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 Pirarubicin

pirarubicin is an analogue of the anthracycline antineoplastic antibiotic doxorubicin. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin and exhibits activity against some doxorubicin-resistant cell lines. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

  1: Chen Z, Liu G, Chen M, Chen X, Wu M, Chen X. An instrument-based screening assay for DNA-targeted anticancer drugs using resonance light scattering. Comb Chem High Throughput Screen. 2010 Jun;13(5):383-92. PubMed PMID: 20156144.

2: Vautravers C, Rat P, Cercueil JP, Moreau T, Horiot JC, Chauffert B. Hepatocellular carcinoma presenting as paraneoplastic myasthenia gravis. Eur J Intern Med. 2008 Dec;19(8):e86-7. Epub 2008 Jun 10. PubMed PMID: 19046712.

3: Tanaka T, Toujima S, Utsunomiya T, Yukawa K, Umesaki N. Experimental characterization of recurrent ovarian immature teratoma cells after optimal surgery. Oncol Rep. 2008 Jul;20(1):13-23. PubMed PMID: 18575713.

4: Qiao BM, Sun G, Tang Y, Chang JW, Wang WC, Ma TX. [Overexpression of PTEN gene inhibits proliferation of bladder transitional carcinoma cell line EJ]. Zhonghua Zhong Liu Za Zhi. 2007 Apr;29(4):262-5. Chinese. PubMed PMID: 17760251.

5: Wu XX, Zeng Y, Jin XH, Kakehi Y. Enhanced susceptibility of adriamycin-treated human renal cell carcinoma cells to lysis by peripheral blood lymphocytes and tumor infiltrating lymphocytes. Oncol Rep. 2007 Aug;18(2):353-9. PubMed PMID: 17611656.

6: Benoit L, Favoulet P, Ortega-Deballon P, Cheynel N, Anusca A, Bamourou D, Bonnetain F, Rat P, Favre JP, Chauffert B. Attempts to improve locoregional chemotherapy for the prevention of colonic cancer liver metastasis in the rat. Gastroenterol Clin Biol. 2006 Aug-Sep;30(8-9):1019-25. PubMed PMID: 17075453.

7: Lu YF, Zeng J, Liao QH, Lin J, Huang Y, Chen JQ, Tian L, Xie NC. [Comparative study on clinical effect of postoperative arterial infusion chemotherapy and systemic chemotherapy in gastric cancer]. Zhonghua Wei Chang Wai Ke Za Zhi. 2006 Jul;9(4):317-9. Chinese. PubMed PMID: 16886113.

8: Kokawa K, Mabuchi Y, Tanaka K, Yagi S, Utsunomiya T, Oba N, Yata C, Umesaki N. Apoptosis in cervical cancer after balloon-occluded arterial infusion of anticancer drugs. Anticancer Res. 2006 Mar-Apr;26(2B):1413-8. PubMed PMID: 16619552.

9: Tanaka T, Bai T, Yukawa K, Umesaki N. Optimal combination chemotherapy and chemoradiotherapy with etoposide for advanced cervical squamous cancer cells in vitro. Oncol Rep. 2006 Apr;15(4):939-47. PubMed PMID: 16525683.

10: Greish K, Nagamitsu A, Fang J, Maeda H. Copoly(styrene-maleic acid)-pirarubicin micelles: high tumor-targeting efficiency with little toxicity. Bioconjug Chem. 2005 Jan-Feb;16(1):230-6. PubMed PMID: 15656596.

11: Hara Y, Kizaki K, Temma K, Chugun A, Kondo H. Effects of anticancer chemotherapeutic drugs on the acetylcholine receptor-operated potassium current in guinea pig atrial myocytes. Basic Clin Pharmacol Toxicol. 2004 Nov;95(5):234-40. PubMed PMID: 15546478.

