메뉴 건너뛰기




Volumn 32, Issue 4, 2014, Pages 670-681

Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-Class I PI3K inhibitor, in patients with advanced solid tumors

Author keywords

BKM120; Buparlisib; Oncology; PI3K inhibitor; Solid tumors; Targeted therapy

Indexed keywords

AMINOPYRIDINE DERIVATIVE; MORPHOLINE DERIVATIVE; NVP-BKM120; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PIK3CA PROTEIN, HUMAN; PROTEIN KINASE INHIBITOR; PTEN PROTEIN, HUMAN; TUMOR MARKER;

EID: 84904555503     PISSN: 01676997     EISSN: 15730646     Source Type: Journal    
DOI: 10.1007/s10637-014-0082-9     Document Type: Article
Times cited : (166)

References (45)
  • 1
    • 68249093818 scopus 로고    scopus 로고
    • Targeting the phosphoinositide 3-kinase pathway in cancer
    • Liu P, Cheng H, Roberts TM, Zhao JJ (2009) Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov 8(8):627-644
    • (2009) Nat Rev Drug Discov , vol.8 , Issue.8 , pp. 627-644
    • Liu, P.1    Cheng, H.2    Roberts, T.M.3    Zhao, J.J.4
  • 2
    • 65349155706 scopus 로고    scopus 로고
    • Induction of Akt activity by chemotherapy confers acquired resistance
    • Huang WC, Hung MC (2009) Induction of Akt activity by chemotherapy confers acquired resistance. J Formos Med Assoc 108(3):180-194
    • (2009) J Formos Med Assoc , vol.108 , Issue.3 , pp. 180-194
    • Huang, W.C.1    Hung, M.C.2
  • 3
    • 78649701154 scopus 로고    scopus 로고
    • Evolving strategies for overcoming resistance to HER2-directed therapy: Targeting the PI3K/Akt/mTOR pathway
    • Nahta R, O'Regan RM (2010) Evolving strategies for overcoming resistance to HER2-directed therapy: targeting the PI3K/Akt/mTOR pathway. Clin Breast Cancer 10(Suppl 3):S72-S78
    • (2010) Clin Breast Cancer , vol.10 , Issue.SUPPL. 3
    • Nahta, R.1    O'Regan, R.M.2
  • 4
    • 81755162797 scopus 로고    scopus 로고
    • Phosphatidylinositol 3-kinase and antiestrogen resistance in breast cancer
    • Miller TW, Balko JM, Arteaga CL (2011) Phosphatidylinositol 3-kinase and antiestrogen resistance in breast cancer. J Clin Oncol 29(33):4452-4461
    • (2011) J Clin Oncol , vol.29 , Issue.33 , pp. 4452-4461
    • Miller, T.W.1    Balko, J.M.2    Arteaga, C.L.3
  • 6
    • 77949881462 scopus 로고    scopus 로고
    • The PI3K pathway as drug target in human cancer
    • Courtney KD, Corcoran RB, Engelman JA (2010) The PI3K pathway as drug target in human cancer. J Clin Oncol 28(6):1075-1083
    • (2010) J Clin Oncol , vol.28 , Issue.6 , pp. 1075-1083
    • Courtney, K.D.1    Corcoran, R.B.2    Engelman, J.A.3
  • 7
    • 54549108740 scopus 로고    scopus 로고
    • Comprehensive genomic characterization defines human glioblastoma genes and core pathways
    • The Cancer Genome Atlas Research Network
    • The Cancer Genome Atlas Research Network (2008) Comprehensive genomic characterization defines human glioblastoma genes and core pathways. Nature 455(7216):1061-1068
    • (2008) Nature , vol.455 , Issue.7216 , pp. 1061-1068
  • 8
    • 84866894408 scopus 로고    scopus 로고
    • Comprehensive genomic characterization of squamous cell lung cancers
    • Cancer Genome Atlas Research Network
    • Cancer Genome Atlas Research Network, Hammerman PS, Hayes DN, Wilkerson MD, Schultz N, Bose R et al (2012) Comprehensive genomic characterization of squamous cell lung cancers. Nature 489(7417):519-525
    • (2012) Nature , vol.489 , Issue.7417 , pp. 519-525
    • Hammerman, P.S.1    Hayes, D.N.2    Wilkerson, M.D.3    Schultz, N.4    Bose, R.5
  • 9
    • 84877028141 scopus 로고    scopus 로고
    • Comprehensive molecular portraits of human breast tumours
    • Cancer Genome Atlas Network
    • Cancer Genome Atlas Network (2012) Comprehensive molecular portraits of human breast tumours. Nature 490(7418):61-70
    • (2012) Nature , vol.490 , Issue.7418 , pp. 61-70
  • 10
