Efficacy of PI3K inhibitors in advanced breast cancer

PD-1 and PD-L1 Immune Checkpoint Blockade to Treat Breast Cancer

Hartkopf, A. D., Taran, F., Wallwiener, M., Walter, C. B., Krämer, B., Grischke, E., & Brucker, S. Y. (2016) · Breast Care · doi:10.1159/000453569 · Cited by 30,989

Evaluation of Factors Related to Late Recurrence - Later than 10 Years after the Initial Treatment - in Primary Breast Cancer

Nishimura, R., Osako, T., Nishiyama, Y., Tashima, R., Nakano, M., Fujisue, M., Toyozumi, Y., & Arima, N. (2013) · Oncology · doi:10.1159/000353099 · Cited by 13,239

Comprehensive molecular portraits of human breast tumours

The Cancer Genome Atlas Network (2012) · Nature · doi:10.1038/nature11412 · Cited by 12,129

PTEN , a Putative Protein Tyrosine Phosphatase Gene Mutated in Human Brain, Breast, and Prostate Cancer

Li, J., Yen, C., Liaw, D., Podsypanina, K., Bose, S., Wang, S. I., Puc, J., Miliaresis, C., Rodgers, L., McCombie, R., et al. (1997) · Science · doi:10.1126/science.275.5308.1943 · Cited by 4,785

The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism

Engelman, J. A., Luo, J., & Cantley, L. C. (2006) · Nature Reviews Genetics · doi:10.1038/nrg1879 · Cited by 3,330

Palbociclib and letrozole in advanced breast cancer

Finn, R. S., Martin, M., Rugo, H. S., Jones, S., Im, S.-A., Gelmon, K., Harbeck, N., Lipatov, O. N., Walshe, J. M., Moulder, S., et al. (2016) · New England Journal of Medicine · doi:10.1056/nejmoa1607303 · Cited by 3,007

The PI3K Pathway in Human Disease

Fruman, D. A., Chiu, H., Hopkins, B. D., Bagrodia, S., Cantley, L. C., & Abraham, R. T. (2017) · Cell · doi:10.1016/j.cell.2017.07.029 · Cited by 2,749

Alpelisib for PIK3CA -Mutated, Hormone Receptor–Positive Advanced Breast Cancer

André, F., Ciruelos, E., Rubovszky, G., Campone, M., Loibl, S., Rugo, H. S., Iwata, H., Conte, P., Mayer, I. A., Kaufman, B., et al. (2019) · New England Journal of Medicine · doi:10.1056/nejmoa1813904 · Cited by 2,622

Fulvestrant plus palbociclib versus fulvestrant plus placebo for treatment of hormone-receptor-positive, HER2-negative metastatic breast cancer that progressed on previous endocrine therapy (PALOMA-3): final analysis of the multicentre, double-blind, phase 3 randomised controlled trial

Cristofanilli, M., Turner, N. C., Bondarenko, I., Ro, J., Im, S.-A., Masuda, N., Colleoni, M., DeMichele, A., Loi, S., Verma, S., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(15)00613-0 · Cited by 1,827

The emerging mechanisms of isoform-specific PI3K signalling

Vanhaesebroeck, B., Guillermet-Guibert, J., Graupera, M., & Bilanges, B. (2010) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2882 · Cited by 1,767

MONARCH 3: Abemaciclib As Initial Therapy for Advanced Breast Cancer

Goetz, M. P., Toi, M., Campone, M., Sohn, J., Paluch-Shimon, S., Huober, J., Park, I. H., Trédan, O., Chen, S.-C., Manso, L., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.75.6155 · Cited by 1,744

Interaction of oestrogen receptor with the regulatory subunit of phosphatidylinositol-3-OH kinase

Simoncini, T., Hafezi‐Moghadam, A., Brazil, D. P., Ley, K. F., Chin, W. W., & Liao, J. K. (2000) · Nature · doi:10.1038/35035131 · Cited by 1,436

A transforming mutation in the pleckstrin homology domain of AKT1 in cancer

Carpten, J. D., Faber, A. L., Horn, C. L., Donoho, G. P., Briggs, S., Robbins, C. M., Hostetter, G. H., Boguslawski, S. J., Moses, T. Y., Savage, S., et al. (2007) · Nature · doi:10.1038/nature05933 · Cited by 1,322

An integrative genomic and proteomic analysis of pik3ca, pten, and akt mutations in breast cancer.

