Targeting the PI3K pathway in cancer: are we making headway?

mTOR Signaling in Growth, Metabolism, and Disease

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Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex

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Nivolumab versus Everolimus in Advanced Renal-Cell Carcinoma

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Temsirolimus, Interferon Alfa, or Both for Advanced Renal-Cell Carcinoma

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Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

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Efficacy of everolimus in advanced renal cell carcinoma: a double-blind, randomised, placebo-controlled phase III trial

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Everolimus for Advanced Pancreatic Neuroendocrine Tumors

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Everolimus in Postmenopausal Hormone-Receptor–Positive Advanced Breast Cancer

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Targeting the phosphoinositide 3-kinase pathway in cancer

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Targeting PI3K signalling in cancer: opportunities, challenges and limitations

Engelman, J. A. (2009) · Nature Reviews Cancer · doi:10.1038/nrc2664 · Cited by 2,445 · see citing works

Tracking the Evolution of Non–Small-Cell Lung Cancer

Jamal-Hanjani, M., Wilson, G. A., McGranahan, N., Birkbak, N. J., Watkins, T. B. K., Veeriah, S., Shafi, S., Johnson, D. H., Mitter, R., Rosenthal, R., et al. (2017) · New England Journal of Medicine · doi:10.1056/nejmoa1616288 · Cited by 2,349 · see citing works

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

Prahallad, A., Sun, C., Huang, S., Di Nicolantonio, F., Salazar, R., Zecchin, D., Beijersbergen, R. L., Bardelli, A., & Bernards, R. (2012) · Nature · doi:10.1038/nature10868 · Cited by 2,051 · see citing works

Vemurafenib in Multiple Nonmelanoma Cancers with <i>BRAF</i> V600 Mutations

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PI3K and cancer: lessons, challenges and opportunities

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Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

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PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting

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Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers

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mTOR and cancer: insights into a complex relationship

Sabatini, D. M. (2006) · Nature Reviews Cancer · doi:10.1038/nrc1974 · Cited by 1,322 · see citing works

Everolimus for the treatment of advanced, non-functional neuroendocrine tumours of the lung or gastrointestinal tract (RADIANT-4): a randomised, placebo-controlled, phase 3 study

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The mTOR‐regulated phosphoproteome reveals a mechanism of mTORC1‐mediated inhibition of growth factor signaling

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PI3Kδ Inhibition by Idelalisib in Patients with Relapsed Indolent Lymphoma

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Everolimus for Subependymal Giant-Cell Astrocytomas in Tuberous Sclerosis

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Cabozantinib versus everolimus in advanced renal cell carcinoma (METEOR): final results from a randomised, open-label, phase 3 trial

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Everolimus for angiomyolipoma associated with tuberous sclerosis complex or sporadic lymphangioleiomyomatosis (EXIST-2): a multicentre, randomised, double-blind, placebo-controlled trial

Bissler, J. J., Kingswood, J. C., Radzikowska, E., Zonnenberg, B. A., Frost, M., Белоусова, Е. Д., Sauter, M., Nonomura, N., Brakemeier, S., de Vries, P. J., et al. (2013) · The Lancet · doi:10.1016/s0140-6736(12)61767-x · Cited by 880 · see citing works

Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells

Henau, O. D., Rausch, M. P., Winkler, D. A., Campesato, L. F., Liu, C., Hirschhorn-Cymerman, D., Budhu, S., Ghosh, A., Pink, M. M., Tchaicha, J. H., et al. (2016) · Nature · doi:10.1038/nature20554 · Cited by 862 · see citing works

Phosphoproteomic Analysis Identifies Grb10 as an mTORC1 Substrate That Negatively Regulates Insulin Signaling

Yu, Y., Yoon, S.-O., Poulogiannis, G., Yang, Q., Ma, X. M., Villén, J., Kubica, N., Hoffman, G. R., Cantley, L. C., Gygi, S. P., et al. (2011) · Science · doi:10.1126/science.1199484 · Cited by 855 · see citing works

Subclonal diversification of primary breast cancer revealed by multiregion sequencing

Yates, L. R., Gerstung, M., Knappskog, S., Desmedt, C., Gundem, G., Loo, P. V., Aas, T., Alexandrov, L. B., Larsimont, D., Davies, H., et al. (2015) · Nature Medicine · doi:10.1038/nm.3886 · Cited by 813 · see citing works

PI3K in lymphocyte development, differentiation and activation

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Autophagy as a target for anticancer therapy

Jankú, F., McConkey, D. J., Hong, D. S., & Kurzrock, R. (2011) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2011.71 · Cited by 803 · see citing works

Efficacy and safety of everolimus for subependymal giant cell astrocytomas associated with tuberous sclerosis complex (EXIST-1): a multicentre, randomised, placebo-controlled phase 3 trial

Franz, D. N., Belousova, E., Sparagana, S., Bebin, E. M., Frost, M., Kuperman, R., Witt, O., Kohrman, M. H., Flamini, J. R., Wu, J. Y., et al. (2013) · The Lancet · doi:10.1016/s0140-6736(12)61134-9 · Cited by 794 · see citing works

Development of PI3K inhibitors: lessons learned from early clinical trials

Rodon, J. A., Dienstmann, R., Serra, V., & Tabernero, J. M. (2013) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2013.10 · Cited by 770 · see citing works

Molecular targets for cancer therapy in the PI3K/AKT/mTOR pathway

Polivka, J., & Janku, F. (2014) · Pharmacology &amp; Therapeutics · doi:10.1016/j.pharmthera.2013.12.004 · Cited by 765 · see citing works

Essential roles of PI(3)K–p110β in cell growth, metabolism and tumorigenesis

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Genome Sequencing Identifies a Basis for Everolimus Sensitivity

Iyer, G., Hanrahan, A. J., Milowsky, M. I., Al‐Ahmadie, H. A., Scott, S. N., Janakiraman, M., Pirun, M., Sander, C., Socci, N. D., Ostrovnaya, I., et al. (2012) · Science · doi:10.1126/science.1226344 · Cited by 688 · see citing works

Phase I, Dose-Escalation Study of BKM120, an Oral Pan-Class I PI3K Inhibitor, in Patients With Advanced Solid Tumors

Bendell, J. C., Rodon, J. A., Burris, H. A., de Jonge, M. J. A., Verweij, J., Birle, D. C., Demanse, D., Buck, S. S. D., Ru, Q. C., Peters, M., et al. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2011.36.1360 · Cited by 687 · see citing works

Clonal status of actionable driver events and the timing of mutational processes in cancer evolution

McGranahan, N., Favero, F., de Bruin, E. C., Birkbak, N. J., Szallasi, Z., & Swanton, C. (2015) · Science Translational Medicine · doi:10.1126/scitranslmed.aaa1408 · Cited by 685 · see citing works

Convergent loss of PTEN leads to clinical resistance to a PI(3)Kα inhibitor

Juric, D., Castel, P., Griffith, M., Griffith, O. L., Won, H. H., Ellis, H., Ebbesen, S. H., Ainscough, B. J., Ramu, A., Iyer, G., et al. (2015) · Nature · doi:10.1038/nature13948 · Cited by 588 · see citing works

