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Parkinson's disease (PD) is a progressive neurodegenerative disorder characterized by a range of non-motor and motor symptom.
Figure 1: Paper cover image
Identification of Lewy bodies and substantia nigra degeneration at autopsy is the gold standard for diagnosing PD, and the process of pathological misfolding (leading to the formation of Lewy bodies) is associated with further deleterious changes including, but not limited to: neuroinflammation, lysosomal dysfunction, and oxidation stress, and ultimately neuronal death, underlies disease progression, suggesting that ASYN is a promising therapeutic target in P.
Current treatments for Parkinson's disease provide only partial relief of symptoms, but do not slow the progression of Parkinson's diseas.
UCB0599 (the R-enantiomer of NPT200-11) is a brain-permeable, orally available small molecule that disrupts the first of the ASYN aggregation cascade by preventing misfolding on lipid membranes and the formation of ASYN aggregates step.
With this, Johan Willem Smit et a.
The safety/tolerability and single-dose and multiple-dose PK of UCB0599 and its metabolites were investigated in two Phase 1 studies in healthy participants (HPs), in which food effects and its association with itraconazole (ITZ) were evaluated ) of possible interactions (UP0030 [randomized, placebo-controlled, dose-escalation, crossover study, N = 65] and UP0078 [open-label study, N = 22].
Figure 2: The results of the paper
In all studies, UCB0599 showed rapid absorption and a linear, time-independent PK profile; PK of multiple doses of UCB0599 could be predicted from single-dose exposur.
No apparent food effect was observed; co-administration with ITZ affected the disposition of UCB0599 (~3-fold and ~2- to 3-fold increase in maximum plasma concentration and area under the curve, respectively), however, this did not affect its safety profil.
The significance of this study is that: 73 HP and 21 PD participants received doses of UCB0599; the acceptable safety/tolerability profile and predictable PK support continued development of UCB0599 for slowing PD progressio.
Original source:Smit JW, Basile P, Prato MK, et a.