Stemke-Hale, K., Gonzalez-Angulo, A. M., Lluch, A., Neve, R. M., Kuo, W.-L., Davies, M., Carey, M., Hu, Z., Guan, Y., Sahin, A., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-07-6854 · Cited by 1,054

Overall survival with ribociclib plus endocrine therapy in breast cancer

Im, S.-A., Lu, Y.-S., Bardia, A., Harbeck, N., Colleoni, M., Franke, F., Chow, L., Sohn, J., Lee, K.-S., Campos-Gomez, S., et al. (2019) · New England Journal of Medicine · doi:10.1056/nejmoa1903765 · Cited by 1,001

PIK3CA Mutations Correlate with Hormone Receptors, Node Metastasis, and ERBB2, and Are Mutually Exclusive with PTEN Loss in Human Breast Carcinoma

Saal, L. H., Holm, K., Maurer, M. S., Memeo, L., Su, T., Wang, X., Yu, J. S., Malmström, P.-O., MANSUKHANI, M. M., Enoksson, J., et al. (2005) · Cancer Research · doi:10.1158/0008-5472-can-04-3913 · Cited by 877

Molecular alterations of the AKT2 oncogene in ovarian and breast carcinomas

Bellacosa, A., de Feo, D., Godwin, A. K., Bell, D. W., Cheng, J. Q., Altomare, D. A., Wan, M., Dubeau, L., Scambia, G., Masciullo, V., et al. (1995) · International Journal of Cancer · doi:10.1002/ijc.2910640412 · Cited by 837

PI3K in lymphocyte development, differentiation and activation

Okkenhaug, K., & Vanhaesebroeck, B. (2003) · Nature reviews. Immunology · doi:10.1038/nri1056 · Cited by 824

Early Adaptation and Acquired Resistance to CDK4/6 Inhibition in Estrogen Receptor–Positive Breast Cancer

Herrera-Abreu, M. T., Palafox, M., Asghar, U. S., Rivas, M. A., Cutts, R. J., García-Murillas, I., Pearson, A., Guzmán, M., Rodríguez, O., Grueso, J., et al. (2016) · Cancer Research · doi:10.1158/0008-5472.can-15-0728 · Cited by 781

The Identification of 2-(1 H -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., Chuckowree, I., Clarke, P. A., Depledge, P., Eccles, S. A., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800295d · Cited by 756

Navigating metabolic pathways to enhance antitumour immunity and immunotherapy

Li, X., Wenes, M., Romero, P. J., Huang, S. C., Fendt, S., & Ho, P. (2019) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-019-0203-7 · Cited by 750

Genomic characterization of metastatic breast cancers

Bertucci, F., Ng, C. K. Y., Patsouris, A., Droin, N. M., Piscuoglio, S., Carbuccia, N., Soria, J., Dien, A. T., Adnani, Y., Kamal, M. T., et al. (2019) · Nature · doi:10.1038/s41586-019-1056-z · Cited by 723

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

Jia, S., Liu, Z., Zhang, S., Liu, P., Zhang, L., Lee, S., Zhang, J., Signoretti, S., Loda, M. F., Roberts, T. M., et al. (2008) · Nature · doi:10.1038/nature07091 · Cited by 702

The Genetic Landscape and Clonal Evolution of Breast Cancer Resistance to Palbociclib plus Fulvestrant in the PALOMA-3 Trial

O’Leary, B., Cutts, R. J., Liu, Y., Hrebien, S., Huang, X., Fenwick, K., André, F., Loibl, S., Loi, S., García-Murillas, I., et al. (2018) · Cancer Discovery · doi:10.1158/2159-8290.cd-18-0264 · Cited by 657

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

PI 3-kinase p110β: a new target for antithrombotic therapy

Jackson, S. P., Schoenwaelder, S. M., Goncalves, I., Nesbitt, W. S., Yap, C. L., Wright, C. E., Kenche, V. B., Anderson, K. E., Dopheide, S. M., Yuan, Y., et al. (2005) · Nature Medicine · doi:10.1038/nm1232 · Cited by 582