Adaptive Randomization of Veliparib–Carboplatin Treatment in Breast Cancer

Rugo, H. S., Olopade, O. I., DeMichele, A. M., Yau, C. S. F., Veer, L. V. ‘., Buxton, M., Hogarth, M. A., Hylton, N. M., Paoloni, M. C., Perlmutter, J., et al. (2016) · New England Journal of Medicine · doi:10.1056/nejmoa1513749 · Cited by 556 · see citing works

First-in-Man Clinical Trial of the Oral Pan-AKT Inhibitor MK-2206 in Patients With Advanced Solid Tumors

Yap, T. A., Li, Y., Patnaik, A., Fearen, I., Olmos, D., Papadopoulos, K. P., Baird, R. D., Delgado, L., Taylor, A. B., Lupinacci, L. C., et al. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2011.35.5263 · Cited by 540 · see citing works

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. M., Im, S., Iwata, H., Cortés, J., Laurentiis, M. D., Jiang, Z., Arteaga, C. L., Jonat, W., Clemons, M. J., Ito, Y., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30376-5 · Cited by 529 · see citing works

Ipatasertib plus paclitaxel versus placebo plus paclitaxel as first-line therapy for metastatic triple-negative breast cancer (LOTUS): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

Kim, S., Dent, R. A., Im, S., Espié, M., Blau, S. H., Tan, A. R., Isakoff, S. J., Oliveira, M., Saura, C., Wongchenko, M. J., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30450-3 · Cited by 478 · see citing works

Adaptive Randomization of Neratinib in Early Breast Cancer

Park, J. W., Liu, M., Yee, D., Yau, C. S. F., Veer, L. V. ‘., Symmans, W. F., Paoloni, M. C., Perlmutter, J., Hylton, N. M., Hogarth, M. A., et al. (2016) · New England Journal of Medicine · doi:10.1056/nejmoa1513750 · Cited by 456 · see citing works

PI3K/AKT/mTOR Inhibitors in Patients With Breast and Gynecologic Malignancies Harboring PIK3CA Mutations

Jankú, F., Wheler, J. J., Westin, S. N., Moulder, S., Naing, A., Tsimberidou, A. M., Fu, S., Falchook, G. S., Hong, D. S., Garrido‐Laguna, I., et al. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2011.36.1196 · Cited by 448 · see citing works

Phosphatidylinositol 3-Kinase α–Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

Juric, D., Rodon, J. A., Tabernero, J. M., Jankú, F., Burris, H. A., Schellens, J. H. M., Middleton, M. R., Berlin, J. D., Schüler, M., Gil-Martín, M., et al. (2018) · Journal of Clinical Oncology · doi:10.1200/jco.2017.72.7107 · Cited by 436 · see citing works

PI3K inhibition results in enhanced estrogen receptor function and dependence in hormone receptor–positive breast cancer

Bosch, A., Li, Z., Bergamaschi, A., Ellis, H., Toska, E., Prat, A., Tao, J. J., Spratt, D. E., Viola, N. T., Castel, P., et al. (2015) · Science Translational Medicine · doi:10.1126/scitranslmed.aaa4442 · Cited by 432 · see citing works

A diverse array of cancer-associated mTOR mutations are hyperactivating and can predict rapamycin sensitivity

Grabiner, B., Nardi, V., Birsoy, K., Possemato, R., Shen, K., Sinha, S., Jordan, A. A., Beck, A. H., & Sabatini, D. (2014) · Cancer Discovery · doi:10.1158/2159-8290.cd-13-0929 · Cited by 418 · see citing works

Selumetinib in women with recurrent low-grade serous carcinoma of the ovary or peritoneum: an open-label, single-arm, phase 2 study

Farley, J. H., Brady, W. E., Vathipadiekal, V., Lankes, H. A., Coleman, R. L., Morgan, M. A., Mannel, R. S., Yamada, S. D., Mutch, D. G., Rodgers, W. H., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(12)70572-7 · Cited by 417 · see citing works

Phosphatidylinositol 3-Kinase and Antiestrogen Resistance in Breast Cancer

Miller, T. W., Balko, J. M., & Arteaga, C. L. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2010.34.4879 · Cited by 415 · see citing works

Phosphatidylinositol 3-Kinase Inhibition by Copanlisib in Relapsed or Refractory Indolent Lymphoma

Dreyling, M. H., Santoro, A., Mollica, L. R., Leppä, S., Follows, G., Lenz, G., Kim, W. S., Nagler, A., Panayiotidis, P. G., Demeter, J., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.75.4648 · Cited by 397 · see citing works

Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind, placebo-controlled, phase 3 trial

Leo, A. D., Johnston, S. R. D., Lee, K. S., Ciruelos, E., Lønning, P. E., Janni, W., O'Regan, R. M., Mouret‐Reynier, M., Kalev, D. N., Egle, D., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30688-5 · Cited by 382 · see citing works

Deregulation of the PI3K and KRAS signaling pathways in human cancer cells determines their response to everolimus

Nicolantonio, F. D., Arena, S., Tabernero, J. M., Grosso, S., Molinari, F., Macarulla, T. M., Russo, M., Cancelliere, C., Zecchin, D., Mazzucchelli, L., et al. (2010) · Journal of Clinical Investigation · doi:10.1172/jci37539 · Cited by 343 · see citing works

PIK3CA Mutations in Patients with Advanced Cancers Treated with PI3K/AKT/mTOR Axis Inhibitors

Jankú, F., Tsimberidou, A. M., Garrido‐Laguna, I., Wang, X., Luthra, R., Hong, D. S., Naing, A., Falchook, G. S., Moroney, J. W., Piha-Paul, S. A., et al. (2011) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-10-0994 · Cited by 331 · see citing works

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., Van Cutsem, E., Pérez-García, J., Stathis, A., Britten, C. D., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1814 · Cited by 324 · see citing works

Response and Acquired Resistance to Everolimus in Anaplastic Thyroid Cancer

Wagle, N., Grabiner, B. C., Allen, E. M. V., Amin‐Mansour, A., Taylor-Weiner, A. N., Rosenberg, M. W., Gray, N. S., Barletta, J. A., Guo, Y., Swanson, S., et al. (2014) · New England Journal of Medicine · doi:10.1056/nejmoa1403352 · Cited by 321 · see citing works

A Phase Ib Study of Alpelisib (BYL719), a PI3Kα-Specific Inhibitor, with Letrozole in ER+/HER2− Metastatic Breast Cancer

Mayer, I. A., Abramson, V. G., Formisano, L., Balko, J. M., Estrada, M. V., Sanders, M. E., Juric, D., Solit, D. B., Berger, M. F., Won, H. H., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-0134 · Cited by 320 · see citing works

AKT Inhibition in Solid Tumors With AKT1 Mutations

Hyman, D. M., Smyth, L. M., Donoghue, M. T. A., Westin, S. N., Bedard, P. L., Dean, E. J., Bando, H., El-Khoueiry, A. B., Fidalgo, J. A. P., Mita, A. C., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.73.0143 · Cited by 309 · see citing works

