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Chemical Compound Review

Atrasentan     (2R,3R,4S)-4- benzo[1,3]dioxol-5-yl-1...

Synonyms: Xinlay, CHEMBL9194, ABT-627, SureCN34654, ABT627, ...
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Disease relevance of Arasentan


High impact information on Arasentan


Chemical compound and disease context of Arasentan


Biological context of Arasentan


Anatomical context of Arasentan

  • METHODS: Twenty male Sprague-Dawley rats received either 5 mg/kg of A-127722 or vehicle (n=10 per group) intravenously 30 minutes and subcutaneously 4 hours after middle cerebral artery occlusion (MCAO) [18].
  • METHODS: Atrasentan uptake was measured in HeLa cells transfected to express major alleles of organic anion transporting polypeptide 1B1 (OATP1B1) [17].
  • Local pretreatment with BQ-123 or A-127722 (150 pmol), two selective and chemically unrelated endothelin ET(A) receptor antagonists, inhibits neutrophil and eosinophil accumulation in LPS-induced pleurisy at 24 h but not neutrophil migration at 4 h [19].
  • 6. The data are consistent with choroidal arteriolar smooth muscle cells having two types of Et(A) receptor, one where BQ123 is an antagonist and ABT-627 an agonist, where ligands dissociate freely and this receptor is coupled to inhibition of L-type Ca(2+) channels [20].
  • ABT-627 did reduce the accumulation of macrophages in both stains (36 to 53%) whereas it blocked by 76% the influx of eosinophils in Balb/c but not in C57Bl/6 mice [21].

Associations of Arasentan with other chemical compounds


Gene context of Arasentan


Analytical, diagnostic and therapeutic context of Arasentan

  • In nude mice, the ET(A)R-selective antagonist atrasentan inhibits the growth and the neoangiogenesis of cervical carcinoma cell xenografts [29].
  • In a phase I, single-center, double-blind, randomized, three-period, crossover design, the effects of orally administered ABT-627, a selective ET(A) receptor antagonist, on renal hemodynamics during ET-1 infusion were evaluated [22].
  • The pressor response to intravenous injection of Big endothelin-1 (1 nmol/kg, intravenously) was inhibited by > 50% in rats given A-127722 at 10 mg/kg per d, which confirms the efficacy of A-127722 in blocking ETA-mediated responses when placed in drinking water [30].
  • Atrasentan was rapidly absorbed after oral administration; mean time to maximum observed concentration ranged from 0.3 to 1.7 h [31].
  • The beneficial effect of A-127722 was limited to animals in which successful reperfusion was demonstrated [18].


