Skip to main content
. 2020 Oct 9;21(20):7443. doi: 10.3390/ijms21207443

Table 1.

Therapeutic agents targeting Aβ peptides in Alzheimer’s disease (AD).

Therapeutic Agents Targeting Amyloidogenic Events Action Ref.
Novel beta-secretase inhibitor (KMI-429) with hydroxy-methyl-carbonyl (HMC) isostere Beta-site APP-cleaving enzyme (BACE1) blockers [52]
N-benzoyl-oxy-carbonyl-valine-leucine-leucinal (Z-VLL-CHO, C25H39N3O5) β-secretase inhibitor, BACE1 blocker [2]
Beta-secretase inhibitor GRL-8234 β-secretase inhibitor [54,55,56,57]
Iso-liquiritigenin BACE1 inhibitor [59]
(R)-6-[(1,1′-biphenyl)-4-ylmethoxy]-1,2,3,4-tetrahydro-N,N-dimethyl-2-naphthalene-ethan-amine hydrochloride monohydrate (TAK-070, C27H31NO) BACE1 inhibitor [54]
BIIB042 γ-secretase modulator [63]
NGP328 and NGP555 γ-secretase modulator [64]
SGSM-36 γ-secretase modulator [67]
LY450139 γ-secretase inhibitor [54]
Aβ fragments in conjugation with poly-lysine Active immunotherapeutic agents [2]
NAB61 Passive immunotherapeutic agent [78]
Anti-beta-amyloid monoclonal antibody (BAM-10) Passive immunotherapeutic agent [81]
Neprilysin (NEP) Aβ load-reducing enzyme [2]
Endothelin-converting enzyme (ECE) Aβ load-reducing enzyme [84]
Protein kinase C epsilon (PKCε) ECE enhancer, Aβ load reducer [85]
Serine protease plasmin Amyloid degradation [87]
Matrix metalloproteinases (MMPs) Amyloid degradation [88,89,90]
Estrogen MMP-2, -9 enhancer, Aβ clearance [91]
ATP-binding cassette (ABC) transporters Prevent Aβ accumulation [2]
Low-density lipoprotein receptor-related protein 1 (LRP1) Prevent Aβ accumulation [2]
Aβ16-20 Aβ-aggregation inhibitor [94]
Aβ15-25 Aβ-aggregation inhibitor [13]
OR-2 Aβ-aggregation inhibitor [97]
RI-OR2 Aβ-aggregation inhibitor [98]
Aggregated human beta-amyloidAN1792 Active immunotherapeutic reagent [71]
Bapineuzumab Monoclonal antibody [54]
Glucagon-like peptide (GLP-1) Aβ accumulation inhibitor [115]
Statins Aβ degradation promoter [54]
Non-steroidal anti-inflammatory drugs (NSAIDs) (i.e., ibuprofen) Curbed Aβ levels and ROS mitigation, γ-secretase modulator [119,120,121]
Bismuth oxychloride (BiOCl) nanosheets Destabilization of β-sheets [123]
Congo red Amyloid-inhibiting dye [124,125]
Methylene blue Amyloid-inhibiting dye [126,127]
Thioflavin T Amyloid-inhibiting dye [128]
Orcein Amyloid-inhibiting dye [129]
Curcumin Amyloid-inhibiting dye [130]
Epi-gallocatechin-3-gallate (EGCG) Aβ fibrillization inhibitor [133]
Silibinin Aβ aggregation inhibitor [134]
Proline β-sheet breaker [135]
NeuroDefend Aβ load reduction [136]
Naturally obtained dietary flavonoids CDK-5 and GSK-3β inhibitors, secretase enzyme modulators, Aβ aggregation inhibitors [137,138]
Autacoid local injury antagonist amides (ALIAmides) (palmitoyl ethanol amide, PEA) Anti-inflammatory, anti-hyperalgesia and lipid metabolism regulator [107,110]
Ultra-micronized form of PEA and luteolin Neuroinflammation amelioration [107,108]