-
1
-
-
79952114854
-
PI3K: from the bench to the clinic and back
-
Vanhaesebroeck, B., Vogt, P.K., Rommel, C., PI3K: from the bench to the clinic and back. Curr Top Microbiol Immunol 347 (2010), 1–19.
-
(2010)
Curr Top Microbiol Immunol
, vol.347
, pp. 1-19
-
-
Vanhaesebroeck, B.1
Vogt, P.K.2
Rommel, C.3
-
2
-
-
68249093818
-
Targeting the phosphoinositide 3-kinase pathway in cancer
-
Liu, P., Cheng, H., Roberts, T.M., Zhao, J.J., Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov 8 (2009), 627–644.
-
(2009)
Nat Rev Drug Discov
, vol.8
, pp. 627-644
-
-
Liu, P.1
Cheng, H.2
Roberts, T.M.3
Zhao, J.J.4
-
3
-
-
33746257209
-
The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism
-
Engelman, J.A., Luo, J., Cantley, L.C., The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet 7 (2006), 606–619.
-
(2006)
Nat Rev Genet
, vol.7
, pp. 606-619
-
-
Engelman, J.A.1
Luo, J.2
Cantley, L.C.3
-
4
-
-
84876731682
-
PI3K pathway inhibitors: better not left alone
-
Markman, B., Tao, J.J., Scaltriti, M., PI3K pathway inhibitors: better not left alone. Curr Pharm Des 19 (2013), 895–906.
-
(2013)
Curr Pharm Des
, vol.19
, pp. 895-906
-
-
Markman, B.1
Tao, J.J.2
Scaltriti, M.3
-
5
-
-
84899850988
-
Picking the point of inhibition: a comparative review of PI3K/AKT/mTOR pathway inhibitors
-
Dienstmann, R., Rodon, J., Serra, V., Tabernero, J., Picking the point of inhibition: a comparative review of PI3K/AKT/mTOR pathway inhibitors. Mol Cancer Ther 13 (2014), 1021–1031.
-
(2014)
Mol Cancer Ther
, vol.13
, pp. 1021-1031
-
-
Dienstmann, R.1
Rodon, J.2
Serra, V.3
Tabernero, J.4
-
6
-
-
63749106157
-
Should individual PI3 kinase isoforms be targeted in cancer?
-
Jia, S., Roberts, T.M., Zhao, J.J., Should individual PI3 kinase isoforms be targeted in cancer?. Curr Opin Cell Biol 21 (2009), 199–208.
-
(2009)
Curr Opin Cell Biol
, vol.21
, pp. 199-208
-
-
Jia, S.1
Roberts, T.M.2
Zhao, J.J.3
-
7
-
-
0027432424
-
Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses
-
Arcaro, A., Wymann, M.P., Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses. Biochem J 296:Pt 2 (1993), 297–301.
-
(1993)
Biochem J
, vol.296
, pp. 297-301
-
-
Arcaro, A.1
Wymann, M.P.2
-
8
-
-
0028170210
-
A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002)
-
Vlahos, C.J., Matter, W.F., Hui, K.Y., Brown, R.F., A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002). J Biol Chem 269 (1994), 5241–5248.
-
(1994)
J Biol Chem
, vol.269
, pp. 5241-5248
-
-
Vlahos, C.J.1
Matter, W.F.2
Hui, K.Y.3
Brown, R.F.4
-
9
-
-
84887942578
-
Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics
-
Akinleye, A., Avvaru, P., Furqan, M., Song, Y., Liu, D., Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics. J Hematol Oncol, 6, 2013, 88.
-
(2013)
J Hematol Oncol
, vol.6
, pp. 88
-
-
Akinleye, A.1
Avvaru, P.2
Furqan, M.3
Song, Y.4
Liu, D.5
-
10
-
-
85026544201
-
-
Afinitor (everolimus) [package insert]. Novartis Pharmaceuticals Corporation. East Hanover, NJ.
-
Afinitor (everolimus) [package insert]. Novartis Pharmaceuticals Corporation. East Hanover, NJ; 2016.
-
(2016)
-
-
-
11
-
-
85026555430
-
-
Torisel (temsirolimus) [package insert]. Philadelphia, PA 1: Wyeth Pharmaceuticals Inc., Pfizer Inc.; 2016.
-
Torisel (temsirolimus) [package insert]. Philadelphia, PA 19101: Wyeth Pharmaceuticals Inc., Pfizer Inc.; 2016.
-
(1910)
-
-
-
12
-
-
77951729433
-
FDA approval summary: temsirolimus as treatment for advanced renal cell carcinoma
-
Kwitkowski, V.E., Prowell, T.M., Ibrahim, A., Farrell, A.T., Justice, R., Mitchell, S.S., et al. FDA approval summary: temsirolimus as treatment for advanced renal cell carcinoma. Oncologist 15 (2010), 428–435.
-
(2010)
Oncologist
, vol.15
, pp. 428-435
-
-
Kwitkowski, V.E.1
Prowell, T.M.2
Ibrahim, A.3
Farrell, A.T.4
Justice, R.5
Mitchell, S.S.6
-
13
-
-
84863078767
-
Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer
-
Baselga, J., Campone, M., Piccart, M., Burris, H.A. 3rd, Rugo, H.S., Sahmoud, T., et al. Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer. N Engl J Med 366 (2012), 520–529.
-
(2012)
N Engl J Med
, vol.366
, pp. 520-529
-
-
Baselga, J.1
Campone, M.2
Piccart, M.3
Burris, H.A.4
Rugo, H.S.5
Sahmoud, T.6
-
14
-
-
84879373437
-
Bringing target-matched PI3King from the bench to the clinic
-
Janku, F., Bringing target-matched PI3King from the bench to the clinic. Cell Cycle 12 (2013), 1817–1818.
-
(2013)
Cell Cycle
, vol.12
, pp. 1817-1818
-
-
Janku, F.1
-
15
-
-
84955501929
-
Identification of variant-specific functions of PIK3CA by rapid phenotyping of rare mutations
-
Dogruluk, T., Tsang, Y.H., Espitia, M., Chen, F., Chen, T., Chong, Z., et al. Identification of variant-specific functions of PIK3CA by rapid phenotyping of rare mutations. Cancer Res 75 (2015), 5341–5354.
-
(2015)
Cancer Res
, vol.75
, pp. 5341-5354
-
-
Dogruluk, T.1
Tsang, Y.H.2
Espitia, M.3
Chen, F.4
Chen, T.5
Chong, Z.6
-
16
-
-
84895906492
-
Assessing PIK3CA and PTEN in early-phase trials with PI3K/AKT/mTOR inhibitors
-
Janku, F., Hong, D.S., Fu, S., Piha-Paul, S.A., Naing, A., Falchook, G.S., et al. Assessing PIK3CA and PTEN in early-phase trials with PI3K/AKT/mTOR inhibitors. Cell Rep 6 (2014), 377–387.
-
(2014)
Cell Rep
, vol.6
, pp. 377-387
-
-
Janku, F.1
Hong, D.S.2
Fu, S.3
Piha-Paul, S.A.4
Naing, A.5
Falchook, G.S.6
-
17
-
-
85026549207
-
Targeting PI3K overcomes in vivo resistance to everolimus in estrogen receptor (ER+) breast cancer
-
O'Brien, N., Tong, L., Ayala, R., Issakhanian, S., McDonald, K., Hurvitz, S., et al. Targeting PI3K overcomes in vivo resistance to everolimus in estrogen receptor (ER+) breast cancer. Cancer Res, 73(suppl; abstr PD1-5), 2013.
