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Cediranib

Description of Cediranib (AZD-2171): Cediranib is an indole ether quinazoline derivative with antineoplastic activities. Competing with adenosine triphosphate, cediranib binds to and inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer: AstraZeneca Pharmaceuticals LP.

According to http://en.wikipedia.org/wiki/Cediranib, Cediranib is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases. It is being developed by AstraZeneca as a possible anti-cancer chemotherapeutic agent for oral administration. Beginning in 2007, it is undergoing Phase I clinical trials for the treatment of non-small cell lung cancer, kidney cancer, and colorectal cancer in adults, as well as tumors of the central nervous system in children. Phase I trials of interactions with other drugs used in cancer treatment are also underway. On February 27, 2008, AstraZeneca announced that the use of Recentin in non-small cell lung cancer will not progress into phase III after failing to meet its main goal. On 8th March 2010, AstraZeneca issued a press-release stating that Recentin had failed Phase III clinical trials for use in first-line metastatic colorectal cancer when it was compared clinically with the market-leader Avastin.

1: Morelli MP, Brown AM, Pitts TM, Tentler JJ, Ciardiello F, Ryan A, Jürgensmeier JM, Eckhardt SG. Targeting vascular endothelial growth factor receptor-1 and -3 with cediranib (AZD2171): effects on migration and invasion of gastrointestinal cancer cell lines. Mol Cancer Ther. 2009 Sep;8(9):2546-58. Epub 2009 Sep 15. PubMed PMID: 19755510; PubMed Central PMCID: PMC2819052.

2: Tao LY, Liang YJ, Wang F, Chen LM, Yan YY, Dai CL, Fu LW. Cediranib (recentin, AZD2171) reverses ABCB1- and ABCC1-mediated multidrug resistance by inhibition of their transport function. Cancer Chemother Pharmacol. 2009 Oct;64(5):961-9. Epub 2009 Mar 3. PubMed PMID: 19255759.

3: Siemann DW, Brazelle WD, Jürgensmeier JM. The vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor cediranib (Recentin; AZD2171) inhibits endothelial cell function and growth of human renal tumor xenografts. Int J Radiat Oncol Biol Phys. 2009 Mar 1;73(3):897-903. PubMed PMID: 19215823; PubMed Central PMCID: PMC2788500.

4: Robertson JD, Botwood NA, Rothenberg ML, Schmoll HJ. Phase III trial of FOLFOX plus bevacizumab or cediranib (AZD2171) as first-line treatment of patients with metastatic colorectal cancer: HORIZON III. Clin Colorectal Cancer. 2009 Jan;8(1):59-60. PubMed PMID: 19203899.

5: Williams KJ, Telfer BA, Shannon AM, Babur M, Stratford IJ, Wedge SR. Inhibition of vascular endothelial growth factor signalling using cediranib (RECENTIN; AZD2171) enhances radiation response and causes substantial physiological changes in lung tumour xenografts. Br J Radiol. 2008 Oct;81 Spec No 1:S21-7. PubMed PMID: 18819995.

6: Bradley DP, Tessier JJ, Lacey T, Scott M, Jürgensmeier JM, Odedra R, Mills J, Kilburn L, Wedge SR. Examining the acute effects of cediranib (RECENTIN, AZD2171) treatment in tumor models: a dynamic contrast-enhanced MRI study using gadopentate. Magn Reson Imaging. 2009 Apr;27(3):377-84. Epub 2008 Sep 23. PubMed PMID: 18814988.

7: Curwen JO, Musgrove HL, Kendrew J, Richmond GH, Ogilvie DJ, Wedge SR. Inhibition of vascular endothelial growth factor-a signaling induces hypertension: examining the effect of cediranib (recentin; AZD2171) treatment on blood pressure in rat and the use of concomitant antihypertensive therapy. Clin Cancer Res. 2008 May 15;14(10):3124-31. PubMed PMID: 18483380.

8: Laurie SA, Gauthier I, Arnold A, Shepherd FA, Ellis PM, Chen E, Goss G, Powers J, Walsh W, Tu D, Robertson J, Puchalski TA, Seymour L. Phase I and pharmacokinetic study of daily oral AZD2171, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with carboplatin and paclitaxel in patients with advanced non-small-cell lung cancer: the National Cancer Institute of Canada clinical trials group. J Clin Oncol. 2008 Apr 10;26(11):1871-8. PubMed PMID: 18398152.

9: Smith NR, James NH, Oakley I, Wainwright A, Copley C, Kendrew J, Womersley LM, Jürgensmeier JM, Wedge SR, Barry ST. Acute pharmacodynamic and antivascular effects of the vascular endothelial growth factor signaling inhibitor AZD2171 in Calu-6 human lung tumor xenografts. Mol Cancer Ther. 2007 Aug;6(8):2198-208. PubMed PMID: 17699717.

10: Hanrahan EO, Heymach JV. Vascular endothelial growth factor receptor tyrosine kinase inhibitors vandetanib (ZD6474) and AZD2171 in lung cancer. Clin Cancer Res. 2007 Aug 1;13(15 Pt 2):s4617-22. Review. PubMed PMID: 17671152.