    • 84856826293 scopus 로고    scopus 로고
    • Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor
    • Maira SM, Pecchi S, Huang A, Burger M, Knapp M, Sterker D et al (2012) Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther 11(2):317-328
    • (2012) Mol Cancer Ther , vol.11 , Issue.2 , pp. 317-328
    • Maira, S.M.1    Pecchi, S.2    Huang, A.3    Burger, M.4    Knapp, M.5    Sterker, D.6
  • 12
    • 84923058135 scopus 로고    scopus 로고
    • NVP-BKM120, a pan class I PI3K inhibitor impairs microvascular permeability and tumor growth as detected by DCEMRI and IFP measurements via radio-telemetry: Comparison with NVP-BEZ235
    • abstract 4472
    • Schnell CR, Arnal S, Becquet M, Allegrini P, Voliva C, Cozens R et al (2010) NVP-BKM120, a pan class I PI3K inhibitor impairs microvascular permeability and tumor growth as detected by DCEMRI and IFP measurements via radio-telemetry: comparison with NVP-BEZ235. American Association for Cancer Research Congress. [abstract 4472]
    • (2010) American Association for Cancer Research Congress
    • Schnell, C.R.1    Arnal, S.2    Becquet, M.3    Allegrini, P.4    Voliva, C.5    Cozens, R.6
  • 13
    • 85081454799 scopus 로고    scopus 로고
    • NVP-BKM120, a novel inhibitor of phosphoinosotide 3- kinase in phase I/II clinical trials, shows significant antitumor activity in xenograft and primary tumor models
    • abstract
    • Maira M, Menezes D, Pecchi S, Shoemaker K, Burger M, Schnell C et al (2010) NVP-BKM120, a novel inhibitor of phosphoinosotide 3- kinase in phase I/II clinical trials, shows significant antitumor activity in xenograft and primary tumor models. AACR Meeting Abstracts. 4497 (abstract)
    • (2010) AACR Meeting Abstracts , vol.4497
    • Maira, M.1    Menezes, D.2    Pecchi, S.3    Shoemaker, K.4    Burger, M.5    Schnell, C.6
  • 14
    • 84901982336 scopus 로고    scopus 로고
    • Biological characterization of NVP-BKM120, a novel inhibitor of phosphoinosotide 3-kinase in phase I/II clinical trials
    • abstract
    • Voliva CF, Pecchi S, Burger M, Nagel T, Schnell C, Fritsch C et al (2010) Biological characterization of NVP-BKM120, a novel inhibitor of phosphoinosotide 3-kinase in phase I/II clinical trials. AACR Meeting Abstracts 4498 (abstract)
    • (2010) AACR Meeting Abstracts , vol.4498
    • Voliva, C.F.1    Pecchi, S.2    Burger, M.3    Nagel, T.4    Schnell, C.5    Fritsch, C.6
  • 15
    • 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 (2012) Phase I, dose-escalation study of BKM120, an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. J Clin Oncol 30(3):282-290
    • (2012) J Clin Oncol , vol.30 , Issue.3 , pp. 282-290
    • Bendell, J.C.1    Rodon, J.2    Burris, H.A.3    De Jonge, M.4    Verweij, J.5    Birle, D.6
  • 16
    • 33646815612 scopus 로고    scopus 로고
    • A brief measure for assessing generalized anxiety disorder: The GAD-7
    • DOI 10.1001/archinte.166.10.1092
    • Spitzer RL, Kroenke K, Williams JB, Lowe B (2006) A brief measure for assessing generalized anxiety disorder: the GAD-7. Arch Intern Med 166(10):1092-1097 (Pubitemid 43765180)
    • (2006) Archives of Internal Medicine , vol.166 , Issue.10 , pp. 1092-1097
    • Spitzer, R.L.1    Kroenke, K.2    Williams, J.B.W.3    Lowe, B.4
  • 17
    • 0034853189 scopus 로고    scopus 로고
    • The PHQ-9: Validity of a brief depression severity measure
    • DOI 10.1046/j.1525-1497.2001.016009606.x
    • Kroenke K, Spitzer RL, Williams JB (2001) The PHQ-9: validity of a brief depression severity measure. J Gen Intern Med 16(9):606-613 (Pubitemid 32823891)
    • (2001) Journal of General Internal Medicine , vol.16 , Issue.9 , pp. 606-613
    • Kroenke, K.1    Spitzer, R.L.2    Williams, J.B.W.3
  • 18
    • 0031920799 scopus 로고    scopus 로고
    • Cancer phase I clinical trials: Efficient dose escalation with overdose control
