메뉴 건너뛰기




Volumn 18, Issue 15, 2012, Pages 4173-4182

A multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors

Author keywords

[No Author keywords available]

Indexed keywords

4 DIALLYLAMINOMETHYLENE 1,3,4,7,10,11,12,13,14,15,16,17 DODECAHYDRO 6 HYDROXY 1 METHOXYMETHYL 10,13 DIMETHYL 3,7,17 TRIOXO 2 OXACYCLOPENTA[A]PHENANTHREN 11 YL ACETATE; PHOSPHATIDYLINOSITOL 3 KINASE;

EID: 84864493357     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-12-0714     Document Type: Article
Times cited : (156)

References (41)
  • 1
    • 0036185848 scopus 로고    scopus 로고
    • The protein kinase B/Akt signalling pathway in human malignancy
    • DOI 10.1016/S0898-6568(01)00271-6, PII S0898656801002716
    • Nicholson KM, Anderson NG. The protein kinase B/Akt signalling pathway in human malignancy. Cell Signal 2002;14:381-95. (Pubitemid 34214843)
    • (2002) Cellular Signalling , vol.14 , Issue.5 , pp. 381-395
    • Nicholson, K.M.1    Anderson, N.G.2
  • 2
    • 33847314539 scopus 로고    scopus 로고
    • The phosphatidyl inositol 3-kinase signaling network: Implications for human breast cancer
    • DOI 10.1038/sj.onc.1210202, PII 1210202
    • Dillon RL, White DE, Muller WJ. The phosphatidyl inositol 3-kinase signaling network: implications for human breast cancer. Oncogene 2007;26:1338-45. (Pubitemid 46328463)
    • (2007) Oncogene , vol.26 , Issue.9 , pp. 1338-1345
    • Dillon, R.L.1    White, D.E.2    Muller, W.J.3
  • 3
    • 74049107249 scopus 로고    scopus 로고
    • PI3K pathway activation in breast cancer is associated with the basal-like phenotype and cancer-specific mortality
    • Lopez-Knowles E, O'Toole SA, McNeil CM, Millar EK, Qiu MR, Crea P, et al. PI3K pathway activation in breast cancer is associated with the basal-like phenotype and cancer-specific mortality. Int J Cancer 2010;126:1121-31.
    • (2010) Int J Cancer , vol.126 , pp. 1121-1131
    • Lopez-Knowles, E.1    O'Toole, S.A.2    McNeil, C.M.3    Millar, E.K.4    Qiu, M.R.5    Crea, P.6
  • 6
    • 33645226001 scopus 로고    scopus 로고
    • Molecular analysis of the PI3K-AKT pathway in uterine cervical neoplasia: Frequent PIK3CA amplification and AKT phosphorylation
    • Bertelsen BI, Steine SJ, Sandvei R, Molven A, Laerum OD. Molecular analysis of the PI3K-AKT pathway in uterine cervical neoplasia: frequent PIK3CA amplification and AKT phosphorylation. Int J Cancer 2006;118:1877-83.
    • (2006) Int J Cancer , vol.118 , pp. 1877-1883
    • Bertelsen, B.I.1    Steine, S.J.2    Sandvei, R.3    Molven, A.4    Laerum, O.D.5
  • 7
    • 33646706052 scopus 로고    scopus 로고
    • Oncogenic PI3K and its role in cancer
    • DOI 10.1097/01.cco.0000198021.99347.b9, PII 0000162220060100000013
    • Samuels Y, Ericson K. Oncogenic PI3K and its role in cancer. Curr Opin Oncol 2006;18:77-82. (Pubitemid 43740454)
    • (2006) Current Opinion in Oncology , vol.18 , Issue.1 , pp. 77-82
    • Samuels, Y.1    Ericson, K.2
  • 9
    • 80052177544 scopus 로고    scopus 로고
    • Exome sequencing of head and neck squamous cell carcinoma reveals inactivating mutations in NOTCH1
    • Agrawal N, Frederick MJ, Pickering CR, Bettegowda C, Chang K, Li RJ, et al. Exome sequencing of head and neck squamous cell carcinoma reveals inactivating mutations in NOTCH1. Science 2011;333:1154-7.
    • (2011) Science , vol.333 , pp. 1154-1157
    • Agrawal, N.1    Frederick, M.J.2    Pickering, C.R.3    Bettegowda, C.4    Chang, K.5    Li, R.J.6