-
(2013)
Cancer Res
, vol.73
-
-
O'Brien, N.1
Tong, L.2
Ayala, R.3
Issakhanian, S.4
McDonald, K.5
Hurvitz, S.6
-
18
-
-
84856826293
-
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-Kinase inhibitor
-
Maira, S.M., Pecchi, S., Huang, A., Burger, M., Knapp, M., Sterker, D., et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-Kinase inhibitor. Mol Cancer Ther 11 (2012), 317–328.
-
(2012)
Mol Cancer Ther
, vol.11
, pp. 317-328
-
-
Maira, S.M.1
Pecchi, S.2
Huang, A.3
Burger, M.4
Knapp, M.5
Sterker, D.6
-
19
-
-
84904555503
-
Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors
-
Rodon, J., Brana, I., Siu, L.L., De Jonge, M.J., Homji, N., Mills, D., et al. Phase I dose-escalation and -expansion study of buparlisib (BKM120), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Invest New Drugs 32 (2014), 670–681.
-
(2014)
Invest New Drugs
, vol.32
, pp. 670-681
-
-
Rodon, J.1
Brana, I.2
Siu, L.L.3
De Jonge, M.J.4
Homji, N.5
Mills, D.6
-
20
-
-
85026517287
-
-
NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines). Breast Cancer. Version 2.
-
National Comprehensive Cancer Network. NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines). Breast Cancer. Version 2; 2016.
-
(2016)
-
-
-
21
-
-
84901986884
-
Targeting the PI3K/AKT/mTOR pathway in estrogen receptor-positive breast cancer
-
Ciruelos Gil, E.M., Targeting the PI3K/AKT/mTOR pathway in estrogen receptor-positive breast cancer. Cancer Treat Rev 40 (2014), 862–871.
-
(2014)
Cancer Treat Rev
, vol.40
, pp. 862-871
-
-
Ciruelos Gil, E.M.1
-
22
-
-
84964318224
-
A phase I trial of BKM120 (buparlisib) in combination with fulvestrant in postmenopausal women with estrogen receptor-positive metastatic breast cancer
-
Ma, C.X., Luo, J., Naughton, M., Ademuyiwa, F., Suresh, R., Griffith, M., et al. A phase I trial of BKM120 (buparlisib) in combination with fulvestrant in postmenopausal women with estrogen receptor-positive metastatic breast cancer. Clin Cancer Res 22 (2016), 1583–1591.
-
(2016)
Clin Cancer Res
, vol.22
, pp. 1583-1591
-
-
Ma, C.X.1
Luo, J.2
Naughton, M.3
Ademuyiwa, F.4
Suresh, R.5
Griffith, M.6
-
23
-
-
85020030586
-
Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial
-
Baselga, J., Im, S.A., Iwata, H., Cortes, J., De Laurentiis, M., Jiang, Z., et al. Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol 18 (2017), 904–916.
-
(2017)
Lancet Oncol
, vol.18
, pp. 904-916
-
-
Baselga, J.1
Im, S.A.2
Iwata, H.3
Cortes, J.4
De Laurentiis, M.5
Jiang, Z.6
-
24
-
-
85019827682
-
BELLE-3: a phase III study of buparlisib + fulvestrant in postmenopausal women with HR+, HER2-, aromatase inhibitor-treated, locally advanced or metastatic breast cancer, who progressed on or after mTOR inhibitor-based treatment
-
Di Leo, A., Keun, S., Ciruelos, E., Lønning, P., Janni, W., O'Regan, R., et al. BELLE-3: a phase III study of buparlisib + fulvestrant in postmenopausal women with HR+, HER2-, aromatase inhibitor-treated, locally advanced or metastatic breast cancer, who progressed on or after mTOR inhibitor-based treatment. Cancer Res, 77(suppl; abstr S4-07), 2017.
-
(2017)
Cancer Res
, vol.77
-
-
Di Leo, A.1
Keun, S.2
Ciruelos, E.3
Lønning, P.4
Janni, W.5
O'Regan, R.6
-
25
-
-
84904724740
-
Stand up to cancer phase Ib study of pan-phosphoinositide-3-kinase inhibitor buparlisib with letrozole in estrogen receptor-positive/human epidermal growth factor receptor 2-negative metastatic breast cancer
-
Mayer, I.A., Abramson, V.G., Isakoff, S.J., Forero, A., Balko, J.M., Kuba, M.G., et al. Stand up to cancer phase Ib study of pan-phosphoinositide-3-kinase inhibitor buparlisib with letrozole in estrogen receptor-positive/human epidermal growth factor receptor 2-negative metastatic breast cancer. J Clin Oncol 32 (2014), 1202–1209.
-
(2014)
J Clin Oncol
, vol.32
, pp. 1202-1209
-
-
Mayer, I.A.1
Abramson, V.G.2
Isakoff, S.J.3
Forero, A.4
Balko, J.M.5
Kuba, M.G.6
-
26
-
-
79952840115
-
Testing for HER2 in breast cancer: a continuing evolution
-
Shah, S., Chen, B., Testing for HER2 in breast cancer: a continuing evolution. Patholog Res Int, 2011, 2010, 903202.
-
(2010)
Patholog Res Int
, vol.2011
, pp. 903202
-
-
Shah, S.1
Chen, B.2
-
27
-
-
84856826293
-
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor
-
Maira, S.M., Pecchi, S., Huang, A., Burger, M., Knapp, M., Sterker, D., et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. Mol Cancer Ther 11 (2012), 317–328.
-
(2012)
Mol Cancer Ther
, vol.11
, pp. 317-328
-
-
Maira, S.M.1
Pecchi, S.2
Huang, A.3
Burger, M.4
Knapp, M.5
Sterker, D.6
-
28
-
-
84898730243
-
Phase Ib study of buparlisib plus trastuzumab in patients with HER2-positive advanced or metastatic breast cancer that has progressed on trastuzumab-based therapy
-
Saura, C., Bendell, J., Jerusalem, G., Su, S., Ru, Q., Buck, S., et al. Phase Ib study of buparlisib plus trastuzumab in patients with HER2-positive advanced or metastatic breast cancer that has progressed on trastuzumab-based therapy. Clin Cancer Res 20 (2014), 1935–1945.
-
(2014)
Clin Cancer Res
, vol.20
, pp. 1935-1945
-
-
Saura, C.1
Bendell, J.2
Jerusalem, G.3
Su, S.4
Ru, Q.5
Buck, S.6
-
29
-
-
84862649113
-
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, M.L., et al. Multiorgan metastasis of human HER-2 + breast cancer in Rag2−/−;Il2rg−/− mice and treatment with PI3K inhibitor. PLoS ONE, 7, 2012, e39626.
-
(2012)
PLoS ONE
, vol.7
, pp. e39626
-
-
Nanni, P.1
Nicoletti, G.2
Palladini, A.3
Croci, S.4
Murgo, A.5
Ianzano, M.L.6
-
30
-
-
84879474924
-
Preclinical and preliminary clinical activity of NVP-BKM120, an oral pan-class I PI3K inhibitor, in the brain
-
Maira, M., Schnell, C., Lollini, P., Chouaid, C., Schmid, P., Nanni, P., et al. Preclinical and preliminary clinical activity of NVP-BKM120, an oral pan-class I PI3K inhibitor, in the brain. Ann Oncol, 23(suppl; abstr 1675P), 2012.
-
(2012)
Ann Oncol
, vol.23
-
-
Maira, M.1
Schnell, C.2
Lollini, P.3
Chouaid, C.4
Schmid, P.5
Nanni, P.6
-
31
-
-
57349194139
-
Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers
-
Engelman, J.A., Chen, L., Tan, X., Crosby, K., Guimaraes, A.R., Upadhyay, R., et al. Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nat Med 14 (2008), 1351–1356.