PIK3CA Mutation H1047R Is Associated with Response to PI3K/AKT/mTOR Signaling Pathway Inhibitors in Early-Phase Clinical Trials

Jankú, F., Wheler, J. J., Naing, A., Falchook, G. S., Hong, D. S., Stepanek, V. M. T., Fu, S., Piha-Paul, S. A., Lee, J. J., Luthra, R., et al. (2012) · Cancer Research · doi:10.1158/0008-5472.can-12-1726 · Cited by 300 · see citing works

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. N., Johnston, S. R. D., Morales, S. M., Yardley, D. A., Melichar, B., Forero, A., Lee, S. C., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)00106-6 · Cited by 295 · see citing works

Resistance to BRAF Inhibition in BRAF-Mutant Colon Cancer Can Be Overcome with PI3K Inhibition or Demethylating Agents

Mao, M., Tian, F., Mariadason, J. M., Tsao, C. C., Lemos, R., Dayyani, F., Gopal, Y. N. V., Jiang, Z.-Q., Wistuba, I. I., Tang, X. M., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-1446 · Cited by 290 · see citing works

Idelalisib given front-line for treatment of chronic lymphocytic leukemia causes frequent immune-mediated hepatotoxicity

Lampson, B. L., Kasar, S. N., Matos, T. R., Morgan, E. A., Rassenti, L. Z., Davids, M. S., Fisher, D. C., Freedman, A. S., Jacobson, C. A., Armand, P. A., et al. (2016) · Blood · doi:10.1182/blood-2016-03-707133 · Cited by 288 · see citing works

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, N. T., Lemos, R., Wipf, P., Yacoub, A., Mitchell, C., Siwak, D. R., Mills, G. B., Dent, P., Kirkpatrick, D. L., & Powis, G. (2008) · Cancer Research · doi:10.1158/0008-5472.can-07-6656 · Cited by 275 · see citing works

Idelalisib or placebo in combination with bendamustine and rituximab in patients with relapsed or refractory chronic lymphocytic leukaemia: interim results from a phase 3, randomised, double-blind, placebo-controlled trial

Zelenetz, A. D., Barrientos, J. C., Brown, J. R., Coiffier, B., Delgado, J., Egyed, M., Ghia, P., Illés, Á., Jurczak, W. J., Marlton, P. V., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30671-4 · Cited by 251 · see citing works

Results of an international randomized phase III trial of the mammalian target of rapamycin inhibitor ridaforolimus versus placebo to control metastatic sarcomas in patients after benefit from prior chemotherapy

Demetri, G. D., Chawla, S. P., Ray-Coquard, I., Le Cesne, A., Staddon, A. P., Milhem, M. M., Penel, N., Riedel, R. F., Bui-Nguyen, B., Cranmer, L. D., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.45.5766 · Cited by 245 · see citing works

Phosphoinositide 3-kinase (PI3K) pathway inhibitors in solid tumors: From laboratory to patients

Jankú, F. (2017) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2017.07.005 · Cited by 245 · see citing works

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., Weiss, G. J., Sachdev, J. C., Chadha, M. K., Fulk, M., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw282 · Cited by 240 · see citing works

Assessing PIK3CA and PTEN in Early-Phase Trials with PI3K/AKT/mTOR Inhibitors

Jankú, F., Hong, D. S., Fu, S., Piha-Paul, S. A., Naing, A., Falchook, G. S., Tsimberidou, A. M., Stepanek, V. M. T., Moulder, S., Lee, J. J., et al. (2014) · Cell Reports · doi:10.1016/j.celrep.2013.12.035 · Cited by 237 · see citing works

A Phase Ib Dose-Escalation Study of Encorafenib and Cetuximab with or without Alpelisib in Metastatic <i>BRAF</i> -Mutant Colorectal Cancer

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Mutations in TSC1, TSC2, and MTOR are associated with response to rapalogs in patients with metastatic Renal Cell Carcinoma

Kwiatkowski, D., Choueiri, T., Fay, A., Rini, B., Thorner, A., de Velasco, G., Tyburczy, M., Hamieh, L., Albigès, L., Agarwal, N., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2631 · Cited by 207 · see citing works

PIK3CA Mutations Frequently Coexist with RAS and BRAF Mutations in Patients with Advanced Cancers

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Drugging PI3K in cancer: refining targets and therapeutic strategies

Yap, T. A., Bjerke, L. M., Clarke, P. A., & Workman, P. (2015) · Current Opinion in Pharmacology · doi:10.1016/j.coph.2015.05.016 · Cited by 204 · see citing works

The BATTLE-2 Study: A Biomarker-Integrated Targeted Therapy Study in Previously Treated Patients With Advanced Non–Small-Cell Lung Cancer

Papadimitrakopoulou, V. A., Lee, J. J., Wistuba, I. I., Tsao, A. S., Fossella, F. V., Kalhor, N., Gupta, S. K., Byers, L. A., Izzo, J. G., Gettinger, S. N., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2015.66.0084 · Cited by 183 · see citing works

A randomized adaptive phase II/III study of buparlisib, a pan-class I PI3K inhibitor, combined with paclitaxel for the treatment of HER2– advanced breast cancer (BELLE-4)

Martín, M., Chan, A., Dirix, L. Y., O’Shaughnessy, J., Hegg, R., Manikhas, A., Shtivelband, M. I., Криворотько, П. В., López, N. B., Campone, M., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw562 · Cited by 180 · see citing works

A First-in-Human Phase I Study of the ATP-Competitive AKT Inhibitor Ipatasertib Demonstrates Robust and Safe Targeting of AKT in Patients with Solid Tumors

Saura, C., Roda, D., Roselló, S., Oliveira, M., Macarulla, T. M., Fidalgo, J. A. P., Morales‐Barrera, R., Sanchis, J. M., Musib, L. C., Budha, N. R., et al. (2016) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-0512 · Cited by 173 · see citing works

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., Vo, A. C. H., Klucher, K. M., Herbst, R. S., Eckhardt, S., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-0714 · Cited by 169 · see citing works

Functional Characterization of an Isoform-Selective Inhibitor of PI3K-p110β as a Potential Anticancer Agent

Ni, J., Liu, Q., Xie, S., Carlson, C. B., Von, T., Vogel, K. W., Riddle, S., Benes, C. H., Eck, M. J., Roberts, T. M., et al. (2012) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0003 · Cited by 162 · see citing works

Phase I Dose-Escalation Study of Taselisib, an Oral PI3K Inhibitor, in Patients with Advanced Solid Tumors

Juric, D., Krop, I. E., Ramanathan, R. K., Wilson, T. R., Ware, J. A., Bohorquez, S. M. S., Savage, H. M., Sampath, D., Salphati, L., Lin, R., et al. (2017) · Cancer Discovery · doi:10.1158/2159-8290.cd-16-1080 · Cited by 161 · see citing works

Biomarkers of Response to Akt Inhibitor MK-2206 in Breast Cancer

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KLF1 mutations are relatively more common in a thalassemia endemic region and ameliorate the severity of β-thalassemia