  • 12
    • 38949121953 scopus 로고    scopus 로고
    • PIK3CA gene mutations and amplifications in uterine cancers, identified by methods that avoid confounding by PIK3CA pseudogene sequences
    • Miyake T, Yoshino K, Enomoto T, Takata T, Ugaki H, Kim A, et al. PIK3CA gene mutations and amplifications in uterine cancers, identified by methods that avoid confounding by PIK3CA pseudogene sequences. Cancer Lett 2008;261:120-6.
    • (2008) Cancer Lett , vol.261 , pp. 120-126
    • Miyake, T.1    Yoshino, K.2    Enomoto, T.3    Takata, T.4    Ugaki, H.5    Kim, A.6
  • 14
    • 0033551070 scopus 로고    scopus 로고
    • New insights into tumor suppression: PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway
    • DOI 10.1073/pnas.96.8.4240
    • Cantley LC, Neel BG. New insights into tumor suppression: PTEN suppresses tumor formation by restraining the phosphoinositide 3-kinase/AKT pathway. Proc Natl Acad Sci U S A 1999;96:4240-5. (Pubitemid 29190320)
    • (1999) Proceedings of the National Academy of Sciences of the United States of America , vol.96 , Issue.8 , pp. 4240-4245
    • Cantley, L.C.1    Neel, B.G.2
  • 15
    • 51849084360 scopus 로고    scopus 로고
    • The PTEN-PI3K pathway: Of feedbacks and cross-talks
    • Carracedo A, Pandolfi PP. The PTEN-PI3K pathway: of feedbacks and cross-talks. Oncogene 2008;27:5527-41.
    • (2008) Oncogene , vol.27 , pp. 5527-5541
    • Carracedo, A.1    Pandolfi, P.P.2
  • 16
    • 54549108740 scopus 로고    scopus 로고
    • Comprehensive genomic characterization defines human glioblastoma genes and core pathways
    • Comprehensive genomic characterization defines human glioblastoma genes and core pathways. Nature 2008;455:1061-8.
    • (2008) Nature , vol.455 , pp. 1061-1068
  • 17
    • 33846557325 scopus 로고    scopus 로고
    • Coexistence of the loss of heterozygosity at the PTEN locus and HER2 overexpression enhances the Akt activity thus leading to a negative progesterone receptor expression in breast carcinoma
    • DOI 10.1007/s10549-006-9295-8
    • Tokunaga E, Oki E, Kimura Y, Yamanaka T, Egashira A, Nishida K, et al. Coexistence of the loss of heterozygosity at the PTEN locus and HER2 overexpression enhances the Akt activity thus leading to a negative progesterone receptor expression in breast carcinoma. Breast Cancer Res Treat 2007;101:249-57. (Pubitemid 46169878)
    • (2007) Breast Cancer Research and Treatment , vol.101 , Issue.3 , pp. 249-257
    • Tokunaga, E.1    Oki, E.2    Kimura, Y.3    Yamanaka, T.4    Egashira, A.5    Nishida, K.6    Koga, T.7    Morita, M.8    Kakeji, Y.9    Maehara, Y.10
  • 19
    • 79952660192 scopus 로고    scopus 로고
    • New phosphatidylinositol 3-kinase inhibitors for cancer
    • Bowles DW, Jimeno A. New phosphatidylinositol 3-kinase inhibitors for cancer. Expert Opin Investig Drugs 2011;20:507-18.
    • (2011) Expert Opin Investig Drugs , vol.20 , pp. 507-518
    • Bowles, D.W.1    Jimeno, A.2
  • 20
    • 67749122122 scopus 로고    scopus 로고
    • Targeting PI3K signalling in cancer: Opportunities, challenges and limitations
    • Engelman JA. Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer 2009;9:550-62.
    • (2009) Nat Rev Cancer , vol.9 , pp. 550-562
    • Engelman, J.A.1
  • 21
  • 23
    • 77951252587 scopus 로고    scopus 로고
    • Brain-derived neurotrophic factor induces proliferation, migration, and VEGF secretion in human multiple myeloma cells via activation of MEK-ERK and PI3K/AKT signaling