-
(2008)
Nat Med
, vol.14
, pp. 1351-1356
-
-
Engelman, J.A.1
Chen, L.2
Tan, X.3
Crosby, K.4
Guimaraes, A.R.5
Upadhyay, R.6
-
32
-
-
84857136594
-
Multi-level targeting of the phosphatidylinositol-3-kinase pathway in non-small cell lung cancer cells
-
Zito, C.R., Jilaveanu, L.B., Anagnostou, V., Rimm, D., Bepler, G., Maira, S.M., et al. Multi-level targeting of the phosphatidylinositol-3-kinase pathway in non-small cell lung cancer cells. PLoS ONE, 7, 2012, e31331.
-
(2012)
PLoS ONE
, vol.7
, pp. e31331
-
-
Zito, C.R.1
Jilaveanu, L.B.2
Anagnostou, V.3
Rimm, D.4
Bepler, G.5
Maira, S.M.6
-
33
-
-
77955092315
-
PTEN mutations and relationship to EGFR, ERBB2, KRAS, and TP53 mutations in non-small cell lung cancers
-
Jin, G., Kim, M.J., Jeon, H.S., Choi, J.E., Kim, D.S., Lee, E.B., et al. PTEN mutations and relationship to EGFR, ERBB2, KRAS, and TP53 mutations in non-small cell lung cancers. Lung Cancer 69 (2010), 279–283.
-
(2010)
Lung Cancer
, vol.69
, pp. 279-283
-
-
Jin, G.1
Kim, M.J.2
Jeon, H.S.3
Choi, J.E.4
Kim, D.S.5
Lee, E.B.6
-
34
-
-
84940105287
-
Safety and efficacy of buparlisib (BKM120) in patients with PI3K pathway-activated non-small cell lung cancer: Results from the phase II BASALT-1 study
-
Vansteenkiste, J.F., Canon, J.L., Braud, F.D., Grossi, F., De Pas, T., Gray, J.E., et al. Safety and efficacy of buparlisib (BKM120) in patients with PI3K pathway-activated non-small cell lung cancer: Results from the phase II BASALT-1 study. J Thorac Oncol 10 (2015), 1319–1327.
-
(2015)
J Thorac Oncol
, vol.10
, pp. 1319-1327
-
-
Vansteenkiste, J.F.1
Canon, J.L.2
Braud, F.D.3
Grossi, F.4
De Pas, T.5
Gray, J.E.6
-
35
-
-
84944238588
-
Current treatment options for recurrent or metastatic head and neck squamous cell carcinoma
-
Sacco, A.G., Cohen, E.E., Current treatment options for recurrent or metastatic head and neck squamous cell carcinoma. J Clin Oncol 33 (2015), 3305–3313.
-
(2015)
J Clin Oncol
, vol.33
, pp. 3305-3313
-
-
Sacco, A.G.1
Cohen, E.E.2
-
36
-
-
84855371890
-
Dual inhibition of the PI3K/mTOR pathway increases tumor radiosensitivity by normalizing tumor vasculature
-
Fokas, E., Im, J.H., Hill, S., Yameen, S., Stratford, M., Beech, J., et al. Dual inhibition of the PI3K/mTOR pathway increases tumor radiosensitivity by normalizing tumor vasculature. Cancer Res 72 (2012), 239–248.
-
(2012)
Cancer Res
, vol.72
, pp. 239-248
-
-
Fokas, E.1
Im, J.H.2
Hill, S.3
Yameen, S.4
Stratford, M.5
Beech, J.6
-
37
-
-
85010910535
-
Buparlisib and paclitaxel in patients with platinum-pretreated recurrent or metastatic squamous cell carcinoma of the head and neck (BERIL-1): a randomised, double-blind, placebo-controlled phase 2 trial
-
Soulieres, D., Faivre, S., Mesia, R., Remenar, E., Li, S.H., Karpenko, A., et al. Buparlisib and paclitaxel in patients with platinum-pretreated recurrent or metastatic squamous cell carcinoma of the head and neck (BERIL-1): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet Oncol 18 (2017), 323–335.
-
(2017)
Lancet Oncol
, vol.18
, pp. 323-335
-
-
Soulieres, D.1
Faivre, S.2
Mesia, R.3
Remenar, E.4
Li, S.H.5
Karpenko, A.6
-
38
-
-
85026536542
-
A pilot study of the pan-class I PI3K inhibitor buparlisib in combination with cetuximab in patients with recurrent/metastatic head and neck cancer
-
Brisson, R., Dekker, A., De Souza, J., Saloura, V., Vokes, E., Seiwert, T., A pilot study of the pan-class I PI3K inhibitor buparlisib in combination with cetuximab in patients with recurrent/metastatic head and neck cancer. J Clin Oncol, 35(suppl; abstr 6039), 2017.
-
(2017)
J Clin Oncol
, vol.35
-
-
Brisson, R.1
Dekker, A.2
De Souza, J.3
Saloura, V.4
Vokes, E.5
Seiwert, T.6
-
39
-
-
84878652051
-
PI3K and MEK inhibitor combinations: examining the evidence in selected tumor types
-
Britten, C.D., PI3K and MEK inhibitor combinations: examining the evidence in selected tumor types. Cancer Chemother Pharmacol 71 (2013), 1395–1409.
-
(2013)
Cancer Chemother Pharmacol
, vol.71
, pp. 1395-1409
-
-
Britten, C.D.1
-
40
-
-
78650026316
-
KRAS and BRAF: drug targets and predictive biomarkers
-
Vakiani, E., Solit, D.B., KRAS and BRAF: drug targets and predictive biomarkers. J Pathol 223 (2011), 219–229.
-
(2011)
J Pathol
, vol.223
, pp. 219-229
-
-
Vakiani, E.1
Solit, D.B.2
-
41
-
-
84871968444
-
PIK3CA mutation H1047R is associated with response to PI3K/AKT/mTOR signaling pathway inhibitors in early-phase clinical trials
-
Janku, F., Wheler, J.J., Naing, A., Falchook, G.S., Hong, D.S., Stepanek, V.M., et al. PIK3CA mutation H1047R is associated with response to PI3K/AKT/mTOR signaling pathway inhibitors in early-phase clinical trials. Cancer Res 73 (2013), 276–284.
-
(2013)
Cancer Res
, vol.73
, pp. 276-284
-
-
Janku, F.1
Wheler, J.J.2
Naing, A.3
Falchook, G.S.4
Hong, D.S.5
Stepanek, V.M.6
-
42
-
-
84863338519
-
PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations
-
Janku, F., Wheler, J.J., Westin, S.N., Moulder, S.L., Naing, A., Tsimberidou, A.M., et al. PI3K/AKT/mTOR inhibitors in patients with breast and gynecologic malignancies harboring PIK3CA mutations. J Clin Oncol 30 (2012), 777–782.
-
(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
-
43
-
-
84923182481
-
A phase Ib dose-escalation study of the oral pan-PI3K inhibitor buparlisib (BKM120) in combination with the oral MEK1/2 inhibitor trametinib (GSK1120212) in patients with selected advanced solid tumors
-
Bedard, P.L., Tabernero, J., Janku, F., Wainberg, Z.A., Paz-Ares, L., Vansteenkiste, J., et al. A phase Ib dose-escalation study of the oral pan-PI3K inhibitor buparlisib (BKM120) in combination with the oral MEK1/2 inhibitor trametinib (GSK1120212) in patients with selected advanced solid tumors. Clin Cancer Res 21 (2015), 730–738.
-
(2015)
Clin Cancer Res
, vol.21
, pp. 730-738
-
-
Bedard, P.L.1
Tabernero, J.2
Janku, F.3
Wainberg, Z.A.4
Paz-Ares, L.5
Vansteenkiste, J.6
-
44
-
-
52449106253
-
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin -4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
-
Folkes, A.J., Ahmadi, K., Alderton, W.K., Alix, S., Baker, S.J., Box, G., et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin -4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J Med Chem 51 (2008), 5522–5532.
