A Study Assessing the Safety and Pharmacokinetic Profile of Modified Release Formulations of Tolcapone

NCT03633591 | Completed Phase 1

• 2 other identifiers: TOLC101MR2017-003070-13
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief Summary

The purpose of this study is to assess the pharmacokinetic profiles of tolcapone in healthy subjects after administration of one or two oral doses of multiple modified release prototype formulations.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (5)

• Pharmacokinetic Assessment: Time to maximum concentration (Tmax)

  Time to maximum concentration (Tmax)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment: Maximum observed concentration (Cmax)

  Maximum observed concentration (Cmax)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment: Area under the curve (AUC)

  Area under the curve (AUC)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment: Plasma half-life (t1/2)

  Plasma half-life (t1/2)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment: Relative bioavailability (Frel)

  Relative bioavailability (Frel)

  Pre-dose to 24 hours post-dose

Secondary Outcomes (6)

• Pharmacokinetic Assessment of 3-O-Methyltolcapone: Time to maximum concentration (Tmax)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment of 3-O-Methyltolcapone: Maximum observed concentration (Cmax)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment of 3-O-Methyltolcapone: Area under the curve (AUC)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment of 3-O-Methyltolcapone: Plasma half-life (t1/2)

  Pre-dose to 24 hours post-dose

• Pharmacokinetic Assessment of 3-O-Methyltolcapone: Relative Bioavailability (Frel)

  Pre-dose to 24 hours post-dose

Study Arms (1)

Modified Release Prototypes of Tolcapone

EXPERIMENTAL

Drug: Tolcapone; Drug: Tolcapone Modified Release Prototype; Drug: Tolcapone Divided Dose

Interventions

Tolcapone DRUG

Multiple doses of tolcapone tablets in the fasted state

Also known as: Tasmar

Modified Release Prototypes of Tolcapone

Tolcapone Modified Release Prototype DRUG

A single dose of tolcapone modified release prototype in the fasted state

Modified Release Prototypes of Tolcapone

Tolcapone Divided Dose DRUG

Tolcapone (suspension) in equal divided doses in the fasted state

Modified Release Prototypes of Tolcapone

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Healthy males or non-pregnant, non-lactating healthy females
• Age 18 to 65 years of age at the time of signing informed consent
• Body mass index (BMI) of 18.0 to 32.0 kg/m2 or, if outside the range, considered not clinically significant by the investigator
• Must be willing and able to communicate and participate in the whole study
• Must provide written informed consent
• Must agree to use an adequate method of contraception

You may not qualify if:

• Subjects who have received any IMP in a clinical research study within the previous 3 months prior to first dose.
• Subjects who are study site employees, or immediate family members of a study site or sponsor employee.
• Subjects who have previously been enrolled in this study.
• History of any drug or alcohol abuse in the past 2 years.
• Current smokers and those who have smoked within the last 12 months. A breath carbon monoxide reading of greater than 10 ppm at screening
• Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
• Females of childbearing potential who are pregnant or lactating
• Subjects who do not have suitable veins for multiple venepunctures / cannulation as assessed by the investigator at screening
• Clinically significant abnormal biochemistry, hematology or urinalysis as judged by the investigator
• Hemoglobin below the lower limit of normal
• ALT or AST outside the normal reference range at screening or admission.
• Confirmed positive drugs of abuse test result
• Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results
• History of clinically significant cardiovascular, neurological, renal, hepatic, chronic respiratory or gastrointestinal disease, or psychiatric disorder, as judged by the investigator
• Subjects with a history of cholecystectomy or gall stones

Sponsors & Collaborators

• Corino Therapeutics, Inc.: lead
• Quotient Sciences: collaborator

Study Sites (1)

Quotient Sciences

Ruddington, Nottingham, NG11 6JS, United Kingdom

Location

MeSH Terms

Interventions

Tolcapone

Intervention Hierarchy (Ancestors)

Benzophenones; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons; Organic Chemicals; Nitrophenols; Phenols; Ketones; Nitro Compounds

Study Officials

• Litza McKenzie

  Quotient Sciences

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 10, 2018
• First Posted: August 16, 2018
• Study Start: June 25, 2018
• Primary Completion: October 22, 2018
• Study Completion: October 22, 2018
• Last Updated: January 31, 2019

Record last verified: 2019-01

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)