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A Patnaik, L J Appleman, A W Tolcher, K P Papadopoulos, M Beeram, D W Rasco, G J Weiss, J C Sachdev, M Chadha, M Fulk, S Ejadi, J M Mountz, M T Lotze, F G S Toledo, E Chu, M Jeffers, C Peña, C Xia, S Reif, I Genvresse, R K Ramanathan
BACKGROUND: To evaluate the safety, tolerability, pharmacokinetics, and maximum tolerated dose (MTD) of copanlisib, a phosphatidylinositol 3-kinase inhibitor, in patients with advanced solid tumors or non-Hodgkin's lymphoma (NHL). PATIENTS AND METHODS: Phase I dose-escalation study including patients with advanced solid tumors or NHL, and a cohort of patients with type 2 diabetes mellitus. Patients received three weekly intravenous infusions of copanlisib per 28-day cycle over the dose range 0...
October 2016: Annals of Oncology: Official Journal of the European Society for Medical Oncology
Seiichi Okabe, Tetsuzo Tauchi, Yuko Tanaka, Juri Sakuta, Kazuma Ohyashiki
ABL tyrosine kinase inhibitor (TKI) therapy has improved the survival of patients with Philadelphia (Ph) chromosome-positive leukemia. However, ABL TKIs cannot eradicate leukemia stem cells. Therefore, new therapeutic approaches for Ph-positive leukemia are needed. Aberrant activation of phosphoinositide 3-kinase (PI3K) signaling is important for the initiation and maintenance of human cancers. Copanlisib (BAY80-6946) is a potent inhibitor of PI3Kα and PI3K-δ. Here we investigated the efficacy of combination therapy of copanlisib with an ABL TKI (imatinib, nilotinib, or ponatinib) using BCR-ABL-positive cells...
July 14, 2016: Oncotarget
William J Scott, Martin F Hentemann, R Bruce Rowley, Cathy O Bull, Susan Jenkins, Ann M Bullion, Jeffrey Johnson, Anikó Redman, Arthur H Robbins, William Esler, R Paul Fracasso, Timothy Garrison, Mark Hamilton, Martin Michels, Jill E Wood, Dean P Wilkie, Hong Xiao, Joan Levy, Enrico Stasik, Ningshu Liu, Martina Schaefer, Michael Brands, Julien Lefranc
The phosphoinositide 3-kinase (PI3K) pathway is aberrantly activated in many disease states, including tumor cells, either by growth factor receptor tyrosine kinases or by the genetic mutation and amplification of key pathway components. A variety of PI3K isoforms play differential roles in cancers. As such, the development of PI3K inhibitors from novel compound classes should lead to differential pharmacological and pharmacokinetic profiles and allow exploration in various indications, combinations, and dosing regimens...
July 19, 2016: ChemMedChem
Laurence Booth, Thomas Albers, Jane L Roberts, Mehrad Tavallai, Andrew Poklepovic, Iryna O Lebedyeva, Paul Dent
We have recently demonstrated that multi-kinase inhibitors such as sorafenib and pazopanib can suppress the detection of chaperones by in situ immuno-fluorescence, which is further enhanced by phosphodiesterase 5 inhibitors. Sorafenib and pazopanib inhibited the HSP90 ATPase activity with IC50 values of ~1.0 μM and ~75 nM, respectively. Pazopanib docked in silico with two possible poses into the HSP90 ATP binding pocket. Pazopanib and sildenafil combined to reduce the total protein levels of HSP1H/p105 and c-MYC and to reduce their co-localization...
May 31, 2016: Oncotarget
Elisa Göckeritz, Susan Kerwien, Michael Baumann, Marion Wigger, Verena Vondey, Lars Neumann, Thomas Landwehr, Clemens M Wendtner, Christian Klein, Ningshu Liu, Michael Hallek, Lukas P Frenzel, Günter Krause
Pharmacological inhibition of phosphatiylinositide-3-kinase (PI3K)-mediated signaling holds great promise for treating chronic lymphocytic leukemia (CLL). Therefore we assessed three structurally related PI3K inhibitors targeting the PI3K-δ isoform for their ability to inhibit the survival of freshly isolated CLL cells. The purely PI3K-δ-selective inhibitor idelalisib was compared to copanlisib (BAY 80-6946) and duvelisib (IPI-145), with isoform target profiles that additionally include PI3K-α or PI3K-γ, respectively...
November 1, 2015: International Journal of Cancer. Journal International du Cancer
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