-
(2008)
J Med Chem
, vol.51
, pp. 5522-5532
-
-
Folkes, A.J.1
Ahmadi, K.2
Alderton, W.K.3
Alix, S.4
Baker, S.J.5
Box, G.6
-
45
-
-
84920538174
-
First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors
-
Sarker, D., Ang, J.E., Baird, R., Kristeleit, R., Shah, K., Moreno, V., et al. First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors. Clin Cancer Res 21 (2015), 77–86.
-
(2015)
Clin Cancer Res
, vol.21
, pp. 77-86
-
-
Sarker, D.1
Ang, J.E.2
Baird, R.3
Kristeleit, R.4
Shah, K.5
Moreno, V.6
-
46
-
-
84964950086
-
Pictilisib for oestrogen receptor-positive, aromatase inhibitor-resistant, advanced or metastatic breast cancer (FERGI): a randomised, double-blind, placebo-controlled, phase 2 trial
-
Krop, I.E., Mayer, I.A., Ganju, V., Dickler, M., Johnston, S., Morales, S., et al. Pictilisib for oestrogen receptor-positive, aromatase inhibitor-resistant, advanced or metastatic breast cancer (FERGI): a randomised, double-blind, placebo-controlled, phase 2 trial. Lancet Oncol 17 (2016), 811–821.
-
(2016)
Lancet Oncol
, vol.17
, pp. 811-821
-
-
Krop, I.E.1
Mayer, I.A.2
Ganju, V.3
Dickler, M.4
Johnston, S.5
Morales, S.6
-
47
-
-
85016766194
-
Pictilisib plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study
-
Vuylsteke, P., Huizing, M., Petrakova, K., Roylance, R., Laing, R., Chan, S., et al. Pictilisib plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study. Ann Oncol 27 (2016), 2059–2066.
-
(2016)
Ann Oncol
, vol.27
, pp. 2059-2066
-
-
Vuylsteke, P.1
Huizing, M.2
Petrakova, K.3
Roylance, R.4
Laing, R.5
Chan, S.6
-
48
-
-
84864493357
-
A multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors
-
Hong, D.S., Bowles, D.W., Falchook, G.S., Messersmith, W.A., George, G.C., O'Bryant, C.L., et al. A multicenter phase I trial of PX-866, an oral irreversible phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors. Clin Cancer Res 18 (2012), 4173–4182.
-
(2012)
Clin Cancer Res
, vol.18
, pp. 4173-4182
-
-
Hong, D.S.1
Bowles, D.W.2
Falchook, G.S.3
Messersmith, W.A.4
George, G.C.5
O'Bryant, C.L.6
-
49
-
-
84883742774
-
A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours
-
Bowles, D.W., Ma, W.W., Senzer, N., Brahmer, J.R., Adjei, A.A., Davies, M., et al. A multicenter phase 1 study of PX-866 in combination with docetaxel in patients with advanced solid tumours. Br J Cancer 109 (2013), 1085–1092.
-
(2013)
Br J Cancer
, vol.109
, pp. 1085-1092
-
-
Bowles, D.W.1
Ma, W.W.2
Senzer, N.3
Brahmer, J.R.4
Adjei, A.A.5
Davies, M.6
-
50
-
-
84933178034
-
A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer
-
Jimeno, A., Bauman, J.E., Weissman, C., Adkins, D., Schnadig, I., Beauregard, P., et al. A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer. Oral Oncol 51 (2015), 383–388.
-
(2015)
Oral Oncol
, vol.51
, pp. 383-388
-
-
Jimeno, A.1
Bauman, J.E.2
Weissman, C.3
Adkins, D.4
Schnadig, I.5
Beauregard, P.6
-
51
-
-
84902489842
-
A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic non-small-cell lung cancer
-
Levy, B., Spira, A., Becker, D., Evans, T., Schnadig, I., Camidge, D.R., et al. A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic non-small-cell lung cancer. J Thorac Oncol 9 (2014), 1031–1035.
-
(2014)
J Thorac Oncol
, vol.9
, pp. 1031-1035
-
-
Levy, B.1
Spira, A.2
Becker, D.3
Evans, T.4
Schnadig, I.5
Camidge, D.R.6
-
52
-
-
52949127312
-
An integrated genomic analysis of human glioblastoma multiforme
-
Parsons, D.W., Jones, S., Zhang, X., Lin, J.C., Leary, R.J., Angenendt, P., et al. An integrated genomic analysis of human glioblastoma multiforme. Science 321 (2008), 1807–1812.
-
(2008)
Science
, vol.321
, pp. 1807-1812
-
-
Parsons, D.W.1
Jones, S.2
Zhang, X.3
Lin, J.C.4
Leary, R.J.5
Angenendt, P.6
-
53
-
-
84857204726
-
Abrogation of PIK3CA or PIK3R1 reduces proliferation, migration, and invasion in glioblastoma multiforme cells
-
Weber, G.L., Parat, M.O., Binder, Z.A., Gallia, G.L., Riggins, G.J., Abrogation of PIK3CA or PIK3R1 reduces proliferation, migration, and invasion in glioblastoma multiforme cells. Oncotarget 2 (2011), 833–849.
-
(2011)
Oncotarget
, vol.2
, pp. 833-849
-
-
Weber, G.L.1
Parat, M.O.2
Binder, Z.A.3
Gallia, G.L.4
Riggins, G.J.5
-
54
-
-
84940778136
-
Phase II study of PX-866 in recurrent glioblastoma
-
Pitz, M.W., Eisenhauer, E.A., MacNeil, M.V., Thiessen, B., Easaw, J.C., Macdonald, D.R., et al. Phase II study of PX-866 in recurrent glioblastoma. Neuro Oncol 17 (2015), 1270–1274.
-
(2015)
Neuro Oncol
, vol.17
, pp. 1270-1274
-
-
Pitz, M.W.1
Eisenhauer, E.A.2
MacNeil, M.V.3
Thiessen, B.4
Easaw, J.C.5
Macdonald, D.R.6
-
55
-
-
84892181757
-
Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors
-
Shapiro, G.I., Rodon, J., Bedell, C., Kwak, E.L., Baselga, J., Brana, I., et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of SAR245408 (XL147), an oral pan-class I PI3K inhibitor, in patients with advanced solid tumors. Clin Cancer Res 20 (2014), 233–245.
-
(2014)
Clin Cancer Res
, vol.20
, pp. 233-245
-
-
Shapiro, G.I.1
Rodon, J.2
Bedell, C.3
Kwak, E.L.4
Baselga, J.5
Brana, I.6
-
56
-
-
84925503345
-
Phase I/II study of pilaralisib (SAR245408) in combination with trastuzumab or trastuzumab plus paclitaxel in trastuzumab-refractory HER2-positive metastatic breast cancer
-
Tolaney, S., Burris, H., Gartner, E., Mayer, I.A., Saura, C., Maurer, M., et al. Phase I/II study of pilaralisib (SAR245408) in combination with trastuzumab or trastuzumab plus paclitaxel in trastuzumab-refractory HER2-positive metastatic breast cancer. Breast Cancer Res Treat 149 (2015), 151–161.
-
(2015)
Breast Cancer Res Treat
, vol.149
, pp. 151-161
-
-
Tolaney, S.1
Burris, H.2
Gartner, E.3
Mayer, I.A.4
Saura, C.5
Maurer, M.6
-
57
-
-
84868528894
-
The PI3K/AKT/mTOR pathway as a therapeutic target in endometrial cancer
-
Slomovitz, B.M., Coleman, R.L., The PI3K/AKT/mTOR pathway as a therapeutic target in endometrial cancer. Clin Cancer Res 18 (2012), 5856–5864.
