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The PI3K inhibitor buparlisib suppresses osteoclast formation and tumour cell growth in bone metastasis of lung cancer, as evidenced by multimodality molecular imaging.

Wang S, Niu X, Bao X, Wang Q, Zhang J, Lu S, Wang Y, Xu L, Wang M, Zhang J.

Oncol Rep. 2019 May;41(5):2636-2646. doi: 10.3892/or.2019.7080. Epub 2019 Mar 20.


Treatment with the PI3K inhibitor buparlisib (NVP-BKM120) suppresses the growth of established patient-derived GBM xenografts and prolongs survival in nude rats.

Netland IA, Førde HE, Sleire L, Leiss L, Rahman MA, Skeie BS, Miletic H, Enger PØ, Goplen D.

J Neurooncol. 2016 Aug;129(1):57-66. doi: 10.1007/s11060-016-2158-1. Epub 2016 Jun 9.


Buparlisib with thoracic radiotherapy and its effect on tumour hypoxia: A phase I study in patients with advanced non-small cell lung carcinoma.

McGowan DR, Skwarski M, Bradley KM, Campo L, Fenwick JD, Gleeson FV, Green M, Horne A, Maughan TS, McCole MG, Mohammed S, Muschel RJ, Ng SM, Panakis N, Prevo R, Strauss VY, Stuart R, Tacconi EMC, Vallis KA, McKenna WG, Macpherson RE, Higgins GS.

Eur J Cancer. 2019 Apr 13;113:87-95. doi: 10.1016/j.ejca.2019.03.015. [Epub ahead of print]


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 SA, Iwata H, Cortés J, De Laurentiis M, Jiang Z, Arteaga CL, Jonat W, Clemons M, Ito Y, Awada A, Chia S, Jagiełło-Gruszfeld A, Pistilli B, Tseng LM, Hurvitz S, Masuda N, Takahashi M, Vuylsteke P, Hachemi S, Dharan B, Di Tomaso E, Urban P, Massacesi C, Campone M.

Lancet Oncol. 2017 Jul;18(7):904-916. doi: 10.1016/S1470-2045(17)30376-5. Epub 2017 May 30. Erratum in: Lancet Oncol. 2019 Feb;20(2):e71-e72.


The effect of the PI3K inhibitor BKM120 on tumour growth and osteolytic bone disease in multiple myeloma.

Martin SK, Gan ZY, Fitter S, To LB, Zannettino AC.

Leuk Res. 2015 Mar;39(3):380-7. doi: 10.1016/j.leukres.2014.12.015. Epub 2015 Jan 7.


Evaluation of In Vitro Activity of the Class I PI3K Inhibitor Buparlisib (BKM120) in Pediatric Bone and Soft Tissue Sarcomas.

Anderson JL, Park A, Akiyama R, Tap WD, Denny CT, Federman N.

PLoS One. 2015 Sep 24;10(9):e0133610. doi: 10.1371/journal.pone.0133610. eCollection 2015.


Targeting survival and cell trafficking in multiple myeloma and Waldenstrom macroglobulinemia using pan-class I PI3K inhibitor, buparlisib.

Sahin I, Azab F, Mishima Y, Moschetta M, Tsang B, Glavey SV, Manier S, Zhang Y, Sacco A, Roccaro AM, Azab AK, Ghobrial IM.

Am J Hematol. 2014 Nov;89(11):1030-6. doi: 10.1002/ajh.23814. Epub 2014 Aug 12.


Micro-CT combined with bioluminescence imaging: a dynamic approach to detect early tumor-bone interaction in a tumor osteolysis murine model.

Fritz V, Louis-Plence P, Apparailly F, Noël D, Voide R, Pillon A, Nicolas JC, Müller R, Jorgensen C.

Bone. 2007 Apr;40(4):1032-40. Epub 2006 Dec 15.


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 JF, Canon JL, De Braud F, Grossi F, De Pas T, Gray JE, Su WC, Felip E, Yoshioka H, Gridelli C, Dy GK, Thongprasert S, Reck M, Aimone P, Vidam GA, Roussou P, Wang YA, Di Tomaso E, Soria JC.

