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Ropidoxuridine

Ropidoxuridine is a novel, orally available, thymidine analogue and prodrug for IUdR, which demonstrated a survival advantage in Phase II studies in anaplastic astrocytoma, a type of glioma. Preclinical studies have also demonstrated that Ropidoxuridine has dose responsive and synergistic effects when combined with radiation in human glioblastoma models. Ropidoxuridine has also shown reduced toxicity, with better tissue incorporation and improved anti-tumor activity when compared to IUdR in nonclinical models. Ropidoxuridine is currently in Phase I clinical trials in patients with colorectal, gastric, and pancreatic cancer, and other solid tumors. In addition, a Phase I/II clinical trial in malignant glioma is planned. see http://www.docguide.com/news/content.nsf/news/852571020057CCF68525718800485D5C.

Current developer:     Hana Biosciences, Inc。

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16. Seo, Yuji; Yan, Tao; Schupp, Jane E.; Colussi, Valdir; Taylor, Kerri L.; Kinsella, Timothy J. Differential Radiosensitization in DNA Mismatch Repair-Proficient and -Deficient Human Colon Cancer Xenografts with 5-Iodo-2-pyrimidinone-2'-deoxyribose. Clinical Cancer Research (2004), 10(22), 7520-7528. CODEN: CCREF4 ISSN:1078-0432. CAN 143:40069 AN 2004:1024812

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35. Seo Yuji; Yan Tao; Schupp Jane E; Radivoyevitch Tomas; Kinsella Timothy J Schedule-dependent drug effects of oral 5-iodo-2-pyrimidinone-2'-deoxyribose as an in vivo radiosensitizer in U251 human glioblastoma xenografts. Clinical cancer research : an official journal of the American Association for Cancer Research (2005), 11(20), 7499-507. Journal code: 9502500. ISSN:1078-0432. PubMed ID 16243824 AN 2005565222

36. Seo Yuji; Yan Tao; Schupp Jane E; Colussi Valdir; Taylor Kerri L; Kinsella Timothy J Differential radiosensitization in DNA mismatch repair-proficient and -deficient human colon cancer xenografts with 5-iodo-2-pyrimidinone-2'-deoxyribose. Clinical cancer research : an official journal of the American Association for Cancer Research (2004), 10(22), 7520-8. Journal code: 9502500. ISSN:1078-0432. PubMed ID 15569982 AN 2004595850

37. Kinsella T J; Schupp J E; Davis T W; Berry S E; Hwang H S; Warren K; Balis F; Barnett J; Sands H Preclinical study of the systemic toxicity and pharmacokinetics of 5-iodo-2-deoxypyrimidinone-2'-deoxyribose as a radiosensitizing prodrug in two, non-rodent animal species: implications for phase I study design. Clinical cancer research : an official journal of the American Association for Cancer Research (2000), 6(9), 3670-9. Journal code: 9502500. ISSN:1078-0432. PubMed ID 10999760 AN 2000447188

38. Kinsella T J; Vielhuber K A; Kunugi K A; Schupp J; Davis T W; Sands H Preclinical toxicity and efficacy study of a 14-day schedule of oral 5-iodo-2-pyrimidinone-2'-deoxyribose as a prodrug for 5-iodo-2'-deoxyuridine radiosensitization in U251 human glioblastoma xenografts. Clinical cancer research : an official journal of the American Association for Cancer Research (2000), 6(4), 1468-75. Journal code: 9502500. ISSN:1078-0432. PubMed ID 10778979 AN 2000239250

39. Kinsella T J; Kunugi K A; Vielhuber K A; Potter D M; Fitzsimmons M E; Collins J M Preclinical evaluation of 5-iodo-2-pyrimidinone-2'-deoxyribose as a prodrug for 5-iodo-2'-deoxyuridine-mediated radiosensitization in mouse and human tissues. Clinical cancer research : an official journal of the American Association for Cancer Research (1998), 4(1), 99-109. Journal code: 9502500. ISSN:1078-0432. PubMed ID 9516958 AN 1998177602

40. Kinsella T J; Kunugi K A; Vielhuber K A; McCulloch W; Liu S H; Cheng Y C An in vivo comparison of oral 5-iodo-2'-deoxyuridine and 5-iodo-2-pyrimidinone-2'-deoxyribose toxicity, pharmacokinetics, and DNA incorporation in athymic mouse tissues and the human colon cancer xenograft, HCT-116. Cancer research (1994), 54(10), 2695-700. Journal code: 2984705R. ISSN:0008-5472. PubMed ID 8168099 AN 1994221601

41. Chang C N; Doong S L; Cheng Y C Conversion of 5-iodo-2-pyrimidinone-2'-deoxyribose to 5-iodo-deoxyuridine by aldehyde oxidase. Implication in hepatotropic drug design. Biochemical pharmacology (1992), 43(10), 2269-73. Journal code: 0101032. ISSN:0006-2952. PubMed ID 1599512 AN 1992287174

42. Lewandowski G A; Cheng Y C Mechanism and mode of action of 5-iodo-2-pyrimidinone 2'-deoxyribonucleoside, a potent anti-herpes simplex virus compound, in herpes simplex virus-infected cells. Molecular pharmacology (1991), 39(1), 27-33. Journal code: 0035623. ISSN:0026-895X. PubMed ID 1846219 AN 1991101624

43. Efange S M; Alessi E M; Shih H C; Cheng Y C; Bardos T J Synthesis and biological activities of 2-pyrimidinone nucleosides. 2. 5-Halo-2-pyrimidinone 2'-deoxyribonucleosides. Journal of medicinal chemistry (1985), 28(7), 904-10. Journal code: 9716531. ISSN:0022-2623. PubMed ID 2989522 AN 1985237324