Hyperactivation of phosphatidylinositol-3 kinase promotes escape from hormone dependence in estrogen receptor–positive human breast cancer

Miller, T. W., Hennessy, B. T., Gonzalez-Angulo, A. M., Fox, E. M., Mills, G. B., Chen, H., Higham, C., Garcı́a-Echeverrı́a, C., Shyr, Y., & Arteaga, C. L. (2010) · Journal of Clinical Investigation · doi:10.1172/jci41680 · Cited by 555

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 538

Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor

Maira, S.-M., Pecchi, S., Huang, A., Burger, M. T., Knapp, M. S., Sterker, D., Schnell, C., Guthy, D. A., Nagel, T., Wiesmann, M., et al. (2011) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-11-0474 · Cited by 533

Angiogenesis selectively requires the p110α isoform of PI3K to control endothelial cell migration

Graupera, M., Guillermet-Guibert, J., Foukas, L., Phng, L.-K., Cain, R., Salpekar, A., Pearce, W., Meek, S., Millán, J., Cutillas, P., et al. (2008) · Nature · doi:10.1038/nature06892 · Cited by 532

CDK4/6 Inhibition in Cancer: Beyond Cell Cycle Arrest

Goel, S., DeCristo, M. J., McAllister, S. S., & Zhao, J. J. (2018) · Trends in Cell Biology · doi:10.1016/j.tcb.2018.07.002 · Cited by 506

Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials

Fritsch, C. M., Huang, A., Chatenay‐Rivauday, C., Schnell, C., Reddy, A., Liu, M., Kauffmann, A., Guthy, D. A., Erdmann, D., Pover, A. D., et al. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0865 · Cited by 504

Picking the Point of Inhibition: A Comparative Review of PI3K/AKT/mTOR Pathway Inhibitors

Dienstmann, R., Rodon, J. A., Serra, V., & Tabernero, J. M. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0639 · Cited by 474

Combining a PI3K Inhibitor with a PARP Inhibitor Provides an Effective Therapy for BRCA1-Related Breast Cancer

Juvekar, A., Burga, L. N., Hu, H., Lunsford, E. P., Ibrahim, Y. H., Balmañà, J., Rajendran, A., Papa, A., Spencer, K., Lyssiotis, C. A., et al. (2012) · Cancer Discovery · doi:10.1158/2159-8290.cd-11-0336 · Cited by 468

Critical role for the p110α phosphoinositide-3-OH kinase in growth and metabolic regulation

Foukas, L. C., Claret, M., Pearce, W., Okkenhaug, K., Meek, S., Peskett, E., Sancho, S., Smith, A. J. H., Withers, D. J., & Vanhaesebroeck, B. (2006) · Nature · doi:10.1038/nature04694 · Cited by 463

Signalling by PI3K isoforms: insights from gene-targeted mice

Vanhaesebroeck, B., Ali, K., Bilancio, A., Geering, B., & Foukas, L. C. (2005) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2005.02.008 · Cited by 450

p110δ, a novel phosphoinositide 3-kinase in leukocytes

Vanhaesebroeck, B., Welham, M. J., Kotani, K., Stein, R. C., Warne, P. H., Zvelebil, M., Higashi, K., Volinia, S., Downward, J., & Waterfield, M. D. (1997) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.94.9.4330 · Cited by 445

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 441

CDK 4/6 inhibitors sensitize PIK3CA mutant breast cancer to PI3K inhibitors

Vora, S. R., Juric, D., Kim, N., Mino-Kenudson, M., Huynh, T., Costa, C., Lockerman, E. L., Pollack, S. F., Liu, M., Li, X., et al. (2014) · Cancer Cell · doi:10.1016/j.ccr.2014.05.020 · Cited by 438

PIK3CA Mutation Associates with Improved Outcome in Breast Cancer

Kalinsky, K. M., Jacks, L. M., Heguy, A., Patil, S. N., Drobnjak, M., Bhanot, U. K., Hedvat, C. V., Traina, T. A., Solit, D. B., Gerald, W. L., et al. (2009) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-0632 · Cited by 407

Neoadjuvant Endocrine Therapy for Estrogen Receptor–Positive Breast Cancer: A Systematic Review and Meta-analysis

