Pharmacokinetics of Rising Single-doses of BIA 6-512 and Their Effect on the Levodopa Pharmacokinetics

• Register: ClinicalTrials.gov
• Last refreshed on: 16 December 2017
• Main ID: NCT03091868
• Date of registration: 21/03/2017
• Prospective Registration: No
• Primary sponsor: Bial - Portela C S.A.
• Public title: Pharmacokinetics of Rising Single-doses of BIA 6-512 and Their Effect on the Levodopa Pharmacokinetics
• Scientific title: A Double-blind, Randomised, Placebo-controlled Study in Healthy Volunteers to Investigate the Tolerability and Pharmacokinetics of Rising Single-doses of BIA 6-512 and Their Effect on the Levodopa Pharmacokinetics When Administered in Combination With a Single-dose of Levodopa/Carbidopa 100/25 mg or With a Single-dose of Levodopa/Carbidopa 100/25 mg Plus a Single-dose of Entacapone 200 mg
• Date of first enrolment: November 3, 2004
• Target sample size: 80
• Recruitment status: Completed
• URL: https://clinicaltrials.gov/show/NCT03091868
• Study type: Interventional
• Study design: Allocation: Randomized. Intervention model: Sequential Assignment. Primary purpose: Treatment. Masking: Double (Participant, Investigator).
• Phase: Phase 1

Countries of recruitment

Portugal

Key inclusion & exclusion criteria

Inclusion Criteria:

- Male or female subjects aged between 18 and 45 years, inclusive.

- Subjects of body mass index (BMI) between 19 and 30 kg/m2, inclusive.

- Subjects who were healthy as determined by pre-study medical history, physical
examination, vital signs, complete neurological examination and 12-lead ECG.

- Subjects who had clinical laboratory tests clinically acceptable at screening and
admission.

- Subjects who had negative tests for HBsAg, anti-HCVAb and anti-HIV-1 and anti-HIV-2 Ab
at screening.

- Subjects who had a negative screen for alcohol and drugs of abuse at screening and
admission.

- Subjects who were non-smokers or who smoked less than 10 cigarettes or equivalent per
day.

- Subjects who were able and willing to give written informed consent.

- (If female) She was sterile or, if of childbearing potential, she used one of the
following methods of contraception: double barrier, intrauterine device or abstinence.

- (If female) She had a negative urine pregnancy test at screening and admission.

Exclusion Criteria:

- Subjects who did not conform to the above inclusion criteria, OR

- Subjects who had a clinically relevant history or presence of respiratory,
gastrointestinal, renal, hepatic, haematological, lymphatic, neurological,
cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological,
dermatological, endocrine, connective tissue diseases or disorders.

- Subjects who had a clinically relevant surgical history.

- Subjects who had a clinically relevant family history.

- Subjects who had a history of relevant atopy.

- Subjects who had a history of relevant drug hypersensitivity.

- Subjects who had a history of alcoholism or drug abuse.

- Subjects who consumed more than 21 units of alcohol a week.

- Subjects who had a significant infection or known inflammatory process on screening or
admission.

- Subjects who had acute gastrointestinal symptoms at the time of screening or admission
(e.g., nausea, vomiting, diarrhoea, heartburn).

- Subjects who had used prescription or over-the-counter medication within 2 weeks of
admission.

- Subjects who had used any investigational drug or participated in any clinical trial
within 3 months prior to screening.

- Subjects who had donated or received any blood or blood products within 3 months prior
to screening.

- Subjects who were vegetarians, vegans or have medical dietary restrictions.

- Subjects who cannot communicate reliably with the investigator.

- Subjects who were unlikely to co-operate with the requirements of the study.

- (If female) She was pregnant or breast-feeding.

- (If female) She was of childbearing potential and she did not use an approved
effective contraceptive method or she used oral contraceptives.



Age minimum: 18 Years
Age maximum: 45 Years
Gender: All

Health Condition(s) or Problem(s) studied

Parkinson Disease

Intervention(s)

Drug: Placebo oral capsule

Drug: Sinemet® 100/25

Drug: BIA 6-512 100 mg

Drug: Comtan®

Drug: BIA 6-512 25 mg

Primary Outcome(s)

Area under the plasma concentration versus time curve (AUC) from time zero to the last sampling time at which concentrations were at or above the limit of quantification (AUC0-t) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

AUC from time zero to the infinity (AUC0-8) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Elimination rate constant (?z) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Maximum observed plasma drug concentration (Cmax) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Apparent elimination half-life (t1/2) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Apparent elimination half-life (t1/2) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Elimination rate constant (?z) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Time at which the Cmax occurred (tmax) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Area under the plasma concentration versus time curve (AUC) from time zero to the last sampling time at which concentrations were at or above the limit of quantification (AUC0-t) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

AUC from time zero to the infinity (AUC0-8) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Maximum observed plasma drug concentration (Cmax) - Day 2 [Time Frame: ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Time at which the Cmax occurred (tmax) - Day 1 [Time Frame: pre-dose, ¼, ½, ¾, 1, 1½, 2, 3, 4, 6, 8, 12, 16 and 24 hours post-dose]

Secondary ID(s)

BIA-6512-102

Source(s) of Monetary Support

Please refer to primary and secondary sponsors