12: Favoulet P, Benoit L, Osmak L, Polycarpe E, Esquis P, Duvillard C, Guiu B, Rat P, Favre JP, Chauffert B. Prevention of peritoneal carcinomatosis from colon cancer cell seeding using a pirarubicin solution in rats and nude mice. World J Surg. 2004 May;28(5):451-6. Epub 2004 Apr 19. PubMed PMID: 15085402.

13: Cashman DJ, Kellogg GE. A computational model for anthracycline binding to DNA: tuning groove-binding intercalators for specific sequences. J Med Chem. 2004 Mar 11;47(6):1360-74. PubMed PMID: 14998326.

14: Bun SS, Voeurng V, Bun H. Interspecies variability and drug interactions of loxapine metabolism in liver microsomes. Eur J Drug Metab Pharmacokinet. 2003 Oct-Dec;28(4):295-300. PubMed PMID: 14743971.

15: Hara I, Miyake H, Takechi Y, Eto H, Gotoh A, Fujisawa M, Okada H, Arakawa S, Kamidono S; Kobe Urogenital Tumor Study Group. Clinical outcome of conservative therapy for stage T1, grade 3 transitional cell carcinoma of the bladder. Int J Urol. 2003 Jan;10(1):19-24. PubMed PMID: 12534921.

16: Suh D, Oh YK, Ahn B, Hur MW, Kim HJ, Lee MH, Joo HS, Auh C. Comparative binding of antitumor drugs to DNA containing the telomere repeat sequence. Exp Mol Med. 2002 Nov 30;34(5):326-31. PubMed PMID: 12526095.

17: Kiyomiya K, Satoh J, Horie H, Kurebe M, Nakagawa H, Matsuo S. Correlation between nuclear action of anthracycline anticancer agents and their binding affinity to the proteasome. Int J Oncol. 2002 Nov;21(5):1081-5. PubMed PMID: 12370758.

18: Kiyomiya K, Kurebe M, Nakagawa H, Matsuo S. The role of the proteasome in apoptosis induced by anthracycline anticancer agents. Int J Oncol. 2002 Jun;20(6):1205-9. PubMed PMID: 12012000.

19: Kobayashi M, Wood PA, Hrushesky WJ. Circadian chemotherapy for gynecological and genitourinary cancers. Chronobiol Int. 2002 Jan;19(1):237-51. Review. PubMed PMID: 11962679.

20: Shiota M, Shirai T, Tateyama I. [A patient with recurrent uterine cervical cancer successfully treated by combined modality therapy including local injection of anticancer agents based on CDDP]. Gan To Kagaku Ryoho. 2000 Nov;27(13):2117-21. Japanese. PubMed PMID: 11103245.

21: Wu XX, Mizutani Y, Kakehi Y, Yoshida O, Ogawa O. Enhancement of Fas-mediated apoptosis in renal cell carcinoma cells by adriamycin. Cancer Res. 2000 Jun 1;60(11):2912-8. PubMed PMID: 10850437.

22: Marbeuf-Gueye C, Salerno M, Quidu P, Garnier-Suillerot A. Inhibition of the P-glycoprotein- and multidrug resistance protein-mediated efflux of anthracyclines and calceinacetoxymethyl ester by PAK-104P. Eur J Pharmacol. 2000 Mar 17;391(3):207-16. PubMed PMID: 10729360.

23: Hiwasa T, Chen Z, Nomura J, Yamamori H, Tashiro T, Nakajima N, Suzuki N. Differential sensitivity to mitomycin C between human RSa cell line and its derivative UVr-1. Anticancer Res. 1999 Sep-Oct;19(5B):3915-20. PubMed PMID: 10628331.

24: Mizutani Y, Yoshida O, Miki T, Bonavida B. Synergistic cytotoxicity and apoptosis by Apo-2 ligand and adriamycin against bladder cancer cells. Clin Cancer Res. 1999 Sep;5(9):2605-12. PubMed PMID: 10499639.

