Summary: An analog of DEOXYURIDINE that inhibits viral DNA synthesis. The drug is used as an antiviral agent.

Top Publications

  1. Seth A, Misra A, Umrigar D. Topical liposomal gel of idoxuridine for the treatment of herpes simplex: pharmaceutical and clinical implications. Pharm Dev Technol. 2004;9:277-89 pubmed
    The optimization of the method of preparation of idoxuridine (IDU) liposomes by the reverse phase evaporation (REV) method was carried out by three variables at three levels (3(3)) factorial design...
  2. Elmroth K, Stenerlow B. DNA-incorporated 125I induces more than one double-strand break per decay in mammalian cells. Radiat Res. 2005;163:369-73 pubmed
    ..Thus, in addition to DSBs produced close to the decay site, DSBs may also be induced within neighboring chromatin fibers, releasing smaller DNA fragments that are not detected by conventional DSB assays. ..
  3. Maggs D, Clarke H. In vitro efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyclovir against feline herpesvirus type-1. Am J Vet Res. 2004;65:399-403 pubmed
    To establish the in vitro efficacy of 4 novel drugs (ie, ganciclovir, cidofovir, penciclovir, and foscarnet) against feline herpesvirus type-1 (FHV-1) and compare their antiviral efficacy with that of acyclovir and idoxuridine.
  4. Fauth E, Zankl H. Comparison of spontaneous and idoxuridine-induced micronuclei by chromosome painting. Mutat Res. 1999;440:147-56 pubmed
    ..library (CSL) DNA probes for all human chromosomes were used to study about 9000 micronuclei (MN) in normal and idoxuridine (IUdR)-treated lymphocyte cultures of female and male donors...
  5. Kassis A, Dahman B, Adelstein S. In vivo therapy of neoplastic meningitis with methotrexate and 5. Acta Oncol. 2000;39:731-7 pubmed
    ..79); (ii) 125IUdR injection results in a statistically significant delay (p < 0.01) in the onset of paralysis (M= 39 days); (iii) MTX administration prior to 122IUdR injection further increases the therapeutic efficacy (M = 45 days). ..
  6. Majumdar S, Gunda S, Mitra A. Functional expression of a sodium dependent nucleoside transporter on rabbit cornea: Role in corneal permeation of acyclovir and idoxuridine. Curr Eye Res. 2003;26:175-83 pubmed
    ..transporters on the rabbit cornea and to delineate mechanism of corneal permeation of acyclovir (ACV) and idoxuridine (IDU). Methods...
  7. Taverna P, Hwang H, Schupp J, Radivoyevitch T, Session N, Reddy G, et al. Inhibition of base excision repair potentiates iododeoxyuridine-induced cytotoxicity and radiosensitization. Cancer Res. 2003;63:838-46 pubmed
    ..Thus, a genetic or biochemical impairment of BER results in increased IdUrd-induced cytotoxicity and radiosensitization in mammalian cells...
  8. Karnas S, Moiseenko V, Yu E, Truong P, Battista J. Monte Carlo simulations and measurement of DNA damage from x-ray-triggered auger cascades in iododeoxyuridine (IUdR). Radiat Environ Biophys. 2001;40:199-206 pubmed
    ..The accentuated DNA damage may have major consequences for cell survival and may be exploitable in kilovoltage photon activation therapy (PAT) of tumors sensitized with iodine. ..
  9. Shinohara K, Nakano H, Ohara H. Detection of Auger enhancement induced in HeLa cells labeled with iododeoxyuridine and irradiated with 150 kV x-rays--Effects of cysteamine and dimethylsulfoxide. Acta Oncol. 1996;35:869-75 pubmed
    ..The results suggest that at least a portion of Auger enhancement is not protectable by cysteamine and is hard to be protected by both protectors cysteamine and dimethylsulfoxide. ..