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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., Braña, I., Pandya, S. S., Scheffold, C., Laird, A. D., Nguyen, L. T., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-1777 · Cited by 152 · see citing works

A Phase I Open-Label Study to Identify a Dosing Regimen of the Pan-AKT Inhibitor AZD5363 for Evaluation in Solid Tumors and in PIK3CA -Mutated Breast and Gynecologic Cancers

Banerji, U., Dean, E. J., Fidalgo, J. A. P., Batist, G., Bedard, P. L., You, B., Westin, S. N., Kabos, P., Garrett, M. D., Tall, M., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-17-2260 · Cited by 151 · see citing works

FDA Approval: Idelalisib Monotherapy for the Treatment of Patients with Follicular Lymphoma and Small Lymphocytic Lymphoma

Miller, B. W., Przepiorka, D., de Claro, R. A., Lee, K., Nie, L., Simpson, N. E., Gudi, R., Saber, H., Shord, S. S., Bullock, J. M., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-2522 · Cited by 147 · see citing works

Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors

Markman, B., Tabernero, J. M., Krop, I. E., Shapiro, G. I., Siu, L. L., Chen, L. C., Mita, M. M., Cuero, M. M., Stutvoet, S., Birle, D. C., et al. (2012) · Annals of Oncology · doi:10.1093/annonc/mds011 · Cited by 147 · see citing works

A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors

Mateo, J., Ganji, G., Lemech, C., Burris, H. A., Han, S., Swales, K. E., Decordova, S., DeYoung, M. P., Smith, D. A., Sundaram, S. K., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-17-0725 · Cited by 146 · see citing works

San Antonio Breast Cancer Symposium

Fricker, J. (2008) · The Lancet Oncology · doi:10.1016/s1470-2045(08)70329-2 · Cited by 142 · see citing works

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., Zauderer, M. G., Lolkema, M. P., Apt, D., Yeh, R.-F., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2225 · Cited by 141 · see citing works

Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL

Barr, P. M., Saylors, G. B., Spurgeon, S. E. F., Cheson, B. D., Greenwald, D. R., O'Brien, S. M., Liem, A. K. D., Mclntyre, R. E., Joshi, A., Abella-Dominicis, E., et al. (2016) · Blood · doi:10.1182/blood-2015-12-683516 · Cited by 141 · see citing works

Phase I pharmacokinetic and pharmacodynamic study of the pan-PI3K/mTORC vascular targeted pro-drug SF1126 in patients with advanced solid tumours and B-cell malignancies

Mahadevan, D., Chiorean, E. G., Harris, W. B., Hoff, D. D. V., Stejskal-Barnett, A., Qi, W., Anthony, S. P., Younger, A., Rensvold, D., Cordova-Marks, F. M., et al. (2012) · European Journal of Cancer · doi:10.1016/j.ejca.2012.06.027 · Cited by 136 · see citing works

Randomized Open-Label Phase II Trial of Apitolisib (GDC-0980), a Novel Inhibitor of the PI3K/Mammalian Target of Rapamycin Pathway, Versus Everolimus in Patients With Metastatic Renal Cell Carcinoma

Powles, T. B., Lackner, M. R., Oudard, S. M., Escudier, B. J., Ralph, C., Brown, J. E., Hawkins, R. E., Castellano, D., Rini, B. I., Staehler, M. D., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2015.64.8808 · Cited by 135 · see citing works

Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma

Naing, A., Aghajanian, C. A., Raymond, É., Olmos, D., Schwartz, G., Oelmann, E. M., Grinsted, L. M., Burke, W., Taylor, R., Kaye, S. B., et al. (2012) · British Journal of Cancer · doi:10.1038/bjc.2012.368 · Cited by 131 · see citing works

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. C., Spicer, J. F., Kwak, E. L., Pandya, S. S., Millham, R., Borzillo, G. V., Pierce, K. J., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1306 · Cited by 123 · see citing works

Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma

Matulonis, U. A., Vergote, I. B., Backes, F. J., Martin, L. P., McMeekin, S., Birrer, M. J., Campana, F., Xu, Y., Égile, C., & Ghamande, S. A. (2014) · Gynecologic Oncology · doi:10.1016/j.ygyno.2014.12.019 · Cited by 122 · see citing works

Phase II study of PX-866 in recurrent glioblastoma

Pitz, M. W., Eisenhauer, E. A., MacNeil, M. V., Thiessen, B. A., Easaw, J. C., Macdonald, D. R., Eisenstat, D. D., Kakumanu, A. S., Salim, M., Chalchal, H. I., et al. (2015) · Neuro-Oncology · doi:10.1093/neuonc/nou365 · Cited by 121 · see citing works

Role of PI3Kδ and PI3Kγ in inflammatory arthritis and tissue localization of neutrophils

Randis, T. M., Puri, K. D., Zhou, H., et al. (2008) · European Journal of Immunology · doi:10.1002/eji.200838266 · Cited by 119 · see citing works

Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092

Yu, Y., Savage, R. E., Eathiraj, S., Meade, J., Wick, M. J., Hall, T. G., Abbadessa, G., & Schwartz, B. E. (2015) · PLoS ONE · doi:10.1371/journal.pone.0140479 · Cited by 117 · see citing works

Pictilisib PI3Kinase inhibitor (a phosphatidylinositol 3-kinase [PI3K] inhibitor) 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. T., Petráková, K., Roylance, R. R., Laing, R. W., Chan, S. Y. T., Abell, F., Gendreau, S. B., Rooney, I. A., Apt, D., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw320 · Cited by 116 · see citing works

RICTOR Amplification Defines a Novel Subset of Patients with Lung Cancer Who May Benefit from Treatment with mTORC1/2 Inhibitors

Cheng, H., Zou, Y., Ross, J. S., Wang, K., Liu, X., Halmos, B., Ali, S. M., Liu, H., Verma, A., Montagna, C., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-14-0971 · Cited by 104 · see citing works

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. D., Infante, J. R., Bauer, T. M., Burris, H. A., Greco, F. A., Shih, K. C., Thompson, D. S., Lane, C. M., Finney, L. H., et al. (2015) · Investigational New Drugs · doi:10.1007/s10637-015-0218-6 · Cited by 101 · see citing works

A Phase Ib Study of BEZ235, a Dual Inhibitor of Phosphatidylinositol 3-Kinase (PI3K) and Mammalian Target of Rapamycin (mTOR), in Patients With Advanced Renal Cell Carcinoma

Carlo, M. I., Molina, A. M., Lakhman, Y., et al. (2016) · The Oncologist · doi:10.1634/theoncologist.2016-0145 · Cited by 101 · see citing works

A First-in-Human, Phase I, Dose-Escalation Study of TAK-117, a Selective PI3Kα Isoform Inhibitor, in Patients with Advanced Solid Malignancies

Juric, D., Bono, J. S. D., LoRusso, P. M., Nemunaitis, J. J., Heath, E. I., Kwak, E. L., Macarulla, T. M., Geuna, E., Miguel, M. J. D., Patel, C. A., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-2888 · Cited by 100 · see citing works