25: Morikawa N, Mori T, Kamenofuchi Y, Kawashima H, Takeyama M, Hori S. Dose-related increases in cerebrospinal fluid concentrations of methotrexate in a postoperative patient with glioblastoma. Ann Pharmacother. 1999 Sep;33(9):952-6. PubMed PMID: 10492499.

26: Ikeda R, Chikazawa I, Kobayashi Y, Shiroma K, Nakade T, Suga K, Shiba N, Nakajima C, Moriyama M, Kawamura K, Miyazawa K, Tanaka T, Tsugawa R, Suzuki K, Sato H, Kikuyama A. [Prophylaxis of recurrence in superficial bladder carcinoma by intravesical chemotherapy--comparative study between instillation of combined double anticancer agents and single anticancer agent]. Gan To Kagaku Ryoho. 1999 Mar;26(4):509-14. Japanese. PubMed PMID: 10097748.

27: Ohtsubo K, Mouri H, Sakai J, Akasofu M, Yamaguchi Y, Watanabe H, Gabata T, Motoo Y, Okai T, Sawabu N. Pancreatic cancer associated with granulocyte-colony stimulating factor production confirmed by immunohistochemistry. J Clin Gastroenterol. 1998 Dec;27(4):357-60. PubMed PMID: 9855271.

28: Pereira E, Tarasiuk J, Garnier-Suillerot A. Kinetic analysis in living cells of the inhibition of the P-glycoprotein-mediated efflux of anthracyclines by vinca alkaloids. Chem Biol Interact. 1998 Jul 3;114(1-2):61-76. PubMed PMID: 9744556.

29: Morikawa N, Mori T, Takeyama M, Hori S. Pharmacokinetics of intra-arterially administered pirarubicin in plasma and cerebrospinal fluid of patients with glioma. Biol Pharm Bull. 1998 Mar;21(3):297-9. PubMed PMID: 9556164.

30: Tanaka T, Chang L, Umesaki N, Ogita S. Clonal analysis of cancer cells that survived anticancer drug treatment. Osaka City Med J. 1997 Dec;43(2):259-65. PubMed PMID: 9540347.

31: Marbeuf-Gueye C, Broxterman HJ, Dubru F, Priebe W, Garnier-Suillerot A. Kinetics of anthracycline efflux from multidrug resistance protein-expressing cancer cells compared with P-glycoprotein-expressing cancer cells. Mol Pharmacol. 1998 Jan;53(1):141-7. PubMed PMID: 9443942.

32: Ogihara M, Aikawa K, Ishibashi K, Yamaguchi O, Shiraiwa Y, Koseki K. [Neoadjuvant intra-arterial chemotherapy based on chemosensitivity tests for locally invasive bladder cancer]. Hinyokika Kiyo. 1997 Aug;43(8):555-60. Japanese. PubMed PMID: 9310777.

33: Takahashi T, Mitsuhashi N, Sakurai H, Murata O, Kitamoto Y, Matsumoto H, Higuchi K, Niibe H. Thermal enhancement of pirarubicin (THP-adriamycin) by mild hyperthermia in vitro. Int J Hyperthermia. 1997 May-Jun;13(3):317-24. PubMed PMID: 9222814.

34: Belhoussine R, Morjani H, Manfait M. [Effect of quinine on the multiple drug resistance and intracellular distribution of pirarubicin in LR73 tumor cells: a comparative study with verapamil and S9788 by confocal laser microspectrofluorometry]. Bull Cancer. 1997 Apr;84(4):343-9. Review. French. PubMed PMID: 9238156.

35: Mizutani Y, Okada Y, Yoshida O, Fukumoto M, Bonavida B. Doxorubicin sensitizes human bladder carcinoma cells to Fas-mediated cytotoxicity. Cancer. 1997 Mar 15;79(6):1180-9. PubMed PMID: 9070496.

