메뉴 건너뛰기




Volumn 65, Issue 2, 2010, Pages 235-241

Phase I first-in-human clinical study of S-trans, trans- farnesylthiosalicylic acid (salirasib) in patients with solid tumors

Author keywords

FTS; Pharmacokinetics; Phase I; Solid tumors; Toxicity

Indexed keywords

ANTINEOPLASTIC AGENT; DIPHENOXYLATE; FARNESYLTHIOSALICYLIC ACID; LOPERAMIDE; SALIRASIB; UNCLASSIFIED DRUG; DRUG DERIVATIVE; FARNESOL; SALICYLIC ACID DERIVATIVE;

EID: 71349085359     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00280-009-1027-4     Document Type: Article
Times cited : (35)

References (28)
  • 1
    • 0032717521 scopus 로고    scopus 로고
    • Concepts in Ras-directed therapy
    • 10.1517/13543784.8.12.2121 1:CAS:528:DyaK1MXns1eisLk%3D 11139843 (December)
    • Y Kloog AD Cox M Sinensky 1999 Concepts in Ras-directed therapy Expert Opin Investig Drugs 8 12 2121 2140 10.1517/13543784.8.12.2121 1:CAS:528:DyaK1MXns1eisLk%3D 11139843 (December)
    • (1999) Expert Opin Investig Drugs , vol.8 , Issue.12 , pp. 2121-2140
    • Kloog, Y.1    Cox, A.D.2    Sinensky, M.3
  • 2
    • 0027239613 scopus 로고
    • Function and regulation of ras
    • 10.1146/annurev.bi.62.070193.004223 1:CAS:528:DyaK3sXlsFCjuro%3D 8352603
    • DR Lowy BM Willumsen 1993 Function and regulation of ras Annu Rev Biochem 62 851 891 10.1146/annurev.bi.62.070193.004223 1:CAS:528:DyaK3sXlsFCjuro%3D 8352603
    • (1993) Annu Rev Biochem , vol.62 , pp. 851-891
    • Lowy, D.R.1    Willumsen, B.M.2
  • 3
    • 0034175984 scopus 로고    scopus 로고
    • Understanding Ras: 'It ain't over 'til it's over'
    • DOI 10.1016/S0962-8924(00)01740-2, PII S0962892400017402
    • JM Shields K Pruitt A McFall A Shaub CJ Der 2000 Understanding Ras: 'it ain't over 'til it's over' Trends Cell Biol 10 4 147 154 10.1016/S0962-8924(00) 01740-2 1:CAS:528:DC%2BD3cXit1Sqtr0%3D 10740269 (April) (Pubitemid 30171309)
    • (2000) Trends in Cell Biology , vol.10 , Issue.4 , pp. 147-154
    • Shields, J.M.1    Pruitt, K.2    McFall, A.3    Shaub, A.4    Der, C.J.5
  • 4
    • 0037264633 scopus 로고    scopus 로고
    • Targeting RAS signalling pathways in cancer therapy
    • DOI 10.1038/nrc969
    • J Downward 2003 Targeting RAS signalling pathways in cancer therapy Nat Rev Cancer 3 1 11 22 10.1038/nrc969 1:CAS:528:DC%2BD38XpvVertbo%3D 12509763 (January) (Pubitemid 37328883)
    • (2003) Nature Reviews Cancer , vol.3 , Issue.1 , pp. 11-22
    • Downward, J.1
  • 5
    • 0024376173 scopus 로고
    • Ras oncogenes in human cancer: A review
    • 1:CAS:528:DyaL1MXltlWksL4%3D 2547513 (1 September)
    • JL Bos 1989 Ras oncogenes in human cancer: a review Cancer Res 49 17 4682 4689 1:CAS:528:DyaL1MXltlWksL4%3D 2547513 (1 September)
    • (1989) Cancer Res , vol.49 , Issue.17 , pp. 4682-4689
    • Bos, J.L.1
  • 6
    • 0028959539 scopus 로고
    • Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth
    • 10.1021/jm00008a004 1:CAS:528:DyaK2MXkvVWruro%3D 7731012 (14 April)
