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  Barasertib

Aarasertib  is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, barasertib specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:  AstraZeneca, Inc

Phase I study of  barasertib (AZD1152).  barasertib (AZD1152) is a highly potent and selective Aurora B kinase inhibitor. The safety, efficacy and pharmacokinetic (PK) profile of barasertib were investigated in Japanese patients with advanced acute myeloid leukemia. Barasertib (50-1200mg) was administered as a continuous 7-day intravenous infusion every 21 days. No dose-limiting toxicities were reported and barasertib 1200mg was chosen for further evaluation in Japanese patients. Neutropenia and febrile neutropenia were the most commonly reported adverse events. The PK profile was similar to Western patients. A promising overall hematologic response rate of 19% was achieved, which warrants further investigation in these patients. (source: Leuk Res. 2011 Oct;35(10):1384-9. ).

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1: Löwenberg B, Muus P, Ossenkoppele G, Rousselot P, Cahn JY, Ifrah N, Martinelli G, Amadori S, Berman E, Sonneveld P, Jongen-Lavrencic M, Rigaudeau S, Stockman P, Goudie A, Faderl S, Jabbour E, Kantarjian H. Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia. Blood. 2011 Dec 1;118(23):6030-6. Epub 2011 Oct 5. PubMed PMID: 21976672.

2: Keizer RJ, Zandvliet AS, Beijnen JH, Schellens JH, Huitema AD. Two-stage model-based design of cancer phase I dose escalation trials: evaluation using the phase I program of barasertib (AZD1152). Invest New Drugs. 2011 May 28. [Epub ahead of print] PubMed PMID: 21626115.

3: Tsuboi K, Yokozawa T, Sakura T, Watanabe T, Fujisawa S, Yamauchi T, Uike N, Ando K, Kihara R, Tobinai K, Asou H, Hotta T, Miyawaki S. A Phase I study to assess the safety, pharmacokinetics and efficacy of barasertib (AZD1152), an Aurora B kinase inhibitor, in Japanese patients with advanced acute myeloid leukemia. Leuk Res. 2011 Oct;35(10):1384-9. Epub 2011 May 11. PubMed PMID: 21565405.

4: Mori N, Ishikawa C, Senba M, Kimura M, Okano Y. Effects of AZD1152, a selective Aurora B kinase inhibitor, on Burkitt's and Hodgkin's lymphomas. Biochem Pharmacol. 2011 May 1;81(9):1106-15. Epub 2011 Mar 1. Erratum in: Biochem Pharmacol. 2011 Nov 1;82(9):1252. PubMed PMID: 21371446.

5: Azzariti A, Bocci G, Porcelli L, Fioravanti A, Sini P, Simone GM, Quatrale AE, Chiarappa P, Mangia A, Sebastian S, Del Bufalo D, Del Tacca M, Paradiso A. Aurora B kinase inhibitor AZD1152: determinants of action and ability to enhance chemotherapeutics effectiveness in pancreatic and colon cancer. Br J Cancer. 2011 Mar 1;104(5):769-80. Epub 2011 Feb 8. PubMed PMID: 21304529; PubMed Central PMCID: PMC3048212.

6: Moroz MA, Kochetkov T, Cai S, Wu J, Shamis M, Nair J, de Stanchina E, Serganova I, Schwartz GK, Banerjee D, Bertino JR, Blasberg RG. Imaging colon cancer response following treatment with AZD1152: a preclinical analysis of [18F]fluoro-2-deoxyglucose and 3'-deoxy-3'-[18F]fluorothymidine imaging. Clin Cancer Res. 2011 Mar 1;17(5):1099-110. Epub 2011 Jan 18. PubMed PMID: 21245090; PubMed Central PMCID: PMC3079195.

7: Niermann KJ, Moretti L, Giacalone NJ, Sun Y, Schleicher SM, Kopsombut P, Mitchell LR, Kim KW, Lu B. Enhanced radiosensitivity of androgen-resistant prostate cancer: AZD1152-mediated Aurora kinase B inhibition. Radiat Res. 2011 Apr;175(4):444-51. Epub 2011 Jan 11. PubMed PMID: 21222513; PubMed Central PMCID: PMC3133747.

8: Libertini S, Abagnale A, Passaro C, Botta G, Barbato S, Chieffi P, Portella G. AZD1152 negatively affects the growth of anaplastic thyroid carcinoma cells and enhances the effects of oncolytic virus dl922-947. Endocr Relat Cancer. 2011 Jan 13;18(1):129-41. Print 2011 Feb. PubMed PMID: 21071467.

9: Boss DS, Witteveen PO, van der Sar J, Lolkema MP, Voest EE, Stockman PK, Ataman O, Wilson D, Das S, Schellens JH. Clinical evaluation of AZD1152, an i.v. inhibitor of Aurora B kinase, in patients with solid malignant tumors. Ann Oncol. 2011 Feb;22(2):431-7. Epub 2010 Oct 5. PubMed PMID: 20924078.

