Research Topics
| B P ImbimboSummaryAffiliation: Chiesi Farmaceutici Country: Italy Publications
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Detail Information
Publications
Therapeutic intervention for Alzheimer's disease with γ-secretase inhibitors: still a viable option?Bruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Via Palermo 26 A, Parma, Italy
Expert Opin Investig Drugs 20:325-41. 2011..Understanding the reasons for this failure may be important for future research on effective treatments for this devastating disease...
Conformation-sensitive antibodies against alzheimer amyloid-beta by immunization with a thioredoxin-constrained B-cell epitope peptideNadia Moretto
Department of Biochemistry and Molecular Biology, Chiesi Farmaceutici, University of Parma, 43100 Parma, Italy
J Biol Chem 282:11436-45. 2007..The data indicate that a conformational epitope shared by oligomers and fibrils can be mimicked by a thioredoxin-constrained Abeta fragment repeat and identify Trx(Abeta15)4 as a promising new tool for AD immunotherapy...- In vitro and in vivo profiling of CHF5022 and CHF5074 Two beta-amyloid1-42 lowering agentsBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Via Palermo 26 A, 43100 Parma, Italy
Pharmacol Res 55:318-28. 2007..105) with CHF5022 concentration in the brain. CHF5022 and CHF5074 thus appear to have a promising in vitro and in vivo profile. This warrants further evaluation of their long-term effects on Abeta brain pathology... - 1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicityBruno P Imbimbo
Research and Development, Chiesi Farmaceutici, Via Palermo 26 A, 43100 Parma, Italy
J Pharmacol Exp Ther 323:822-30. 2007..CHF5074 is therefore a promising therapeutic agent for Alzheimer's disease... - Therapeutic potential of gamma-secretase inhibitors and modulatorsBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Parma, Italy
Curr Top Med Chem 8:54-61. 2008..A large ongoing Phase 3 study with (R)-flurbiprofen, a claimed selective Abeta42 lowering agent, will tell us if allosteric modulation of gamma-secretase is clinically effective... - Solanezumab for the treatment of mild-to-moderate Alzheimer's diseaseBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Parma, Italy
Expert Rev Clin Immunol 8:135-49. 2012.... - γ-secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopesBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Via Palermo 26 A, 43100 Parma, Italy
Curr Top Med Chem 11:1555-70. 2011..New Notch-sparing γ-secretase inhibitors and more potent, more brain penetrant γ-secretase modulators are being developed with the hope of overcoming the previous setbacks... - An update on the efficacy of non-steroidal anti-inflammatory drugs in Alzheimer's diseaseBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Via Palermo 26 A, 43100 Parma, Italy
Expert Opin Investig Drugs 18:1147-68. 2009.... - Semagacestat, a gamma-secretase inhibitor for the potential treatment of Alzheimer's diseaseBruno P Imbimbo
Chiesi Farmaceutici SpA, Research and Development Department, Via Palermo 26 A, 43100 Parma, Italy
Curr Opin Investig Drugs 10:721-30. 2009..Semagacestat is the most advanced gamma-secretase inhibitor and represents a major hope among therapies designed to slow the rate of cognitive decline of patients with AD... - Why did tarenflurbil fail in Alzheimer's disease?Bruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Parma, Italy
J Alzheimers Dis 17:757-60. 2009..In addition, based on previous negative results with several anti-inflammatory drugs in AD, it is hypothesized that the residual anti-inflammatory activity of tarenflurbil may have a detrimental effect on disease progression... 
CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's diseaseB P Imbimbo
Research and Development, Chiesi Farmaceutici, Via Palermo, Parma, Italy
Br J Pharmacol 156:982-93. 2009....- Pharmacodynamic-tolerability relationships of cholinesterase inhibitors for Alzheimer's diseaseB P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Parma, Italy
CNS Drugs 15:375-90. 2001..Other contributing pharmacodynamic factors are the rate of onset of and fluctuations in acetylcholinesterase inhibition at steady state... - The potential role of non-steroidal anti-inflammatory drugs in treating Alzheimer's diseaseBruno P Imbimbo
Chiesi Farmaceutici, Research and Development Department, Via Palermo 26 A, 43100 Parma, Italy
Expert Opin Investig Drugs 13:1469-81. 2004..Thus, new NSAID analogues are being developed with potent and selective inhibitory activity on Abeta42 but with either lack of COX inhibitory activity or reduced gastrointestinal toxicity potential... - Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretionIlaria Peretto
Research and Development, Chiesi Farmaceutici S.p.A, Via Palermo 26/A, 43100 Parma, Italy
J Med Chem 48:5705-20. 2005..Studies in a transgenic mice model of AD showed that selected compounds significantly decreased plasma Abeta42 concentrations. These new flurbiprofen analogues represent potential drug candidates to be developed for the treatment of AD... - CHF5074, a novel gamma-secretase modulator, restores hippocampal neurogenesis potential and reverses contextual memory deficit in a transgenic mouse model of Alzheimer's diseaseBruno P Imbimbo
Research and Development, Chiesi Farmaceutici, Parma, Italy
J Alzheimers Dis 20:159-73. 2010..040). These effects were associated to a complete reversal of contextual memory deficit (p=0.006). Contextual memory significantly correlated with synaptophysin immunoreactivity in the cortex (r=0.548, p=0.0038)... - Pathophysiology of Alzheimer's diseaseBruno P Imbimbo
Research and Development Department, Chiesi Farmaceutici, Parma, Italy
Neuroimaging Clin N Am 15:727-53, ix. 2005..Progress is needed in understanding the mechanisms that link beta-amyloid accumulation and neuronal death. The next 5 years will be crucial in this respect... - Safety, pharmacokinetics, and pharmacodynamics of CHF 3381, a novel N-methyl-D-aspartate antagonist, after single oral doses in healthy subjectsAntoine Tarral
Biotrial, Technopole Atalante Villejean, Rennes, France
J Clin Pharmacol 43:901-11. 2003..The ingestion of food seems to not affect the extent of absorption of the drug. Minor effects on the central nervous system were detected at doses equal to or greater than 300 mg... - High throughput screening of beta-amyloid secretion inhibitors using homogenous time-resolved fluorescenceHugo Albrecht
Discovery Partners International, Integrated Drug Discovery Division, Allschwil, Switzerland
Comb Chem High Throughput Screen 7:745-56. 2004..7 were achieved in a 384-well format. High throughput screening of 56,913 potential Abeta production inhibitors led to identification of new non-cytotoxic and cell permeable compounds with potencies in the submicromolar range... - Steady-state pharmacokinetics and pharmacodynamics of CHF3381, a novel antineuropathic pain agent, in healthy subjectsBeatrice Astruc
Biotrial, 7 9 rue Jean Louis Bertrand, 35000 Rennes, France
Br J Clin Pharmacol 59:405-14. 2005..To evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic profiles of CHF3381, a dual NMDA and MAO-A inhibitor, after multiple oral doses in healthy subjects... - Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1)Ilaria Peretto
NiKem Research, Via Zambeletti 25, 20021 Baranzate, Milan, Italy
J Med Chem 50:1571-83. 2007..8 nM and for M2 receptor Ki = 1141 nM. Functional in vitro studies on selected compounds confirmed the antagonist activity toward the M3 receptor and functional selectivity toward the M2 receptor...