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Volumn 95, Issue 5, 2012, Pages 327-336

An Evaluation of Reproductive and Developmental Toxicity of Sitaxentan (Thelin) in Rats

Author keywords

Development; Endothelin; Fertility; Fetus; Postnatal; Prenatal; Sitaxentan; Toxicity

Indexed keywords

SITAXSENTAN;

EID: 84867342891     PISSN: 15429733     EISSN: 15429741     Source Type: Journal    
DOI: 10.1002/bdrb.21021     Document Type: Article
Times cited : (9)

References (45)
  • 2
    • 0026583343 scopus 로고
    • Massive amounts of immunoreactive endothelin in human seminal fluid
    • Casey ML, Byrd W, MacDonald PC. 1992. Massive amounts of immunoreactive endothelin in human seminal fluid. J Clin Endocrinol Metab 74(1):223-225.
    • (1992) J Clin Endocrinol Metab , vol.74 , Issue.1 , pp. 223-225
    • Casey, M.L.1    Byrd, W.2    MacDonald, P.C.3
  • 5
    • 84863643008 scopus 로고    scopus 로고
    • Evaluation of sitaxentan (Thelin®) toxicity in juvenile rats and regulatory interactions during the development of a European Medicines Agency Paediatric Investigation Plan
    • Regulatory Toxicology and Pharmacology 64:43-50.
    • Cross D, Derzi M, Horsley E, Owen K, Stavros F. 2012. Evaluation of sitaxentan (Thelin®) toxicity in juvenile rats and regulatory interactions during the development of a European Medicines Agency Paediatric Investigation Plan. Regulatory Toxicology and Pharmacology 64:43-50.
    • (2012)
    • Cross, D.1    Derzi, M.2    Horsley, E.3    Owen, K.4    Stavros, F.5
  • 6
    • 0003979209 scopus 로고    scopus 로고
    • New York, NY: Pfizer Inc.
    • Data on File. 2006. New York, NY: Pfizer Inc.
    • (2006) Data on File
  • 7
    • 0026023179 scopus 로고
    • Binding sites for iodinated endothelin-1, endothelin-2 and endothelin-3 demonstrated on human uterine glandular epithelial cells by quantitative high-resolution autoradiography
    • Davenport AP, Cameron IT, Smith SK, Brown MJ. 1991. Binding sites for iodinated endothelin-1, endothelin-2 and endothelin-3 demonstrated on human uterine glandular epithelial cells by quantitative high-resolution autoradiography. J Endocrinol 129(1):149-154.
    • (1991) J Endocrinol , vol.129 , Issue.1 , pp. 149-154
    • Davenport, A.P.1    Cameron, I.T.2    Smith, S.K.3    Brown, M.J.4
  • 10
    • 84881226210 scopus 로고
    • ICH Topic S 5 (R2) Detection of toxicity to reproduction for medicinal products & toxicity to male fertility
    • European Medicines Agency. Available at: Accessed January 30, 2012.
    • European Medicines Agency. 1994. ICH Topic S 5 (R2) Detection of toxicity to reproduction for medicinal products & toxicity to male fertility Available at: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2009/09/WC500002809.pdf. Accessed January 30, 2012.
    • (1994)
  • 11
    • 84881246522 scopus 로고    scopus 로고
    • Thelin scientific discussion: European Public Assessment Report
    • European Medicines Agency. Available at: Accessed January 30, 2012.
    • European Medicines Agency. 2007. Thelin scientific discussion: European Public Assessment Report. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Scientific_Discussion/human/000679/WC500037904.pdf. Accessed January 30, 2012.
    • (2007)
  • 12
    • 0027517566 scopus 로고
    • Rat testicular myoid cells respond to endothelin: characterization of binding and signal transduction pathway
    • Filippini A, Tripiciano A, Palombi F, Teti A, Paniccia R, Stefanini M, Ziparo E. 1993. Rat testicular myoid cells respond to endothelin: characterization of binding and signal transduction pathway. Endocrinology 133(4):1789-1796.
    • (1993) Endocrinology , vol.133 , Issue.4 , pp. 1789-1796
    • Filippini, A.1    Tripiciano, A.2    Palombi, F.3    Teti, A.4    Paniccia, R.5    Stefanini, M.6    Ziparo, E.7
  • 14
    • 79951841117 scopus 로고    scopus 로고
    • Liver toxicity of sitaxentan in pulmonary arterial hypertension
    • Galie N, Hoeper MM, Simon J, Gibbs R, Simonneau G. 2011. Liver toxicity of sitaxentan in pulmonary arterial hypertension. Eur Heart J 32(4):386-387.
