Embryo/fetal toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in rats and rabbits

Birth Defects Research Part B - Developmental and Reproductive Toxicology

Volumn 71, Issue 3, 2004, Pages 161-170

  Ozolinš, Terence R S ^a   Gupta, U ^a  

^a PFIZER INC   (United States)

Author keywords

Antiestrogen; Estrogen; Lasofoxifene; Malformations; Rabbits; Rats; SERM; Teratology

Indexed keywords

LASOFOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANUS ATRESIA; ARTICLE; BODY WEIGHT; CESAREAN SECTION; CONTROLLED STUDY; DRUG EFFECT; EMBRYOTOXICITY; FEMALE; FETUS; FETUS DEVELOPMENT; FETUS WEIGHT; FOOD INTAKE; MALE; NONHUMAN; OSSIFICATION; PLACENTA WEIGHT; PREGNANCY; PRENATAL DRUG EXPOSURE; PRIORITY JOURNAL; RAT; URETER DILATATION; WEIGHT GAIN;

ANIMALS; ANUS, IMPERFORATE; AREA UNDER CURVE; BODY WEIGHT; BONE AND BONES; DOSE-RESPONSE RELATIONSHIP, DRUG; EMBRYO; EMBRYO IMPLANTATION; ESTROGENS; FEEDING BEHAVIOR; FEMALE; MALE; MATERNAL EXPOSURE; ORGAN SIZE; PELVIS; PLACENTA; PYRROLIDINES; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; REPRODUCTION; SELECTIVE ESTROGEN RECEPTOR MODULATORS; SPECIES SPECIFICITY; TERATOGENS; TETRAHYDRONAPHTHALENES; TIME FACTORS; URETER;

ANIMALIA; ORYCTOLAGUS CUNICULUS;

EID: 3543071769     PISSN: 15429733     EISSN: None     Source Type: Journal    
DOI: 10.1002/bdrb.20010     Document Type: Article

References (54)

