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Effects of Lithium Therapy on Blood-based Therapeutic Targets in Parkinson's Disease.

Phase 1
Completed
Conditions
Parkinson Disease
Interventions
Registration Number
NCT04273932
Lead Sponsor
State University of New York at Buffalo
Brief Summary

This study aims to determine if one of three low doses of lithium therapy for 6 months can engage one or more blood-based therapeutic targets implicated in Parkinson's disease (PD) pathophysiology. Results of this study will help to determine if lithium therapy is worthwhile to further investigate as a potential disease-modifying therapy in PD, the optimal dose to study and the optimal PD subgroup most likely to benefit from lithium therapy.

Detailed Description

Lithium belongs to a class of kinase-targeting therapies, including the diabetes medication exenatide and the cancer medication nilotinib, that have demonstrated promise as disease-modifying therapies for Parkinson's disease (PD). Exenatide was recently shown to engage protein kinase B (Akt) and provide significant symptomatic and possible disease-modifying benefit in PD in a phase 2 randomized controlled trial (RCT). Nilotinib engages c-Abelson kinase (c-Abl) and its disease-modifying effects are currently being investigated in two, phase 2 PD RCTs. Lithium targets Akt, glycogen synthase kinase-3 beta (GSK-3B, a downstream target of Akt) and cyclin-dependent kinase 5 (cdk5, a downstream target of c-Abl) in manners that recapitulate those of exenatide and nilotinib. Also, lithium inhibits inositol monophosphate leading to enhanced autophagy and reduced intracellular levels of alpha-synuclein (a-synuclein), which is believed to be a primary mediator of the progressive neurodegeneration in PD. In addition to a-synuclein, genome-wide association studies (GWAS) have implicated oligomeric tau in the pathogenesis of PD. Pathological mutations in leucine-rich repeat kinase 2 (LRRK2) are the most common genetic cause of a late-onset parkinsonism that is clinically indistinguishable from sporadic PD and very similar pathologically. Pathological LRRK2 mutations affect the activities of Akt, GSK-3B and cdk5 to greatly increase the formation of phosphorylated tau (p-tau) - the precursor to tau oligomer formation - and decrease the activity of the transcriptional cofactor B-catenin - which mediates the transcription of neuronal survival genes implicated in PD such as nuclear receptor related 1 (Nurr1). Through its ability to inhibit GSK-3B, lithium can enhance B-catenin-mediated activity and Nurr1 expression. Lithium was also effective in several PD animal models. Finally, both clinical trial and epidemiologic data suggest that lithium exposures of even \<1mg a day may provide significant disease-modifying effects in neurodegenerative diseases including PD.

The investigators propose to assess the effects of 3 lithium dosages for 6 months on the above targets measured in blood in a randomized, parallel design, proof of concept clinical trial among 18 PD patients. In addition, 2 PD patients will serve as controls and not receive lithium therapy.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
19
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Lithium aspartate 15mg a dayLithium15mg of elemental lithium administered every morning by mouth.
Lithium aspartate 45mg a dayLithium20mg every morning and 25mg every evening of elemental lithium administered by mouth.
Lithium carbonateLithiumThe dose will be titrated based on weekly blood tests to achieve a target serum level of 0.40-0.50mmol/L, which represents an elemental lithium dose of about 85-170mg a day.
Primary Outcome Measures
NameTimeMethod
Plasma alpha-synuclein assessed by ultra-sensitive, immunomagnetic reduction assay (MagQu, LLC, Surprise, AZ).Change from baseline to 24 weeks
Peripheral blood mononuclear cell (PBMC) Nurr1 mRNA levels by real-time polymerase chain reaction.Change from baseline to 24 weeks
PBMC phosphorylated (p) and total (t) levels of pSerine9 and t-glycogen synthase kinase-3BChange from baseline to 24 weeks
Plasma brain-derived neurotrophic factor (BDNF).Change from baseline to 24 weeks
PBMC pThreonine308 and t-protein kinase B (Akt).Change from baseline to 24 weeks
Secondary Outcome Measures
NameTimeMethod
Patient tolerabilityUp to 24 weeks

Assessed by patient reported adverse events.

Trough, steady-state plasma lithium levels by ICP/MSChange from baseline to 24 weeks
Geriatric Depression Scale-15Change from baseline to weeks 12 and 24.

Score range 0-15 with higher values indicating more severe symptoms.

Montreal Cognitive Assessment (MoCA)Change from screening to week 24

Score range 0-30 with higher values indicating more severe symptoms.

Movement Disorder Society-Unified Parkinson's Disease Rating Scale (MDS-UPDRS), Part III (Motor Examination) and question 1.11 (Constipation Problems) in the "on" stateChange from baseline to weeks 12 and 24.

Score range 0-132 with higher values indicating more severe symptoms.

Parkinson's Anxiety ScaleChange from baseline to weeks 12 and 24.

Score range 0-48 with higher values indicating more severe symptoms.

Fatigue Severity ScaleChange from baseline to weeks 12 and 24.

Score range 9-56 with higher values indicating more severe symptoms.

Insomnia Severity IndexChange from baseline to weeks 12 and 24.

Score range 0-28 with higher values indicating more severe symptoms.

Parkinson's Disease Questionnaire-8Change from baseline to weeks 12 and 24.

Score range 0-32 with higher values indicating more severe symptoms.

Trial Locations

Locations (1)

University at Buffalo

🇺🇸

Williamsville, New York, United States

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