. Author manuscript; available in PMC: 2010 Jun 1.

Published in final edited form as: Nat Rev Neurol. 2010 Feb;6(2):99–107. doi: 10.1038/nrneurol.2009.218

Table 1.

Secretase-targeting therapies in human Alzheimer disease trials

Compound	Company	Clinical trial phase	Comments
*α-Secretase activators*
EHT 0202	Exonhit Therapeutics	II	GABA_A receptor modulator that also weakly inhibits phosphodiesterase 4
EVP-6,124	EnVivo	II	α-7 nicotinic acetylcholine receptor agonist, also in trials for schizophrenia
PRX-03,140	Epix/GlaxoSmithKline	II	Partial 5-HT₄receptor agonist
*β-Secretase inhibitors*
CTS-2166	CoMentis	I	Selectively binds to the active site of β-secretase; shown to lower plasma Aβ in humans; no cerebrospinal fluid data presented to date
*γ-Secretase inhibitors*
LY450139	Eli Lilly	III	Relatively nonselective GSI
Begacestat	Wyeth	I	Notch-sparing GSI
BMS-708,163	Bristol-Myers Squibb	II	Notch-sparing GSI
MK-0572	Merck	I	Also being evaluated in combination therapy in breast cancer
*γ-Secretase modulators*
Tarenflurbil	Myriad	Completed phase III	No effect on cognitive or functional outcomes

Abbreviations: 5-HT₄, 5-hydroxytryptamine 4; Aβ, amyloid-β peptide; GABA_A, γ-aminobutyric acid A; GSI, γ-secretase inhibitor.