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Salirasib is a salicylic acid derivative with potential antineoplastic activity. Salirasib dislodges all Ras isoforms from their membrane-anchoring sites, thereby preventing activation of RAS signaling cascades that mediated cell proliferation, differentiation, and senescence. RAS signaling is believed to be abnormally activated in one-third of human cancers, including cancers of the pancreas, colon, lung and breast. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Salirasib binds to a cell membrane anchor protein thereby selectively blocking a cascade of biochemical signals known as the Ras signaling pathway. The Ras pathway plays an important role in tumor growth and is believed to be abnormally activated in one-third of human cancers, including cancers of the pancreas, colon, lung and breast. Up to 90% of human pancreatic cancers are driven by aberrant oncogenic Ras signaling. For detail please see Concordia Pharmaceutical's website

Current developer:  Concordia Pharmaceuticals

B1. Neurath, A. Robert; Lackman-Smith, Carol. Prevention of human immunodeficiency virus type 1 transmission by pharmaceuticals targeted to host proteins required for virus infection? Consideration of Farnesyl thiosalicylic acid, a Ras inhibitor. Journal of Antivirals & Antiretrovirals (2009), 1(2), 072-075. CODEN: JAAOC9 ISSN:1948-5964. AN 2010:397564

2. Yaari-Stark, Shira; Shaked, Maayan; Nevo-Caspi, Yael; Jacob-Hircsh, Jasmine; Shamir, Ron; Rechavi, Gideon; Kloog, Yoel. Ras inhibits endoplasmic reticulum stress in human cancer cells with amplified Myc. International Journal of Cancer (2010), 126(10), 2268-2281. CODEN: IJCNAW ISSN:0020-7136. CAN 152:451033 AN 2010:392292

3. Tsimberidou, Apostolia Maria; Rudek, Michelle A.; Hong, David; Ng, Chaan S.; Blair, Jessica; Goldsweig, Howard; Kurzrock, Razelle. Phase 1 first-in-human clinical study of S-trans, trans-farnesylthiosalicylic acid (salirasib) in patients with solid tumors. Cancer Chemotherapy and Pharmacology (2010), 65(2), 235-241. CODEN: CCPHDZ ISSN:0344-5704. CAN 152:421750 AN 2009:1464193

4. Goldberg, Liat; Haklai, Roni; Bauer, Victor; Heiss, Aaron; Kloog, Yoel. New Derivatives of Farnesylthiosalicylic Acid (Salirasib) for Cancer Treatment: Farnesylthiosalicylamide Inhibits Tumor Growth in Nude Mice Models. Journal of Medicinal Chemistry (2009), 52(1), 197-205. CODEN: JMCMAR ISSN:0022-2623. CAN 150:28393 AN 2008:1500762

5. Goldberg, Liat; Ocherashvilli, Aharon; Daniels, Dianne; Last, David; Cohen, Zvi R.; Tamar, Gregory; Kloog, Yoel; Mardor, Yael. Salirasib (farnesyl thiosalicylic acid) for brain tumor treatment: a convection-enhanced drug delivery study in rats. Molecular Cancer Therapeutics (2008), 7(11), 3609-3616. CODEN: MCTOCF ISSN:1535-7163. CAN 150:70750 AN 2008:1353107

6. Zhao, Ming; He, Ping; Xu, Linping; Hidalgo, Manuel; Laheru, Dan; Rudek, Michelle A. Determination of salirasib (S-trans,trans-farnesylthiosalicylic acid) in human plasma using liquid chromatography-tandem mass spectrometry. Journal of Chromatography, B: Analytical Technologies in the Biomedical and Life Sciences (2008), 869(1-2), 142-145. CODEN: JCBAAI ISSN:1570-0232. CAN 149:69463 AN 2008:722666

7. Rotblat, Barak; Ehrlich, Marcello; Haklai, Roni; Kloog, Yoel. The Ras inhibitor farnesylthiosalicylic acid (Salirasib) disrupts the spatiotemporal localization of active Ras: a potential treatment for cancer. Methods in Enzymology (2008), 439(Small GTPAses in Disease, Part B), 467-489. CODEN: MENZAU ISSN:0076-6879. CAN 149:94412 AN 2008:622547

8. Haklai, Roni; Elad-Sfadia, Galit; Egozi, Yaakov; Kloog, Yoel. Orally administered FTS (salirasib) inhibits human pancreatic tumor growth in nude mice. Cancer Chemotherapy and Pharmacology (2007), Volume Date 2008, 61(1), 89-96. CODEN: CCPHDZ ISSN:0344-5704. CAN 148:205540 AN 2007:1108791