J Thorac Oncol. 2015 Sep;10(9):1319-1327. doi: 10.1097/JTO.0000000000000607.


Differential expression of the RANKL/RANK/OPG system is associated with bone metastasis in human non-small cell lung cancer.

Peng X, Guo W, Ren T, Lou Z, Lu X, Zhang S, Lu Q, Sun Y.

PLoS One. 2013;8(3):e58361. doi: 10.1371/journal.pone.0058361. Epub 2013 Mar 13.


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, O'Shaughnessy J, Hegg R, Manikhas A, Shtivelband M, Krivorotko P, Batista López N, Campone M, Ruiz Borrego M, Khan QJ, Beck JT, Ramos Vázquez M, Urban P, Goteti S, Di Tomaso E, Massacesi C, Delaloge S.

Ann Oncol. 2017 Feb 1;28(2):313-320. doi: 10.1093/annonc/mdw562.


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 IA, Abramson VG, Isakoff SJ, Forero A, Balko JM, Kuba MG, Sanders ME, Yap JT, Van den Abbeele AD, Li Y, Cantley LC, Winer E, Arteaga CL.

J Clin Oncol. 2014 Apr 20;32(12):1202-9. doi: 10.1200/JCO.2013.54.0518. Epub 2014 Mar 24.


The anticancer effects of Cucurbitacin I inhibited cell growth of human non‑small cell lung cancer through PI3K/AKT/p70S6K pathway.

Zhu X, Huang H, Zhang J, Liu H, Ao R, Xiao M, Wu Y.

Mol Med Rep. 2018 Feb;17(2):2750-2756. doi: 10.3892/mmr.2017.8141. Epub 2017 Nov 22.


Spatiotemporal assessment of spontaneous metastasis formation using multimodal in vivo imaging in HER2+ and triple negative metastatic breast cancer xenograft models in mice.

Fricke IB, De Souza R, Costa Ayub L, Francia G, Kerbel R, Jaffray DA, Zheng J.

PLoS One. 2018 May 3;13(5):e0196892. doi: 10.1371/journal.pone.0196892. eCollection 2018.


Loss of RUNX3 expression promotes cancer-associated bone destruction by regulating CCL5, CCL19 and CXCL11 in non-small cell lung cancer.

Kim HJ, Park J, Lee SK, Kim KR, Park KK, Chung WY.

J Pathol. 2015 Dec;237(4):520-31. doi: 10.1002/path.4597. Epub 2015 Sep 28.


BENC-511, a novel PI3K inhibitor, suppresses metastasis of non-small cell lung cancer cells by modulating β-catenin/ZEB1 regulatory loop.

Zhang Q, Zhou L, Guan Y, Cheng Y, Han X.

Chem Biol Interact. 2018 Oct 1;294:18-27. doi: 10.1016/j.cbi.2018.08.010. Epub 2018 Aug 17.


RANKL inhibition blocks osteolytic lesions and reduces skeletal tumor burden in models of non-small-cell lung cancer bone metastases.

Miller RE, Jones JC, Tometsko M, Blake ML, Dougall WC.

J Thorac Oncol. 2014 Mar;9(3):345-54. doi: 10.1097/JTO.0000000000000070.


Buparlisib is a brain penetrable pan-PI3K inhibitor.

de Gooijer MC, Zhang P, Buil LCM, Çitirikkaya CH, Thota N, Beijnen JH, van Tellingen O.

Sci Rep. 2018 Jul 17;8(1):10784. doi: 10.1038/s41598-018-29062-w.


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 Pena L, Nekljudova V, Zardavas D, Michiels S, Denkert C, Rezai M, Bermejo B, Untch M, Lee SC, Turri S, Urban P, Kümmel S, Steger G, Gombos A, Lux M, Piccart MJ, Von Minckwitz G, Baselga J, Loi S.

Eur J Cancer. 2017 Nov;85:133-145. doi: 10.1016/j.ejca.2017.08.020. Epub 2017 Sep 17.

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