36: Inoue K, Kasahara K, Inoue Y, Inoue K, Yamashita M, Morioka M, Fujita Y, Shuin T. [The efficacy of ATP sensitivity assay on intravesical prophylactic instillation for superficial bladder cancer]. Nippon Hinyokika Gakkai Zasshi. 1996 Dec;87(12):1281-8. Japanese. PubMed PMID: 8997075.

37: Gallois L, Fiallo M, Laigle A, Priebe W, Garnier-Suillerot A. The overall partitioning of anthracyclines into phosphatidyl-containing model membranes depends neither on the drug charge nor the presence of anionic phospholipids. Eur J Biochem. 1996 Nov 1;241(3):879-87. PubMed PMID: 8944778.

38: Yoshida M, Fujioka A, Nakano K, Yuasa C, Toko T, Takeda S, Unemi N. Activity of menogaril against various malignant lymphoma cell lines and a human lymphoma xenograft in mice. Anticancer Res. 1996 Sep-Oct;16(5A):2875-9. PubMed PMID: 8917401.

39: Fujimura T, Yonemura Y, Minami M, Sato T, Kawamura T, Nojima N, Kinami S, Hirono Y, Fushida S, Nishimura G, Noguchi M, Miwa K, Miyazaki I, Shiobara S. [Chemohyperthermic peritoneal perfusion and high-dose chemotherapy followed by peripheral blood stem cell transplantation in advanced colon cancer--a case report]. Gan To Kagaku Ryoho. 1996 Sep;23(11):1578-80. Japanese. PubMed PMID: 8854810.

40: Sakaguchi S, Sakaguchi H, Matsuo N, Anai H, Ohkura A, Hirohashi S, Imai T, Ohishi H, Akada S, Morikawa H, Uchida H. [Drug distribution of pelvic intraarterial infusion chemotherapy by bilateral internal iliac arterial catheter placement with coil occlusion of superior, inferior gluteal and obturator arteries]. Gan To Kagaku Ryoho. 1996 Sep;23(11):1495-8. Japanese. PubMed PMID: 8854788.

41: Sugiyama Y, Saji S, Miya K, Fukada D, Umemoto T, Kunieda K, Takao H, Kato M, Kawai M. [Locoregional therapy for liver metastases of colorectal cancer]. Gan To Kagaku Ryoho. 1996 Sep;23(11):1433-6. Japanese. PubMed PMID: 8854772.

42: Okuyama S, Sato A. Pirarubicin pasting for radiotherapy of inoperable colorectal cancers. Tohoku J Exp Med. 1996 Jul;179(3):223-6. PubMed PMID: 8888512.

43: Ogihara M, Aikawa K, Ishibashi K, Irisawa C, Shiraiwa Y, Koseki K, Ishiwata H. [Efficacy of the chemosensitivity test using collagen gel matrix-supported culture system for urogenital tumors]. Nippon Hinyokika Gakkai Zasshi. 1996 Apr;87(4):740-7. Japanese. PubMed PMID: 8691695.

44: Pereira E, Teodori E, Dei S, Gualtieri F, Garnier-Suillerot A. Reversal of multidrug resistance by verapamil analogues. Biochem Pharmacol. 1995 Aug 8;50(4):451-7. PubMed PMID: 7646549.

45: Fujii M, Ohno Y, Kanzaki J. [Effects of anticancer drugs and combination effects of anthracyclines on the hypoxic cells of head and neck cancer]. Gan To Kagaku Ryoho. 1995 Apr;22(5):647-52. Japanese. PubMed PMID: 7717716.

46: Hayashida S, Hirasawa T, Uchiyama K, Mitsui H, Nasu T, Shinohara Y. [The preventive effect of granisetron on digestive tract symptoms induced by arterial infusion of anticancer and hypertensive agents in combination with radiotherapy--a study of forty patients with bladder cancer]. Gan To Kagaku Ryoho. 1995 Apr;22(5):639-46. Japanese. PubMed PMID: 7717715.

47: Takeuchi T. Antitumor antibiotics discovered and studied at the Institute of Microbial Chemistry. J Cancer Res Clin Oncol. 1995;121(9-10):505-10. Review. PubMed PMID: 7559728.