9. Zundelevich, Adi; Elad-Sfadia, Galit; Haklai, Ronit; Kloog, Yoel. Suppression of lung cancer tumor growth in a nude mouse model by the Ras inhibitor salirasib (farnesylthiosalicylic acid). Molecular Cancer Therapeutics (2007), 6(6), 1765-1773. CODEN: MCTOCF ISSN:1535-7163. CAN 147:250093 AN 2007:654894

10. Blum, Roy; Elkon, Ran; Yaari, Shira; Zundelevich, Adi; Jacob-Hirsch, Jasmine; Rechavi, Gideon; Shamir, Ron; Kloog, Yoel. Gene Expression Signature of Human Cancer Cell Lines Treated with the Ras Inhibitor Salirasib (S-Farnesylthiosalicylic Acid). Cancer Research (2007), 67(7), 3320-3328. CODEN: CNREA8 ISSN:0008-5472. CAN 146:454468 AN 2007:445719

11. Yaari-Stark Shira; Shaked Maayan; Nevo-Caspi Yael; Jacob-Hircsh Jasmine; Shamir Ron; Rechavi Gideon; Kloog Yoel Ras inhibits endoplasmic reticulum stress in human cancer cells with amplified Myc. International journal of cancer. Journal international du cancer (2010), 126(10), 2268-81. Journal code: 0042124. E-ISSN:1097-0215. PubMed ID 19998334 AN 2010215169

12. Goldberg Liat; Haklai Roni; Bauer Victor; Heiss Aaron; Kloog Yoel New derivatives of farnesylthiosalicylic acid (salirasib) for cancer treatment: farnesylthiosalicylamide inhibits tumor growth in nude mice models. Journal of medicinal chemistry (2009), 52(1), 197-205. Journal code: 9716531. E-ISSN:1520-4804. PubMed ID 19072665 AN 2009046646

13. Goldberg Liat; Ocherashvilli Aharon; Daniels Dianne; Last David; Cohen Zvi R; Tamar Gregory; Kloog Yoel; Mardor Yael Salirasib (farnesyl thiosalicylic acid) for brain tumor treatment: a convection-enhanced drug delivery study in rats. Molecular cancer therapeutics (2008), 7(11), 3609-16. Journal code: 101132535. ISSN:1535-7163. PubMed ID 19001442 AN 2008732623

14. Zhao Ming; He Ping; Xu Linping; Hidalgo Manuel; Laheru Dan; Rudek Michelle A Determination of salirasib (S-trans,trans-farnesylthiosalicylic acid) in human plasma using liquid chromatography-tandem mass spectrometry. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences (2008), 869(1-2), 142-5. Journal code: 101139554. ISSN:1570-0232. PubMed ID 18534927 AN 2008385208

15. Rotblat Barak; Ehrlich Marcello; Haklai Roni; Kloog Yoel The Ras inhibitor farnesylthiosalicylic acid (Salirasib) disrupts the spatiotemporal localization of active Ras: a potential treatment for cancer. Methods in enzymology (2008), 439 467-89. Journal code: 0212271. ISSN:0076-6879. PubMed ID 18374183 AN 2008216519

16. Haklai Roni; Elad-Sfadia Galit; Egozi Yaakov; Kloog Yoel Orally administered FTS (salirasib) inhibits human pancreatic tumor growth in nude mice. Cancer chemotherapy and pharmacology (2008), 61(1), 89-96. Journal code: 7806519. ISSN:0344-5704. PubMed ID 17909812 AN 2007588457

17. Zundelevich Adi; Elad-Sfadia Galit; Haklai Ronit; Kloog Yoel Suppression of lung cancer tumor growth in a nude mouse model by the Ras inhibitor salirasib (farnesylthiosalicylic acid). Molecular cancer therapeutics (2007), 6(6), 1765-73. Journal code: 101132535. ISSN:1535-7163. PubMed ID 17541036 AN 2007357125

18. Blum Roy; Elkon Ran; Yaari Shira; Zundelevich Adi; Jacob-Hirsch Jasmine; Rechavi Gideon; Shamir Ron; Kloog Yoel Gene expression signature of human cancer cell lines treated with the ras inhibitor salirasib (S-farnesylthiosalicylic acid). Cancer research (2007), 67(7), 3320-8. Journal code: 2984705R. ISSN:0008-5472. PubMed ID 17409441 AN 2007232983