-
(2012)
Clin Cancer Res
, vol.18
, pp. 5856-5864
-
-
Slomovitz, B.M.1
Coleman, R.L.2
-
58
-
-
84923108243
-
Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma
-
Matulonis, U., Vergote, I., Backes, F., Martin, L.P., McMeekin, S., Birrer, M., et al. Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma. Gynecol Oncol 136 (2015), 246–253.
-
(2015)
Gynecol Oncol
, vol.136
, pp. 246-253
-
-
Matulonis, U.1
Vergote, I.2
Backes, F.3
Martin, L.P.4
McMeekin, S.5
Birrer, M.6
-
59
-
-
84887453307
-
BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110alpha and p110delta activities in tumor cell lines and xenograft models
-
Liu, N., Rowley, B.R., Bull, C.O., Schneider, C., Haegebarth, A., Schatz, C.A., et al. BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110alpha and p110delta activities in tumor cell lines and xenograft models. Mol Cancer Ther 12 (2013), 2319–2330.
-
(2013)
Mol Cancer Ther
, vol.12
, pp. 2319-2330
-
-
Liu, N.1
Rowley, B.R.2
Bull, C.O.3
Schneider, C.4
Haegebarth, A.5
Schatz, C.A.6
-
60
-
-
85009147568
-
First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas
-
Patnaik, A., Appleman, L.J., Tolcher, A.W., Papadopoulos, K.P., Beeram, M., Rasco, D.W., et al. First-in-human phase I study of copanlisib (BAY 80-6946), an intravenous pan-class I phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors and non-Hodgkin's lymphomas. Ann Oncol 27 (2016), 1928–1940.
-
(2016)
Ann Oncol
, vol.27
, pp. 1928-1940
-
-
Patnaik, A.1
Appleman, L.J.2
Tolcher, A.W.3
Papadopoulos, K.P.4
Beeram, M.5
Rasco, D.W.6
-
61
-
-
51049109033
-
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
-
Maira, S.M., Stauffer, F., Brueggen, J., Furet, P., Schnell, C., Fritsch, C., et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther 7 (2008), 1851–1863.
-
(2008)
Mol Cancer Ther
, vol.7
, pp. 1851-1863
-
-
Maira, S.M.1
Stauffer, F.2
Brueggen, J.3
Furet, P.4
Schnell, C.5
Fritsch, C.6
-
62
-
-
53049087363
-
Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging
-
Schnell, C.R., Stauffer, F., Allegrini, P.R., O'Reilly, T., McSheehy, P.M., Dartois, C., et al. Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging. Cancer Res 68 (2008), 6598–6607.
-
(2008)
Cancer Res
, vol.68
, pp. 6598-6607
-
-
Schnell, C.R.1
Stauffer, F.2
Allegrini, P.R.3
O'Reilly, T.4
McSheehy, P.M.5
Dartois, C.6
-
63
-
-
51849111524
-
NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations
-
Serra, V., Markman, B., Scaltriti, M., Eichhorn, P.J., Valero, V., Guzman, M., et al. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations. Cancer Res 68 (2008), 8022–8030.
-
(2008)
Cancer Res
, vol.68
, pp. 8022-8030
-
-
Serra, V.1
Markman, B.2
Scaltriti, M.3
Eichhorn, P.J.4
Valero, V.5
Guzman, M.6
-
64
-
-
63749129788
-
PI3K and mTOR inhibitors: a new generation of targeted anticancer agents
-
Brachmann, S., Fritsch, C., Maira, S.M., Garcia-Echeverria, C., PI3K and mTOR inhibitors: a new generation of targeted anticancer agents. Curr Opin Cell Biol 21 (2009), 194–198.
-
(2009)
Curr Opin Cell Biol
, vol.21
, pp. 194-198
-
-
Brachmann, S.1
Fritsch, C.2
Maira, S.M.3
Garcia-Echeverria, C.4
-
65
-
-
84890125270
-
Dual PI3K/mTOR inhibitor NVP-BEZ235 sensitizes docetaxel in castration resistant prostate cancer
-
Yasumizu, Y., Miyajima, A., Kosaka, T., Miyazaki, Y., Kikuchi, E., Oya, M., Dual PI3K/mTOR inhibitor NVP-BEZ235 sensitizes docetaxel in castration resistant prostate cancer. J Urol 191 (2014), 227–234.
-
(2014)
J Urol
, vol.191
, pp. 227-234
-
-
Yasumizu, Y.1
Miyajima, A.2
Kosaka, T.3
Miyazaki, Y.4
Kikuchi, E.5
Oya, M.6
-
66
-
-
84869122157
-
RAD001 enhances the potency of BEZ235 to inhibit mTOR signaling and tumor growth
-
Nyfeler, B., Chen, Y., Li, X., Pinzon-Ortiz, M., Wang, Z., Reddy, A., et al. RAD001 enhances the potency of BEZ235 to inhibit mTOR signaling and tumor growth. PLoS ONE, 7, 2012, e48548.
-
(2012)
PLoS ONE
, vol.7
, pp. e48548
-
-
Nyfeler, B.1
Chen, Y.2
Li, X.3
Pinzon-Ortiz, M.4
Wang, Z.5
Reddy, A.6
-
67
-
-
84903840245
-
Targeting PI3K/mTOR overcomes resistance to HER2-targeted therapy independent of feedback activation of AKT
-
O'Brien, N.A., McDonald, K., Tong, L., von Euw, E., Kalous, O., Conklin, D., et al. Targeting PI3K/mTOR overcomes resistance to HER2-targeted therapy independent of feedback activation of AKT. Clin Cancer Res 20 (2014), 3507–3520.
-
(2014)
Clin Cancer Res
, vol.20
, pp. 3507-3520
-
-
O'Brien, N.A.1
McDonald, K.2
Tong, L.3
von Euw, E.4
Kalous, O.5
Conklin, D.6
-
68
-
-
84939949523
-
A phase 1 study of the sachet formulation of the oral dual PI3K/mTOR inhibitor BEZ235 given twice daily (BID) in patients with advanced solid tumors
-
Bendell, J.C., Kurkjian, C., Infante, J.R., Bauer, T.M., Burris, H.A. 3rd, Greco, F.A., et al. A phase 1 study of the sachet formulation of the oral dual PI3K/mTOR inhibitor BEZ235 given twice daily (BID) in patients with advanced solid tumors. Invest New Drugs 33 (2015), 463–471.
-
(2015)
Invest New Drugs
, vol.33
, pp. 463-471
-
-
Bendell, J.C.1
Kurkjian, C.2
Infante, J.R.3
Bauer, T.M.4
Burris, H.A.5
Greco, F.A.6
-
69
-
-
84923336919
-
Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma
-
Liu, T., Sun, Q., Li, Q., Yang, H., Zhang, Y., Wang, R., et al. Dual PI3K/mTOR inhibitors, GSK2126458 and PKI-587, suppress tumor progression and increase radiosensitivity in nasopharyngeal carcinoma. Mol Cancer Ther 14 (2015), 429–439.
-
(2015)
Mol Cancer Ther
, vol.14
, pp. 429-439
-
-
Liu, T.1
Sun, Q.2
Li, Q.3
Yang, H.4
Zhang, Y.5
Wang, R.6
-
70
-
-
84942824586
-
Synergistic anticancer efficacy of MEK inhibition and dual PI3K/mTOR inhibition in castration-resistant prostate cancer
-
Park, H., Kim, Y., Sul, J.W., Jeong, I.G., Yi, H.J., Ahn, J.B., et al. Synergistic anticancer efficacy of MEK inhibition and dual PI3K/mTOR inhibition in castration-resistant prostate cancer. Prostate 75 (2015), 1747–1759.