1. Aponte G, Leung P, Gross P, Yamada T. 1984. Effects of somatostatin on food intake in rats. Life Sci 35:741-746.
2. Barker, DJ, Gluckman PD, Robinson JS. 1995. Conference report: fetal origins of adult disease-report of the First International Study Group, Sydney, 29-30 October 1994. Placenta 16:317-320.
3. Bickis M, Krewski D. 1985. Statistical design and analysis of the long-term carcinogenicity bioassay. In: Clayson DB, Krewski D, Munro I, editors. Toxicological risk assessment. Vol. 1. Boca Raton: CRC Press.
4. Black LJ, Sato M, Rowley ER, Magee DE, Bekele A, Williams DC, Cullinan GJ, Bendele R, Kauffman RF, Bensch WR, Frolik CA, Termine JD, Bryant HU. 1994. Raloxifene (LY139481 HCl) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats. J Clin Invest 93:63-69.
5. Buelke-Sam J, Cohen IR, Wierda D, Griffey KI, Fisher LF, Francis PC. 1998. The selective estrogen receptor modulator, raloxifene: a segment II/III delivery study in rats. Reprod Toxicol 12:271-288.
6. Byrd RA, Francis PC. 1998. The selective estrogen receptor modulator, raloxifene: segment II studies in rats and rabbits. Reprod Toxicol 12:261-270.
7. Cappon GD, Horimoto M, Hurtt ME. 2004. Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in male rats. Birth Defects Res B 71:142-149 (this issue).
8. Cahn SWC, Leathem JH. 1977. Placental steroidogenesis in the rat: Comparison of normal and giant placentae. Endocrinology 100:1418-1422.
9. Clark JH, Markaverich BM. 1982. The agonistic-antagonistic properties of clomiphene: a review. Pharmacol Ther 15:467-519.
10. Cohen LA, Pittman B, Wang CX, Aliaga C, Yu L, Moyer JD. 2001. LAS, a novel selective estrogen receptor modulator with chemopreventive and therapeutic activity in the N-nitroso-N-methyl urea-induced rat mammary tumor model. Cancer Res. 61:8683-8688.
11. Couse JF, Curtis Hewitt S, Bunch DO, Sar M, Walker VR, Davis BJ, Korach KS. 1999. Postnatal sex reversal of ovaries in mice lacking estrogen receptors α and β. Science 286:2328-2331.
12. Couse JF, Korach KS. 1999. Estrogen receptor null mice: what have we learned and where will they lead us? Endocrine Rev 20:358-417.
13. Csapo AI, Csapo EF. 1973. Ovariectomy induced placental hypertrophy. Prostaglandins 4:189-200.
14. Dawson AB. 1925. The age order of epiphyseal union in the long bones of the albino rat. Anatomical Rec 31:1-17.
15. Dempster AP, Selwyn MR, Patel CM, Roth AJ. 1984. Statistical and computational aspects of mixed model analysis. Appl Stat 33:203-214.
16. Diener RM, Hsu BYD. 1967. Effects of certain phenolic ethers on the rat fetus. Toxicol Appl Pharmacol 10:565-576.
17. Dhingra K. 1999. Antiestrogens-tamoxifen, SERM and beyond. Invest New Drugs 17:285-311.
18. Dupont S, Krust A, Gansmuller A, Dierich A, Chambon P, Mark M. 2000. Effect of single and compound knockouts of estrogen receptors α (ERα) and β (ERβ) on mouse reproductive phenotypes. Development 127:4277-4291.
19. Food and Drug Administration. 1977. Tamoxifen: various scientific/medical reviews of NDA 17-970.
20. Furr BJ, Valcaccia B, Challis FRG. 1976. The effects of Nolvadex (tamoxifen citrate; ICI46,474) on pregnancy in rabbits. J Reprod Fertil 48:367-369.
21. Gray JM, Wade GN. 1981. Food intake, body weight and adiposity in female rats: actions and interactions of progestins and antiestrogens. Am J Physiol 240:E474-481.
22. Hollander M, Wolfe DA. 1973. Nonparametric statistical methods. New York: John Wiley.
23. Jauniaux E, Jurkovic D, Gulbis B, Collins WP, Zaidi J, Campbell S. 1994. Investigation of the acid-base balance of coelomic and amniotic fluids in early human pregnancy. Am J Obstet Gynecol 170:1365-1369.
24. Kauffman RF, Bryant HU. 1996. Selective estrogen receptor modulators. Drugs News Persp 8:531-539.
25. Ke HZ, Paralkar VM, Grasser WA, Crawford DT, Qi H, Simmons HA, Pirie CM, Chidsey-Frink KL, Owen TA, Smock SL, Chen HK, Jee WSS, Cameron KO, Rosati RL, Brown TA, Dasilva-Jardine P, Thompson DD. 1998. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus, and body composition in rat models. Endocrinology 139:2068-2076.
26. Ke HZ, Qi H, Crawford DT, Chidsey-Frink KL, Simmons HA, Thompson DD. 2000. Lasofoxifene (CP-336,156), a selective estrogen receptor modulator, prevents bone loss induced by aging and orchidectomy in the adult rat. Endocrinology 141:1338-1344.
27. Ke HZ, Qi H, Chidsey-Frink KL, Crawford DT, Thompson DD. 2001. Lasofoxifene (CP-336,156) protects against the age-related changes in bone mass, bone strength, and total serum cholesterol in intact aged male rats. J Bone Miner Res 16:765-773.
