Avagacestat (BMS-708163)性质、用途与生产工艺 生物活性 Avagacestat (BMS-708163)是口服生物有效的,选择性的γ-分泌酶抑制剂,作用于Aβ40和Aβ42时,IC50分别为0.3 nM和0.27 nM,比作用于Notch选择性高193倍。Phase 2。 体外研究 BMS-708163 抑制Notch 过程时显示出低选择性。 体内研究 鼠和犬口服处理...
The logit model was then used to simulate the expected AE-related dropout rate at intermediate doses not tested in the phase 2 study. Conclusions The exposure-AEDCs relationship, using a logistic regression approach, indicated an increase in the probability of AEDCs with increased avagacestat ...
Background: BMS-708163, in Phase II development for Alzheimer's Disease, selectively inhibits A尾 synthesis relative to Notch, and is a potent and orally active 纬-secretase inhibitor. The primary objective of this open-label, nonrandomized, single-sequence study was to assess the effects of ...
(2011) Safety and tolerability of BMS-708163 in a phase II study in mild-to-moderate Alzheimer's disease. Alzheimer's Dementia 7 (Supp), S695-S696.Schwinning, S. & Kelly, C.K. ( 2013 ) Plant competition, temporal niches and implications for productivity and adaptability to climate ...
Single doses of BMS-708163 were chosen to match (200 mg), or exceed (800 mg), peak concentrations achieved at steady state in Phase 2 studies following 125 mg QD. Two distinct sets of ECG data were collected during the study: serial triplicate ECG measurements and single 12-lead safety ...
A phase ii study of the gamma-secretase inhibitor avagacestat (bms-708163) in predementia Alzheimer's disease. Alzheimers Dement. J. Alzheimers Assoc. 2013, 9, 283. [CrossRef]
Background The 纬 -secretase inhibitor (GSI) avagacestat, which selectively inhibits amyloid-beta (A尾) synthesis, was evaluated in patients with predementia Alzheimer's disease in a multicenter, double-blind, phase 2 safety trial (CN156-018). 纬-Secretase can also cleave Notch transmembrane ...
Sperling R, Bronen R, Greenberg S, et al. Three cases of apparent vasogenic edema (VE) from a phase 2 clinical trial of the gamma secretase inhibitor BMS-708163 in patients with mild-to-moderate AD. Alzheimers Dement 2011;7(suppl):S377...