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Amsilarotene

Description of amsilarotene: amsilarotene (TAC-101) is a retinobenzoic acid with potential antineoplastic activity. TAC-101 inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   Taiho Pharma Inc.

 1: Nakayama Y, Inoue Y, Minagawa N, Onitsuka K, Nagata J, Shibao K, Hirata K, Sako T, Nagata N, Yamaguchi K. Chemopreventive effect of 4-[3,5-Bis(trimethylsilyl) benzamido] benzoic acid (TAC-101) on MNU-induced colon carcinogenesis in a rat model. Anticancer Res. 2009 Jun;29(6):2059-65. PubMed PMID: 19528465.

2: Katsuki H, Kurimoto E, Takemori S, Kurauchi Y, Hisatsune A, Isohama Y, Izumi Y, Kume T, Shudo K, Akaike A. Retinoic acid receptor stimulation protects midbrain dopaminergic neurons from inflammatory degeneration via BDNF-mediated signaling. J Neurochem. 2009 Jul;110(2):707-18. Epub 2009 May 15. PubMed PMID: 19457078.

3: Eshima K, Fukaya S, Sugimoto A, Mori T, Yokoi H, Yamamoto Y, Sugiura S, Honda S, Masuko N, Murakami K, Yamasaki Y, Kagechika H. Contribution of AP-1 interference induced by TAC-101 to tumor growth suppression in a hepatocellular carcinoma model. Tumour Biol. 2009;30(1):1-7. Epub 2009 Jan 12. PubMed PMID: 19142034.

4: Yamanoi Y, Nishihara H. Direct and selective arylation of tertiary silanes with rhodium catalyst. J Org Chem. 2008 Sep 5;73(17):6671-8. Epub 2008 Aug 6. PubMed PMID: 18681401.

5: Higginbotham KB, Lozano R, Brown T, Patt YZ, Arima T, Abbruzzese JL, Thomas MB. A phase I/II trial of TAC-101, an oral synthetic retinoid, in patients with advanced hepatocellular carcinoma. J Cancer Res Clin Oncol. 2008 Dec;134(12):1325-35. Epub 2008 May 27. PubMed PMID: 18504614.

6: Ezawa S, Suzuki N, Ohie S, Higashiguchi A, Hosoi F, Kitazato K, Susumu N, Aoki D. A synthetic retinoid, TAC-101 (4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid), plus cisplatin: potential new therapy for ovarian clear cell adenocarcinoma. Gynecol Oncol. 2008 Mar;108(3):627-31. Epub 2007 Nov 28. PubMed PMID: 18048092.

7: Inoue Y, Nakayama Y, Sako T, Minagawa N, Abe Y, Nagato M, Kadowaki K, Katsuki T, Matsumoto K, Tsurudome Y, Shibao K, Hirata K, Nagata N. 4- [3,5-bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) induced fas expression and activated caspase-3 and -8 in a DLD-1 colon cancer cell line. In Vivo. 2007 Mar-Apr;21(2):381-7. PubMed PMID: 17436592.

8: Sako T, Nakayama Y, Minagawa N, Inoue Y, Onitsuka K, Katsuki T, Tsurudome Y, Shibao K, Hirata K, Nagata N, Ohie S, Kohno K, Itoh H. 4-[3,5-Bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) induces apoptosis in colon cancer partially through the induction of Fas expression. In Vivo. 2005 Jan-Feb;19(1):125-32. PubMed PMID: 15796164.

9: Shudo K, Kagechika H, Yamazaki N, Igarashi M, Tateda C. A synthetic retinoid Am80 (tamibarotene) rescues the memory deficit caused by scopolamine in a passive avoidance paradigm. Biol Pharm Bull. 2004 Nov;27(11):1887-9. Erratum in: Biol Pharm Bull. 2005 Dec;28(12):2346. PubMed PMID: 15516744.

10: Minagawa N, Nakayama Y, Inoue Y, Onitsuka K, Katsuki T, Tsurudome Y, Shibao K, Hirata K, Sako T, Nagata N, Ohie S, Kohno K, Itoh H. 4-[3,5-Bis(trimethylsilyl)benzamido] benzoic acid inhibits angiogenesis in colon cancer through reduced expression of vascular endothelial growth factor. Oncol Res. 2004;14(9):407-14. PubMed PMID: 15490972.

11: Suzuki N, Aoki D, Oie S, Horiuchi M, Hasegawa Y, Ezawa S, Suzuki A, Susumu N, Hosoi F, Kitazato K, Nozawa S. A novel retinoid, 4-[3,5-bis (trimethylsilyl) benzamido] benzoic acid (TAC-101), induces apoptosis of human ovarian carcinoma cells and shows potential as a new antitumor agent for clear cell adenocarcinoma. Gynecol Oncol. 2004 Sep;94(3):643-9. PubMed PMID: 15350353.

12: Yoshimura K, Uchida G, Okazaki M, Kitano Y, Harii K. Differential expression of heparin-binding EGF-like growth factor (HB-EGF) mRNA in normal human keratinocytes induced by a variety of natural and synthetic retinoids. Exp Dermatol. 2003;12 Suppl 2:28-34. PubMed PMID: 14756521.

13: Satake K, Takagi E, Ishii A, Kato Y, Imagawa Y, Kimura Y, Tsukuda M. Anti-tumor effect of vitamin A and D on head and neck squamous cell carcinoma. Auris Nasus Larynx. 2003 Dec;30(4):403-12. PubMed PMID: 14656567.