48: Koga K, Iizuka E, Sato A, Ekimoto H, Okada M. Characteristic antitumor activity of cytarabine ocfosfate against human colorectal adenocarcinoma xenografts in nude mice. Cancer Chemother Pharmacol. 1995;36(6):459-62. PubMed PMID: 7554036.

49: Suzuki K, Orikasa S, Hoshi S, Yoshikawa K, Saitoh S, Ohyama C, Satoh M, Kawamura S. [Combination therapy of high energy under water shock waves and anticancer drugs for subcutaneous murine bladder cancer (MBT-2)]. Nippon Hinyokika Gakkai Zasshi. 1994 Oct;85(10):1464-73. Japanese. PubMed PMID: 7990295.

50: Sasaki M, Hashimoto H, Yachiku S. [Studies on enhancement of drug absorption through the bladder mucosa]. Nippon Hinyokika Gakkai Zasshi. 1994 Sep;85(9):1353-62. Japanese. PubMed PMID: 7967297.

51: Asaishi K, Okazaki M, Okazaki A, Toda K, Masuoka H, Hirata K, Narimatsu E. [The significance of intra-arterial infusion therapy for neoadjuvant chemotherapy]. Gan To Kagaku Ryoho. 1994 Jun;21 Suppl 2:264-71. Japanese. PubMed PMID: 8037491.

52: Nakashima T, Masuda A, Yano G, Maehara Y. [Basic and clinical evaluation of the effect of pirarubicin against head and neck cancer--chemosensitivity test and a comparative study with doxorubicin]. Gan To Kagaku Ryoho. 1994 Apr;21(5):633-9. Japanese. PubMed PMID: 8154889.

53: Inoue H, Miyazono N, Kanetsuki I, Hori A, Tanaka D, Fukukura Y, Matsumoto Y, Nishida H, Ueno K, Nakajo M, et al. [Anticancer and side effect of arterial subsegmental chemoembolization using cisplatinum/pirarubicin lipiodol suspension (CTLS) for hepatocellular carcinoma]. Gan To Kagaku Ryoho. 1993 Oct;20(13):1973-6. Japanese. PubMed PMID: 7692822.

54: Temma K, Akera T, Chugun A, Kondo H, Hagane K, Hirano S. Comparison of cardiac actions of doxorubicin, pirarubicin and aclarubicin in isolated guinea-pig heart. Eur J Pharmacol. 1993 Apr 6;234(2-3):173-81. PubMed PMID: 8482324.

55: Une Y, Uchino J, Yasuhara M, Misawa K, Kamiyama T, Shimamura T, Sato N, Nakajima Y, Hata Y. Intra-arterial infusion chemotherapy on unresectable hepatocellular carcinoma under occlusion of hepatic arterial flow. Clin Ther. 1993 Mar-Apr;15(2):347-54. PubMed PMID: 8390917.

56: Takeshita T, Inoue H, Miyazono N, Hori A, Harada O, Satake M, Kanetsuki I, Nishida H, Sagara K, Shinmaki H, et al. [Anticancer effect and side effect of arterial chemoembolization using cis-diamine-dichloroplatinum (II)/4-0-tetrahydropyranyl-adriamycin-lipiodol (CTL) suspension on hepatocellular carcinoma]. Gan To Kagaku Ryoho. 1992 Sep;19(11):1867-72. Japanese. PubMed PMID: 1381572.

57: Herait P, Poutignat N, Marty M, Bugat R. Early assessment of a new anticancer drug analogue--are the historical comparisons obsolete? The French experience with pirarubicin. Eur J Cancer. 1992;28A(10):1670-6. PubMed PMID: 1389483.