Spring, L. M., Gupta, A., Reynolds, K. L., Gadd, M. A., Ellisen, L. W., Isakoff, S. J., Moy, B., & Bardia, A. (2016) · JAMA Oncology · doi:10.1001/jamaoncol.2016.1897 · Cited by 396

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 392

Biomarker Analyses in CLEOPATRA: A Phase III, Placebo-Controlled Study of Pertuzumab in Human Epidermal Growth Factor Receptor 2–Positive, First-Line Metastatic Breast Cancer

Baselga, J. M., Cortés, J., Im, S., Clark, E., Ross, G. A., Kiermaier, A. C., & Swain, S. M. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2013.54.5384 · Cited by 364

Targeting the PI3-kinase pathway in triple-negative breast cancer

Pascual, J., & Turner, N. C. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz133 · Cited by 339

Outcome and molecular landscape of patients with PIK3CA-mutated metastatic breast cancer

Mosele, F., Stefanovska, B., Lusque, A., Dien, A. T., Garberis, I., Droin, N. M., Tourneau, C. L., Sablin, M., Lacroix, L., Enrico, D. H., et al. (2020) · Annals of Oncology · doi:10.1016/j.annonc.2019.11.006 · Cited by 316

Detection of Tumor PIK3CA Status in Metastatic Breast Cancer Using Peripheral Blood

Higgins, M. J., Jelovac, D., Barnathan, E., Blair, B., Slater, S. A., Powers, P., Zorzi, J., Jeter, S. C., Oliver, G. R., Fetting, J. H., et al. (2012) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-11-2696 · Cited by 311

PI3K pathway activation in breast cancer is associated with the basal‐like phenotype and cancer‐specific mortality

López‐Knowles, E., O'Toole, S. A., McNeil, C. M., Millar, E. K. A., Qiu, M. R., Crea, P., Daly, R. J., Musgrove, E. A., & Sutherland, R. L. (2009) · International Journal of Cancer · doi:10.1002/ijc.24831 · Cited by 302

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 302

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., Baird, R., Kristeleit, R., Shah, K., Moreno, V., Clarke, P., Raynaud, F., Levy, G., Ware, J., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-0947 · Cited by 285

Phosphoinositide 3-Kinase p110β Activity: Key Role in Metabolism and Mammary Gland Cancer but Not Development

Ciraolo, E., Iezzi, M., Marone, R., Marengo, S., Curcio, C., Costa, C., Azzolino, O., Gonella, C., Rubinetto, C., Wu, H., et al. (2008) · Science Signaling · doi:10.1126/scisignal.1161577 · Cited by 276

Alpelisib Plus Fulvestrant in PIK3CA -Altered and PIK3CA -Wild-Type Estrogen Receptor–Positive Advanced Breast Cancer

Juric, D., Jankú, F., Rodon, J. A., Burris, H. A., Mayer, I. A., Schüler, M., Seggewiß-Bernhardt, R., Gil-Martín, M., Middleton, M. R., Baselga, J. M., et al. (2018) · JAMA Oncology · doi:10.1001/jamaoncol.2018.4475 · Cited by 249

New insights on PI3K/AKT pathway alterations and clinical outcomes in breast cancer

Yang, S. X., Polley, E. C., & Lipkowitz, S. (2016) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2016.03.004 · Cited by 240

PIK3CA mutations are associated with reduced pathological complete response rates in primary HER2-positive breast cancer: pooled analysis of 967 patients from five prospective trials investigating lapatinib and trastuzumab

Loibl, S., Majewski, I. J., Guarneri, V., Nekljudova, V., Holmes, E. M., Bria, E., Denkert, C., Schem, C., Sotiriou, C. P., Loi, S., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw197 · Cited by 230

Relationship between Tumor Biomarkers and Efficacy in EMILIA, a Phase III Study of Trastuzumab Emtansine in HER2-Positive Metastatic Breast Cancer

Baselga, J. M., Phillips, G. D. L., Verma, S., Ro, J., Huober, J., Guardino, A. E., Samant, M. K., Olsen, S., de Haas, S. L., & Pegram, M. D. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2499 · Cited by 227

Trastuzumab-DM1 causes tumour growth inhibition by mitotic catastrophe in trastuzumab-resistant breast cancer cells in vivo