    • D Marciano G Ben-Baruch M Marom Y Egozi R Haklai Y Kloog 1995 Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth J Med Chem 38 8 1267 1272 10.1021/jm00008a004 1:CAS:528:DyaK2MXkvVWruro%3D 7731012 (14 April)
    • (1995) J Med Chem , vol.38 , Issue.8 , pp. 1267-1272
    • Marciano, D.1    Ben-Baruch, G.2    Marom, M.3    Egozi, Y.4    Haklai, R.5    Kloog, Y.6
  • 7
    • 0032717429 scopus 로고    scopus 로고
    • Targeting of K-Ras 4B by S-trans, trans-farnesyl thiosalicylic acid
    • 10.1016/S0167-4889(99)00144-5 1:CAS:528:DyaK1MXnslyltrc%3D 10590312 (9 December)
    • G Elad A Paz R Haklai D Marciano A Cox Y Kloog 1999 Targeting of K-Ras 4B by S-trans, trans-farnesyl thiosalicylic acid Biochim Biophys Acta 1452 3 228 242 10.1016/S0167-4889(99)00144-5 1:CAS:528:DyaK1MXnslyltrc%3D 10590312 (9 December)
    • (1999) Biochim Biophys Acta , vol.1452 , Issue.3 , pp. 228-242
    • Elad, G.1    Paz, A.2    Haklai, R.3    Marciano, D.4    Cox, A.5    Kloog, Y.6
  • 8
    • 0033400494 scopus 로고    scopus 로고
    • Farnesylthiosalicylic acid inhibits the growth of human Merkel cell carcinoma in SCID mice
    • 10.1007/s001099900052 1:CAS:528:DC%2BD3cXmsFSlsw%3D%3D 10619439 (November)
    • B Jansen E Heere-Ress H Schlagbauer-Wadl, et al. 1999 Farnesylthiosalicylic acid inhibits the growth of human Merkel cell carcinoma in SCID mice J Mol Med 77 11 792 797 10.1007/s001099900052 1:CAS:528: DC%2BD3cXmsFSlsw%3D%3D 10619439 (November)
    • (1999) J Mol Med , vol.77 , Issue.11 , pp. 792-797
    • Jansen, B.1    Heere-Ress, E.2    Schlagbauer-Wadl, H.3
  • 10
    • 0030943198 scopus 로고    scopus 로고
    • Characterization of Ha-Ras, N-Ras, Ki-Ras4A, and Ki-Ras4B as in vitro substrates for farnesyl protein transferase and geranylgeranyl protein transferase type I
    • DOI 10.1074/jbc.272.15.10232
    • FL Zhang P Kirschmeier D Carr, et al. 1997 Characterization of Ha-ras, N-ras, Ki-Ras4A, and Ki-Ras4B as in vitro substrates for farnesyl protein transferase and geranylgeranyl protein transferase type I J Biol Chem 272 15 10232 10239 10.1074/jbc.272.15.10232 1:CAS:528:DyaK2sXisFOmurg%3D 9092572 (11 April) (Pubitemid 27171703)
    • (1997) Journal of Biological Chemistry , vol.272 , Issue.15 , pp. 10232-10239
    • Zhang, F.L.1    Kirschmeier, P.2    Carr, D.3    James, L.4    Bond, R.W.5    Wang, L.6    Patton, R.7    Windsor, W.T.8    Syto, R.9    Zhang, R.10    Bishop, W.R.11
  • 11
    • 0027323459 scopus 로고
    • Benzodiazepine peptidomimetics: Potent inhibitors of Ras farnesylation in animal cells
    • 10.1126/science.8316834 1:CAS:528:DyaK3sXltlWjtLg%3D 8316834 (25 June)
    • GL James JL Goldstein MS Brown, et al. 1993 Benzodiazepine peptidomimetics: potent inhibitors of Ras farnesylation in animal cells Science 260 5116 1937 1942 10.1126/science.8316834 1:CAS:528:DyaK3sXltlWjtLg%3D 8316834 (25 June)
    • (1993) Science , vol.260 , Issue.5116 , pp. 1937-1942
    • James, G.L.1    Goldstein, J.L.2    Brown, M.S.3
  • 12
    • 0027248872 scopus 로고
    • Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor
    • 10.1126/science.8316833 1:CAS:528:DyaK3sXltlWjtLs%3D 8316833 (25 June)