    • (2011) Eur Heart J , vol.32 , Issue.4 , pp. 386-387
    • Galie, N.1    Hoeper, M.M.2    Simon, J.3    Gibbs, R.4    Simonneau, G.5
  • 17
    • 0028282650 scopus 로고
    • The level of endothelin-like immunoreactivity in seminal fluid correlates positively with semen volume and negatively with plasma gonadotrophin levels
    • Hammami MM, Haq A, AlSedairy S. 1994. The level of endothelin-like immunoreactivity in seminal fluid correlates positively with semen volume and negatively with plasma gonadotrophin levels. Clin Endocrinol (Oxf) 40(3):361-366.
    • (1994) Clin Endocrinol (Oxf) , vol.40 , Issue.3 , pp. 361-366
    • Hammami, M.M.1    Haq, A.2    AlSedairy, S.3
  • 19
    • 0031181999 scopus 로고    scopus 로고
    • Localization of endothelin-1 and endothelin-receptors A and B in human epididymis
    • Harneit S, Paust HJ, Mukhopadhyay AK, Ergun S. 1997b. Localization of endothelin-1 and endothelin-receptors A and B in human epididymis. Mol Hum Reprod 3(7):579-584.
    • (1997) Mol Hum Reprod , vol.3 , Issue.7 , pp. 579-584
    • Harneit, S.1    Paust, H.J.2    Mukhopadhyay, A.K.3    Ergun, S.4
  • 20
    • 71049136486 scopus 로고    scopus 로고
    • Pulmonary hypertension in pregnancy: two cases and review of the literature
    • Higton AM, Whale C, Musk M, Gabbay E. 2009. Pulmonary hypertension in pregnancy: two cases and review of the literature. Intern Med J 39(11):766-770.
    • (2009) Intern Med J , vol.39 , Issue.11 , pp. 766-770
    • Higton, A.M.1    Whale, C.2    Musk, M.3    Gabbay, E.4
  • 21
    • 0028639196 scopus 로고
    • Targeted and natural (piebald-lethal) mutations of endothelin-B receptor gene produce megacolon associated with spotted coat color in mice
    • Hosoda K, Hammer RE, Richardson JA, Baynash AG, Cheung JC, Giaid A, Yanagisawa M. 1994. Targeted and natural (piebald-lethal) mutations of endothelin-B receptor gene produce megacolon associated with spotted coat color in mice. Cell 79(7):1267-1276.
    • (1994) Cell , vol.79 , Issue.7 , pp. 1267-1276
    • Hosoda, K.1    Hammer, R.E.2    Richardson, J.A.3    Baynash, A.G.4    Cheung, J.C.5    Giaid, A.6    Yanagisawa, M.7
  • 22
    • 34548800378 scopus 로고    scopus 로고
    • Treatment of pulmonary arterial hypertension in pregnancy
    • Huang S, DeSantis ER. 2007. Treatment of pulmonary arterial hypertension in pregnancy. Am J Health Syst Pharm 64(18):1922-1926.
    • (2007) Am J Health Syst Pharm , vol.64 , Issue.18 , pp. 1922-1926
    • Huang, S.1    DeSantis, E.R.2
  • 23
    • 4644290657 scopus 로고    scopus 로고
    • Treatment of pulmonary arterial hypertension
    • Humbert M, Sitbon O, Simonneau G. 2004. Treatment of pulmonary arterial hypertension. N Engl J Med 351(14):1425-1436.
    • (2004) N Engl J Med , vol.351 , Issue.14 , pp. 1425-1436
    • Humbert, M.1    Sitbon, O.2    Simonneau, G.3
  • 24
    • 0036671015 scopus 로고    scopus 로고
    • (18)F-Endothelin-1, a positron emission tomography (PET) radioligand for the endothelin receptor system: radiosynthesis and in vivo imaging using microPET
    • Lond)
    • Johnstrom P, Harris NG, Fryer TD, Barret O, Clark JC, Pickard JD, Davenport AP. 2002. (18)F-Endothelin-1, a positron emission tomography (PET) radioligand for the endothelin receptor system: radiosynthesis and in vivo imaging using microPET. Clin Sci (Lond) 103(Suppl 48):4S-8S.
    • (2002) Clin Sci , vol.103 , Issue.SUPPL. 48
    • Johnstrom, P.1    Harris, N.G.2    Fryer, T.D.3    Barret, O.4    Clark, J.C.5    Pickard, J.D.6    Davenport, A.P.7
  • 27
    • 84867378066 scopus 로고    scopus 로고
    • Full prescribing information. Foster City, CA: Gilead Sciences Inc.
    • Letairis (ambrisentan). 2008. Full prescribing information. Foster City, CA: Gilead Sciences Inc.
    • (2008) Letairis (ambrisentan)
  • 28
    • 0034619523 scopus 로고    scopus 로고
    • Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel class of cardiovascular drugs
    • Luscher TF, Barton M. 2000. Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel class of cardiovascular drugs. Circulation 102(19):2434-2440.