Barok, M., Tanner, M., Köninki, K., & Isola, J. J. (2011) · Breast Cancer Research · doi:10.1186/bcr2868 · Cited by 226

Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies

Hanker, A. B., Pfefferle, A. D., Balko, J. M., Kuba, M. G., Young, C. D., Sánchez, V., Sutton, C. R., Cheng, H., Perou, C. M., Zhao, J. J., et al. (2013) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1303204110 · Cited by 203

Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1H-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Ndubaku, C. O., Heffron, T. P., Staben, S. T., Baumgardner, M., Blaquière, N., Bradley, E. K., Bull, R., Do, S., Dotson, J., Dudley, D. A., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm4003632 · Cited by 182

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

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., Sanders, M. E., Yap, J. T., den Abbeele, A. D. V., Li, Y., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2013.54.0518 · Cited by 179

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

Phase I study of alpelisib (BYL-719) and trastuzumab emtansine (T-DM1) in HER2-positive metastatic breast cancer (MBC) after trastuzumab and taxane therapy

Jain, S., Shah, A. N., Santa-Maria, C. A., Siziopikou, K. P., RADEMAKER, A. W., Helenowski, I., Cristofanilli, M., & Gradishar, W. J. (2018) · Breast Cancer Research and Treatment · doi:10.1007/s10549-018-4792-0 · Cited by 151

Specific Roles of the p110α Isoform of Phosphatidylinsositol 3-Kinase in Hepatic Insulin Signaling and Metabolic Regulation

Sopasakis, V. R., Liu, P., Suzuki, R., Kondo, T., Winnay, J. N., Tran, T. T., Asano, T., Smyth, G., Sajan, M. P., Farese, R. V., et al. (2010) · Cell Metabolism · doi:10.1016/j.cmet.2010.02.002 · Cited by 148

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

Phase III study of taselisib (GDC-0032) + fulvestrant (FULV) v FULV in patients (pts) with estrogen receptor (ER)-positive, PIK3CA -mutant (MUT), locally advanced or metastatic breast cancer (MBC): Primary analysis from SANDPIPER.

Baselga, J. M., Dent, S. F., Cortés, J., Im, Y., Dieras, V. C., Harbeck, N., Krop, I. E., Verma, S., Wilson, T. R., Jin, H., et al. (2018) · Journal of Clinical Oncology · doi:10.1200/jco.2018.36.18_suppl.lba1006 · Cited by 138

PIK3CA mutations, PTEN, and pHER2 expression and impact on outcome in HER2-positive early-stage breast cancer patients treated with adjuvant chemotherapy and trastuzumab

Jensen, J. D., Knoop, A. S., Lænkholm, A., Grauslund, M., Jensen, M., Santoni‐Rugiu, E., Andersson, M., & Ewertz, M. (2011) · Annals of Oncology · doi:10.1093/annonc/mdr546 · Cited by 135

Phosphatidyl-inositol-3-kinase alpha catalytic subunit mutation and response to neoadjuvant endocrine therapy for estrogen receptor positive breast cancer

Ellis, M. J., Li, L., Crowder, R. J., Yu, T., Hoog, J., Snider, J., Davies, S. R., DeSchryver, K., Evans, D. B., Steinseifer, J., et al. (2009) · Breast Cancer Research and Treatment · doi:10.1007/s10549-009-0575-y · Cited by 130

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

Neoadjuvant buparlisib plus trastuzumab and paclitaxel for women with HER2+ primary breast cancer: A randomised, double-blind, placebo-controlled phase II trial (NeoPHOEBE)

Loibl, S., de la Peña, L., Nekljudova, V., Zardavas, D., Michiels, S., Denkert, C., Rezai, M., Bermejo, B., Untch, M., Lee, S. C., et al. (2017) · European Journal of Cancer · doi:10.1016/j.ejca.2017.08.020 · Cited by 103

A Phase II Randomized Study of Neoadjuvant Letrozole Plus Alpelisib for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Breast Cancer (NEO-ORB)

Mayer, I. A., Prat, A., Egle, D., Blau, S. H., Fidalgo, J. A. P., Gnant, M., Fasching, P. A., Colleoni, M. A., Wolff, A. C., Winer, E. P., et al. (2019) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-18-3160 · Cited by 100