A randomized, phase II trial of cetuximab 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., Shirai, K., Choi, M., Laskin, J. J., Kochenderfer, M. D., Spira, A. I., Cline-Burkhardt, V. J. M., Winquist, E., Hausman, D. F., Walker, L. N., et al. (2014) · Annals of Oncology · doi:10.1093/annonc/mdu574 · Cited by 99 · see citing works

TAK ‐228 (formerly MLN 0128), an investigational oral dual TORC 1/2 inhibitor: A phase I dose escalation study in patients with relapsed or refractory multiple myeloma, non‐Hodgkin lymphoma, or Waldenström's macroglobulinemia

Ghobrial, I. M., Siegel, D. S. D., Vij, R., Berdeja, J. G., Richardson, P. G. G., Neuwirth, R. B., Patel, C. G., Zohren, F., & Wolf, J. L. (2016) · American Journal of Hematology · doi:10.1002/ajh.24300 · Cited by 99 · see citing works

A multicenter, single‐arm, open‐label, phase 2 study of apitolisib (GDC‐0980) for the treatment of recurrent or persistent endometrial carcinoma (MAGGIE study)

Makker, V., Recio, F. O., Ma, L., Matulonis, U. A., Lauchle, J., Parmar, H. R., Gilbert, H., Ware, J. A., Zhu, R., Lu, S., et al. (2016) · Cancer · doi:10.1002/cncr.30286 · Cited by 93 · see citing works

San Antonio Breast Cancer Symposium 2016

Gourd, K. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30658-1 · Cited by 89 · see citing works

Phase Ib dose-finding study of abiraterone acetate plus buparlisib (BKM120) or dactolisib (BEZ235) in patients with castration-resistant prostate cancer

Massard, C., Chi, K. N., Castellano, D., Bono, J. S. D., Gravis, G., Dirix, L. Y., Machiels, J., Mita, A. C., Mellado, B., Turri, S., et al. (2017) · European Journal of Cancer · doi:10.1016/j.ejca.2017.01.024 · Cited by 88 · see citing works

Molecular Profiling of Patients with Colorectal Cancer and Matched Targeted Therapy in Phase I Clinical Trials

Dienstmann, R., Serpico, D., Rodon, J. A., Saura, C., Macarulla, T. M., Élez, E., Alsina, M., Capdevila, J., Pérez-García, J. M., Sánchez-Ollé, G., et al. (2012) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-12-0290 · Cited by 83 · see citing works

A phase II trial of lenalidomide plus rituximab in previously untreated follicular non-Hodgkin’s lymphoma (NHL): CALGB 50803 (Alliance)

Martin, P., Jung, S., Pitcher, B. N., Bartlett, N. L., Blum, K. A., Shea, T., Hsi, E. D., Ruan, J., Smith, S. E., Leonard, J. P., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx496 · Cited by 83 · see citing works

Interrogating Two Schedules of the AKT Inhibitor MK-2206 in Patients with Advanced Solid Tumors Incorporating Novel Pharmacodynamic and Functional Imaging Biomarkers

Yap, T. A., Li, Y., Patnaik, A., Tunariu, N., Biondo, A., Fearen, I., Papadopoulos, K. P., Olmos, D., Baird, R. D., Delgado, L., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-0868 · Cited by 81 · see citing works

Weekly nab -Rapamycin in Patients with Advanced Nonhematologic Malignancies: Final Results of a Phase I Trial

Gonzalez-Angulo, A. M., Meric‐Bernstam, F., Chawla, S. P., Falchook, G. S., Hong, D. S., Akçakanat, A., Chen, H., Naing, A., Fu, S., Wheler, J. J., et al. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-3110 · Cited by 81 · see citing works

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. R., Schnadig, I. D., Beauregard, P., Bowles, D. W., Spira, A. I., Levy, B. P., Seetharamu, N., et al. (2015) · Oral Oncology · doi:10.1016/j.oraloncology.2014.12.013 · Cited by 78 · see citing works

Phase I study of PF-04691502, a small-molecule, oral, dual inhibitor of PI3K and mTOR, in patients with advanced cancer

Britten, C. D., Adjei, A. A., Millham, R., Houk, B. E., Borzillo, G. V., Pierce, K. J., Wainberg, Z. A., & LoRusso, P. M. (2014) · Investigational New Drugs · doi:10.1007/s10637-013-0062-5 · Cited by 78 · see citing works

A phase I dose‐escalation study to assess safety, tolerability, pharmacokinetics, and preliminary efficacy of the dual mTORC1/mTORC2 kinase inhibitor CC‐223 in patients with advanced solid tumors or multiple myeloma

Bendell, J. C., Kelley, R. K., Shih, K. C., et al. (2015) · Cancer · doi:10.1002/cncr.29422 · Cited by 77 · see citing works

Responses to Liposomal Doxorubicin, Bevacizumab, and Temsirolimus in Metaplastic Carcinoma of the Breast: Biologic Rationale and Implications for Stem-Cell Research in Breast Cancer

Moulder, S. L., Moroney, J. W., Helgason, T., et al. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2010.34.0604 · Cited by 74 · see citing works

A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies

Mateo, J., Olmos, D., Dumez, H., Poondru, S., Samberg, N. L., Barr, S. M., Tornout, J. M. V., Jie, F., Sandhu, S. K., Tan, D. S. W., et al. (2016) · British Journal of Cancer · doi:10.1038/bjc.2016.59 · Cited by 68 · see citing works

Inhibition of the phosphoinositide 3-kinase pathway for the treatment of patients with metastatic metaplastic breast cancer

Moulder, S. L., Helgason, T., Jankú, F., et al. (2015) · Annals of Oncology · doi:10.1093/annonc/mdv163 · Cited by 65 · see citing works

Duvelisib (IPI-145), a PI3K-δ,γ Inhibitor, Is Clinically Active in Patients with Relapsed/Refractory Chronic Lymphocytic Leukemia

O'Brien, S. M., Patel, M. R., Kahl, B. S., et al. (2014) · Blood · doi:10.1182/blood.v124.21.3334.3334 · Cited by 65 · see citing works

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. N., Brahmer, J. R., Adjei, A. A., Davies, M. A., Lazar, A. J., Vo, A. C. H., Peterson, S., Walker, L. N., et al. (2013) · British Journal of Cancer · doi:10.1038/bjc.2013.474 · Cited by 62 · see citing works

BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling‐dependent tumor growth in mouse models

Politz, O., Siegel, F., Bärfacker, L., Bömer, U., Hägebarth, A., Scott, W. J., Michels, M., Ince, S. J., Neuhaus, R., Meyer, K., et al. (2016) · International Journal of Cancer · doi:10.1002/ijc.30457 · Cited by 61 · see citing works

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. M., Burris, H. A., Gartner, E. M., Mayer, I. A., Saura, C., Maurer, M., Ciruelos, E., García, A. A., Campana, F., Wu, B., et al. (2014) · Breast Cancer Research and Treatment · doi:10.1007/s10549-014-3248-4 · Cited by 59 · see citing works

Phase I Trial of the Pan-PI3K Inhibitor Pilaralisib (SAR245408/XL147) in Patients with Chronic Lymphocytic Leukemia (CLL) or Relapsed/Refractory Lymphoma

Brown, J. R., Davids, M. S., Rodon, J. A., Abrisqueta, P., Kasar, S. N., Lager, J. J., Jiang, J., Égile, C., & Awan, F. T. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-3262 · Cited by 55 · see citing works

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. P., Spira, A. I., Becker, D. J., Evans, T. L., Schnadig, I. D., Camidge, D. R., Bauman, J. E., Hausman, D. F., Walker, L. N., Nemunaitis, J. J., et al. (2014) · Journal of Thoracic Oncology · doi:10.1097/jto.0000000000000183 · Cited by 52 · see citing works

Safety, pharmacokinetics (PK), pharmacodynamics (PD), and clinical activity of the oral AKT inhibitor GSK2141795 (GSK795) in a phase I first-in-human study.