    • DOI 10.1002/(SICI)1097-0258(19980530)17:10<1103::A
    • Babb J, Rogatko A, Zacks S (1998) Cancer Phase I clinical trials: efficient dose escalation with overdose control. Stat Med 17(10):1103-1120 (Pubitemid 28221028)
    • (1998) Statistics in Medicine , vol.17 , Issue.10 , pp. 1103-1120
    • Babb, J.1    Rogatko, A.2    Zacks, S.3
  • 19
    • 0032757213 scopus 로고    scopus 로고
    • 18F]- fluorodeoxyglucose and positron emission tomography: Review and 1999 EORTC recommendations
    • DOI 10.1016/S0959-8049(99)00229-4, PII S0959804999002294
    • Young H, Baum R, Cremerius U, Herholz K, Hoekstra O, Lammertsma AA et al (1999) Measurement of clinical and subclinical tumour response using [18F]-fluorodeoxyglucose and positron emission tomography: review and 1999 EORTC recommendations. european organization for research and treatment of cancer (EORTC) PET study group. Eur J Cancer 35(13):1773-1782 (Pubitemid 29512308)
    • (1999) European Journal of Cancer , vol.35 , Issue.13 , pp. 1773-1782
    • Young, H.1    Baum, R.2    Cremerius, U.3    Herholz, K.4    Hoekstra, O.5    Lammertsma, A.A.6    Pruim, J.7    Price, P.8
  • 21
    • 33244464562 scopus 로고    scopus 로고
    • Critical nodes in signalling pathways: Insights into insulin action
    • DOI 10.1038/nrm1837, PII NRM1837
    • Taniguchi CM, Emanuelli B, Kahn CR (2006) Critical nodes in signalling pathways: insights into insulin action. Nat Rev Mol Cell Biol 7(2):85-96 (Pubitemid 43278292)
    • (2006) Nature Reviews Molecular Cell Biology , vol.7 , Issue.2 , pp. 85-96
    • Taniguchi, C.M.1    Emanuelli, B.2    Kahn, C.R.3
  • 22
    • 33646383684 scopus 로고    scopus 로고
    • A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling
    • Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O et al (2006) A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell 125(4):733-747
    • (2006) Cell , vol.125 , Issue.4 , pp. 733-747
    • Knight, Z.A.1    Gonzalez, B.2    Feldman, M.E.3    Zunder, E.R.4    Goldenberg, D.D.5    Williams, O.6
  • 23
    • 77956572401 scopus 로고    scopus 로고
    • A first-in-human phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors
    • Von Hoff DD, LoRusso P, Tibes R, Shapiro G, Weiss GJ, Ware JA et al (2010) A first-in-human phase I study to evaluate the pan-PI3K inhibitor GDC-0941 administered QD or BID in patients with advanced solid tumors. ASCO Meeting Abstracts 28(15-suppl):2541
    • (2010) ASCO Meeting Abstracts , vol.28 , Issue.15 SUPPL. , pp. 2541
    • Von Hoff, D.D.1    LoRusso, P.2    Tibes, R.3    Shapiro, G.4    Weiss, G.J.5    Ware, J.A.6
  • 24
    • 84856988295 scopus 로고    scopus 로고
    • A dose-escalation study with the novel formulation of the oral pan-class I PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet, in patients with advanced solid tumors
    • Peyton JD, Rodon Ahnert J, Burris H, Britten C, Chen LC, Tabernero J et al (2011) A dose-escalation study with the novel formulation of the oral pan-class I PI3K inhibitor BEZ235, solid dispersion system (SDS) sachet, in patients with advanced solid tumors. ASCO Meeting Abstracts 29(15-suppl):3066
    • (2011) ASCO Meeting Abstracts , vol.29 , Issue.15 SUPPL. , pp. 3066
    • Peyton, J.D.1    Rodon Ahnert, J.2    Burris, H.3    Britten, C.4    Chen, L.C.5    Tabernero, J.6
  • 25
    • 80054740282 scopus 로고    scopus 로고
    • A first-in-human phase I study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QD in patients with advanced solid tumors
    • abstract 3020 (poster presentation)
    • Wagner AJ, Bendell JC, Dolly S, Morgan JA, Ware JA, Fredrickson J et al (2011) A first-in-human phase I study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QD in patients with advanced solid tumors. J Clin Oncol 29(suppl):abstract 3020 (poster presentation)
    • (2011) J Clin Oncol , vol.29 , Issue.SUPPL.
