Efficacy and Safety of ABT-126 in Subjects with Mild-to-Moderate Alzheimer's Disease on Stable Doses of Acetylcholinesterase Inhibitors: A Randomized, Double-Blind, Placebo-Controlled Study

被引:29
作者
Florian, Hana [1 ]
Meier, Andreas [1 ,5 ]
Gauthier, Serge [2 ]
Lipschitz, Stanley [3 ]
Lin, Yunzhi [1 ,6 ]
Tang, Qi [1 ]
Othman, Ahmed A. [1 ,4 ]
Robieson, Weining Z. [1 ]
Gault, Laura M. [1 ]
机构
[1] AbbVie Inc, 1 North Waukegan Rd,Bldg AP31-1, N Chicago, IL 60064 USA
[2] McGill Univ, Res Ctr Studies Aging, Montreal, PQ, Canada
[3] Dr Stanley Lipschitz Clin, Rosebank, Johannesburg, South Africa
[4] Cairo Univ, Fac Pharm, Dept Pharmaceut, Cairo, Egypt
[5] Pfizer Inc, Cambridge, MA USA
[6] Takeda Pharmaceut USA Inc, Deerfield, IL USA
关键词
ABT-126; Acetylcholinesterase inhibitors; alzheimer's disease; dementia; nicotinic acetylcholine receptors; NICOTINIC PARTIAL AGONIST; ANTIPSYCHOTIC EFFICACY; RECEPTOR; SCHIZOPHRENIA; COGNITION; DEFICITS; EVP-6124; MEMORY; GTS-21; TRIAL;
D O I
10.3233/JAD-150978
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Background: ABT-126 is a potent, selective alpha 7 nicotinic acetylcholine receptor agonist with putative procognitive effects as a monotherapy in treating Alzheimer's disease (AD). Objective: This randomized, double-blind, placebo-controlled multicenter study (NCT01549834) investigated the efficacy and safety of ABT-126 in subjects with mild-to-moderate AD who were taking stable doses of acetylcholinesterase inhibitors (AChEIs). Methods: Subjects received 25mg ABT-126 (n = 143), 75 mg ABT-126 (n = 145), or placebo (n = 146) once daily for 24 weeks. Subjects who completed the 24-week double-blind study were eligible to enroll in a 28-week open-label extension study (NCT01690195) and received 75mg ABT-126 daily. The primary efficacy endpoint was the change from baseline to week 24 in the 11-item total score of the Alzheimer's Disease Assessment Scale-Cognitive Subscale (ADAS-Cog). Results: Neither dose of ABT-126 demonstrated significant improvement compared with placebo in the primary efficacy endpoint. However, 25 mg ABT-126 demonstrated significant improvement compared with placebo in ADAS-Cog scores at week 4 (least squares mean difference, -1.21; standard error, 0.51; p < 0.010, one-sided); 75 mg ABT-126 did not demonstrate significant improvements in ADAS-Cog scores compared with placebo at any time point. A treatment effect was not observed for any secondary efficacy measures of cognition, function, or global improvement. ABT-126 was generally well tolerated; the most common adverse events were agitation, constipation, diarrhea, fall, and headache. Conclusions: Overall, the efficacy profile of ABT-126 did not warrant further development as add-on therapy to AChEIs to treat mild-to-moderate AD.
引用
收藏
页码:1237 / 1247
页数:11
相关论文
共 20 条
[1]   Pro-Cognitive and Antipsychotic Efficacy of the α7 Nicotinic Partial Agonist SSR180711 in Pharmacological and Neurodevelopmental Latent Inhibition Models of Schizophrenia [J].
Barak, Segev ;
Arad, Michal ;
De Levie, Amaya ;
Black, Mark D. ;
Griebel, Guy ;
Weiner, Ina .
NEUROPSYCHOPHARMACOLOGY, 2009, 34 (07) :1753-1763
[2]   In Vivo Pharmacological Characterization of a Novel Selective α7 Neuronal Nicotinic Acetylcholine Receptor Agonist ABT-107: Preclinical Considerations in Alzheimer's Disease [J].
Bitner, R. Scott ;
Bunnelle, William H. ;
Decker, Michael W. ;
Drescher, Karla U. ;
Kohlhaas, Kathy L. ;
Markosyan, Stella ;
Marsh, Kennan C. ;
Nikkel, Arthur L. ;
Browman, Kaitlin ;
Radek, Rich ;
Anderson, David J. ;
Buccafusco, Jerry ;
Gopalakrishnan, Murali .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2010, 334 (03) :875-886
[3]  
Burghaus L, 2000, MOL BRAIN RES, V76, P385
[4]   Effects of the nicotinic α7 receptor partial agonist GTS-21 on NMDA-glutamatergic receptor related deficits in sensorimotor gating and recognition memory in rats [J].
Callahan, Patrick M. ;
Terry, Alvin V., Jr. ;
Tehim, Ashok .
PSYCHOPHARMACOLOGY, 2014, 231 (18) :3695-3706
[5]   Immediate and Sustained Improvements in Working Memory After Selective Stimulation of α7 Nicotinic Acetylcholine Receptors [J].
Castner, Stacy A. ;
Smagin, Gennady N. ;
Piser, Timothy M. ;
Wang, Yi ;
Smith, Jeffrey S. ;
Christian, Edward P. ;
Mrzljak, Ladislav ;
Williams, Graham V. .
BIOLOGICAL PSYCHIATRY, 2011, 69 (01) :12-18
[6]   Alzheimer disease: Current concepts and emerging diagnostic and therapeutic strategies [J].
Clark, CM ;
Karlawish, JHT .
ANNALS OF INTERNAL MEDICINE, 2003, 138 (05) :400-410
[7]   Safety and clinical effects of EVP-6124 in subjects with Alzheimer's disease currently or previously receiving an acetylcholinesterase inhibitor medication [J].
Deardorff, William James ;
Shobassy, Ahmad ;
Grossberg, George T. .
EXPERT REVIEW OF NEUROTHERAPEUTICS, 2015, 15 (01) :7-17
[8]  
Gault L., 2013, ALZHEIMERS DEMENT, V9, P138
[9]   Decreased protein levels of nicotinic receptor subunits in the hippocampus and temporal cortex of patients with Alzheimer's disease [J].
Guan, ZZ ;
Zhang, X ;
Ravid, R ;
Nordberg, A .
JOURNAL OF NEUROCHEMISTRY, 2000, 74 (01) :237-243
[10]   Nicotinic acetylcholine receptors: From basic science to therapeutics [J].
Hurst, Raymond ;
Rollema, Hans ;
Bertrand, Daniel .
PHARMACOLOGY & THERAPEUTICS, 2013, 137 (01) :22-54