    • (2000) Circulation , vol.102 , Issue.19 , pp. 2434-2440
    • Luscher, T.F.1    Barton, M.2
  • 29
    • 0032891535 scopus 로고    scopus 로고
    • Endothelin-1- and endothelin-receptors in lung biopsies of patients with pulmonary hypertension due to congenital heart disease
    • Lutz J, Gorenflo M, Habighorst M, Vogel M, Lange PE, Hocher B. 1999. Endothelin-1- and endothelin-receptors in lung biopsies of patients with pulmonary hypertension due to congenital heart disease. Clin Chem Lab Med 37(4):423-428.
    • (1999) Clin Chem Lab Med , vol.37 , Issue.4 , pp. 423-428
    • Lutz, J.1    Gorenflo, M.2    Habighorst, M.3    Vogel, M.4    Lange, P.E.5    Hocher, B.6
  • 31
    • 64849109410 scopus 로고    scopus 로고
    • ACCF/AHA2009 expert consensus document on pulmonary hypertension a report of the American College of Cardiology Foundation Task Force on Expert Consensus Documents and the American Heart Association developed in collaboration with the American College of Chest Physicians; American Thoracic Society, Inc.; and the Pulmonary Hypertension Association
    • McLaughlin VV, Archer SL, Badesch DB, Barst RJ, Farber HW, Lindner JR, Mathier MA, McGoon MD, Park MH, Rosenson RS, Rubin LJ, Tapson VF, Varga J. 2009. ACCF/AHA2009 expert consensus document on pulmonary hypertension a report of the American College of Cardiology Foundation Task Force on Expert Consensus Documents and the American Heart Association developed in collaboration with the American College of Chest Physicians; American Thoracic Society, Inc.; and the Pulmonary Hypertension Association. J Am Coll Cardiol 53(17):1573-1619.
    • (2009) J Am Coll Cardiol , vol.53 , Issue.17 , pp. 1573-1619
    • McLaughlin, V.V.1    Archer, S.L.2    Badesch, D.B.3    Barst, R.J.4    Farber, H.W.5    Lindner, J.R.6    Mathier, M.A.7    McGoon, M.D.8    Park, M.H.9    Rosenson, R.S.10    Rubin, L.J.11    Tapson, V.F.12    Varga, J.13
  • 32
    • 36249026290 scopus 로고    scopus 로고
    • The ovarian endothelin network: an evolving story
    • Meidan R, Levy N. 2007. The ovarian endothelin network: an evolving story. Trends Endocrinol Metab 18(10):379-385.
    • (2007) Trends Endocrinol Metab , vol.18 , Issue.10 , pp. 379-385
    • Meidan, R.1    Levy, N.2
  • 33
    • 17144432229 scopus 로고    scopus 로고
    • Eisenmenger's syndrome in a 27 week pregnancy-management with bosentan and sildenafil
    • Molelekwa V, Akhter P, McKenna P, Bowen M, Walsh K. 2005. Eisenmenger's syndrome in a 27 week pregnancy-management with bosentan and sildenafil. Ir Med J 98(3):87-88.
    • (2005) Ir Med J , vol.98 , Issue.3 , pp. 87-88
    • Molelekwa, V.1    Akhter, P.2    McKenna, P.3    Bowen, M.4    Walsh, K.5
  • 34
    • 84863849179 scopus 로고    scopus 로고
    • An overview of the preclinical toxicity and potential carcinogenicity of sitaxentan (Thelin®), a potent endothelin receptor antagonist (ETA) developed for pulmonary arterial hypertension
    • Regulatory Toxicology and Pharmacology 64:95-103.
    • Owen K, Derzi M, Horsley E, Cross D, Stavros F. 2012. An overview of the preclinical toxicity and potential carcinogenicity of sitaxentan (Thelin®), a potent endothelin receptor antagonist (ETA) developed for pulmonary arterial hypertension. Regulatory Toxicology and Pharmacology 64:95-103.
    • (2012)
    • Owen, K.1    Derzi, M.2    Horsley, E.3    Cross, D.4    Stavros, F.5
  • 36
    • 0029813755 scopus 로고    scopus 로고
    • The increase in human plasma immunoreactive endothelin but not big endothelin-1 or its C-terminal fragment induced by systemic administration of the endothelin antagonist TAK-044
    • Plumpton C, Ferro CJ, Haynes WG, Webb DJ, Davenport AP. 1996. The increase in human plasma immunoreactive endothelin but not big endothelin-1 or its C-terminal fragment induced by systemic administration of the endothelin antagonist TAK-044. Br J Pharmacol 119(2):311-314.
    • (1996) Br J Pharmacol , vol.119 , Issue.2 , pp. 311-314