    • Wagner, A.J.1    Bendell, J.C.2    Dolly, S.3    Morgan, J.A.4    Ware, J.A.5    Fredrickson, J.6
  • 26
    • 80054748915 scopus 로고    scopus 로고
    • Phase I first-in-human study of the PI3 kinase inhibitor GSK2126458 (GSK458) in patients with advanced solid tumors (study P3K112826)
    • Munster PN, van der Noll R, Voest EE, Dees EC, Tan AR, Specht JM et al (2011) Phase I first-in-human study of the PI3 kinase inhibitor GSK2126458 (GSK458) in patients with advanced solid tumors (study P3K112826). ASCO Meeting Abstracts 29(15-suppl):3018
    • (2011) ASCO Meeting Abstracts , vol.29 , Issue.15 SUPPL. , pp. 3018
    • Munster, P.N.1    Van Der Noll, R.2    Voest, E.E.3    Dees, E.C.4    Tan, A.R.5    Specht, J.M.6
  • 27
    • 84862649113 scopus 로고    scopus 로고
    • Multiorgan metastasis of human HER-2(+) breast cancer in Rag2(-/-);Il2rg(-/-) mice and treatment with PI3K inhibitor
    • Nanni P, Nicoletti G, Palladini A, Croci S, Murgo A, Ianzano ML et al (2012) Multiorgan metastasis of human HER-2(+) breast cancer in Rag2(-/-);Il2rg(-/-) mice and treatment with PI3K inhibitor. PLoS One 7(6):e39626
    • (2012) PLoS One , vol.7 , Issue.6
    • Nanni, P.1    Nicoletti, G.2    Palladini, A.3    Croci, S.4    Murgo, A.5    Ianzano, M.L.6
  • 28
    • 57349164057 scopus 로고    scopus 로고
    • Hyperactivity, memory deficit and anxiety-related behaviors in mice lacking the p85alpha subunit of phosphoinositide-3 kinase
    • Tohda C, Nakanishi R, Kadowaki M (2009) Hyperactivity, memory deficit and anxiety-related behaviors in mice lacking the p85alpha subunit of phosphoinositide-3 kinase. Brain Dev 31(1):69-74
    • (2009) Brain Dev , vol.31 , Issue.1 , pp. 69-74
    • Tohda, C.1    Nakanishi, R.2    Kadowaki, M.3
  • 29
    • 57649192506 scopus 로고    scopus 로고
    • Phosphatidylinositide dependent kinase deficiency increases anxiety and decreases GABA and serotonin abundance in the amygdala
    • Ackermann TF, Hortnagl H, Wolfer DP, Colacicco G, Sohr R, Lang F et al (2008) Phosphatidylinositide dependent kinase deficiency increases anxiety and decreases GABA and serotonin abundance in the amygdala. Cell Physiol Biochem 22(5-6):735-744
    • (2008) Cell Physiol Biochem , vol.22 , Issue.5-6 , pp. 735-744
    • Ackermann, T.F.1    Hortnagl, H.2    Wolfer, D.P.3    Colacicco, G.4    Sohr, R.5    Lang, F.6
  • 30
    • 32644480629 scopus 로고    scopus 로고
    • The role of the phosphatidylinositide 3-kinaseprotein kinase B pathway in schizophrenia
    • Kalkman HO (2006) The role of the phosphatidylinositide 3-kinaseprotein kinase B pathway in schizophrenia. Pharmacol Ther 110(1):117-134
    • (2006) Pharmacol Ther , vol.110 , Issue.1 , pp. 117-134
    • Kalkman, H.O.1
  • 34
    • 79956021682 scopus 로고    scopus 로고
    • Changes in 18F-fluorodeoxyglucose and 18F-fluorodeoxythymidine positron emission tomography imaging in patients with non-small cell lung cancer treated with erlotinib
    • Mileshkin L, Hicks RJ, Hughes BG, Mitchell PL, Charu V, Gitlitz BJ et al (2011) Changes in 18F-fluorodeoxyglucose and 18F-fluorodeoxythymidine positron emission tomography imaging in patients with non-small cell lung cancer treated with erlotinib. Clin Cancer Res 17(10):3304-3315
    • (2011) Clin Cancer Res , vol.17 , Issue.10 , pp. 3304-3315
    • Mileshkin, L.1    Hicks, R.J.2    Hughes, B.G.3    Mitchell, P.L.4    Charu, V.5    Gitlitz, B.J.6
  • 35
    • 84863746052 scopus 로고    scopus 로고
    • Marked, homogeneous, and early [18F]fluorodeoxyglucose-positron emission tomography responses to vemurafenib in BRAF-mutant advanced melanoma