  1. Effect of endothelin-A receptor blockade with atrasentan on tumor progression in men with hormone-refractory prostate cancer: a randomized, phase II, placebo-controlled trial. Carducci, M.A., Padley, R.J., Breul, J., Vogelzang, N.J., Zonnenberg, B.A., Daliani, D.D., Schulman, C.C., Nabulsi, A.A., Humerickhouse, R.A., Weinberg, M.A., Schmitt, J.L., Nelson, J.B. J. Clin. Oncol. (2003) [Pubmed]
  2. Therapeutic targeting of the endothelin a receptor in human ovarian carcinoma. Rosanò, L., Spinella, F., Salani, D., Di Castro, V., Venuti, A., Nicotra, M.R., Natali, P.G., Bagnato, A. Cancer Res. (2003) [Pubmed]
  3. Endothelin axis is a target of the lung metastasis suppressor gene RhoGDI2. Titus, B., Frierson, H.F., Conaway, M., Ching, K., Guise, T., Chirgwin, J., Hampton, G., Theodorescu, D. Cancer Res. (2005) [Pubmed]
  4. Atrasentan, an endothelin-receptor antagonist for refractory adenocarcinomas: safety and pharmacokinetics. Carducci, M.A., Nelson, J.B., Bowling, M.K., Rogers, T., Eisenberger, M.A., Sinibaldi, V., Donehower, R., Leahy, T.L., Carr, R.A., Isaacson, J.D., Janus, T.J., Andre, A., Hosmane, B.S., Padley, R.J. J. Clin. Oncol. (2002) [Pubmed]
  5. Perinecrotic hypoxia contributes to ischemia/reperfusion-accelerated outgrowth of colorectal micrometastases. van der Bilt, J.D., Soeters, M.E., Duyverman, A.M., Nijkamp, M.W., Witteveen, P.O., van Diest, P.J., Kranenburg, O., Borel Rinkes, I.H. Am. J. Pathol. (2007) [Pubmed]
  6. Phase I safety study of escalating doses of atrasentan in adults with recurrent malignant glioma. Phuphanich, S., Carson, K.A., Grossman, S.A., Lesser, G., Olson, J., Mikkelsen, T., Desideri, S., Fisher, J.D. Neuro-oncology (2008) [Pubmed]
  7. Myocardial fibrosis in DOCA-salt hypertensive rats: effect of endothelin ET(A) receptor antagonism. Ammarguellat, F., Larouche, I., Schiffrin, E.L. Circulation (2001) [Pubmed]
  8. Vascular endothelin-1 gene expression and effect on blood pressure of chronic ETA endothelin receptor antagonism after nitric oxide synthase inhibition with L-NAME in normal rats. Sventek, P., Turgeon, A., Schiffrin, E.L. Circulation (1997) [Pubmed]
  9. Endothelin-1 promotes epithelial-to-mesenchymal transition in human ovarian cancer cells. Rosanò, L., Spinella, F., Di Castro, V., Nicotra, M.R., Dedhar, S., de Herreros, A.G., Natali, P.G., Bagnato, A. Cancer Res. (2005) [Pubmed]
  10. Arrhythmogenic effects induced by coronary conversion of pulmonary big endothelin to endothelin: aggravation of this phenomenon in heritable hyperlipidemia. Alexiou, K., Dschietzig, T., Simsch, O., Laule, M., Hundertmark, J., Baumann, G., Stangl, K. J. Am. Coll. Cardiol. (1998) [Pubmed]
  11. Different contributions of endothelin-A and endothelin-B receptors in the pathogenesis of deoxycorticosterone acetate-salt-induced hypertension in rats. Matsumura, Y., Hashimoto, N., Taira, S., Kuro, T., Kitano, R., Ohkita, M., Opgenorth, T.J., Takaoka, M. Hypertension (1999) [Pubmed]
  12. Cardioprotective effects of atrasentan, an endothelin-A receptor antagonist, but not of nitric oxide in diabetic mice with myocyte-specific overexpression of endothelial nitric oxide synthase. Wölkart, G., Stessel, H., Saad, Z., Kirchengast, M., Brunner, F. Br. J. Pharmacol. (2006) [Pubmed]
  13. Randomized phase II study of atrasentan alone or in combination with zoledronic acid in men with metastatic prostate cancer. Michaelson, M.D., Kaufman, D.S., Kantoff, P., Oh, W.K., Smith, M.R. Cancer (2006) [Pubmed]
  14. Effects of ETA and ETB Receptor Blockade on Post-ischemic Cardiac Dysfunction and Norepinephrine Overflow in Isolated Rat Hearts. Yamamoto, S., Matsumoto, N., Kanazawa, M., Fujita, M., Takaoka, M., Matsumura, Y. J. Cardiovasc. Pharmacol. (2004) [Pubmed]
  15. Endothelin-1 decreases gap junctional intercellular communication by inducing phosphorylation of connexin 43 in human ovarian carcinoma cells. Spinella, F., Rosanò, L., Di Castro, V., Nicotra, M.R., Natali, P.G., Bagnato, A. J. Biol. Chem. (2003) [Pubmed]