Neoadjuvant letrozole plus taselisib versus letrozole plus placebo in postmenopausal women with oestrogen receptor-positive, HER2-negative, early-stage breast cancer (LORELEI): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

Saura, C., Hlauschek, D., Oliveira, M., Zardavas, D., Jallitsch-Halper, A., de la Peña, L., Nuciforo, P. G., Ballestrero, A., Dubsky, P. C., Lombard, J. M., et al. (2019) · The Lancet Oncology · doi:10.1016/s1470-2045(19)30334-1 · Cited by 98

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. R., Naughton, M., Ademuyiwa, F. O., Suresh, R., Griffith, M., Griffith, O. L., Skidmore, Z. L., Spies, N. C., Ramu, A., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-1745 · Cited by 96

Consensus on precision medicine for metastatic cancers: a report from the MAP conference

Swanton, C., Soria, J., Bardelli, A., Biankin, A. V., Caldas, C., Chandarlapaty, S., de Koning, L., Dive, C., Feunteun, J., Leung, S.-Y., et al. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw192 · Cited by 94

Increased pathological complete response rate after a long-term neoadjuvant letrozole treatment in postmenopausal oestrogen and/or progesterone receptor-positive breast cancer

Allevi, G., Strina, C., Andreis, D., Zanoni, V., Bazzola, L., Bonardi, S., Foroni, C., Milani, M., Cappelletti, M. R., Gussago, F., et al. (2013) · British Journal of Cancer · doi:10.1038/bjc.2013.151 · Cited by 85

Prognostic role of PIK3CA mutations and their association with hormone receptor expression in breast cancer: a meta-analysis

Pang, B., Cheng, S., Sun, S., An, C., Liu, Z., Xue, F., & Liu, G. (2014) · Scientific Reports · doi:10.1038/srep06255 · Cited by 84

Duvelisib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Phosphoinositide 3-Kinases

Rodrigues, D. A., Sagrillo, F. S., & Fraga, C. A. M. (2019) · Pharmaceuticals · doi:10.3390/ph12020069 · Cited by 83

The PI 3-kinase isoforms p110α and p110β have differential roles in PDGF- and insulin-mediated signaling

Hooshmand-Rad, R., Hájková, L., Klint, P., Karlsson, R., Vanhaesebroeck, B., Claesson, L., & Heldin, C. (2000) · Journal of Cell Science · doi:10.1242/jcs.113.2.207 · Cited by 79

Abstract GS3-08: Alpelisib + fulvestrant for advanced breast cancer: Subgroup analyses from the phase III SOLAR-1 trial

Juric, D., Ciruelos, E., Rubovszky, G., Campone, M., Loibl, S., Rugo, H., Iwata, H., Conte, P., Mayer, I., Kaufman, B., et al. (2019) · Cancer Research · doi:10.1158/1538-7445.sabcs18-gs3-08 · Cited by 62

PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer

Guérin, M., Rezaï, K., Isambert, N., Campone, M., Autret, A., Pakradouni, J., Provansal, M., Camerlo, J., Sabatier, R., Bertucci, F., et al. (2017) · European Journal of Cancer · doi:10.1016/j.ejca.2017.08.025 · Cited by 62

Double-Blind, Placebo-Controlled, Multicenter, Randomized, Phase IIB Neoadjuvant Study of Letrozole-Lapatinib in Postmenopausal Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative, Operable Breast Cancer

Guarneri, V., Generali, D., Frassoldati, A., Artioli, F., Boni, C., Cavanna, L., Tagliafico, E., Maiorana, A., Bottini, A., Cagossi, K., et al. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2013.51.4737 · Cited by 61

Phase II study of buparlisib (BKM120) and trastuzumab in patients with HER2+ locally advanced or metastatic breast cancer resistant to trastuzumab-based therapy

Pistilli, B., Pluard, T., Urruticoechea, A., Farci, D., Kong, A., Bachelot, T., Chan, S., Han, H., Jerusalem, G., Urban, P., et al. (2017) · Breast Cancer Research and Treatment · doi:10.1007/s10549-017-4596-7 · Cited by 53

Spotlight on copanlisib and its potential in the treatment of relapsed/refractory follicular lymphoma: evidence to date