    • Sun CY, Hu Y, Huang J, Chu ZB, Zhang L, She XM, et al. Brain-derived neurotrophic factor induces proliferation, migration, and VEGF secretion in human multiple myeloma cells via activation of MEK-ERK and PI3K/AKT signaling. Tumour Biol 2010;31:121-8.
    • (2010) Tumour Biol , vol.31 , pp. 121-128
    • Sun, C.Y.1    Hu, Y.2    Huang, J.3    Chu, Z.B.4    Zhang, L.5    She, X.M.6
  • 24
    • 3142679468 scopus 로고    scopus 로고
    • Synthesis and biological evaluation of synthetic viridins derived fromC (20)-heteroalkylation of the steroidal PI-3-kinase inhibitor wortmannin
    • Wipf P, Minion DJ, Halter RJ, Berggren MI, Ho CB, Chiang GG, et al. Synthesis and biological evaluation of synthetic viridins derived fromC (20)-heteroalkylation of the steroidal PI-3-kinase inhibitor wortmannin. Org Biomol Chem 2004;2:1911-20.
    • (2004) Org Biomol Chem , vol.2 , pp. 1911-1920
    • Wipf, P.1    Minion, D.J.2    Halter, R.J.3    Berggren, M.I.4    Ho, C.B.5    Chiang, G.G.6
  • 25
    • 84878726561 scopus 로고    scopus 로고
    • 17-Hydroxy-PX-866, the primary metabolite of PX-866, an irreversible, pan-isoform inhibitor of phosphatidylinositol-3 (PI3) kinase, has increased activity in biochemical and cellular assays
    • [abstract]. Seattle, WA: Oncothyreon Inc.
    • Klucher K, Vo A, Walker C, Rosler R, Taylor J, Millard J, et al. 17-Hydroxy-PX-866, the primary metabolite of PX-866, an irreversible, pan-isoform inhibitor of phosphatidylinositol-3 (PI3) kinase, has increased activity in biochemical and cellular assays [abstract]. In: AACR Special Conference on Targeting PI3K/mTOR Signaling in Cancer; 2011 Feb 24-27. Seattle, WA: Oncothyreon Inc.; 2011.
    • (2011) AACR Special Conference on Targeting PI3K/mTOR Signaling in Cancer; 2011 Feb 24-27
    • Klucher, K.1    Vo, A.2    Walker, C.3    Rosler, R.4    Taylor, J.5    Millard, J.6
  • 28
    • 33644685228 scopus 로고    scopus 로고
    • The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts
    • Ihle NT, Paine-Murrieta G, Berggren MI, Baker A, Tate WR, Wipf P, et al. The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts. Mol Cancer Ther 2005;4:1349-57.
    • (2005) Mol Cancer Ther , vol.4 , pp. 1349-1357
    • Ihle, N.T.1    Paine-Murrieta, G.2    Berggren, M.I.3    Baker, A.4    Tate, W.R.5    Wipf, P.6
  • 29
    • 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
    • Therasse P, Arbuck SG, Eisenhauer EA, Wanders J, Kaplan RS, Rubinstein L, et al. 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 2000;92:205-16.
    • (2000) J Natl Cancer Inst , vol.92 , pp. 205-216
    • Therasse, P.1    Arbuck, S.G.2    Eisenhauer, E.A.3    Wanders, J.4    Kaplan, R.S.5    Rubinstein, L.6
  • 31
    • 84856071447 scopus 로고    scopus 로고
    • Phase I, dose-escalation study of BKM120, an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors
    • Bendell JC, Rodon J, Burris HA, de Jonge M, Verweij J, Birle D, et al. Phase I, dose-escalation study of BKM120, an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. J Clin Oncol 2012;30:282-90.
    • (2012) J Clin Oncol , vol.30 , pp. 282-290
    • Bendell, J.C.1    Rodon, J.2    Burris, H.A.3    De Jonge, M.4    Verweij, J.5    Birle, D.6
  • 32
    • 84863828298 scopus 로고    scopus 로고
    • Aphase Ib study to evaluate the PI3-kinase inhibitor GDC-0941 with paclitaxel (P) and carboplatin (C), with and without bevacizumab (BEV), in patients with advanced non-small cell lung cancer (NSCLC)
