Results 31 to 40 of about 114,558 (301)

Phase 1 dose escalation study of the allosteric AKT inhibitor BAY 1125976 in advanced solid cancer-Lack of association between activating AKT mutation and AKT inhibition-derived efficacy [PDF]

, 2019
This open-label, phase I first-in-human study (NCT01915576) of BAY 1125976, a highly specific and potent allosteric inhibitor of AKT1/2, aimed to evaluate the safety, pharmacokinetics, and maximum tolerated dose of BAY 1125976 in patients with advanced ...
Boix, Oliver, Hess, Dagmar, Hurvitz, Sara A, Joerger, Markus, Lagkadinou, Eleni, Ma, Cynthia, Moulder, Stacy, Ocker, Matthias, Rentzsch, Christine, Rudolph, Marion, Schneeweiss, Andreas, Thiele, Silke, Tsimberidou, Apostolia M, Varga, Andrea, Wilkinson, Gary   +14 more
core   +3 more sources

Narrow temporal therapeutic window for NMDA antagonist protection against focal cerebral ischaemia

Neurobiology of Disease, 1995
N-methyl-d-aspartate (NMDA) receptor antagonists have been shown to protect against focal cerebral ischaemia when administered either before or soon after the onset of ischaemia.
Gary K. Steinberg, Nariman Panahian, Miguel A. Pérez-Pinzón, Guo-Hua Sun, Marlene W. Modi, Jerry Sepinwall   +5 more
doaj   +1 more source

Nifurtimox Is Effective Against Neural Tumor Cells and Is Synergistic with Buthionine Sulfoximine. [PDF]

, 2016
Children with aggressive neural tumors have poor survival rates and novel therapies are needed. Previous studies have identified nifurtimox and buthionine sulfoximine (BSO) as effective agents in children with neuroblastoma and medulloblastoma.
Du, Michael, Scorsone, Kathleen A, Woodfield, Sarah E, Zage, Peter E, Zhang, Linna   +4 more
core   +1 more source

A Phase I Study of Abiraterone Acetate Combined with BEZ235, a Dual PI3K/mTOR Inhibitor, in Metastatic Castration Resistant Prostate Cancer. [PDF]

, 2017
Lessons learnedThe combination of standard dose abiraterone acetate and BEZ235, a pan-class I PI3K and mTORC1/2 inhibitor, was poorly tolerated in men with progressive mCRPC.Although the clinical development of BEZ235 has been discontinued in prostate ...
Friedlander, Terence, Hsieh, Andrew C, Kim, Won, Lin, Amy M, Louttit, Mirela, Ryan, Charles J, Wei, Xiao X   +6 more
core   +1 more source

Oral Apolipoprotein A-I Mimetic D-4F Lowers HDL-Inflammatory Index in High-Risk Patients: A First-in-Human Multiple-Dose, Randomized Controlled Trial. [PDF]

, 2017
A single dose of the apolipoprotein (apo)A-I mimetic peptide D-4F rendered high-density lipoprotein (HDL) less inflammatory, motivating the first multiple-dose study. We aimed to assess safety/tolerability, pharmacokinetics, and pharmacodynamics of daily,
Bloedon, LeAnne T., Duffy, Danielle, Dunbar, Richard L., Fogelman, Alan M., Movva, Rajesh, Navab, Mohamad, Norris, Robert B., Rader, Daniel J.   +7 more
core   +2 more sources

The pharmacokinetics of the injectable dosage form of GK-2 in rabbits

Фармакокинетика и Фармакодинамика, 2020
The pharmacokinetics of the nerve growth factor mimetic GK-2 (dimeric dipeptide mimetic of the 4-th loop NGF, a derivative of fluoro-substituted 5-[2-(5-fluoropyrid-3-yl) -ethyl)]-2,8-dimethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole) in rabbits after a
R. V. Shevchenko, A. A. Litvin, G. B. Kolyvanov, P. O. Bochkov, O. G. Gribakina, A. A. Novitskiy, V. P. Zherdev   +6 more
doaj   +1 more source

Modeling of Large Pharmacokinetic Data Using Nonlinear Mixed-Effects: A Paradigm Shift in Veterinary Pharmacology. A Case Study With Robenacoxib in Cats [PDF]

, 2016
The objective of this study was to model the pharmacokinetics (PKs) of robenacoxib in cats using a nonlinear mixed‐effects (NLME) approach, leveraging all available information collected from cats receiving robenacoxib s.c.
Beal, Benet, Dziak, Fink, Giraudel, Jung, King, Lainesse, Lascelles, Lavielle, Lavielle, Lees, Lehr, Martin-Jiménez, Mochel, Mochel, Pelligand, Pelligand, Savic, Sheiner, Sheiner, Sheiner, Silber, Thomasy, Toutain, Toutain, Toutain, Xu   +27 more
core   +2 more sources

A phase I pharmacokinetic and pharmacodynamic study of the oral mitogen-activated protein kinase kinase (MEK) inhibitor, WX-554, in patients with advanced solid tumours [PDF]

, 2016
Purpose: We performed a multi-centre phase I study to assess the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of the orally available small molecule mitogen-activated protein kinase kinase (MEK) 1/2 inhibitor, WX-554, and to determine the ...
Allen, Rodger, Anthoney, Alan, Banerji, Udai, Bevan, Paul, Boddy, Alan V., Buerkle, Markus, Coyle, Vicky, Cresti, Nicola, Dean, Emma, Drew, Yvette, Evans, T.R. Jefferey, Greystoke, Alastair, Griffin, Melanie J., Jamieson, David, Mala, Carola, Merriman, Mark, Plummer, Ruth, Ranson, Malcolm, Rodgers, Lisa, Sludden, Julieann, Swales, Karen, Wilson, Richard H.   +21 more
core   +2 more sources

Overcoming the challenges of cancer drug resistance through bacterial-mediated therapy. [PDF]

, 2019
Despite tremendous efforts to fight cancer, it remains a major public health problem and a leading cause of death worldwide. With increased knowledge of cancer pathways and improved technological platforms, precision therapeutics that specifically target
Bivona, Trever G, Chang, Samantha, Hernández, Amanda C, Keasling, Jay D, Kothari, Ankita, Mao, Jian-Hua, Snijders, Antoine M, Wang, Jessica, Zargar, Amin   +8 more
core   +1 more source

A novel approach to quantitate biodistribution and transduction of adeno-associated virus gene therapy using radiolabeled AAV vectors in mice

Molecular Therapy: Methods & Clinical Development
An understanding of recombinant adeno-associated virus (AAV) biodistribution profiles is an important element of a preclinical development program. Here, we have developed a radiolabeling strategy utilizing the co-delivery of 125I (non-residualizing) and
Hongzhi Wang, Ran Li, Shraddha Sadekar, Amrita V. Kamath, Ben-Quan Shen   +4 more
doaj   +1 more source