobin, F.L., Greller, L.D., Cho, C.R. & Suva, L.J. Modeling the interactions between osteoblast and osteoclast activities in bone remodeling. J. Theor. Biol. 229, 293-309 (2004
43. Post, T.M., Cremers, S.C., Kerbusch, T. & Danhof, M. Bone physiology, disease and treatment: Towards disease system analysis in osteoporosis. Clin. Pharmacokinet. 49, 89-118 (2010
44. Schmidt, S., Post, T.M., Peletier, L.A., Boroujerdi, M.A. & Danhof, M. Coping with time scales in disease systems analysis: Application to bone remodeling. J. Pharmacokinet. Pharmacodyn. 38, 873-900 (2011
45. Vincent, K., Kennedy, S. & Stratton, P. Pain scoring in endometriosis: Entry criteria and outcome measures for clinical trials. Report from the Art and Science of Endometriosis meeting. Fertil. Steril. 93, 62-67 (2010
46. Agresti, A. Categorical Data Analysis (John Wiley & Sons: New York, 1990
47. Lunn, D.J., Thomas, A., Best, N. & Spiegelhalter, D. WinBUGS - a Bayesian modelling framework: Concepts, structure, and extensibility. Stat. Comput. 10, 325-337 (2000
48. R Development Core Team. R: A language and environment for statistical computing. (R Foundation for Statistical Computing, Vienna, Austria, 2008