-
(2015)
Prostate
, vol.75
, pp. 1747-1759
-
-
Park, H.1
Kim, Y.2
Sul, J.W.3
Jeong, I.G.4
Yi, H.J.5
Ahn, J.B.6
-
71
-
-
84966292102
-
First-in-human phase I study of GSK2126458, an oral pan-class I phosphatidylinositol-3-kinase inhibitor, in patients with advanced solid tumor malignancies
-
Munster, P., Aggarwal, R., Hong, D., Schellens, J.H., van der Noll, R., Specht, J., et al. First-in-human phase I study of GSK2126458, an oral pan-class I phosphatidylinositol-3-kinase inhibitor, in patients with advanced solid tumor malignancies. Clin Cancer Res 22 (2016), 1932–1939.
-
(2016)
Clin Cancer Res
, vol.22
, pp. 1932-1939
-
-
Munster, P.1
Aggarwal, R.2
Hong, D.3
Schellens, J.H.4
van der Noll, R.5
Specht, J.6
-
72
-
-
84979599471
-
A phase Ib dose-escalation study of the MEK inhibitor trametinib in combination with the PI3K/mTOR inhibitor GSK2126458 in patients with advanced solid tumors
-
Grilley-Olson, J.E., Bedard, P.L., Fasolo, A., Cornfeld, M., Cartee, L., Razak, A.R., et al. A phase Ib dose-escalation study of the MEK inhibitor trametinib in combination with the PI3K/mTOR inhibitor GSK2126458 in patients with advanced solid tumors. Invest New Drugs 34 (2016), 740–749.
-
(2016)
Invest New Drugs
, vol.34
, pp. 740-749
-
-
Grilley-Olson, J.E.1
Bedard, P.L.2
Fasolo, A.3
Cornfeld, M.4
Cartee, L.5
Razak, A.R.6
-
73
-
-
79955996030
-
Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor
-
Mallon, R., Feldberg, L.R., Lucas, J., Chaudhary, I., Dehnhardt, C., Santos, E.D., et al. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin Cancer Res 17 (2011), 3193–3203.
-
(2011)
Clin Cancer Res
, vol.17
, pp. 3193-3203
-
-
Mallon, R.1
Feldberg, L.R.2
Lucas, J.3
Chaudhary, I.4
Dehnhardt, C.5
Santos, E.D.6
-
74
-
-
84927624149
-
First-in-human study of PF-05212384 (PKI-587), a small-molecule, intravenous, dual inhibitor of PI3K and mTOR in patients with advanced cancer
-
Shapiro, G.I., Bell-McGuinn, K.M., Molina, J.R., Bendell, J., Spicer, J., Kwak, E.L., et al. First-in-human study of PF-05212384 (PKI-587), a small-molecule, intravenous, dual inhibitor of PI3K and mTOR in patients with advanced cancer. Clin Cancer Res 21 (2015), 1888–1895.
-
(2015)
Clin Cancer Res
, vol.21
, pp. 1888-1895
-
-
Shapiro, G.I.1
Bell-McGuinn, K.M.2
Molina, J.R.3
Bendell, J.4
Spicer, J.5
Kwak, E.L.6
-
75
-
-
83355163329
-
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway
-
Wallin, J.J., Edgar, K.A., Guan, J., Berry, M., Prior, W.W., Lee, L., et al. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther 10 (2011), 2426–2436.
-
(2011)
Mol Cancer Ther
, vol.10
, pp. 2426-2436
-
-
Wallin, J.J.1
Edgar, K.A.2
Guan, J.3
Berry, M.4
Prior, W.W.5
Lee, L.6
-
76
-
-
84975089435
-
Phase I study of apitolisib (GDC-0980), dual phosphatidylinositol-3-kinase and mammalian target of rapamycin kinase inhibitor, in patients with advanced solid tumors
-
Dolly, S.O., Wagner, A.J., Bendell, J.C., Kindler, H.L., Krug, L.M., Seiwert, T.Y., et al. Phase I study of apitolisib (GDC-0980), dual phosphatidylinositol-3-kinase and mammalian target of rapamycin kinase inhibitor, in patients with advanced solid tumors. Clin Cancer Res 22 (2016), 2874–2884.
-
(2016)
Clin Cancer Res
, vol.22
, pp. 2874-2884
-
-
Dolly, S.O.1
Wagner, A.J.2
Bendell, J.C.3
Kindler, H.L.4
Krug, L.M.5
Seiwert, T.Y.6
-
77
-
-
85026548929
-
A phase 1 study of the PI3K/mTOR inhibitor PQR309 evaluating safety, pharmacokinetics (PK) and pharmacodynamics (PD) in patients (pts) with advanced solid tumors
-
Adjei, A.A., Dy, G.K., Zhao, Y., Ma, W.W., Opyrchal, M., Bakhribah, H., et al. A phase 1 study of the PI3K/mTOR inhibitor PQR309 evaluating safety, pharmacokinetics (PK) and pharmacodynamics (PD) in patients (pts) with advanced solid tumors. J Clin Oncol, 34(suppl; abstr 2560), 2016.
-
(2016)
J Clin Oncol
, vol.34
-
-
Adjei, A.A.1
Dy, G.K.2
Zhao, Y.3
Ma, W.W.4
Opyrchal, M.5
Bakhribah, H.6
-
78
-
-
84899785427
-
Characterization of the novel and specific PI3Kalpha inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials
-
Fritsch, C., Huang, A., Chatenay-Rivauday, C., Schnell, C., Reddy, A., Liu, M., et al. Characterization of the novel and specific PI3Kalpha inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther 13 (2014), 1117–1129.
-
(2014)
Mol Cancer Ther
, vol.13
, pp. 1117-1129
-
-
Fritsch, C.1
Huang, A.2
Chatenay-Rivauday, C.3
Schnell, C.4
Reddy, A.5
Liu, M.6
-
79
-
-
84932645192
-
Phase I study of the PI3K-alpha inhibitor BYL719, as a single agent in patients with advanced solid tumors (sAT)
-
Juric, D., Burris, H., Schuler, M., Schellens, J., Berlin, J., Seggewiss-Bernhardt, R., et al. Phase I study of the PI3K-alpha inhibitor BYL719, as a single agent in patients with advanced solid tumors (sAT). Ann Oncol, 25(suppl; abstr 451PD), 2014.
-
(2014)
Ann Oncol
, vol.25
-
-
Juric, D.1
Burris, H.2
Schuler, M.3
Schellens, J.4
Berlin, J.5
Seggewiss-Bernhardt, R.6
-
80
-
-
85026551247
-
Combined alpelisib (BYL719) and fulvestrant in PIK3CA mutant or wild-type estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer
-
In: 33rd Annual Miami Breast Cancer Conference, Abstract 334.
-
Juric D, André F, Rugo H, Mayer I, Loibl S, Sheng Q, et al. Combined alpelisib (BYL719) and fulvestrant in PIK3CA mutant or wild-type estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer. In: 33rd Annual Miami Breast Cancer Conference 2016, Abstract 334.
-
(2016)
-
-
Juric, D.1
André, F.2
Rugo, H.3
Mayer, I.4
Loibl, S.5
Sheng, Q.6
-
81
-
-
85105191128
-
Targeting HER3 and PI3k in head and neck squamous cancer cells
-
Sheng, Q., Wang, H.Q., Das, R., Chen, Y., Liang, J., Cao, A., et al. Targeting HER3 and PI3k in head and neck squamous cancer cells. Cancer Res, 73(suppl; abstr 4261), 2013.
