Effect of Food on Opicapone
- Registration Number
- NCT03116308
- Lead Sponsor
- Bial - Portela C S.A.
- Brief Summary
The purpose of this study is to investigate the effect of food on the catechol-O-Methyltransferase (COMT) activity after repeated doses of opicapone (OPC, development code BIA 9-1067) in healthy subjects and to characterize the effects of food on the pharmacokinetics (PK) and tolerability of OPC after repeated doses.
- Detailed Description
Single-centre, open-label, single-arm study in 28 healthy subjects. Subjects received a single-dose of 50 mg OPC once-daily (QD) in the evening for 12 days. On Day 1 (D1), 50 mg OPC was orally administered in the evening (reference hour for all other administrations) after a minimum of 6 hours fast. From D2 to D8 subjects were in ambulatory and received 50 mg OPC once-daily (evening administration after 2 hours fast). On D9, 50 mg OPC was orally administered in the evening after a minimum of 6 hours fast. On D10, 50 mg OPC was orally administered in the evening, thirty minutes after the start of a moderate meal (with a previous 6 hours fast). On D11 and D12 subjects received the last doses of 50 mg OPC (evening administration after 2 hours fast).
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- All
- Target Recruitment
- 28
- Able and willing to give written informed consent and to comply with the study restrictions.
- Male or female subjects aged between 18 and 45 years, inclusive.
- Body mass index (BMI) between 19 and 30 kg/m2, inclusive.
- Healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead ECG.
- Negative tests for HBsAg, anti-HCV Ab and HIV-1 and HIV-2 Ab at screening.
- Clinical laboratory test results clinically acceptable at screening and admission.
- Negative screen for alcohol and drugs of abuse at screening and admission.
- Non-smokers or ex-smokers for at least 3 months.
- If female:
- Not of childbearing potential by reason of surgery or, if of childbearing potential, she uses an effective non-hormonal method of contraception (intrauterine device or intrauterine system; condom or occlusive cap [diaphragm or cervical or vault caps] with spermicidal foam or gel or film or cream or suppository; true abstinence; or vasectomized male partner, provided that he is the sole partner of that subject) for all the duration of the study.
- Negative serum pregnancy test at screening and a negative urine pregnancy test on admission.
- 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.
- Clinically relevant surgical history.
- Clinically relevant abnormality in the coagulation tests.
- Clinically relevant abnormality in the liver function tests.
- History of relevant atopy or drug hypersensitivity, particularly to any COMT inhibitor.
- History of alcoholism or drug abuse.
- Consume more than 14 units of alcohol a week.
- Significant infection or known inflammatory process at screening or admission.
- Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission.
- Used medicines within 2 weeks of admission that may affect the safety or other study assessments, in the investigator's opinion.
- Previously received OPC.
- Used any investigational drug or participated in any clinical trial within 90 days prior to screening.
- Participated in more than 2 clinical trials within the 12 months prior to screening.
- Donated or received any blood or blood products within the 3 months prior to screening.
- Vegetarians, vegans or have medical dietary restrictions.
- Cannot communicate reliably with the investigator.
- Unlikely to co-operate with the requirements of the study.
- If female:
- Pregnant or breast-feeding.
- Of childbearing potential and not used an approved effective contraceptive method or she uses oral contraceptives.
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SINGLE_GROUP
- Arm && Interventions
Group Intervention Description 50 mg OPC Opicapone (OPC) Subjects received 50 mg OPC once-daily in the evening for 12 days. On D9 subjects were to receive 50 mg OPC in the evening after a minimum 6 hours fast. On D10 subjects were to receive the QD dose of 50 mg OPC thirty minutes after the start of moderate meal (with a previous 6 hours fast)
- Primary Outcome Measures
Name Time Method Time to occurrence of Emax (tEmax) - Day 9 (fasted state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
Maximum observed effect on COMT activity (Emax) - Day 9 (fasted state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
Area under the effect-time curve (AUEC) - Day 9 (fasted state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
Maximum observed effect on COMT activity (Emax) - Day 10 (fed state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
Time to occurrence of Emax (tEmax) - Day 10 (fed state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
Area under the effect-time curve (AUEC) - Day 10 (fed state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacodynamic parameters for opicapone
- Secondary Outcome Measures
Name Time Method Maximum observed plasma concentration (Cmax) - Day 10 (fed state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacokinetic parameters for opicapone
Time of occurrence of Cmax (tmax) - Day 10 (fed state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacokinetic parameters for opicapone
Maximum observed plasma concentration (Cmax) - Day 9 (fasted state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacokinetic parameters for opicapone
Time of occurrence of Cmax (tmax) - Day 9 (fasted state) Before and ½, 1, 2, 3, 4, 6, 12 and 24 h post-dose Pharmacokinetic parameters for opicapone