  16. Endothelin A Receptor Blockade Reduces Diabetic Renal Injury via an Anti-Inflammatory Mechanism. Sasser, J.M., Sullivan, J.C., Hobbs, J.L., Yamamoto, T., Pollock, D.M., Carmines, P.K., Pollock, J.S. J. Am. Soc. Nephrol. (2007) [Pubmed]
  17. Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Katz, D.A., Carr, R., Grimm, D.R., Xiong, H., Holley-Shanks, R., Mueller, T., Leake, B., Wang, Q., Han, L., Wang, P.G., Edeki, T., Sahelijo, L., Doan, T., Allen, A., Spear, B.B., Kim, R.B. Clin. Pharmacol. Ther. (2006) [Pubmed]
  18. A novel endothelin antagonist, A-127722, attenuates ischemic lesion size in rats with temporary middle cerebral artery occlusion: a diffusion and perfusion MRI study. Tatlisumak, T., Carano, R.A., Takano, K., Opgenorth, T.J., Sotak, C.H., Fisher, M. Stroke (1998) [Pubmed]
  19. Effects of endothelin ETA receptor antagonism on granulocyte and lymphocyte accumulation in LPS-induced inflammation. Sampaio, A.L., Rae, G.A., Henriques, M.G. J. Leukoc. Biol. (2004) [Pubmed]
  20. Evidence for two endothelin Et(A) receptor subtypes in rabbit arteriolar smooth muscle. Curtis, T.M., Scholfield, C.N. Br. J. Pharmacol. (2001) [Pubmed]
  21. Effects of a selective ET(A)-receptor antagonist, atrasentan (ABT-627), in murine models of allergic asthma: demonstration of mouse strain specificity. Gosselin, M., Goulet, S., Wu-Wong, J.R., Wessale, J.L., Opgenorth, T.J., Boulet, L.P., Battistini, B. Clin. Sci. (2002) [Pubmed]
  22. Selective ET(A) receptor antagonism with ABT-627 attenuates all renal effects of endothelin in humans. Honing, M.L., Hijmering, M.L., Ballard, D.E., Yang, Y.P., Padley, R.J., Morrison, P.J., Rabelink, T.J. J. Am. Soc. Nephrol. (2000) [Pubmed]
  23. Endothelin-1 receptor blockade prevents renal injury in experimental hypercholesterolemia. Chade, A.R., Best, P.J., Rodriguez-Porcel, M., Herrmann, J., Zhu, X., Sawamura, T., Napoli, C., Lerman, A., Lerman, L.O. Kidney Int. (2003) [Pubmed]
  24. Pyrrolidine-3-carboxylic acids as endothelin antagonists. 3. Discovery of a potent, 2-nonaryl, highly selective ETA antagonist (A-216546). Liu, G., Henry, K.J., Szczepankiewicz, B.G., Winn, M., Kozmina, N.S., Boyd, S.A., Wasicak, J., von Geldern, T.W., Wu-Wong, J.R., Chiou, W.J., Dixon, D.B., Nguyen, B., Marsh, K.C., Opgenorth, T.J. J. Med. Chem. (1998) [Pubmed]
  25. Endothelin receptor antagonists: effect of serum albumin on potency and comparison of pharmacological characteristics. Wu-Wong, J.R., Dixon, D.B., Chiou, W.J., Opgenorth, T.J. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  26. Endothelin a receptor blockade and endothelin B receptor blockade improve hypokalemic nephropathy by different mechanisms. Suga, S., Yasui, N., Yoshihara, F., Horio, T., Kawano, Y., Kangawa, K., Johnson, R.J. J. Am. Soc. Nephrol. (2003) [Pubmed]
  27. Inhibition of cyclooxygenase-1 and -2 expression by targeting the endothelin a receptor in human ovarian carcinoma cells. Spinella, F., Rosanò, L., Di Castro, V., Nicotra, M.R., Natali, P.G., Bagnato, A. Clin. Cancer Res. (2004) [Pubmed]
  28. Endothelin A receptor blockade does not alter PSA secretion in prostate cancer cell lines. Pecher, S., Pflug, B.R., Brink, A.K., Nelson, J.B. Prostate (2004) [Pubmed]
  29. Growth inhibition of cervix carcinoma cells in vivo by endothelin A receptor blockade. Bagnato, A., Cirilli, A., Salani, D., Simeone, P., Muller, A., Nicotra, M.R., Natali, P.G., Venuti, A. Cancer Res. (2002) [Pubmed]
  30. ETA receptor blockade prevents hypertension associated with exogenous endothelin-1 but not renal mass reduction in the rat. Pollock, D.M., Polakowski, J.S. J. Am. Soc. Nephrol. (1997) [Pubmed]
  31. Dose-ranging study of the safety and pharmacokinetics of atrasentan in patients with refractory malignancies. Ryan, C.W., Vogelzang, N.J., Vokes, E.E., Kindler, H.L., Undevia, S.D., Humerickhouse, R., André, A.K., Wang, Q., Carr, R.A., Ratain, M.J. Clin. Cancer Res. (2004) [Pubmed]
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