More Information


  1. Leuner B, Glasper E, Gould E. Thymidine analog methods for studies of adult neurogenesis are not equally sensitive. J Comp Neurol. 2009;517:123-33 pubmed publisher
  2. Sokolov M, Smirnova N, Camerini Otero R, Neumann R, Panyutin I. Microarray analysis of differentially expressed genes after exposure of normal human fibroblasts to ionizing radiation from an external source and from DNA-incorporated iodine-125 radionuclide. Gene. 2006;382:47-56 pubmed
    ..In contrast to cell survival, DNA DSB may not be the major factor modulating changes in gene expression following irradiation. ..
  3. Buchegger F, Vieira J, Blaeuenstein P, Dupertuis Y, Schaffland A, Grannavel C, et al. Preclinical Auger and gamma radiation dosimetry for fluorodeoxyuridine-enhanced tumour proliferation scintigraphy with [123I]iododeoxyuridine. Eur J Nucl Med Mol Imaging. 2003;30:239-46 pubmed
  4. Ludwikow G, Hoebe R, Franken N, Van Oven C, Stap J, Aten J. A method for the selective irradiation of part of a genome. Acta Oncol. 2000;39:693-8 pubmed
    ..Thus, the replication timing of Xq may be used to exclude or to incorporate 125I into the Xq. Other chromatin can be selected and targeted with 125I in a similar way. Examples of possible applications of the method are given. ..
  5. Walicka M, Adelstein S, Kassis A. Chemical modification of 5-[125I]iodo-2'-deoxyuridine toxicity in mammalian cells in vitro. Int J Radiat Biol. 2001;77:625-30 pubmed
    ..The contribution of indirect mechanisms to the toxicity of (125)I decaying within mammalian cell nuclear DNA can be demonstrated not only with DMSO, but also with the hydroxy radical scavengers present in serum. ..
  6. Iwanowicz L, Goodwin A. A new bacilliform fathead minnow rhabdovirus that produces syncytia in tissue culture. Arch Virol. 2002;147:899-915 pubmed
    ..This virus, has tentatively been named the fathead minnow rhabdovirus (FHMRV) and is most similar to the members of the family Rhabdoviridae, but atypical properties like syncytia formation may justify the assignment to a novel taxon. ..
  7. Watanabe R, Nikjoo H. Modelling the effect of incorporated halogenated pyrimidine on radiation-induced DNA strand breaks. Int J Radiat Biol. 2002;78:953-66 pubmed
    ..The importance of energy transfer along the DNA is demonstrated. It is shown that the incorporation of Br/IdU causes a spectral shift towards a greater complexity of clustered DNA damage. ..
  8. El Kazzouli S, Berteina Raboin S, Agrofoglio L. Supported synthesis and functionnalization of 2''-deoxyuridine by Suzuki-Miyaura cross-coupling. Nucleosides Nucleotides Nucleic Acids. 2007;26:1395-8 pubmed
    ..Pd(PPh(3))(4) palladium catalyzed was found to be superior to Pd(OAc)(2) and (NHC)Pd(allyl)Cl for Suzuki-Miyaura palladium-catalyzed reactions. ..
  9. Goethals L, Debucquoy A, Perneel C, Geboes K, Ectors N, De Schutter H, et al. Hypoxia in human colorectal adenocarcinoma: comparison between extrinsic and potential intrinsic hypoxia markers. Int J Radiat Oncol Biol Phys. 2006;65:246-54 pubmed
    ..Only in a minority of tumors did an association exist between the areas stained by pimonidazole and those positive for CA IX. Pimonidazole also did not correlate with expression of other putative intrinsic hypoxia markers (VEGF, EGFR). ..
  10. Dediulescu L, Dediulescu D. [Antiherpetic therapy]. Oftalmologia. 2005;49:72-7 pubmed
  11. Buchegger F, Adamer F, Schaffland A, Kosinski M, Grannavel C, Dupertuis Y, et al. Highly efficient DNA incorporation of intratumourally injected [125I]iododeoxyuridine under thymidine synthesis blocking in human glioblastoma xenografts. Int J Cancer. 2004;110:145-9 pubmed
    ..v. pretreatment with clinically relevant doses of FdUrd and that this approach may be further exploited for diffusion and therapy studies with Auger electron- and/or beta-radiation-emitting radio-IdUrd. ..