Burris, H. A., Siu, L. L., Infante, J. R., Wheler, J. J., Kurkjian, C. D., Opalinska, J., Smith, D. A., Antal, J. M., Gauvin, J., Gonzalez, T., et al. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2011.29.15_suppl.3003 · Cited by 50 · see citing works

a Phase 1 Evaluation of Duvelisib (IPI-145), a PI3K-δ,γ Inhibitor, in Patients with Relapsed/Refractory iNHL

Flinn, I. W., Oki, Y., Patel, M. R., et al. (2014) · Blood · doi:10.1182/blood.v124.21.802.802 · Cited by 48 · see citing works

Target-Based Therapeutic Matching in Early-Phase Clinical Trials in Patients with Advanced Colorectal Cancer and PIK3CA Mutations

Ganesan, P., Jankú, F., Naing, A., Hong, D. S., Tsimberidou, A. M., Falchook, G. S., Wheler, J. J., Piha-Paul, S. A., Fu, S., Stepanek, V. M. T., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0319-t · Cited by 47 · see citing works

First-in-Human Study of CH5132799, an Oral Class I PI3K Inhibitor, Studying Toxicity, Pharmacokinetics, and Pharmacodynamics, in Patients with Metastatic Cancer

Blagden, S. P., Olmin, A., Josephs, D. H., Stavraka, C., Zivi, A., Pinato, D. J., Anthoney, A., Decordova, S., Swales, K. E., Riisnaes, R., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-1315 · Cited by 46 · see citing works

Duvelisib (IPI-145), a Phosphoinositide-3-Kinase-δ,γ Inhibitor, Shows Activity in Patients with Relapsed/Refractory T-Cell Lymphoma

Horwitz, S. M., Porcu, P., Flinn, I. W., et al. (2014) · Blood · doi:10.1182/blood.v124.21.803.803 · Cited by 46 · see citing works

A Randomized, Phase II Trial of Cetuximab With or Without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients With Metastatic Colorectal Carcinoma.

Bowles, D. W., Kochenderfer, M., Cohn, A., Sideris, L., Nguyen, N., Cline-Burkhardt, V., Schnadig, I., Choi, M., Nabell, L., Chaudhry, A., et al. (2016) · Clinical Colorectal Cancer · doi:10.1016/j.clcc.2016.03.004 · Cited by 42 · see citing works

First-In-Human Study Of AMG 319, a Highly Selective, Small Molecule Inhibitor Of PI3Kδ, In Adult Patients With Relapsed Or Refractory Lymphoid Malignancies

Lanasa, M. C., Glenn, M. J., Mato, A. R., et al. (2013) · Blood · doi:10.1182/blood.v122.21.678.678 · Cited by 41 · see citing works

SU2C Phase Ib Study of Paclitaxel and MK-2206 in Advanced Solid Tumors and Metastatic Breast Cancer

Gonzalez-Angulo, A. M., Krop, I. E., Akçakanat, A., Chen, H., Liu, S., Li, Y., Culotta, K. S., Tarco, E., Piha-Paul, S. A., Moulder-Thompson, S. L., et al. (2015) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/dju493 · Cited by 39 · see citing works

Phase I Dose-Escalation Study of Pilaralisib (SAR245408, XL147), a Pan-Class I PI3K Inhibitor, in Combination With Erlotinib in Patients With Solid Tumors

Soria, J., LoRusso, P. A., Bahleda, R., et al. (2015) · The Oncologist · doi:10.1634/theoncologist.2014-0449 · Cited by 38 · see citing works

A Multicenter Phase I Study Evaluating Dual PI3K and BRAF Inhibition with PX-866 and Vemurafenib in Patients with Advanced BRAF V600–Mutant Solid Tumors

Yam, C., Xu, X., Davies, M. A., Gimotty, P. A., Morrissette, J. J. D., Tetzlaff, M. T., Wani, K., Liu, S., Deng, W., Buckley, M. E., et al. (2017) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-17-1807 · Cited by 38 · see citing works

First‐in‐human trial of the PI3Kβ‐selective inhibitor SAR260301 in patients with advanced solid tumors

Bedard, P. L., Davies, M. A., Kopetz, S., Juric, D., Shapiro, G. I., Luke, J. J., Spreafico, A., Wu, B., Castell, C., Gomez, C., et al. (2017) · Cancer · doi:10.1002/cncr.31044 · Cited by 37 · see citing works

Clinical Activity of Duvelisib (IPI-145), a Phosphoinositide-3-Kinase-δ,γ Inhibitor, in Patients Previously Treated with Ibrutinib

Porcu, P., Flinn, I. W., Kahl, B. S., et al. (2014) · Blood · doi:10.1182/blood.v124.21.3335.3335 · Cited by 35 · see citing works

First-in-human phase I trial of the dual mTORC1 and mTORC2 inhibitor AZD2014 in solid tumors.

Banerji, U., Dean, E. J., Gonzalez, M., Greystoke, A., Basu, B., Krebs, M., Puglisi, M., Grinsted, L. M., Oelmann, E. M., Burke, W., et al. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2012.30.15_suppl.3004 · Cited by 32 · see citing works

Adaptively randomized trial of neoadjuvant chemotherapy with or without the Akt inhibitor MK-2206: Graduation results from the I-SPY 2 Trial.