58: Ohyama S, Yonemura Y, Kinoshita K, Ninomiya I, Tugawa K, Kimura H, Miyazaki I, Tanaka M, Endo Y, Sasaki T. [Chemosensitivity test for gastric cancer by in vitro MTT assay]. Gan To Kagaku Ryoho. 1991 Aug;18(10):1593-7. Japanese. PubMed PMID: 1908213.

59: Koseki K, Irisawa C, Shiraiwa Y. [Chemosensitivity test on superficial urinary bladder cancer using the dye exclusion assay--model of intravesical chemotherapy]. Nippon Hinyokika Gakkai Zasshi. 1991 Feb;82(2):268-73. Japanese. PubMed PMID: 1904118.

60: Masuoka H, Asaishi K, Toda K, Okazaki A, Yoshida K, Ohba S, Watanabe Y, Sato H, Okazaki M, Mori M, et al. [Intra-arterial infusion chemotherapeutic effect of stage III breast cancer by survival rates]. Gan To Kagaku Ryoho. 1990 Aug;17(8 Pt 2):1678-81. Japanese. PubMed PMID: 2117900.

61: Watanabe T, Nakasaki H, Mitomi T. Measurement of cross-reactive properties of adriamycin derivatives by the inhibition enzyme-linked immunosorbent assay for adriamycin. Tokai J Exp Clin Med. 1990 Jul;15(4):327-34. PubMed PMID: 2130540.

62: Ohnuma N, Takahashi H, Tanabe M, Yoshida H, Iwakawa M, Kuriyama Y. [Targeting anticancer chemotherapy dispersed in lipid contrast medium in hepatoblastoma in childhood]. Nippon Gan Chiryo Gakkai Shi. 1990 Apr 20;25(4):788-92. Japanese. PubMed PMID: 2164551.

63: Harstrick A, Schmoll HJ, Casper J, Wilke H, Poliwoda H. Activity of cytostatic drugs in two heterotransplanted human testicular cancer cell lines with different sensitivity to standard agents. Eur J Cancer. 1990;26(8):898-901. PubMed PMID: 2145935.

64: Lévi F, Blazsek I, Ferlé-Vidovic A. Circadian and seasonal rhythms in murine bone marrow colony-forming cells affect tolerance for the anticancer agent 4'-O-tetrahydropyranyladriamycin (THP). Exp Hematol. 1988 Sep;16(8):696-701. PubMed PMID: 3402557.

65: Tsukagoshi S. [Pirarubicin (THP-adriamycin)]. Gan To Kagaku Ryoho. 1988 Sep;15(9):2819-27. Review. Japanese. PubMed PMID: 3046496.

66: Okuma K, Ariyoshi Y, Ota K. [Clinical study of acute cardiotoxicity of anti-cancer agents-- analysis using Holter ECG monitoring]. Gan To Kagaku Ryoho. 1988 Jun;15(6):1893-900. Japanese. PubMed PMID: 3164181.

67: Fujita H, Ogawa K, Tone H, Iguchi H, Shomura T, Murata S. Pharmacokinetics of doxorubicin, (2"R)-4'-O-tetrahydropyranyl-adriamycin and aclarubicin. Jpn J Antibiot. 1986 May;39(5):1321-36. PubMed PMID: 3463778.

68: Tone H, Iguchi H, Fujigaki M, Nishio M, Esumi Y, Takaichi M, Tsutsumi S, Yokoshima T. [Pharmacokinetics and disposition of a new anticancer antibiotic (2''R)-4'-O-tetrahydropyranyladriamycin in rats. Distribution and excretion after a single administration]. Jpn J Antibiot. 1986 Feb;39(2):612-28. Japanese. PubMed PMID: 3712761.

69: Inoue K. [Chemotherapy testing for human ovarian cancer using in vitro colony assay]. Gan To Kagaku Ryoho. 1985 Aug;12(8):1593-8. Japanese. PubMed PMID: 2411225.

70: Tsukagoshi S. Overview of new anticancer drugs of interest in Japan. Cancer Treat Rev. 1980 Dec;7(4):215-24. PubMed PMID: 6452201.