  12. Schulz C, Mehta M, Badie B, McGinn C, Robins H, Hayes L, et al. Continuous 28-day iododeoxyuridine infusion and hyperfractionated accelerated radiotherapy for malignant glioma: a phase I clinical study. Int J Radiat Oncol Biol Phys. 2004;59:1107-15 pubmed
    ..IUdr steady-state plasma levels increased with increasing dose and attained levels needed for clinical radiosensitization. Continuous IUdr infusion and HART were both feasible and well tolerated. ..
  13. Ryser J, Bläuenstein P, Remy N, Weinreich R, Hasler P, Novak Hofer I, et al. [76Br]Bromodeoxyuridine, a potential tracer for the measurement of cell proliferation by positron emission tomography, in vitro and in vivo studies in mice. Nucl Med Biol. 1999;26:673-9 pubmed
    ..The difference between the two tracers is small and the extrapolation from mice to human difficult, and thus it cannot be concluded if one of the tracers would be better than the other for imaging of cancer patients. ..
  14. Hard T, Fan P, Kearns D. A fluorescence study of the binding of Hoechst 33258 and DAPI to halogenated DNAs. Photochem Photobiol. 1990;51:77-86 pubmed
    ..Based on this observation and earlier reports that DAPI binds in one of the DNA grooves, we conclude that the high affinity sites for DAPI on DNA are located in the minor groove. ..
  15. Nudler E, Gusarov I, Avetissova E, Kozlov M, Goldfarb A. Spatial organization of transcription elongation complex in Escherichia coli. Science. 1998;281:424-8 pubmed
    ..The results explain how RNA in the integrated unit RBS-HBS-DBS may stabilize the ternary complex, whereas a hairpin in RNA result in its dissociation. ..
  16. Mariani G, Di Sacco S, Bonini R, Di Luca L, Buralli S, Bonora D, et al. Biochemical modulation by 5-fluorouracil and 1-folinic acid of tumor uptake of intra-arterial 5-[123I]iodo-2'deoxyuridine in patients with liver metastases from colorectal cancer. Acta Oncol. 1996;35:941-5 pubmed
  17. Lepri E, Liberati M, Portuese M, Menconi E, Santucci A, Barzi A. In vitro chemosensitivity of newly diagnosed and relapsing acute non-lymphoid leukemia patients. Tumori. 1991;77:25-7 pubmed
    ..Moreover, the chemosensitivity test adopted is a better predictor in newly diagnosed than relapsing patients, as indicated by the concordance between in vitro and in vivo results. ..
  18. Goddu S, Narra V, Harapanhalli R, Howell R, Rao D. Radioprotection by DMSO against the biological effects of incorporated radionuclides in vivo--Comparison with other radioprotectors and evidence for indirect action of Auger electrons. Acta Oncol. 1996;35:901-7 pubmed
    ..The present findings provide supporting evidence that the mechanism responsible for the extreme biological damage caused by DNA-bound Auger emitters is largely radical mediated and therefore indirect in nature...
  19. Fahrig R. Anti-recombinogenic and convertible co-mutagenic effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and other 5-substituted pyrimidine nucleoside analogs in S. cerevisiae MP1. Mutat Res. 1996;372:133-9 pubmed
    ..At higher concentrations the co-carcinogenic effect may be converted into an anti-carcinogenic one. ..
  20. Inoue Y, Ohashi Y, Shimomura Y, Manabe R, Yamada M, Ueda S, et al. Comparative efficacy of three antiviral drugs in mice herpetic keratitis. Jpn J Ophthalmol. 1989;33:125-31 pubmed
    ..These results indicate that DHPG can be a useful antiviral agent in the treatment of herpetic keratitis. ..
  21. Mairs R, Wideman C, Angerson W, Whateley T, Reza M, Reeves J, et al. Comparison of different methods of intracerebral administration of radioiododeoxyuridine for glioma therapy using a rat model. Br J Cancer. 2000;82:74-80 pubmed
    ..These findings are also encouraging for the development of a sustained release system for radiolabelled IUdR for use in the treatment of intracranial tumours, particularly in the immediate postoperative setting. ..