-
(2013)
Cancer Res
, vol.73
-
-
Sheng, Q.1
Wang, H.Q.2
Das, R.3
Chen, Y.4
Liang, J.5
Cao, A.6
-
82
-
-
85026530542
-
Inhibition of PIK3CA with BYL719 can overcome resistance to cetuximab in squamous cell carcinoma of the head and neck (SCCHN)
-
Munster, P., Elkabets, M., Gilbert, J., Razak, A.R.A., Ahn, M., Yen, C., et al. Inhibition of PIK3CA with BYL719 can overcome resistance to cetuximab in squamous cell carcinoma of the head and neck (SCCHN). Mol Cancer Ther, 14(suppl; abstr A46), 2015.
-
(2015)
Mol Cancer Ther
, vol.14
-
-
Munster, P.1
Elkabets, M.2
Gilbert, J.3
Razak, A.R.A.4
Ahn, M.5
Yen, C.6
-
83
-
-
84933678201
-
Phase lb/ll study of the PI3Kα inhibitor BYL719 in combination with cetuximab in recurrent/metastatic squamous cell cancer of the head and neck (SCCHN)
-
Razak, A.R.A., Ahn, M., Yen, C., Solomon, B.J., Lee, S., Wang, H., et al. Phase lb/ll study of the PI3Kα inhibitor BYL719 in combination with cetuximab in recurrent/metastatic squamous cell cancer of the head and neck (SCCHN). J Clin Oncol, 32(suppl; abstr 6044), 2014.
-
(2014)
J Clin Oncol
, vol.32
-
-
Razak, A.R.A.1
Ahn, M.2
Yen, C.3
Solomon, B.J.4
Lee, S.5
Wang, H.6
-
84
-
-
85020402539
-
A phase Ib dose-escalation study of encorafenib and cetuximab with or without alpelisib in metastatic BRAF-mutant colorectal cancer
-
van Geel, R.M.J.M., Tabernero, J., Elez, E., Bendell, J.C., Spreafico, A., Schuler, M., et al. A phase Ib dose-escalation study of encorafenib and cetuximab with or without alpelisib in metastatic BRAF-mutant colorectal cancer. Cancer Discov 7 (2017), 610–619.
-
(2017)
Cancer Discov
, vol.7
, pp. 610-619
-
-
van Geel, R.M.J.M.1
Tabernero, J.2
Elez, E.3
Bendell, J.C.4
Spreafico, A.5
Schuler, M.6
-
85
-
-
84899881210
-
GDC-0032, a beta isoform-sparing PI3K inhibitor: Results of a first-in-human phase Ia dose escalation study
-
Juric, D., Krop, I., Ramanathan, R., Xiao, J., Sanabria, S., Wilson, T., et al. GDC-0032, a beta isoform-sparing PI3K inhibitor: Results of a first-in-human phase Ia dose escalation study. Cancer Res, 73(suppl; abstr LB-64), 2013.
-
(2013)
Cancer Res
, vol.73
-
-
Juric, D.1
Krop, I.2
Ramanathan, R.3
Xiao, J.4
Sanabria, S.5
Wilson, T.6
-
86
-
-
85026555056
-
The PI3K inhibitor, taselisib, has a unique mechanism of action that leads to enhanced potency in PIK3CA mutant models
-
Song, K., Edgar, K., Kirkpatrick, D., Phu, L., Schmidt, S., Nannini, M., et al. The PI3K inhibitor, taselisib, has a unique mechanism of action that leads to enhanced potency in PIK3CA mutant models. Cancer Res, 77(suppl; abstr S6-04), 2017.
-
(2017)
Cancer Res
, vol.77
-
-
Song, K.1
Edgar, K.2
Kirkpatrick, D.3
Phu, L.4
Schmidt, S.5
Nannini, M.6
-
87
-
-
84966942480
-
Discovery of GDC-0032: a beta-sparing PI3K inhibitor active against PIK3CA mutant tumors
-
Olivero, G., Heffron, T., Baumgardner, M., Belvin, M., Ross, L., Blaquiere, N., et al. Discovery of GDC-0032: a beta-sparing PI3K inhibitor active against PIK3CA mutant tumors. Cancer Res, 73(suppl; abstr DDT02-01), 2013.
-
(2013)
Cancer Res
, vol.73
-
-
Olivero, G.1
Heffron, T.2
Baumgardner, M.3
Belvin, M.4
Ross, L.5
Blaquiere, N.6
-
88
-
-
85018510810
-
Phase I dose-escalation study of taselisib, an oral PI3K inhibitor, in patients with advanced solid tumors
-
Juric, D., Krop, I., Ramanathan, R.K., Wilson, T.R., Ware, J.A., Sanabria Bohorquez, S.M., et al. Phase I dose-escalation study of taselisib, an oral PI3K inhibitor, in patients with advanced solid tumors. Cancer Discov 7 (2017), 704–715.
-
(2017)
Cancer Discov
, vol.7
, pp. 704-715
-
-
Juric, D.1
Krop, I.2
Ramanathan, R.K.3
Wilson, T.R.4
Ware, J.A.5
Sanabria Bohorquez, S.M.6
-
89
-
-
85026509256
-
A first-in-human, phase I, dose-escalation study of TAK-117, a selective PI3Kalpha; isoform inhibitor, in patients with advanced solid malignancies
-
Juric, D., De Bono, J.S., LoRusso, P.M., Nemunaitis, J., Heath, E.I., Kwak, J.L., et al. A first-in-human, phase I, dose-escalation study of TAK-117, a selective PI3Kalpha; isoform inhibitor, in patients with advanced solid malignancies. Clin Cancer Res, 2017, 10.1158/1078-0432.CCR-16-2888.
-
(2017)
Clin Cancer Res
-
-
Juric, D.1
De Bono, J.S.2
LoRusso, P.M.3
Nemunaitis, J.4
Heath, E.I.5
Kwak, J.L.6
-
90
-
-
84964671135
-
First-in-human, phase I, dose-escalation study of selective PI3Kα isoform inhibitor MLN1117 in patients (pts) with advanced solid malignancies
-
Juric, D., De Bono, S., LoRusso, P., Zohren, F., Shou, Y., Tabernero, J., First-in-human, phase I, dose-escalation study of selective PI3Kα isoform inhibitor MLN1117 in patients (pts) with advanced solid malignancies. J Clin Oncol, 33(suppl; abstr 512), 2015.
-
(2015)
J Clin Oncol
, vol.33
-
-
Juric, D.1
De Bono, S.2
LoRusso, P.3
Zohren, F.4
Shou, Y.5
Tabernero, J.6
-
91
-
-
84863833204
-
Functional characterization of an isoform-selective inhibitor of PI3K-p110beta as a potential anticancer agent
-
Ni, J., Liu, Q., Xie, S., Carlson, C., Von, T., Vogel, K., et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110beta as a potential anticancer agent. Cancer Discov 2 (2012), 425–433.
-
(2012)
Cancer Discov
, vol.2
, pp. 425-433
-
-
Ni, J.1
Liu, Q.2
Xie, S.3
Carlson, C.4
Von, T.5
Vogel, K.6
-
92
-
-
84856256897
-
Both p110alpha and p110beta isoforms of PI3K can modulate the impact of loss-of-function of the PTEN tumour suppressor
-
Berenjeno, I.M., Guillermet-Guibert, J., Pearce, W., Gray, A., Fleming, S., Vanhaesebroeck, B., Both p110alpha and p110beta isoforms of PI3K can modulate the impact of loss-of-function of the PTEN tumour suppressor. Biochem J 442 (2012), 151–159.
-
(2012)
Biochem J
, vol.442
, pp. 151-159
-
-
Berenjeno, I.M.1
Guillermet-Guibert, J.2
Pearce, W.3
Gray, A.4
Fleming, S.5
Vanhaesebroeck, B.6
-
93
-
-
84879848702
-
PI3K pathway dependencies in endometrioid endometrial cancer cell lines
-
Weigelt, B., Warne, P.H., Lambros, M.B., Reis-Filho, J.S., Downward, J., PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res 19 (2013), 3533–3544.