Tripathy, D., Chien, A. J., Hylton, N. M., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2015.33.15_suppl.524 · Cited by 31 · see citing works

Phase I Dose-Escalation Study of Pilaralisib (SAR245408, XL147) in Combination with Paclitaxel and Carboplatin in Patients with Solid Tumors

Wheler, J. J., Mutch, D. G., Lager, J. J., Castell, C., Liu, L., Jiang, J., & Traynor, A. M. (2017) · The Oncologist · doi:10.1634/theoncologist.2016-0257 · Cited by 30 · see citing works

PI3Kgamma (PI3Kγ) is essential for efficient induction of CXCR3 on activated T cells

Barbi, J. J., Cummings, H., Lu, B., et al. (2008) · Blood · doi:10.1182/blood-2008-02-135715 · Cited by 29 · see citing works

Phase Ib Study of Safety and Pharmacokinetics of the PI3K Inhibitor SAR245408 with the HER3-Neutralizing Human Antibody SAR256212 in Patients with Solid Tumors

Abramson, V. G., Supko, J. G., Ballinger, T. J., Cleary, J. M., Hilton, J. F., Tolaney, S. M., Chau, N. G., Cho, D. C., Pearlberg, J., Lager, J. J., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-1764 · Cited by 29 · see citing works

Primary results of LORELEI: A phase II randomized, double-blind study of neoadjuvant letrozole (LET) plus taselisib versus LET plus placebo (PLA) in postmenopausal patients (pts) with ER+/HER2-negative early breast cancer (EBC)

Saura, C., de Azambuja, E., Hlauschek, D., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx440.001 · Cited by 23 · see citing works

A multicenter phase 1 study of PX-866 and cetuximab in patients with metastatic colorectal carcinoma or recurrent/metastatic squamous cell carcinoma of the head and neck

Bowles, D. W., Senzer, N. N., Hausman, D. F., et al. (2014) · Investigational New Drugs · doi:10.1007/s10637-014-0124-3 · Cited by 22 · see citing works

Abstract C252: A phase 1, dose-escalation study of MLN0128, an investigational oral mammalian target of rapamycin complex 1/2 (mTORC1/2) catalytic inhibitor, in patients (pts) with advanced non-hematologic malignancies.

Infante, J. R., Tabernero, J. M., Cervantes, A. M. R., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-13-c252 · Cited by 19 · see citing works

SANDPIPER: Phase III study of the PI3-kinase (PI3K) inhibitor taselisib (GDC-0032) plus fulvestrant in patients (pts) with estrogen receptor (ER)-positive, HER2-negative locally advanced or metastatic breast cancer (BC) enriched for pts with PIK3CA-mutant tumors.

Baselga, J. M., Cortés, J., Laurentiis, M. D., Dieras, V. C., Harbeck, N., Hsu, J. Y., Ng, V., Schimmöller, F., Wilson, T. R., Im, Y., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.tps617 · Cited by 18 · see citing works

Abstract PD5-5: Phase I study of the PI3Kα inhibitor BYL719 plus fulvestrant in patients with PIK3CA-altered and wild type ER+/HER2- locally advanced or metastatic breast cancer

Jankú, F., Juric, D., Cortés, J., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.sabcs14-pd5-5 · Cited by 17 · see citing works

Abstract B271: A first-in-human Phase I study of ZSTK474, an oral pan-PI3K inhibitor, in patients with advanced solid malignancies.

Lockhart, A. C., Olszanski, A. J., Allgren, R. L., et al. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-13-b271 · Cited by 17 · see citing works

A first in human phase I study of AZD8186, a potent and selective inhibitor of PI3K in patients with advanced solid tumours as monotherapy and in combination with the dual mTORC1/2 inhibitor vistusertib (AZD2014) or abiraterone acetate.

Hansen, A. R., Shapiro, G. I., Do, K. T., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.2570 · Cited by 16 · see citing works

SANDPIPER: Phase III study of the PI3-kinase (PI3K) inhibitor taselisib (GDC-0032) plus fulvestrant in patients (pts) with estrogen receptor (ER)-positive, HER2-negative locally advanced or metastatic breast cancer (BC) enriched for pts with PIK3CA-mutant tumors.

Baselga, J. M., Cortés, J., Laurentiis, M. D., Dent, S. F., Dieras, V. C., Harbeck, N., Hsu, J. Y., Jin, H., Schimmöller, F., Wilson, T. R., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.tps1119 · Cited by 15 · see citing works

Abstract CT089: IPI-549-01 - A Phase 1/1b, first-in-human study of IPI-549, a PI3K-γ inhibitor, as monotherapy and in combination with nivolumab in patients with advanced solid tumors

Tolcher, A. W., Hong, D. S., Sullivan, R. J., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-ct089 · Cited by 12 · see citing works

An Open-Label, Phase Ib Study of Duvelisib (IPI-145) in Combination with Bendamustine, Rituximab or Bendamustine/Rituximab in Select Subjects with Lymphoma or Chronic Lymphocytic Leukemia

Flinn, I. W., Patel, M. R., Maris, M. B., et al. (2014) · Blood · doi:10.1182/blood.v124.21.4422.4422 · Cited by 11 · see citing works

338 Results from a phase 1 study of ARQ 092, a novel pan AKT-inhibitor, in subjects with advanced solid tumors or recurrent malignant lymphoma

Tolcher, A. W., Harb, W. A., Sachdev, J. C., et al. (2015) · European Journal of Cancer · doi:10.1016/s0959-8049(16)30201-5 · Cited by 8 · see citing works

A phase I, first-in-human dose study of the dual PI3K/mTOR inhibitor LY3023414 (LY) in patients (pts) with advanced cancer.

Moore, K. N., Varghese, A. M., Hyman, D. M., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2015.33.15_suppl.11075 · Cited by 8 · see citing works

Take (STAT)5: jazzing up T-cell leukemia

Porcu, P., & Dubovsky, J. A. (2014) · Blood · doi:10.1182/blood-2014-06-576942 · Cited by 6 · see citing works

A pharmacokinetically (PK) and pharmacodynamically (PD) driven phase I trial of the pan-AKT inhibitor AZD5363 with expansion cohorts in PIK3CA mutant breast and gynecological cancers.

Banerji, U., Dean, E. J., Fidalgo, J. A. P., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2015.33.15_suppl.2500 · Cited by 6 · see citing works

A first in human, dose escalation trial of MSC2363318A – a dual p70S6K/Akt inhibitor, for patients with advanced malignancies

Tsimberidou, A. M., Verschraegen, C. F., Heestand, G. M., et al. (2015) · Annals of Oncology · doi:10.1093/annonc/mdv094.1 · Cited by 5 · see citing works

Abstract B100: ASN003, a unique B-RAF inhibitor with additional selective activity against PI3K and mTOR kinases, shows strong antitumor activity in multiple xenograft models

Thompson, S. K., Jaleel, M., Nyavanandi, V. K., et al. (2015) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-15-b100 · Cited by 3 · see citing works

A phase 1 first-in-human (FIH) dose-escalation (DE) study of the oral dual PI3K/mTOR inhibitor PQR309 in patients (pts) with advanced solid tumors: Final DE results.

Kristeleit, R. S., Brown, N. F., Hess, D., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2015.33.15_suppl.2592 · Cited by 3 · see citing works

Abstract 2992: Identification of NOTCH1 inactivating mutation as a therapeutic vulnerability to PI3K/mTOR pathway inhibition in head and neck squamous cell carcinoma (HNSCC)

Sambandam, V., Shen, L., Tong, P., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-2992 · Cited by 1 · see citing works

RAS-targeted therapies: is the undruggable drugged?