    • NE Kohl SD Mosser SJ deSolms, et al. 1993 Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor Science 260 5116 1934 1937 10.1126/science.8316833 1:CAS:528:DyaK3sXltlWjtLs%3D 8316833 (25 June)
    • (1993) Science , vol.260 , Issue.5116 , pp. 1934-1937
    • Kohl, N.E.1    Mosser, S.D.2    Desolms, S.J.3
  • 13
    • 34848874825 scopus 로고    scopus 로고
    • Orally administered FTS (salirasib) inhibits human pancreatic tumor growth in nude mice
    • DOI 10.1007/s00280-007-0451-6
    • R Haklai G Elad-Sfadia Y Egozi Y Kloog 2008 Orally administered FTS (salirasib) inhibits human pancreatic tumor growth in nude mice Cancer Chemother Pharmacol 61 1 89 96 10.1007/s00280-007-0451-6 1:CAS:528:DC%2BD2sXhtFSrtbfN 17909812 (January) (Pubitemid 47512630)
    • (2008) Cancer Chemotherapy and Pharmacology , vol.61 , Issue.1 , pp. 89-96
    • Haklai, R.1    Elad-Sfadia, G.2    Egozi, Y.3    Kloog, Y.4
  • 14
    • 34248173296 scopus 로고    scopus 로고
    • Gene expression signature of human cancer cell lines treated with the Ras inhibitor salirasib (S-farnesylthiosalicylic acid)
    • DOI 10.1158/0008-5472.CAN-06-4287
    • R Blum R Elkon S Yaari, et al. 2007 Gene expression signature of human cancer cell lines treated with the ras inhibitor salirasib (S- farnesylthiosalicylic acid) Cancer Res 67 7 3320 3328 10.1158/0008-5472.CAN-06- 4287 1:CAS:528:DC%2BD2sXksVGks7c%3D 17409441 (1 April) (Pubitemid 46724871)
    • (2007) Cancer Research , vol.67 , Issue.7 , pp. 3320-3328
    • Blum, R.1    Elkon, R.2    Yaari, S.3    Zundelevich, A.4    Jacob-Hirsch, J.5    Rechavi, G.6    Shamir, R.7    Kloog, Y.8
  • 15
    • 33749576587 scopus 로고    scopus 로고
    • Suppression of survivin expression in glioblastoma cells by the Ras inhibitor farnesylthiosalicylic acid promotes caspase-dependent apoptosis
    • DOI 10.1158/1535-7163.MCT-06-0193
    • R Blum J Jacob-Hirsch G Rechavi Y Kloog 2006 Suppression of survivin expression in glioblastoma cells by the Ras inhibitor farnesylthiosalicylic acid promotes caspase-dependent apoptosis Mol Cancer Ther 5 9 2337 2347 10.1158/1535-7163.MCT-06-0193 1:CAS:528:DC%2BD28Xps1ynsb4%3D 16985068 (September) (Pubitemid 44530471)
    • (2006) Molecular Cancer Therapeutics , vol.5 , Issue.9 , pp. 2337-2347
    • Blum, R.1    Jacob-Hirsch, J.2    Rechavi, G.3    Kloog, Y.4
  • 16
    • 13044270403 scopus 로고    scopus 로고
    • Novel Ras antagonist blocks human melanoma growth
    • 10.1073/pnas.96.24.14019 1:CAS:528:DyaK1MXns1Oqu7w%3D 10570191 (23 November)
    • B Jansen H Schlagbauer-Wadl H Kahr, et al. 1999 Novel Ras antagonist blocks human melanoma growth Proc Natl Acad Sci USA 96 24 14019 14024 10.1073/pnas.96.24.14019 1:CAS:528:DyaK1MXns1Oqu7w%3D 10570191 (23 November)
    • (1999) Proc Natl Acad Sci USA , vol.96 , Issue.24 , pp. 14019-14024
    • Jansen, B.1    Schlagbauer-Wadl, H.2    Kahr, H.3
  • 17
    • 0036184738 scopus 로고    scopus 로고
    • The Ras inhibitor S-trans, trans-farnesylthiosalicylic acid chemosensitizes human tumor cells without causing resistance
