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Table 1 Overview of drug formulation and experimental outcomes of Alzheimer’s disease model mice treated with Bexarotene

From: When the dust settles: what did we learn from the bexarotene discussion?

   

Experimental claims

Research group

Drug formulation

Duration of treatment

Target engagement (ApoE/ABCA1)

Decrease of soluble Aβ

Clearance of deposited Aβ/plaques

Behavioral improvements

In vivo microglia activation

Mechanism-based toxicity

Cramer et al. [4]

Bexarotene/Targretin in DMSO or micronized in water

3 to 14 days and 3 months

Increase

Decrease of Aβ40 or Aβ42 >25%

Repeated dosing of 3 to 14 days decreases Aβ deposits by 30 to 75%; 3-month treatment had no effects

Improved context-dependent fear memory. Improved spatial memory. Improved social behavior

Unclear whether different from control

NR

Price et al.[9]

Bexarotene in solutol:ethanol:water (15:10:75)

3 to 7 days

Increase

No effect

No effect

NR

NR

Increased liver weight

Fitz et al. [11]

Targretin in glycerol

15 days

Increase

Decrease of ISF Aβ40 and Aβ42 by 23 to 26%; no effect on extracted soluble Aβ

No effect

Improved spatial memory. Improved long-term memory

NR

NR

Veeraraghavalu et al. [7]

Targretin in DMSO:ethanol:sunflower oil (6.6%:4%:89.6%)

7 days

Increase

Small effects

No effect

NR

No effect

NR

Tesseur et al.[8]

Bexarotene in Captisol and HP-β-CD/Tween

19 days

Increase

No effect

No effect

Unclear effect on social recognition memory and fear memory

NR.

Loss of body weight, irritation and breathing problems, increased grooming

LaClair et al.[10]

Bexarotene in DMSO or corn oil

3 to 14 days

Increase

NR

No effect

No effect on context- or conditioned stimulus- dependent fear memory

No effect

NR

Ulrich et al.[12]

Targretin in water

36 hours

Increase

Decrease of ISF Aβ40 by 45%

NR

NR

NR

NR

  1. Aβ, amyloid beta; ApoE, apolipoprotein E; DMSO, dimethyl sulfoxide; HP-β-CD, 2-hydroxypropyl-β-cyclodextrin; ISF, interstitial fluid; NR, not reported.