14: Lee SJ, Ohashi Y, Sakurai H, Saiki I. TAC-101 inhibits intrahepatic metastasis of orthotopically implanted murine hepatocellular carcinoma. Cancer Lett. 2003 Aug 20;198(2):169-77. PubMed PMID: 12957355.

15: Miyagawa N, Homma T, Kagechika H, Shudo K, Nagai H. Effect of synthetic retinoid, TAC-101, on experimental autoimmune disease. Pharmacology. 2003 Jan;67(1):21-31. PubMed PMID: 12444300.

16: Rizvi NA, Marshall JL, Ness E, Hawkins MJ, Kessler C, Jacobs H, Brenckman WD Jr, Lee JS, Petros W, Hong WK, Kurie JM. Initial clinical trial of oral TAC-101, a novel retinoic acid receptor-alpha selective retinoid, in patients with advanced cancer. J Clin Oncol. 2002 Aug 15;20(16):3522-32. PubMed PMID: 12177113.

17: Miyaguchi T, Nomata K, Noguchi M, Watanabe J, Satoh H, Kanetake H. TAC-101, a novel retinobenzoic-acid derivative, enhances gap junctional intercellular communication among renal epithelial cells treated with renal carcinogens. Anticancer Res. 2001 Nov-Dec;21(6A):4025-30. PubMed PMID: 11911287.

18: Oikawa T, Murakami K, Sano M, Shibata J, Wierzba K, Yamada Y. A potential use of a synthetic retinoid TAC-101 as an orally active agent that blocks angiogenesis in liver metastases of human stomach cancer cells. Jpn J Cancer Res. 2001 Nov;92(11):1225-34. PubMed PMID: 11714448.

19: Shibata J, Murakami K, Aoyagi Y, Oie S, Hashimoto A, Suzuki K, Sano M, Wierzba TT, Yamada Y. The induction of apoptosis and inhibition of AP-1 activity by TAC-101 (4-[3,5-bis(trimethylsilyl) benzamido] benzoic acid) may result in life prolonging effect in animals bearing metastasizing cancer. Anticancer Res. 2000 Sep- Oct;20(5B):3583-90. PubMed PMID: 11131666.

20: Shibata J, Murakami K, Wierzba K, Aoyagi Y, Hashimoto A, Sano M, Toko T, Yamada Y. Anticancer effect of 4-[3,5-bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) against A549 non-small cell lung cancer cell line is related to its anti-invasive activity. Anticancer Res. 2000 Sep-Oct;20(5A):3169-76. PubMed PMID: 11062739.

21: Murakami K, Yamaura T, Suda K, Ohie S, Shibata J, Toko T, Yamada Y, Saiki I. TAC-101 (4-[3,5-bis(trimethylsilyl)benzamido]benzoic acid) inhibits spontaneous mediastinal lymph node metastasis produced by orthotopic implantation of Lewis lung carcinoma. Jpn J Cancer Res. 1999 Nov;90(11):1254-61. PubMed PMID: 10622538.

22: Murakami K, Sakukawa R, Sano M, Hashimoto A, Shibata J, Yamada Y, Saiki I. Inhibition of angiogenesis and intrahepatic growth of colon cancer by TAC-101. Clin Cancer Res. 1999 Sep;5(9):2304-10. PubMed PMID: 10499597.

23: Oikawa T. [Control of tumor-related angiogenesis]. Hum Cell. 1998 Dec;11(4):201-6. Review. Japanese. PubMed PMID: 10363157.

24: Fujimoto K, Hosotani R, Doi R, Wada M, Lee JU, Koshiba T, Miyamoto Y, Tsuji S, Nakajima S, Imamura M. Induction of cell-cycle arrest and apoptosis by a novel retinobenzoic-acid derivative, TAC-101, in human pancreatic-cancer cells. Int J Cancer. 1999 May 17;81(4):637-44. PubMed PMID: 10225456.

25: Murakami K, Matsuura T, Sano M, Hashimoto A, Yonekura K, Sakukawa R, Yamada Y, Saiki I. 4-[3,5-Bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) inhibits the intrahepatic spread of hepatocellular carcinoma and prolongs the life-span of tumor-bearing animals. Clin Exp Metastasis. 1998 Oct;16(7):633-43. PubMed PMID: 9932610.

26: Sakukawa R, Murakami K, Ikeda T, Yamada Y, Saiki I. Effect of 4-[3,5-bis(trimethylsilyl)benzamido] benzoic acid (TAC-101) on the liver metastasis of colon 26-L5 carcinoma cells. Oncol Res. 1998;10(6):287-93. PubMed PMID: 9848099.

27: Murakami K, Wierzba K, Sano M, Shibata J, Yonekura K, Hashimoto A, Sato K, Yamada Y. TAC-101, a benzoic acid derivative, inhibits liver metastasis of human gastrointestinal cancer and prolongs the life-span. Clin Exp Metastasis. 1998 May;16(4):323-31. PubMed PMID: 9626811.

28: Hashimoto Y, Kagechika H, Kawachi E, Fukasawa H, Saito G, Shudo K. Evaluation of differentiation-inducing activity of retinoids on human leukemia cell lines HL-60 and NB4. Biol Pharm Bull. 1996 Oct;19(10):1322-8. PubMed PMID: 8913505.