    • 1:CAS:528:DC%2BD38XitFensrs%3D 11839677 (February)
    • M Gana-Weisz J Halaschek-Wiener B Jansen G Elad R Haklai Y Kloog 2002 The Ras inhibitor S-trans, trans-farnesylthiosalicylic acid chemosensitizes human tumor cells without causing resistance Clin Cancer Res 8 2 555 565 1:CAS:528:DC%2BD38XitFensrs%3D 11839677 (February)
    • (2002) Clin Cancer Res , vol.8 , Issue.2 , pp. 555-565
    • Gana-Weisz, M.1    Halaschek-Wiener, J.2    Jansen, B.3    Elad, G.4    Haklai, R.5    Kloog, Y.6
  • 18
    • 0034594628 scopus 로고    scopus 로고
    • New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada
    • 10.1093/jnci/92.3.205 1:STN:280:DC%2BD3c7it1Gitg%3D%3D 10655437 (2 February)
    • P Therasse SG Arbuck EA Eisenhauer, et al. 2000 New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada J Natl Cancer Inst 92 3 205 216 10.1093/jnci/92.3.205 1:STN:280:DC%2BD3c7it1Gitg%3D%3D 10655437 (2 February)
    • (2000) J Natl Cancer Inst , vol.92 , Issue.3 , pp. 205-216
    • Therasse, P.1    Arbuck, S.G.2    Eisenhauer, E.A.3
  • 19
    • 71349085849 scopus 로고    scopus 로고
    • Concordia Pharmaceuticals, Inc., Ft. Lauderdale, FL, Company report
    • Concordia Pharmaceuticals, Inc., Ft. Lauderdale, FL, Company report
  • 20
    • 0026336726 scopus 로고
    • Analytical methods validation: Bioavailability, bioequivalence and pharmacokinetic studies. Conference report
    • 1:STN:280:DyaK38zoslWktA%3D%3D 1823867 (October-December)
    • VP Shah KK Midha S Dighe, et al. 1991 Analytical methods validation: bioavailability, bioequivalence and pharmacokinetic studies. Conference report Eur J Drug Metab Pharmacokinet 16 4 249 255 1:STN:280:DyaK38zoslWktA%3D%3D 1823867 (October-December)
    • (1991) Eur J Drug Metab Pharmacokinet , vol.16 , Issue.4 , pp. 249-255
    • Shah, V.P.1    Midha, K.K.2    Dighe, S.3
  • 22
    • 3442880458 scopus 로고    scopus 로고
    • A clue to the therapy of neurofibromatosis type 2: NF2/merlin is a PAK1 inhibitor
    • 10.1097/00130404-200401000-00006 1:CAS:528:DC%2BD2cXnvFWkurc%3D 15000491 (January-February)
    • Y Hirokawa A Tikoo J Huynh, et al. 2004 A clue to the therapy of neurofibromatosis type 2: NF2/merlin is a PAK1 inhibitor Cancer J 10 1 20 26 10.1097/00130404-200401000-00006 1:CAS:528:DC%2BD2cXnvFWkurc%3D 15000491 (January-February)
    • (2004) Cancer J , vol.10 , Issue.1 , pp. 20-26
    • Hirokawa, Y.1    Tikoo, A.2    Huynh, J.3
  • 23
    • 33645220442 scopus 로고    scopus 로고
    • The Phosphorylation status of merlin is important for regulating the Ras-ERK pathway
    • 1:CAS:528:DC%2BD2MXht1KqsL7I 16267393 (31 October)
    • JR Jung H Kim SS Jeun JY Lee EJ Koh C Ji 2005 The Phosphorylation status of merlin is important for regulating the Ras-ERK pathway Mol Cells 20 2 196 200 1:CAS:528:DC%2BD2MXht1KqsL7I 16267393 (31 October)
    • (2005) Mol Cells , vol.20 , Issue.2 , pp. 196-200
    • Jung, J.R.1    Kim, H.2    Jeun, S.S.3    Lee, J.Y.4    Koh, E.J.5    Ji, C.6
  • 24
    • 33846702026 scopus 로고    scopus 로고