10: Grundy M, Seedhouse C, Shang S, Richardson J, Russell N, Pallis M. The FLT3 internal tandem duplication mutation is a secondary target of the aurora B kinase inhibitor AZD1152-HQPA in acute myelogenous leukemia cells. Mol Cancer Ther. 2010 Mar;9(3):661-72. Epub 2010 Feb 16. PubMed PMID: 20159992.

11: Tomita M, Tanaka Y, Mori N. Aurora kinase inhibitor AZD1152 negatively affects the growth and survival of HTLV-1-infected T lymphocytes in vitro. Int J Cancer. 2010 Oct 1;127(7):1584-94. Retraction in: Int J Cancer. 2011 Dec 1;129(11):2762-3. PubMed PMID: 20091867.

12: Aihara A, Tanaka S, Yasen M, Matsumura S, Mitsunori Y, Murakata A, Noguchi N, Kudo A, Nakamura N, Ito K, Arii S. The selective Aurora B kinase inhibitor AZD1152 as a novel treatment for hepatocellular carcinoma. J Hepatol. 2010 Jan;52(1):63-71. Epub 2009 Oct 29. PubMed PMID: 19913935.

13: Tao Y, Leteur C, Calderaro J, Girdler F, Zhang P, Frascogna V, Varna M, Opolon P, Castedo M, Bourhis J, Kroemer G, Deutsch E. The aurora B kinase inhibitor AZD1152 sensitizes cancer cells to fractionated irradiation and induces mitotic catastrophe. Cell Cycle. 2009 Oct 1;8(19):3172-81. Epub 2009 Oct 4. PubMed PMID: 19755861.

14: Pluim D, Beijnen JH, Schellens JH, van Tellingen O. Simultaneous determination of AZD1152 (prodrug) and AZD1152-hydroxyquinazoline pyrazol anilide by reversed phase liquid chromatography. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Nov 1;877(29):3549-55. Epub 2009 Aug 28. PubMed PMID: 19744901.

15: Oke A, Pearce D, Wilkinson RW, Crafter C, Odedra R, Cavenagh J, Fitzgibbon J, Lister AT, Joel S, Bonnet D. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8. Epub 2009 Apr 14. PubMed PMID: 19366807; PubMed Central PMCID: PMC2684546.

16: Nair JS, de Stanchina E, Schwartz GK. The topoisomerase I poison CPT-11 enhances the effect of the aurora B kinase inhibitor AZD1152 both in vitro and in vivo. Clin Cancer Res. 2009 Mar 15;15(6):2022-30. Epub 2009 Mar 10. PubMed PMID: 19276280.

17: Guo J, Anderson MG, Tapang P, Palma JP, Rodriguez LE, Niquette A, Li J, Bouska JJ, Wang G, Semizarov D, Albert DH, Donawho CK, Glaser KB, Shah OJ. Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152. Pharmacogenomics J. 2009 Apr;9(2):90-102. Epub 2009 Feb 3. PubMed PMID: 19188929.

18: Walsby E, Walsh V, Pepper C, Burnett A, Mills K. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica. 2008 May;93(5):662-9. Epub 2008 Mar 26. PubMed PMID: 18367484.

19: Tao Y, Zhang P, Girdler F, Frascogna V, Castedo M, Bourhis J, Kroemer G, Deutsch E. Enhancement of radiation response in p53-deficient cancer cells by the Aurora-B kinase inhibitor AZD1152. Oncogene. 2008 May 22;27(23):3244-55. Epub 2007 Dec 17. PubMed PMID: 18084327.

20: Evans RP, Naber C, Steffler T, Checkland T, Maxwell CA, Keats JJ, Belch AR, Pilarski LM, Lai R, Reiman T. The selective Aurora B kinase inhibitor AZD1152 is a potential new treatment for multiple myeloma. Br J Haematol. 2008 Feb;140(3):295-302. Epub 2007 Dec 10. PubMed PMID: 18076711.

21: Wilkinson RW, Odedra R, Heaton SP, Wedge SR, Keen NJ, Crafter C, Foster JR, Brady MC, Bigley A, Brown E, Byth KF, Barrass NC, Mundt KE, Foote KM, Heron NM, Jung FH, Mortlock AA, Boyle FT, Green S. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. PubMed PMID: 17575233.

22: Yang J, Ikezoe T, Nishioka C, Tasaka T, Taniguchi A, Kuwayama Y, Komatsu N, Bandobashi K, Togitani K, Koeffler HP, Taguchi H, Yokoyama A. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep 15;110(6):2034-40. Epub 2007 May 10. PubMed PMID: 17495131.