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Copanlisib

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https://www.readbyqxmd.com/read/28714036/pharmacokinetics-of-intravenous-pan-class-i-phosphatidylinositol-3-kinase-pi3k-inhibitor-14-c-copanlisib-bay-80-6946-in-a-mass-balance-study-in-healthy-male-volunteers
#1
Michael Gerisch, Thomas Schwarz, Dieter Lang, Gabriele Rohde, Stefanie Reif, Isabelle Genvresse, Susanne Reschke, Dorina van der Mey, Camille Granvil
PURPOSE: To determine the pharmacokinetics of radiolabeled copanlisib (BAY 80-6946) in healthy male volunteers and to investigate the disposition and biotransformation of copanlisib. METHODS: A single dose of 12 mg copanlisib containing 2.76 MBq [(14)C]copanlisib was administered as a 1-h intravenous infusion to 6 volunteers with subsequent sampling up to 34 days. Blood, plasma, urine and feces were collected to monitor total radioactivity, parent compound and metabolites...
July 11, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28633365/phase-ii-study-of-copanlisib-a-pi3k-inhibitor-in-relapsed-or-refractory-indolent-or-aggressive-lymphoma
#2
M Dreyling, F Morschhauser, K Bouabdallah, D Bron, D Cunningham, S E Assouline, G Verhoef, K Linton, C Thieblemont, U Vitolo, F Hiemeyer, M Giurescu, J Garcia-Vargas, I Gorbatchevsky, L Liu, K Koechert, C Peña, M Neves, B H Childs, P L Zinzani
Background: Copanlisib is a pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor with predominant activity against the α- and δ- isoforms. Patients and methods: This phase II study evaluated the response rate of copanlisib administered intravenously on days 1, 8, and 15 of a 28-day cycle, in patients with indolent or aggressive malignant lymphoma. Archival tumor tissues were used for immunohistochemistry, gene-expression profiling, and mutation analysis...
June 14, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28288710/possible-novel-agents-in-marginal-zone-lymphoma
#3
REVIEW
Pier Luigi Zinzani, Alessandro Broccoli
Efficacy, safety and mechanisms of action of novel agents in marginal zone lymphoma patients, both with a nodal and extranodal presentation, are reviewed. Data on lenalidomide, bortezomib and (90)yttrium-ibrutumomab tiuxetan are obtained from trials specifically designed for patients affected by marginal zone lymphoma and with various disease presentations. The role of targeted agents, such as obinutuzumab, ibrutinib and idelalisib, and of some very new drugs (venetoclax, copanlisib, ublituximab and TGR-1202) is also discussed, taking into account the most relevant experiences in patients with indolent non-Hodgkin's lymphomas...
March 2017: Best Practice & Research. Clinical Haematology
https://www.readbyqxmd.com/read/28073005/simultaneous-inhibition-of-pi3k%C3%AE-and-pi3k%C3%AE-induces-abc-dlbcl-regression-by-blocking-bcr-dependent-and-independent-activation-of-nf-%C3%AE%C2%BAb-and-akt
#4
Juliane Paul, Maurice Soujon, Antje M Wengner, Sabine Zitzmann-Kolbe, Andrea Sturz, Katja Haike, Koh Hui Keng Magdalene, Sze Huey Tan, Martin Lange, Soo Yong Tan, Dominik Mumberg, Soon Thye Lim, Karl Ziegelbauer, Ningshu Liu
Compared with follicular lymphoma, high PI3Kα expression was more prevalent in diffuse large B cell lymphoma (DLBCL), although both tumor types expressed substantial PI3Kδ. Simultaneous inhibition of PI3Kα and PI3Kδ dramatically enhanced the anti-tumor profile in ABC-DLBCL models compared with selective inhibition of PI3Kδ, PI3Kα, or BTK. The anti-tumor activity was associated with suppression of p-AKT and a mechanism of blocking nuclear factor-κB activation driven by CD79(mut), CARD11(mut), TNFAIP3(mut), or MYD88(mut)...
January 9, 2017: Cancer Cell
https://www.readbyqxmd.com/read/27915408/a-phase-i-study-of-intravenous-pi3k-inhibitor-copanlisib-in-japanese-patients-with-advanced-or-refractory-solid-tumors
#5
Toshihiko Doi, Nozomu Fuse, Takayuki Yoshino, Takashi Kojima, Hideaki Bando, Hideaki Miyamoto, Masato Kaneko, Motonobu Osada, Atsushi Ohtsu
PURPOSE: To evaluate the safety, tolerability, pharmacokinetics, and efficacy of the intravenously administered pan-PI3K inhibitor copanlisib in Japanese patients with advanced or refractory solid tumors. METHODS: A Phase I open-label study in Japanese patients with advanced or refractory solid tumors was carried out. Patients received a single intravenous dose of either copanlisib 0.4 mg/kg or copanlisib 0.8 mg/kg, dosed intermittently on days 1, 8, and 15 of a 28-day cycle...
January 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/27672108/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
#6
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
https://www.readbyqxmd.com/read/27437766/combination-therapy-with-copanlisib-and-abl-tyrosine-kinase-inhibitors-against-philadelphia-chromosome-positive-resistant-cells
#7
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...
August 16, 2016: Oncotarget
https://www.readbyqxmd.com/read/27310202/discovery-and-sar-of-novel-2-3-dihydroimidazo-1-2-c-quinazoline-pi3k-inhibitors-identification-of-copanlisib-bay-80-6946
#8
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
https://www.readbyqxmd.com/read/27259258/multi-kinase-inhibitors-interact-with-sildenafil-and-erbb1-2-4-inhibitors-to-kill-tumor-cells-in-vitro-and-in-vivo
#9
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...
June 28, 2016: Oncotarget
https://www.readbyqxmd.com/read/25912635/efficacy-of-phosphatidylinositol-3-kinase-inhibitors-with-diverse-isoform-selectivity-profiles-for-inhibiting-the-survival-of-chronic-lymphocytic-leukemia-cells
#10
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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