    • Merlin/neurofibromatosis type 2 suppresses growth by inhibiting the activation of Ras and Rac
    • DOI 10.1158/0008-5472.CAN-06-1608
    • H Morrison T Sperka J Manent M Giovannini H Ponta P Herrlich 2007 Merlin/neurofibromatosis type 2 suppresses growth by inhibiting the activation of Ras and Rac Cancer Res 67 2 520 527 10.1158/0008-5472.CAN-06-1608 1:CAS:528:DC%2BD2sXmtVKltw%3D%3D 17234759 (15 January) (Pubitemid 46192188)
    • (2007) Cancer Research , vol.67 , Issue.2 , pp. 520-527
    • Morrison, H.1    Sperka, T.2    Manent, J.3    Giovannini, M.4    Ponta, H.5    Herrlich, P.6
  • 25
    • 33745486561 scopus 로고    scopus 로고
    • The Genetic and Molecular Pathogenesis of NF1 and NF2
    • DOI 10.1016/j.spen.2006.01.007, PII S1071909106000118, Neurocutaneous Disordres
    • KH Yohay 2006 The genetic and molecular pathogenesis of NF1 and NF2 Semin Pediatr Neurol 13 1 21 26 10.1016/j.spen.2006.01.007 16818172 (March) (Pubitemid 43963397)
    • (2006) Seminars in Pediatric Neurology , vol.13 , Issue.1 , pp. 21-26
    • Yohay, K.H.1
  • 26
    • 25844507104 scopus 로고    scopus 로고
    • Farnesylthiosalicylic acid blocks mammalian target of rapamycin signaling in breast cancer cells
    • DOI 10.1002/ijc.21222
    • W Yue J Wang Y Li P Fan RJ Santen 2005 Farnesylthiosalicylic acid blocks mammalian target of rapamycin signaling in breast cancer cells Int J Cancer 117 5 746 754 10.1002/ijc.21222 1:CAS:528:DC%2BD2MXht1ShsbbN 15957161 (10 December) (Pubitemid 41598825)
    • (2005) International Journal of Cancer , vol.117 , Issue.5 , pp. 746-754
    • Yue, W.1    Wang, J.2    Li, Y.3    Fan, P.4    Santen, R.J.5
  • 27
    • 33646079383 scopus 로고    scopus 로고
    • Farnesylthiosalicylic acid: Inhibition of proliferation and enhancement of apoptosis of hormone-dependent breast cancer cells
    • 10.1097/01.cad.0000185184.64980.39 1:CAS:528:DC%2BD2MXht1Glt7%2FK 16317288 (January)
    • RJ Santen AR Lynch LR Neal RA McPherson W Yue 2006 Farnesylthiosalicylic acid: inhibition of proliferation and enhancement of apoptosis of hormone-dependent breast cancer cells Anticancer Drugs 17 1 33 40 10.1097/01.cad.0000185184.64980.39 1:CAS:528:DC%2BD2MXht1Glt7%2FK 16317288 (January)
    • (2006) Anticancer Drugs , vol.17 , Issue.1 , pp. 33-40
    • Santen, R.J.1    Lynch, A.R.2    Neal, L.R.3    McPherson, R.A.4    Yue, W.5
  • 28
    • 26944461271 scopus 로고    scopus 로고
    • The inhibition of human mesangial cell proliferation by S-trans, trans-farnesylthiosalicylic acid
    • DOI 10.1111/j.1523-1755.2005.00425.x, PII 4494617
    • A Khwaja CC Sharpe M Noor Y Kloog BM Hendry 2005 The inhibition of human mesangial cell proliferation by S-trans, trans-farnesylthiosalicylic acid Kidney Int 68 2 474 486 10.1111/j.1523-1755.2005.00425.x 1:CAS:528: DC%2BD2MXpt1Wmsrc%3D 16014024 (August) (Pubitemid 43323102)
    • (2005) Kidney International , vol.68 , Issue.2 , pp. 474-486
    • Khwaja, A.1    Sharpe, C.C.2    Noor, M.3    Kloog, Y.4    Hendry, B.M.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.