11: Gomez-Rivera F, Santillan-Gomez AA, Younes MN, Kim S, Fooshee D, Zhao M, Jasser SA, Myers JN. The tyrosine kinase inhibitor, AZD2171, inhibits vascular endothelial growth factor receptor signaling and growth of anaplastic thyroid cancer in an orthotopic nude mouse model. Clin Cancer Res. 2007 Aug 1;13(15 Pt 1):4519-27. PubMed PMID: 17671138.

12: Drevs J, Siegert P, Medinger M, Mross K, Strecker R, Zirrgiebel U, Harder J, Blum H, Robertson J, Jürgensmeier JM, Puchalski TA, Young H, Saunders O, Unger C. Phase I clinical study of AZD2171, an oral vascular endothelial growth factor signaling inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2007 Jul 20;25(21):3045-54. PubMed PMID: 17634482.

13: Takeda M, Arao T, Yokote H, Komatsu T, Yanagihara K, Sasaki H, Yamada Y, Tamura T, Fukuoka K, Kimura H, Saijo N, Nishio K. AZD2171 shows potent antitumor activity against gastric cancer over-expressing fibroblast growth factor receptor 2/keratinocyte growth factor receptor. Clin Cancer Res. 2007 May 15;13(10):3051-7. PubMed PMID: 17505008.

14: Bradley DP, Tessier JL, Checkley D, Kuribayashi H, Waterton JC, Kendrew J, Wedge SR. Effects of AZD2171 and vandetanib (ZD6474, Zactima) on haemodynamic variables in an SW620 human colon tumour model: an investigation using dynamic contrast-enhanced MRI and the rapid clearance blood pool contrast agent, P792 (gadomelitol). NMR Biomed. 2008 Jan;21(1):42-52. Erratum in: NMR Biomed. 2008 Mar;21(3):302. PubMed PMID: 17458919.

15: Ryan CJ, Stadler WM, Roth B, Hutcheon D, Conry S, Puchalski T, Morris C, Small EJ. Phase I dose escalation and pharmacokinetic study of AZD2171, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinase, in patients with hormone refractory prostate cancer (HRPC). Invest New Drugs. 2007 Oct;25(5):445-51. Epub 2007 Apr 26. PubMed PMID: 17458505.

16: Maris JM, Courtright J, Houghton PJ, Morton CL, Gorlick R, Kolb EA, Lock R, Tajbakhsh M, Reynolds CP, Keir ST, Wu J, Smith MA. Initial testing of the VEGFR inhibitor AZD2171 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Mar;50(3):581-7. PubMed PMID: 17457854.

17: Williams KJ, Telfer BA, Shannon AM, Babur M, Stratford IJ, Wedge SR. Combining radiotherapy with AZD2171, a potent inhibitor of vascular endothelial growth factor signaling: pathophysiologic effects and therapeutic benefit. Mol Cancer Ther. 2007 Feb;6(2):599-606. PubMed PMID: 17308057.

18: Batchelor TT, Sorensen AG, di Tomaso E, Zhang WT, Duda DG, Cohen KS, Kozak KR, Cahill DP, Chen PJ, Zhu M, Ancukiewicz M, Mrugala MM, Plotkin S, Drappatz J, Louis DN, Ivy P, Scadden DT, Benner T, Loeffler JS, Wen PY, Jain RK. AZD2171, a pan-VEGF receptor tyrosine kinase inhibitor, normalizes tumor vasculature and alleviates edema in glioblastoma patients. Cancer Cell. 2007 Jan;11(1):83-95. PubMed PMID: 17222792; PubMed Central PMCID: PMC2748664.

19: Cao C, Albert JM, Geng L, Ivy PS, Sandler A, Johnson DH, Lu B. Vascular endothelial growth factor tyrosine kinase inhibitor AZD2171 and fractionated radiotherapy in mouse models of lung cancer. Cancer Res. 2006 Dec 1;66(23):11409-15. PubMed PMID: 17145887.

20: Meijerink MR, van Cruijsen H, Hoekman K, Kater M, van Schaik C, van Waesberghe JH, Giaccone G, Manoliu RA. The use of perfusion CT for the evaluation of therapy combining AZD2171 with gefitinib in cancer patients. Eur Radiol. 2007 Jul;17(7):1700-13. Epub 2006 Oct 27. PubMed PMID: 17072618.

21: Miller KD, Miller M, Mehrotra S, Agarwal B, Mock BH, Zheng QH, Badve S, Hutchins GD, Sledge GW Jr. A physiologic imaging pilot study of breast cancer treated with AZD2171. Clin Cancer Res. 2006 Jan 1;12(1):281-8. PubMed PMID: 16397053.

22: Denduluri N, Tan AR, Walshe J, Berman A, Yang SX, Chow CK, Swain SM. A pilot study to evaluate the vascular endothelial growth factor receptor tyrosine kinase inhibitor AZD2171 and chemotherapy in locally advanced and inflammatory breast cancer. Clin Breast Cancer. 2005 Dec;6(5):460-3. PubMed PMID: 16381631.

23: Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO, Chester R, Jackson JA, Boffey SJ, Kilburn LL, Barnett S, Richmond GH, Wadsworth PF, Walker M, Bigley AL, Taylor ST, Cooper L, Beck S, Jürgensmeier JM, Ogilvie DJ. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res. 2005 May 15;65(10):4389-400. PubMed PMID: 15899831.