-
(2013)
Clin Cancer Res
, vol.19
, pp. 3533-3544
-
-
Weigelt, B.1
Warne, P.H.2
Lambros, M.B.3
Reis-Filho, J.S.4
Downward, J.5
-
94
-
-
84899639748
-
PI3K isoform dependence of PTEN-deficient tumors can be altered by the genetic context
-
Schmit, F., Utermark, T., Zhang, S., Wang, Q., Von, T., Roberts, T.M., et al. PI3K isoform dependence of PTEN-deficient tumors can be altered by the genetic context. Proc Natl Acad Sci U S A 111 (2014), 6395–6400.
-
(2014)
Proc Natl Acad Sci U S A
, vol.111
, pp. 6395-6400
-
-
Schmit, F.1
Utermark, T.2
Zhang, S.3
Wang, Q.4
Von, T.5
Roberts, T.M.6
-
95
-
-
84994012236
-
Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors
-
Virone-Oddos, A., Bonnevaux, H., Lemaitre, O., Vincent, L., Halley, F., Demers, B., et al. Discovery and characterization of SAR260301, a novel PI3Kβ-selective inhibitor in clinical development for the treatment of PTEN-deficient tumors. Cancer Res, 73(suppl; abstr 3258), 2013.
-
(2013)
Cancer Res
, vol.73
-
-
Virone-Oddos, A.1
Bonnevaux, H.2
Lemaitre, O.3
Vincent, L.4
Halley, F.5
Demers, B.6
-
96
-
-
84938765398
-
A phase I/II, first-in-human dose-escalation study of GSK2636771 in patients (pts) with PTEN-deficient advanced tumors
-
Arkenau, H., Mateo, J., Lemech, C.R., Infante, J.R., Burris, H.A., Bang, Y., et al. A phase I/II, first-in-human dose-escalation study of GSK2636771 in patients (pts) with PTEN-deficient advanced tumors. J Clin Oncol, 32(suppl; abstr 2514), 2014.
-
(2014)
J Clin Oncol
, vol.32
-
-
Arkenau, H.1
Mateo, J.2
Lemech, C.R.3
Infante, J.R.4
Burris, H.A.5
Bang, Y.6
-
97
-
-
84922347215
-
Inhibition of PI3Kbeta signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel
-
Hancox, U., Cosulich, S., Hanson, L., Trigwell, C., Lenaghan, C., Ellston, R., et al. Inhibition of PI3Kbeta signaling with AZD8186 inhibits growth of PTEN-deficient breast and prostate tumors alone and in combination with docetaxel. Mol Cancer Ther 14 (2015), 48–58.
-
(2015)
Mol Cancer Ther
, vol.14
, pp. 48-58
-
-
Hancox, U.1
Cosulich, S.2
Hanson, L.3
Trigwell, C.4
Lenaghan, C.5
Ellston, R.6
-
98
-
-
85006693951
-
First-in-human phase I trial of the PI3Kb-selective inhibitor SAR260301 in patients with advanced solid tumors (NCT01673737)
-
Bedard, P., Davies, M., Kopetz, S., Flaherty, K., Shapiro, G., John Luke, J., et al. First-in-human phase I trial of the PI3Kb-selective inhibitor SAR260301 in patients with advanced solid tumors (NCT01673737). J Clin Oncol, 33(suppl; abstr 2564), 2015.
-
(2015)
J Clin Oncol
, vol.33
-
-
Bedard, P.1
Davies, M.2
Kopetz, S.3
Flaherty, K.4
Shapiro, G.5
John Luke, J.6
-
99
-
-
33645551286
-
Signaling through PI3Kgamma: a common platform for leukocyte, platelet and cardiovascular stress sensing
-
Hirsch, E., Lembo, G., Montrucchio, G., Rommel, C., Costa, C., Barberis, L., Signaling through PI3Kgamma: a common platform for leukocyte, platelet and cardiovascular stress sensing. Thromb Haemost 95 (2006), 29–35.
-
(2006)
Thromb Haemost
, vol.95
, pp. 29-35
-
-
Hirsch, E.1
Lembo, G.2
Montrucchio, G.3
Rommel, C.4
Costa, C.5
Barberis, L.6
-
100
-
-
85026539942
-
Checkpoint blockade therapy is improved by altering the immune suppressive microenvironment with IPI-549, a potent and selective inhibitor of PI3K-gamma, in preclinical models
-
De Henau, O., Merghoub, T., Winkler, D., Sharma, S., Pink, M., Tchaicha, J., et al. Checkpoint blockade therapy is improved by altering the immune suppressive microenvironment with IPI-549, a potent and selective inhibitor of PI3K-gamma, in preclinical models. Cancer Res, 76(suppl; abstr 554), 2016.
-
(2016)
Cancer Res
, vol.76
-
-
De Henau, O.1
Merghoub, T.2
Winkler, D.3
Sharma, S.4
Pink, M.5
Tchaicha, J.6
-
101
-
-
84992103934
-
IPI-549-01-A phase 1/1b first in human study of IPI-549, a PI3K-γ inhibitor, as monotherapy and in combination with pembrolizumab in subjects with advanced solid tumors
-
Tolcher, A., Hong, D., Sullivan, R., Mier, J., Shapiro, G., Pearlberg, J., et al. IPI-549-01-A phase 1/1b first in human study of IPI-549, a PI3K-γ inhibitor, as monotherapy and in combination with pembrolizumab in subjects with advanced solid tumors. J Clin Oncol, 34(suppl; abstr TPS3111), 2016.
-
(2016)
J Clin Oncol
, vol.34
-
-
Tolcher, A.1
Hong, D.2
Sullivan, R.3
Mier, J.4
Shapiro, G.5
Pearlberg, J.6
-
102
-
-
79952690921
-
PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors
-
Janku, F., Tsimberidou, A.M., Garrido-Laguna, I., Wang, X., Luthra, R., Hong, D.S., et al. PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors. Mol Cancer Ther 10 (2011), 558–565.
-
(2011)
Mol Cancer Ther
, vol.10
, pp. 558-565
-
-
Janku, F.1
Tsimberidou, A.M.2
Garrido-Laguna, I.3
Wang, X.4
Luthra, R.5
Hong, D.S.6
-
103
-
-
84925500147
-
Convergent loss of PTEN leads to clinical resistance to a PI(3)Kalpha inhibitor
-
Juric, D., Castel, P., Griffith, M., Griffith, O.L., Won, H.H., Ellis, H., et al. Convergent loss of PTEN leads to clinical resistance to a PI(3)Kalpha inhibitor. Nature 518 (2015), 240–244.
-
(2015)
Nature
, vol.518
, pp. 240-244
-
-
Juric, D.1
Castel, P.2
Griffith, M.3
Griffith, O.L.4
Won, H.H.5
Ellis, H.6
-
104
-
-
84895906492
-
Assessing PIK3CA and PTEN in early-phase trials with PI3K/AKT/mTOR inhibitors
-
Janku, F., Hong, D.S., Fu, S., Piha-Paul, S.A., Naing, A., Falchook, G.S., et al. Assessing PIK3CA and PTEN in early-phase trials with PI3K/AKT/mTOR inhibitors. Cell Rep 6 (2014), 377–387.
-
(2014)
Cell Rep
, vol.6
, pp. 377-387
-
-
Janku, F.1
Hong, D.S.2
Fu, S.3
Piha-Paul, S.A.4
Naing, A.5
Falchook, G.S.6
-
105
-
-
84896401739
-
Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway
-
Polivka, J. Jr, Janku, F., Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway. Pharmacol Ther 142 (2014), 164–175.
-
(2014)
Pharmacol Ther
, vol.142
, pp. 164-175
-
-
Polivka, J.1
Janku, F.2
|