    • abstr 3044
    • Besse B, Soria J,Gomez-Roca C, Ware A, Adjei A, Dy GK, et al.Aphase Ib study to evaluate the PI3-kinase inhibitor GDC-0941 with paclitaxel (P) and carboplatin (C), with and without bevacizumab (BEV), in patients with advanced non-small cell lung cancer (NSCLC). J Clin Oncol 29:2011 (suppl; abstr 3044).
    • (2011) J Clin Oncol , vol.29 , Issue.SUPPL.
    • Besse, B.1    Soria, J.-R.C.2    Ware, A.3    Adjei, A.4    Dy, G.K.5
  • 35
    • 33947514699 scopus 로고    scopus 로고
    • Prognostic value of PIK3CA and phosphorylated AKT expression in ovarian cancer
    • DOI 10.1007/s00428-006-0358-3
    • Woenckhaus J, Steger K, Sturm K, Munstedt K, Franke FE, Fenic I. Prognostic value of PIK3CA and phosphorylated AKT expression in ovarian cancer. Virchows Arch 2007;450:387-95. (Pubitemid 46466383)
    • (2007) Virchows Archiv , vol.450 , Issue.4 , pp. 387-395
    • Woenckhaus, J.1    Steger, K.2    Sturm, K.3    Munstedt, K.4    Franke, F.E.5    Fenic, I.6
  • 37
    • 58249120506 scopus 로고    scopus 로고
    • Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance
    • Ihle NT, Lemos R Jr, Wipf P, Yacoub A, Mitchell C, Siwak D, et al. Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance. Cancer Res 2009;69:143-50.
    • (2009) Cancer Res , vol.69 , pp. 143-150
    • Ihle, N.T.1    Lemos Jr., R.2    Wipf, P.3    Yacoub, A.4    Mitchell, C.5    Siwak, D.6
  • 38
    • 79955983369 scopus 로고    scopus 로고
    • The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations
    • Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res 2011;17:3272-81.
    • (2011) Clin Cancer Res , vol.17 , pp. 3272-3281
    • Tanaka, H.1    Yoshida, M.2    Tanimura, H.3    Fujii, T.4    Sakata, K.5    Tachibana, Y.6
  • 39
    • 81055149891 scopus 로고    scopus 로고
    • PF-04691502, a Potent and Selective Oral Inhibitor of PI3K and mTOR Kinases with Antitumor Activity
    • Yuan J, Mehta PP, Yin MJ, Sun S, Zou A, Chen J, et al. PF-04691502, a Potent and Selective Oral Inhibitor of PI3K and mTOR Kinases with Antitumor Activity. Mol Cancer Ther 2011;10:2189-99.
    • (2011) Mol Cancer Ther , vol.10 , pp. 2189-2199
    • Yuan, J.1    Mehta, P.P.2    Yin, M.J.3    Sun, S.4    Zou, A.5    Chen, J.6
  • 40
    • 84855451538 scopus 로고    scopus 로고
    • Antitumor activity of NVP-BKM120- A selective pan class 1 PI3 Kinase inhibitor showed differential forms of cell death based on P53 status of glioma cells
    • Koul D, Fu J, Shen R, Lafortune TA, Wang S, Tiao N, et al. Antitumor activity of NVP-BKM120- a selective pan class 1 PI3 Kinase inhibitor showed differential forms of cell death based on P53 status of glioma cells. Clin Cancer Res 2012;18:184-95.
    • (2012) Clin Cancer Res , vol.18 , pp. 184-195
    • Koul, D.1    Fu, J.2    Shen, R.3    Lafortune, T.A.4    Wang, S.5    Tiao, N.6
  • 41
    • 84863338519 scopus 로고    scopus 로고
    • PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations
    • Janku F, Wheler JJ, Westin SN, Moulder SL, Naing A, TsimberidouAM, et al. PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations. J Clin Oncol 2012;30:777-82.
    • (2012) J Clin Oncol , vol.30 , pp. 777-782
    • Janku, F.1    Wheler, J.J.2    Westin, S.N.3    Moulder, S.L.4    Naing, A.5    Tsimberidou, A.M.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.