Mensah, F., Blaize, J.-P., & Bryan, L. J. (2018) · OncoTargets and Therapy · doi:10.2147/ott.s142264 · Cited by 50

The next era of treatment for hormone receptor-positive, HER2-negative advanced breast cancer: Triplet combination-based endocrine therapies

Cortés, J., Im, S., Holgado, E., Pérez-García, J. M., Schmid, P., & Chávez‐MacGregor, M. (2017) · Cancer Treatment Reviews · doi:10.1016/j.ctrv.2017.09.011 · Cited by 48

Abstract LB-64: GDC-0032, a beta isoform-sparing PI3K inhibitor: Results of a first-in-human phase Ia dose escalation study.

Juric, D., Krop, I. E., Ramanathan, R. K., Xiao, J. J., Sanabria, S., Wilson, T. R., Choi, Y., Parmar, H. R., Hsu, J. Y., Baselga, J. M., et al. (2013) · Cancer Research · doi:10.1158/1538-7445.am2013-lb-64 · Cited by 43

Abstract P3-14-01: Phase Ib/II study of ribociclib and alpelisib and letrozole in ER+, HER2– breast cancer: Safety, preliminary efficacy and molecular analysis

Juric, D., Ismail-Khan, R. R., Campone, M., García‐Estévez, L., Becerra, C., Boer, R. D., Hamilton, E. P., Mayer, I. A., Hui, R., Lathrop, K., et al. (2016) · Cancer Research · doi:10.1158/1538-7445.sabcs15-p3-14-01 · Cited by 37

Abstract PD4-14: GDC-0077 is a selective PI3Kalpha inhibitor that demonstrates robust efficacy in PIK3CA mutant breast cancer models as a single agent and in combination with standard of care therapies

Hong, R., Edgar, K. A., Song, K., Steven, S., Young, A. E., Hamilton, P., Arrazate, A., de la Cruz, C., Chan, C., Pang, J., et al. (2018) · Cancer Research · doi:10.1158/1538-7445.sabcs17-pd4-14 · Cited by 27

PIK3CA mutations define favorable prognostic biomarkers in operable breast cancer: a systematic review and meta-analysis

Shao, Z.-M., Liu, Y., Jiang, Y., Yu, K., & Zuo, W. (2014) · OncoTargets and Therapy · doi:10.2147/ott.s60115 · Cited by 25

Molecular profiling of ER+ metastatic breast cancers to reveal association of genomic alterations with acquired resistance to CDK4/6 inhibitors.

Razavi, P., dos Anjos, C. H., Brown, D. N., Li, Q., Ping, C., Herbert, J., Colon, J., Liu, D., Mao, M., Norton, L., et al. (2019) · Journal of Clinical Oncology · doi:10.1200/jco.2019.37.15_suppl.1009 · Cited by 17

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

Olivero, A. G., Heffron, T. P., Baumgardner, M., Belvin, M. P., Ross, L. B., Blaquière, N., Bradley, E. K., Castanedo, G. M., Derynck, M. K., Do, S., et al. (2013) · Cancer Research · doi:10.1158/1538-7445.am2013-ddt02-01 · Cited by 15

PIK3CA mutations define favorable prognostic biomarkers in operable breast cancer: a systematic review and meta-analysis

Liu, Y.-R., Jiang, Y.-Z., Zuo, W.-J., Yu, K.-D., & Shao, Z.-M. (2014) · Dove Medical Press (Taylor and Francis Group) · Cited by 11

Phase I study of the PI3K/mTOR inhibitor gedatolisib (PF-05212384) in combination with docetaxel, cisplatin, and dacomitinib.

Wainberg, Z. A., Shapiro, G. I., Curigliano, G., Kristeleit, R. S., Leong, S., Alsina, M., Milella, M., Britten, C. D., Gelmon, K. A., Olszanski, A. J., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.2566 · Cited by 9

Characterization of the mechanism of action and efficacy of MEN1611 (PA799), a novel PI3K inhibitor, in breast cancer preclinical models

Fiascarelli, A., Merlino, G., Capano, S., Paoli, A., Bressan, A., Bigioni, M., Scaltriti, M., Arribas, J., Morales, C. B., Pellacani, A. U. E., et al. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz268.065 · Cited by 9