    • McArthur GA, Puzanov I, Amaravadi R, Ribas A, Chapman P, Kim KB et al (2012) Marked, homogeneous, and early [18F]fluorodeoxyglucose-positron emission tomography responses to vemurafenib in BRAF-mutant advanced melanoma. J Clin Oncol 30(14):1628-1634
    • (2012) J Clin Oncol , vol.30 , Issue.14 , pp. 1628-1634
    • McArthur, G.A.1    Puzanov, I.2    Amaravadi, R.3    Ribas, A.4    Chapman, P.5    Kim, K.B.6
  • 36
    • 84866709651 scopus 로고    scopus 로고
    • Combining a PI3K inhibitor with a PARP inhibitor provides an effective therapy for a mouse model of BRCA1-related breast cancer
    • Juvekar A, Burga LN, Hu H, Lunsford EP, Ibrahim YH, Balmana J et al (2012) Combining a PI3K inhibitor with a PARP inhibitor provides an effective therapy for a mouse model of BRCA1-related breast cancer. Cancer Discov 2(11):1048-1063
    • (2012) Cancer Discov , vol.2 , Issue.11 , pp. 1048-1063
    • Juvekar, A.1    Burga, L.N.2    Hu, H.3    Lunsford, E.P.4    Ibrahim, Y.H.5    Balmana, J.6
  • 37
    • 84866031870 scopus 로고    scopus 로고
    • 3D tumour spheroids as a model to assess the suitability of [18F]FDG-PETas an early indicator of response to PI3K inhibition
    • Kelly CJ, Hussien K, Muschel RJ (2012) 3D tumour spheroids as a model to assess the suitability of [18F]FDG-PETas an early indicator of response to PI3K inhibition. Nucl Med Biol 39(7):986-992
    • (2012) Nucl Med Biol , vol.39 , Issue.7 , pp. 986-992
    • Kelly, C.J.1    Hussien, K.2    Muschel, R.J.3
  • 38
    • 77955288855 scopus 로고    scopus 로고
    • Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus
    • Di Nicolantonio F, Arena S, Tabernero J, Grosso S, Molinari F, Macarulla T et al (2010) Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus. J Clin Invest 120(8):2858-2866
    • (2010) J Clin Invest , vol.120 , Issue.8 , pp. 2858-2866
    • Di Nicolantonio, F.1    Arena, S.2    Tabernero, J.3    Grosso, S.4    Molinari, F.5    Macarulla, T.6
  • 39
    • 84892703881 scopus 로고    scopus 로고
    • Direct inhibition of PI3K in combination with dual HER2 inhibitors is required for optimal antitumor activity in HER2+ breast cancer cells
    • Rexer BN, Chanthaphaychith S, Dahlman KB, Arteaga CL (2014) Direct inhibition of PI3K in combination with dual HER2 inhibitors is required for optimal antitumor activity in HER2+ breast cancer cells. Breast Cancer Res 16(1):R9
    • (2014) Breast Cancer Res , vol.16 , Issue.1
    • Rexer, B.N.1    Chanthaphaychith, S.2    Dahlman, K.B.3    Arteaga, C.L.4
  • 42
    • 49649087385 scopus 로고    scopus 로고
    • Essential roles of PI(3)K-p110beta in cell growth, metabolism and tumorigenesis
    • Jia S, Liu Z, Zhang S, Liu P, Zhang L, Lee SH et al (2008) Essential roles of PI(3)K-p110beta in cell growth, metabolism and tumorigenesis. Nature 454(7205):776-779
    • (2008) Nature , vol.454 , Issue.7205 , pp. 776-779
    • Jia, S.1    Liu, Z.2    Zhang, S.3    Liu, P.4    Zhang, L.5    Lee, S.H.6
  • 44
    • 84858842073 scopus 로고    scopus 로고
    • Tumor genetic testing for patient selection in phase I clinical trials: The case of PI3K inhibitors
    • Juric D, Baselga J (2012) Tumor genetic testing for patient selection in phase I clinical trials: the case of PI3K inhibitors. J Clin Oncol 30(8):765-766
    • (2012) J Clin Oncol , vol.30 , Issue.8 , pp. 765-766
    • Juric, D.1    Baselga, J.2
  • 45
    • 67749122122 scopus 로고    scopus 로고
    • Targeting PI3K signalling in cancer: Opportunities, challenges and limitations
    • Engelman JA (2009) Targeting PI3K signalling in cancer: opportunities, challenges and limitations. Nat Rev Cancer 9(8):550-562
    • (2009) Nat Rev Cancer , vol.9 , Issue.8 , pp. 550-562
    • Engelman, J.A.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.