28. Kennedy J, Baris C, Hoyland JA, Selby PL, Freemont AJ, Braidman IP. 1999. Immunofluorescent localization of estrogen receptor-alpha in growth plates of rabbits, but not rats, at sexual maturity. Bone 24:9-16.
29. Labhesetwar AP. 1971. Effects of an antioestrogen on the corpus luteum of rabbits and rats. J Reprod Fertil 25:295-297.
30. Lotter EC, Krinsky R, Mckay JM, Treener CM, Prote D Jr, Woods SC. 1981. Somatostatin decreases food intake of rats and baboons. J Comp Physiol Psychol 95:278-287.
31. Nishimura M, Iizuki M, Iwaki S, Kast A. 1982. Repairability of drug-induced "wavy ribs" in rat offspring. Arzneimittelforschung 32:1518-1522.
32. Nau H, Scott WJ Jr. 1986. Weak acids may act as teratogens by accumulating in the basic milieu of the early mammalian embryo. Nature 323:276-278.
33. Neven P. 2002. New SERM in development. Eur J Cancer 38(Suppl): S26-S27.
34. Ornoy A. 1973. Transplacental effects of estrogen on osteogenesis in rat fetuses. Pathology 5:183-188.
35. Physician's Desk Reference. 1995. Nolvadex, New Jersey: Medical Economics. p 2758.
36. Rosati RL, Da Silva JP, Cameron KO, Thompson DD, Ke HZ, Toler SM, Brown TA, Pan LC, Ebbinghaus CF, Reinhold AR, Elliott NC, Newhouse BN, Tjoa CM, Sweetnam PM, Cole MJ, Arriola MW, Gauthier JW, Crawford DT, Nickerson DF, Pirie CM, Qi H, Simmons HA, Tkalcevic GT. 1998. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. J Med Chem 41:2928-2931.
37. Roth AJ. 1983. Robust trend tests derived and simulated: analogs of the Welch and Brown-Forsythe Tests. J Am Stat Assoc 78:972-980.
38. Roy EJ, Christie AM, Wade GN. 1977. Central action and a species comparison of the estrogenic effects of an antiestrogen on eating and body weight. Physiol Behav 18:137-140.
39. Sato M, McClintock C, Kim J, Turner CH, Bryant HU, Magee D, Slemenda CW. 1994. Dual-energy x-ray absorptiometry of raloxifene effects on the lumbar vertebrae and femora of ovariectomized rats. J Bone Miner Res 9:715-724.
40. Scalera G, Tarozzi G. 1998. Somatostatin administration alters taste preferences in the rat. Peptides 19:1565-1572.
41. Singh MM, Kamboj VP. 1992. Fetal resorption in rats treated with an antiestrogen in relation to luteal phase nidatory estrogen secretion. Acta Endocrinol 126:444-450.
42. Tannenbaum GS, Gurd W, Lapointe M, Pollak M. 1992. Tamoxifen attenuates pulsatile growth hormone secretion: Mediation in part by somatostatin. Endocrinology 130:3395-3401.
43. Teratostat System User Manual. 1996. Westford, MA: Statistics Unlimited Inc.
44. Terry KK, Cappon, GD, Hurtt, ME, Gupta U. 2004. Reproductive toxicity assessment of lasofoxifene, a selective estrogen receptor modulator (SERM), in female rats. Birth Defects Res B 71:150-160 (this issue).
45. Tornesi B, Carney E. 2003. Changes in pH, protein and osmolarity of the rabbit conceptus during gestation day (GD) 9-12. Birth Defects Res Part B 68:262.
46. Treinen KA, Rehm S, Weir PJ. 1998. An evaluation of the novel selective estrogen receptor modulator, idoxifene, for effects on reproduction in rats and rabbits. Toxicol Sci 41:199-207.
47. Tucker MJ, Adam HK, Patterson JS. 1984. Tamoxifen. In: Laurence DR, McLean AEM, Wetherall M, editors. Safety testing of new drugs. Laboratory predictions and clinical performance. London: Academic Press. p 125-161.
48. Wade GN, Gray JM, Blaustein JD. 1993. Effects of estrogens and antiestrogens on eating behavior, metabolism, and energy balance. Oncology 7:61-68.
49. Wade GN, Heller HW. 1993. Tamoxifen, mimics the effects of estradiol on food intake body weight and body composition in rats. Am J Physiol 264:R1219-1223.
50. Wallen WJ, Belanger MP, Wittnich C. 2002. Body weight and food intake profiles are modulated by sex hormones and tamoxifen in chronically hypertensive rats. J Nutr 132:2246-2250.
51. Wallen WJ, Belanger MP, Wittnich C. 2001. Sex hormones and the selective estrogen receptor modulator tamoxifen modulate weekly body weights and food intakes in adolescent and adult rats. J Nutr 131:2351-2357.
52. Weise M, De-Levis S, Barnes KM, Gafini RI. Abad V, Barin J. 2001. Effects of estrogen on growth plate senescence and epiphyseal fusion. Proc Natl Acad Sci USA 98:6871-6876.
53. Weisenburger WP, Hagler AR, Tassinari MS. 2004. Pre-and postnatal development studies of lasofoxifene, a selective estrogen receptor modulator (SERM), in Sprague-Dawley rats. Birth Defects Res B 71:171-184 (this issue).
54. Wise LD, Beck SL, Beltrame D, Beyer BK, Chahoud I, Clark RL, Clark R, Druga AM, Feuston MH, Guittin P, Henwood SM, Kimmel CA, Lindstrom P, Palmer AK, Petrere JA, Solomon HM, Yasuda M, York RG. 1997. Terminology of developmental abnormalities in common laboratory mammals (version 1). Teratology 55:249-292.