  22. Marquardt H, Hunkapiller M, Hood L, Todaro G. Rat transforming growth factor type 1: structure and relation to epidermal growth factor. Science. 1984;223:1079-82 pubmed
    ..Production of this polypeptide by various neoplastic cells might contribute to the continued expression of the transformed phenotype. ..
  23. Hunskaar S. Giant orf in a patient with chronic lymphocytic leukaemia. Br J Dermatol. 1986;114:631-4 pubmed
    ..Human orf is normally a self-limiting and benign condition but in this case the lesion grew to a size of 60 X 60 X 28 mm. When it was excised, local recurrence was treated with topical idoxuridine.
  24. Nelson J, Diegelmann R, Cohen I. Effect of beta-aminopropionitrile and ascorbate on fibroblast migration. Proc Soc Exp Biol Med. 1988;188:346-52 pubmed
    ..Therefore, the effect of BAPN on migration does not appear to be due to generalized cytotoxicity. These combined studies suggest that compounds such as ascorbate and BAPN which can modify collagen may also modify fibroblast migration. ..
  25. Yan T, Seo Y, Schupp J, Zeng X, Desai A, Kinsella T. Methoxyamine potentiates iododeoxyuridine-induced radiosensitization by altering cell cycle kinetics and enhancing senescence. Mol Cancer Ther. 2006;5:893-902 pubmed
    ..Thus, senescence, a novel ionizing radiation-induced tumor suppression pathway, may be effectively targeted by IUdR/methoxyamine pretreatment, resulting in an improved therapeutic gain for ionizing radiation. ..
  26. Cherry H, Roelofs A, Kurth T, De Bari C. In vivo phenotypic characterisation of nucleoside label-retaining cells in mouse periosteum. Eur Cell Mater. 2014;27:185-95; discussion 195 pubmed
    ..Future studies characterising the MSC niche in vivo could reveal novel therapeutic targets for promoting bone regeneration/repair. ..
  27. GURKAN CAVUSOGLU E, Schupp J, Kinsella T, Loparo K. Quantitative analysis of the effects of iododeoxyuridine and ionising radiation treatment on the cell cycle dynamics of DNA mismatch repair deficient human colorectal cancer cells. IET Syst Biol. 2013;7:114-24 pubmed publisher
    ..The models presented in this work form the foundation for the development of an approach to maximise the therapeutic index for IR and IUdR + IR treatments in MMR-deficient (damage tolerant) cancers. ..
  28. Cho J, Shaughnessy K. Aqueous-phase Sonogashira alkynylation to synthesize 5-substituted pyrimidine and 8-substituted purine nucleosides. Curr Protoc Nucleic Acid Chem. 2012;Chapter 1:Unit1.27 pubmed publisher
    ..The optimal catalyst is derived from palladium acetate, tri-(2,4-dimethyl-5-sulfonatophenyl)phosphane (TXPTS), and CuI. ..
  29. Viertl D, Perillo Adamer F, André P, Ametamey S, Ross T, Kosinski M, et al. 18F-FLT and 125I-IdUrd uptake increase in human tumour cell lines induced by the thymidylate synthase inhibitor FdUrd. Nuklearmedizin. 2012;51:163-9 pubmed publisher
    ..18F-FLT outflow from cells might be an explanation for the observed difference with 125I-IdUrd. ..
  30. Murata K, Imai M, Nakanishi S, Watanabe D, Pastan I, Kobayashi K, et al. Compensation of depleted neuronal subsets by new neurons in a local area of the adult olfactory bulb. J Neurosci. 2011;31:10540-57 pubmed publisher
  31. Ogasawara S, Fujimoto K. SNP genotyping by using photochemical ligation. Angew Chem Int Ed Engl. 2006;45:4512-5 pubmed
  32. Boyd M, Sorensen A, McCluskey A, Mairs R. Radiation quality-dependent bystander effects elicited by targeted radionuclides. J Pharm Pharmacol. 2008;60:951-8 pubmed publisher
    ..It is concluded that radiopharmaceutical-induced bystander effects may depend on LET of the decay particles but are independent of site of intracellular concentration of radionuclide. ..