Moore, A. R., Rosenberg, S. C., McCormick, F., & Malek, S. (2020) · Nature Reviews Drug Discovery · doi:10.1038/s41573-020-0068-6 · Cited by 1,103 · see citing works

Targeting fibrosis: mechanisms and clinical trials

Zhao, M., Wang, L., Wang, M., Zhou, S., Lu, Y., Cui, H., Racanelli, A. C., Zhang, L., Ye, T., Ding, B., et al. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-01070-3 · Cited by 547 · see citing works

mTOR: Role in cancer, metastasis and drug resistance

Murugan, A. K. (2019) · Seminars in Cancer Biology · doi:10.1016/j.semcancer.2019.07.003 · Cited by 483 · see citing works

Targeting KRAS mutant cancers: from druggable therapy to drug resistance

Zhu, C., Guan, X., Zhang, X., Luan, X., Song, Z., Cheng, X., Zhang, W., & Qin, J.-J. (2022) · Molecular Cancer · doi:10.1186/s12943-022-01629-2 · Cited by 231 · see citing works

Development of combination therapies to maximize the impact of KRAS-G12C inhibitors in lung cancer

Molina-Arcas, M., Moore, C., Rana, S., van Maldegem, F., Mugarza, E., Romero-Clavijo, P., Herbert, E., Horswell, S., Li, L.-S., Janes, M. R., et al. (2019) · Science Translational Medicine · doi:10.1126/scitranslmed.aaw7999 · Cited by 203 · see citing works

PI3K/Akt/mTOR Signaling Pathway as a Target for Colorectal Cancer Treatment

Leiphrakpam, P., & Are, C. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25063178 · Cited by 193 · see citing works

Phosphatidylinositol(4,5)bisphosphate: diverse functions at the plasma membrane

Katan, M., & Cockcroft, S. (2020) · Essays in Biochemistry · doi:10.1042/ebc20200041 · Cited by 176 · see citing works

The PI3K subunits, P110α and P110β are potential targets for overcoming P-gp and BCRP-mediated MDR in cancer

Zhang, L., Li, Y., Wang, Q., Chen, Z., Li, X., Wu, Z., Hu, C., Liao, D., Zhang, W., & Chen, Z.-S. (2020) · Molecular Cancer · doi:10.1186/s12943-019-1112-1 · Cited by 152 · see citing works

The metabolic landscape of lung cancer: New insights in a disturbed glucose metabolism

Vanhove, K., Graulus, G.-J., Mesotten, L., Thomeer, M., Derveaux, E., Noben, J.-P., Guedens, W., & Adriaensens, P. (2019) · Frontiers in Oncology · doi:10.3389/fonc.2019.01215 · Cited by 147 · see citing works

Management of toxicity to isoform α-specific PI3K inhibitors

Nunnery, S. E., & Mayer, I. A. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz440 · Cited by 137 · see citing works

Current State and Future Challenges for PI3K Inhibitors in Cancer Therapy

Sirico, M., D’Angelo, A., Gianni, C., Casadei, C., Merloni, F., & De Giorgi, U. (2023) · Cancers · doi:10.3390/cancers15030703 · Cited by 121 · see citing works

Emerging roles of allosteric modulators in the regulation of protein‐protein interactions (PPIs): A new paradigm for PPI drug discovery

Ni, D., Lu, S., & Zhang, J. (2019) · Medicinal Research Reviews · doi:10.1002/med.21585 · Cited by 116 · see citing works

Single-cell resolved imaging reveals intra-tumor heterogeneity in glycolysis, transitions between metabolic states, and their regulatory mechanisms

Kondo, H., Ratcliffe, C. D. H., Hooper, S., Ellis, J., MacRae, J. I., Hennequart, M., Dunsby, C. W., Anderson, K. I., & Sahai, E. (2021) · Cell Reports · doi:10.1016/j.celrep.2021.108750 · Cited by 109 · see citing works

MTOR signaling orchestrates stress-induced mutagenesis, facilitating adaptive evolution in cancer

Cipponi, A., Goode, D. L., Bedo, J., McCabe, M. J., Pajic, M., Croucher, D. R., Rajal, A. G., Junankar, S. R., Saunders, D. N., Lobachevsky, P., et al. (2020) · Science · doi:10.1126/science.aau8768 · Cited by 103 · see citing works

PIM kinase inhibition: co-targeted therapeutic approaches in prostate cancer

Luszczak, S., Kumar, C., Sathyadevan, V. K., Simpson, B. S., Gately, K. A., Whitaker, H. C., & Heavey, S. (2020) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-020-0109-y · Cited by 102 · see citing works

Overcoming Resistance to Drugs Targeting KRAS Mutation

Jiao, D., & Yang, S. (2020) · The Innovation · doi:10.1016/j.xinn.2020.100035 · Cited by 61 · see citing works

D‐1553: A novel <scp>KRAS^G12C</scp> inhibitor with potent and selective cellular and in vivo antitumor activity

Shi, Z., Weng, J., Niu, H., Yang, H., Liu, R., Weng, Y., Zhu, Q., Zhang, Y., Tao, L., Wang, Z., et al. (2023) · Cancer Science · doi:10.1111/cas.15829 · Cited by 38 · see citing works

PH domain-mediated autoinhibition and oncogenic activation of Akt

Bae, H., Viennet, T., Park, E., Chu, N., Salguero, A., Eck, M. J., Arthanari, H., & Cole, P. A. (2022) · eLife · doi:10.7554/elife.80148 · Cited by 31 · see citing works

Systematic Optimization of the iMALDI Workflow for the Robust and Straightforward Quantification of Signaling Proteins in Cancer Cells

Froehlich, B. C., Popp, R., Sobsey, C. A., Ibrahim, S., LeBlanc, A. M., Mohammed, Y., Aguilar‐Mahecha, A., Poetz, O., Chen, M. X., Spatz, A., et al. (2020) · PROTEOMICS – Clinical Applications · doi:10.1002/prca.202000034 · Cited by 9 · see citing works

Difference in adverse-event profiles between mTOR inhibitors, temsirolimus, and everolimus for advanced renal cell carcinoma.

Nozawa, M., Kikuchi, T., Nishimoto, M., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2013.31.6_suppl.461 · Cited by 3 · see citing works

Mammalian Target of Rapamycin Inhibitors in Clinical Practice: Case Reports of Everolimus in Renal Cell Carcinoma

Bracarda, S., Ravaud, A., & Chiodi, M. (2009) · European Urology Supplements · doi:10.1016/j.eursup.2009.08.007 · Cited by 2 · see citing works

Treatment Options in Metastatic Renal Cell Carcinoma: Focus on mTOR Inhibitors

Pal, S. K., & Figlin, R. A. (2010) · Clinical Medicine Insights Oncology · doi:10.4137/cmo.s1590 · Cited by 14 · see citing works

First-Line Mammalian Target of Rapamycin Inhibition in Metastatic Renal Cell Carcinoma: An Analysis of Practice Patterns From the International Metastatic Renal Cell Carcinoma Database Consortium

Harshman, L. C., Kroeger, N., Rha, S. Y., et al. (2014) · Clinical Genitourinary Cancer · doi:10.1016/j.clgc.2014.03.003 · Cited by 12 · see citing works

mTOR pathway inhibition in renal cell carcinoma

Marín, Á. P., Redondo, A., Arranz, E. E., Auñón, P., Fernández, B. C., & Barón, M. G. (2010) · Urologic Oncology Seminars and Original Investigations · doi:10.1016/j.urolonc.2009.11.008 · Cited by 12 · see citing works