    • Plumpton, C.1    Ferro, C.J.2    Haynes, W.G.3    Webb, D.J.4    Davenport, A.P.5
  • 37
    • 34447136110 scopus 로고    scopus 로고
    • Combined targeting of endothelin A receptor and epidermal growth factor receptor in ovarian cancer shows enhanced antitumor activity
    • Rosano L, Di Castro V, Spinella F, Tortora G, Nicotra MR, Natali PG, Bagnato A. 2007. Combined targeting of endothelin A receptor and epidermal growth factor receptor in ovarian cancer shows enhanced antitumor activity. Cancer Res 67(13):6351-6359.
    • (2007) Cancer Res , vol.67 , Issue.13 , pp. 6351-6359
    • Rosano, L.1    Di Castro, V.2    Spinella, F.3    Tortora, G.4    Nicotra, M.R.5    Natali, P.G.6    Bagnato, A.7
  • 38
    • 0035171979 scopus 로고    scopus 로고
    • Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension
    • Rubens C, Ewert R, Halank M, Wensel R, Orzechowski HD, Schultheiss HP, Hoeffken G. 2001. Big endothelin-1 and endothelin-1 plasma levels are correlated with the severity of primary pulmonary hypertension. Chest 120(5):1562-1569.
    • (2001) Chest , vol.120 , Issue.5 , pp. 1562-1569
    • Rubens, C.1    Ewert, R.2    Halank, M.3    Wensel, R.4    Orzechowski, H.D.5    Schultheiss, H.P.6    Hoeffken, G.7
  • 39
    • 0028232705 scopus 로고
    • Mechanisms by which endothelin-1 stimulates increased cytosolic free calcium ion concentrations in single rat Sertoli cells
    • Sharma OP, Flores JA, Leong DA, Veldhuis JD. 1994. Mechanisms by which endothelin-1 stimulates increased cytosolic free calcium ion concentrations in single rat Sertoli cells. Endocrinology 135(1):127-134.
    • (1994) Endocrinology , vol.135 , Issue.1 , pp. 127-134
    • Sharma, O.P.1    Flores, J.A.2    Leong, D.A.3    Veldhuis, J.D.4
  • 40
    • 84867360673 scopus 로고    scopus 로고
    • Thelin (sitaxentan) 100 mg. Summary of Product Characteristics. Sandwich, UK: Pfizer Ltd.
    • Thelin (sitaxentan) 100 mg. 2009. Summary of Product Characteristics. Sandwich, UK: Pfizer Ltd.
    • (2009)
  • 41
    • 84867360674 scopus 로고    scopus 로고
    • Tracleer (bosentan). Full Prescribing Information. South San Francisco, CA: Actelion Pharmaceuticals US, Inc.
    • Tracleer (bosentan). 2009. Full Prescribing Information. South San Francisco, CA: Actelion Pharmaceuticals US, Inc.
    • (2009)
  • 42
    • 0033028390 scopus 로고    scopus 로고
    • Developmental toxicity and toxicokinetics of two endothelin receptor antagonists in rats and rabbits
    • Treinen KA, Louden C, Dennis MJ, Wier PJ. 1999. Developmental toxicity and toxicokinetics of two endothelin receptor antagonists in rats and rabbits. Teratology 59(1):51-59.
    • (1999) Teratology , vol.59 , Issue.1 , pp. 51-59
    • Treinen, K.A.1    Louden, C.2    Dennis, M.J.3    Wier, P.J.4
  • 43
    • 0031747446 scopus 로고    scopus 로고
    • Outcome of pulmonary vascular disease in pregnancy: a systematic overview from 1978 through 1996
    • Weiss BM, Zemp L, Seifert B, Hess OM. 1998. Outcome of pulmonary vascular disease in pregnancy: a systematic overview from 1978 through 1996. J Am Coll Cardiol 31(7):1650-1657.
    • (1998) J Am Coll Cardiol , vol.31 , Issue.7 , pp. 1650-1657
    • Weiss, B.M.1    Zemp, L.2    Seifert, B.3    Hess, O.M.4
  • 45
    • 0025838213 scopus 로고
    • Plasma endothelin concentrations in patients with pulmonary hypertension associated with congenital heart defects. Evidence for increased production of endothelin in pulmonary circulation
    • Yoshibayashi M, Nishioka K, Nakao K, Saito Y, Matsumura M, Ueda T, Temma S, Shirakami G, Imura H, Mikawa H. 1991. Plasma endothelin concentrations in patients with pulmonary hypertension associated with congenital heart defects. Evidence for increased production of endothelin in pulmonary circulation. Circulation 84(6):2280-2285.
    • (1991) Circulation , vol.84 , Issue.6 , pp. 2280-2285
    • Yoshibayashi, M.1    Nishioka, K.2    Nakao, K.3    Saito, Y.4    Matsumura, M.5    Ueda, T.6    Temma, S.7    Shirakami, G.8    Imura, H.9    Mikawa, H.10


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