  33. Turner D, Cortellino S, Schupp J, Caretti E, Loh T, Kinsella T, et al. The DNA N-glycosylase MED1 exhibits preference for halogenated pyrimidines and is involved in the cytotoxicity of 5-iododeoxyuridine. Cancer Res. 2006;66:7686-93 pubmed
    ..These findings establish MED1 as a bona fide repair activity for the removal of halogenated bases and indicate that MED1 may play a significant role in 5IdU cytotoxicity. ..
  34. Wijffels K, Marres H, Peters J, Rijken P, van der Kogel A, Kaanders J. Tumour cell proliferation under hypoxic conditions in human head and neck squamous cell carcinomas. Oral Oncol. 2008;44:335-44 pubmed
    ..The proportion of cells proliferating under hypoxic conditions was small and no correlation with treatment outcome could be found. ..
  35. Santos O, Pant K, Blank E, Ceriani R. 5-Iododeoxyuridine increases the efficacy of the radioimmunotherapy of human tumors growing in nude mice. J Nucl Med. 1992;33:1530-4 pubmed
    ..Our results indicate the potential for increasing the therapeutic effectiveness of radioimmunotherapy of human solid tumors with halogenated pyrimidines. ..
  36. Scherberg N, Bloch I, Gardner P. Site-specific incorporation of [125I]iododeoxyuridine into DNA. Int J Rad Appl Instrum A. 1992;43:923-7 pubmed
    ..The product formed includes the radioiodonucleotide at a single internal site determined by the length of the oligomer. ..
  37. Ou X, Kuang A, Peng X, Zhong Y. Study on the possibility of insulin as a carrier of IUdR for hepatocellular carcinoma-targeted therapy. World J Gastroenterol. 2003;9:1675-8 pubmed
    ..Values of IC(50)1 and KI1 for insulin-IUdR were significantly higher than that for insulin (P<0.01, t=4.537 and 4.813). It is possible to use insulin as a carrier for carcinoma-targeted therapy mediated by receptor. ..
  38. Hoshino S, Sun Z, Uchikura K, Tsugane K, Ceppa E, Bulkley G, et al. Biliary obstruction reduces hepatic killing and phagocytic clearance of circulating microorganisms in rats. J Gastrointest Surg. 2003;7:497-506 pubmed publisher
    ..These findings may help to explain the susceptibility of patients with biliary tract obstruction to the morbidity and mortality of septic complications. ..
  39. Xue L, Butler N, Makrigiorgos G, Adelstein S, Kassis A. Bystander effect produced by radiolabeled tumor cells in vivo. Proc Natl Acad Sci U S A. 2002;99:13765-70 pubmed
  40. Sundell Bergman S, Johanson K, Richter S, Ostbergh P. Enhancement of radiation sensitivity in iododeoxyuridine labelled cells exposed to low energy x-rays. Acta Oncol. 1990;29:623-6 pubmed
    ..2 times as sensitive as the control cells when irradiated with low-energy x-rays. For 137Cs-gamma the ratio was about 1.5. The standard deviations were estimated by Gauss' approximation to be about 0.5 for both irradiation conditions. ..
  41. Ludwikow G, Xiao Y, Hoebe R, Franken N, Darroudi F, Stap J, et al. Induction of chromosome aberrations in unirradiated chromatin after partial irradiation of a cell nucleus. Int J Radiat Biol. 2002;78:239-47 pubmed
  42. Yasui L, Hughes A, Desombre E. Cytotoxicity of 125I-oestrogen decay in non-oestrogen receptor-expressing human breast cancer cells, MDA-231 and oestrogen receptor-expressing MCF-7 cells. Int J Radiat Biol. 2001;77:955-62 pubmed
    ..These results support the hypothesis that the nuclear genome is a critical target for radiation-induced cell death. ..
