Parkinson Disease
Conditions
Brief summary
This is a phase 1, open-label study to assess the pharmacokinetics, pharmacodynamics, safety, and tolerability of opicapone when administered orally once daily for 14 days as adjunctive therapy to carbidopa/levodopa in subjects with Parkinson's disease.
Interventions
DRUGOpicapone
catechol-O-methyltransferase (COMT) inhibitor
Levodopa: dopamine precursor Carbidopa: DOPA decarboxylase inhibitor
Sponsors
Neurocrine Biosciences
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 85 Years
Healthy volunteers
No
Inclusion criteria
1. Have a clinical diagnosis of idiopathic Parkinson's Disease (PD) for at least 3 years with clear improvement with levodopa treatment 2. Be at a stable dose of maintenance medication(s) for PD, including stable doses of CD/LD 3. Subjects of childbearing potential who do not practice total abstinence must agree to use hormonal or two forms of nonhormonal contraception (dual contraception) consistently during the screening, treatment and follow-up periods of the study 4. Have a body mass index (BMI) of 18 to 40 kg/m2 5. Have a modified Hoehn and Yahr stage of ≤4 in the OFF state 6. Be able to tolerate an overnight period of 12 hours without CD/LD 7. Be in good general health and expected to complete the clinical study as designed
Exclusion criteria
1. Are currently pregnant or breastfeeding 2. More than 2 alcoholic beverages daily or more than 14 alcoholic beverages weekly within 7 days of Day -1 or consume any alcohol within 48 hours of Day -1. 3. Have motor fluctuations during the day (ie, effect of levodopa wearing off or having unpredictable off periods), or severe or intolerable levodopa-induced dyskinesia 4. Have had previous exposure to opicapone, or have an allergy, hypersensitivity, or intolerance to opicapone or other COMT inhibitor. 5. Have a history of a medical condition or surgical procedure that might interfere with absorption or metabolism. 6. Have a known history of neuroleptic malignant syndrome 7. Have an unstable medical condition or chronic disease 8. Have taken certain prohibited medications within 28 days of Day -1. 9. Have a known or suspected diagnosis of AIDS, or have tested seropositive for HIV 10. Have hepatitis A or B 11. Have a significant risk of suicidal or violent behavior
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacokinetic evaluation of levodopa following administration of opicapone: maximum plasma concentration (cmax) | up to 15 days | Maximum plasma concentration |
| Pharmacokinetic evaluation of opicapone and its metabolites: Time to maximum plasma concentration (tmax) | up to 19 days | Time to maximum plasma concentration |
| Pharmacokinetic evaluation of levodopa following administration of opicapone: area under the curve (AUC 0-tlast) | up to 15 days | Area under the plasma concentration versus time curve from 0 hours to time before next levodopa dose |
| Pharmacokinetic evaluation of opicapone and its metabolites: area under the curve (AUC 0-24) | up to 19 days | Area under the plasma concentration versus time curve from 0 to 24 hours for analytes with quantifiable concentrations at 24 hours postdose |
| Pharmacokinetic evaluation of opicapone and its metabolites: area under the curve (AUC 0-tlast) | up to 19 days | Area under the plasma concentration versus time curve from 0 hour to the time of the last measurable concentration for analytes below the limit of quantification at 24 hours postdose |
| Pharmacokinetic evaluation of opicapone and its metabolites: Maximum plasma concentration (Cmax) | up to 19 days | Maximum plasma concentration |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Pharmacodynamic evaluation of opicapone on S-COMT activity | up to 19 days | Maximum inhibition of S-COMT activity. |
| Incidence of Treatment-Emergent Adverse Events (safety and tolerability) | up to 19 days | Number of participants with reported adverse events after study treatment. |
Countries
United States
Outcome results
None listed