Cancer Research: 75th Anniversary of the Field's Most Highly Cited Basic Science Journal

Prendergast, G. C. (2016) · Cancer Research · doi:10.1158/0008-5472.can-15-3239 · Cited by 7

Combining PI3K and PARP inhibitors for breast and ovarian cancer treatment

Condorelli, R., & André, F. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx218 · Cited by 7

Outcome and mutational landscape of patients with PIK3CA-mutated metastatic breast cancer (mBC)

Mosele, M. F., Lusque, A., Dien, A. T., Droin, N. M., Tourneau, C. L., Lacroix, L., Bièche, I., Massard, C., Bertucci, F., & André, F. (2019) · Annals of Oncology · doi:10.1093/annonc/mdz100 · Cited by 7

Abstract A050: PIK3CA mutation status in tumor tissue and ctDNA as a biomarker for PFS in patients with HR+, HER2- ABC treated with buparlisib or placebo plus fulvestrant: results from the BELLE-2 and BELLE-3 randomized studies

Baselga, J. M., Sellami, D. B., El-Hashimy, M., Dharan, B., Wang, Y., Scheuer, N., Sankaran, B., & Leo, A. D. (2018) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-17-a050 · Cited by 5

Abstract 2160: MEN1611, a novel α-selective PI3K inhibitor in solid tumors

Merlino, G., Fiascarelli, A., Bigioni, M., Bressan, A., Irrissuto, C., Pellacani, A. U. E., Scaltriti, M., & Binaschi, M. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-2160 · Cited by 5

Will a Better Understanding of the Problem With Transformed Follicular Lymphoma Lead to Better Outcomes?

Link, B. K. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.67.4234 · Cited by 4

Targeting PI3K/Akt signal transduction for cancer therapy

He, Y., Sun, M., Zhang, G. G., Yang, J., Chen, K. S., Xu, W. W., & Li, B. (2021) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-021-00828-5 · Cited by 2,045

Advancements in clinical aspects of targeted therapy and immunotherapy in breast cancer

Ye, F., Dewanjee, S., Li, Y., Jha, N. K., Chen, Z., Kumar, A., vishakha, V., Behl, T., Jha, S. K., & Tang, H. (2023) · Molecular Cancer · doi:10.1186/s12943-023-01805-y · Cited by 619

PI3K inhibitors are finally coming of age

Vanhaesebroeck, B., Perry, M. W. D., Brown, J. R., André, F., & Okkenhaug, K. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00209-1 · Cited by 494

Activation of PI3K/AKT/mTOR Pathway Causes Drug Resistance in Breast Cancer

Dong, C., Wu, J., Chen, Y., Nie, J., & Chen, C. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.628690 · Cited by 404

Long non-coding RNAs towards precision medicine in gastric cancer: early diagnosis, treatment, and drug resistance

Li, Y., Xu, Z., Ruan, S., Mo, S., Qin, J., & Cheng, X. (2020) · Molecular Cancer · doi:10.1186/s12943-020-01219-0 · Cited by 330

PI3K Inhibitors in Breast Cancer Therapy

Ellis, H., & Ma, C. X. (2019) · Current Oncology Reports · doi:10.1007/s11912-019-0846-7 · Cited by 226

PI3K inhibition in breast cancer: Identifying and overcoming different flavors of resistance

Vitale, S. R., Martorana, F., Stella, S., Motta, G., Inzerilli, N., Massimino, M., Tirrò, E., Manzella, L., & Vigneri, P. G. (2021) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2021.103334 · Cited by 47

Alpelisib to treat breast cancer

Copur, M. S. (2020) · Drugs of today · doi:10.1358/dot.2020.56.6.3137526 · Cited by 25

Recent Advances in PI3K Inhibitor HR+/HER2- Advanced Breast Cancer, A Review ArticlePreprint

Mukherjee, D., & Mukherjee, K. K. (2020) · SSRN Electronic Journal

Expert consensus on the clinical application of PI3K/AKT/mTOR inhibitors in the treatment of advanced breast cancer

The Society of Clinical Research of Oncology Medications of China Anticancer Association, & Breast Cancer Expert Committee of National Cancer Quality Control Center (2022) · Cancer Innovation · doi:10.1002/cai2.10 · Cited by 10