  43. Bishayee A, Rao D, Howell R. Radiation protection by cysteamine against the lethal effects of intracellularly localized Auger electron, alpha- and beta-particle emitting radionuclides. Acta Oncol. 2000;39:713-20 pubmed
    ..1, respectively. MEA provides more protection against indirect than direct effects of ionizing radiation, and indirect effects play a role in the radiotoxicity of Auger electron emitters incorporated into the DNA of mammalian cells. ..
  44. Wang Y, Adzuma K. Differential proximity probing of two DNA binding sites in the Escherichia coli recA protein using photo-cross-linking methods. Biochemistry. 1996;35:3563-71 pubmed
    ..These results support the idea that, as predicted by Story and co-workers (1992), the disordered loops are involved in DNA binding. The results also suggest that the two sites are not only functionally but also physically distinct. ..
  45. Minato S, Itoyama Y, Goto I, Yamamoto N. Expression of HTLV-I antigen in cultured peripheral blood mononuclear cells from patients with HTLV-I associated myelopathy. J Neurol Sci. 1988;87:233-44 pubmed
    ..There were no correlations between the HTLV-I Ag expression in cultured cells and the various clinical and laboratory findings, in each case. ..
  46. Lerner A, Bailey E, Nolan D. Complement-requiring neutralizing antibodies in Herpesvirus hominis encephalitis. J Immunol. 1970;104:607-15 pubmed
  47. Fukushima M, Suzuki N, Emura T, Yano S, Kazuno H, Tada Y, et al. Structure and activity of specific inhibitors of thymidine phosphorylase to potentiate the function of antitumor 2'-deoxyribonucleosides. Biochem Pharmacol. 2000;59:1227-36 pubmed
    ..In conclusion, TPI may contribute not only to inhibition of TPase-mediated biological functions but also to potentiation of the biological activity of various 2'-deoxyuridine and thymidine derivatives by combining with them. ..
  48. Buchanan L, Riches A. Testosterone-induced DNA synthesis in cultured rat ventral prostate. I. Effects of cyproterone acetate. J Anat. 1986;148:159-67 pubmed
    ..Thus, this in vitro method provides a useful model for screening the direct effects of antiprostatic drugs. ..
  49. Frum R, Khondker Z, Kaufman D. Temporal differences in DNA replication during the S phase using single fiber analysis of normal human fibroblasts and glioblastoma T98G cells. Cell Cycle. 2009;8:3133-48 pubmed
    ..Our observations suggest models to explain the temporal replication of single and clustered origins, and suggest differences in the replication program in a normal and cancer cell line. ..
  50. Testoni M, Lopez Camelo J, Bianchi M, Bianchi N. Enhancement of chromosome aberrations by the combination of DNA substitution with halogenated deoxyuridine and streptonigrin treatments. Mutat Res. 1996;359:31-7 pubmed
  51. Labetoulle M. [The latest in herpes simplex keratitis therapy]. J Fr Ophtalmol. 2004;27:547-57 pubmed
    ..We can also hope that in the future novel antiviral strategies such as vaccination will reduce the place of herpes keratitis as an indication for corneal graft. ..
  52. Khalili P, Naimi E, Knaus E, Wiebe L. Pharmacokinetics and metabolism of the novel synthetic C-nucleoside, 1-(2-deoxy-beta-D-ribofuranosyl)-2,4-difluoro-5-iodobenzene: a potential mimic of 5-iodo-2'-deoxyuridine. Biopharm Drug Dispos. 2002;23:105-13 pubmed
    ..96). Both glucuronide and sulfate metabolites were present in urine. Glucuronidation was the predominant conjugation pathway. ..
  53. Chi K, Wang H, Wang Y, Chou S, Yu H, Tseng Y, et al. Antisense thymidylate synthase electrogene transfer to increase uptake of radiolabeled iododeoxyuridine in a murine model. J Nucl Med. 2004;45:478-84 pubmed
    ..We designed an in vivo electrogene transfer (EGT) model for delivering antisense TS plasmid (ATS) into tumor to increase the subsequent efficacy of (131)I-IdUrd therapy...