Relative Bioavailability and Bioequivalence Of Different Formulations of Opicapone in Healthy Volunteers

• ClinicalTrials.gov Identifier: NCT02305277
• Recruitment Status: Completed
• First Posted: December 2, 2014
• Results First Posted: November 17, 2015
• Last Update Posted: November 17, 2015
• Sponsor: Bial - Portela C S.A.
• Information provided by (Responsible Party): Bial - Portela C S.A.

Study Description

Brief Summary:

Single-centre, open-label, randomised, three-part, two-way crossover study in 84 healthy volunteers. In each part, the study consisted of two consecutive single-dose treatment periods separated by a washout period of at least 14 days.

Condition or disease	Intervention/treatment	Phase
Parkinson	Drug: BIA 9-1067 (clinical micronized, CM); Drug: BIA 9-1067 (to-be-marketed, TBM)	Phase 1

Study Design

• Study Type: Interventional (Clinical Trial)
• Actual Enrollment: 85 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Masking: None (Open Label)
• Primary Purpose: Treatment
• Official Title: Relative Bioavailability and Bioequivalence Of Different Formulations of Opicapone in Healthy Volunteers
• Study Start Date: March 2014
• Actual Primary Completion Date: June 2014
• Actual Study Completion Date: June 2014

Arms and Interventions

Arm	Intervention/treatment
Experimental: BIA 9-1067 5 mg Sequence 1; volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone
Experimental: BIA 9-1067 25 mg Sequence 1; volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone
Experimental: BIA 9-1067 50 mg Sequence 1; volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: CM Formulation Period 2: TBM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone
Experimental: BIA 9-1067 5 mg Sequence 2; volunteers received a single oral dose of 5 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone
Experimental: BIA 9-1067 25 mg Sequence 2; volunteers received a single oral dose of 25 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone
Experimental: BIA 9-1067 50 mg Sequence 2; volunteers received a single oral dose of 50 mg BIA 9-1067: Period 1: TBM Formulation Period 2: CM Formulation CM - clinical micronized TBM - to-be-marketed	Drug: BIA 9-1067 (clinical micronized, CM); Other Name: OPC, Opicapone; Drug: BIA 9-1067 (to-be-marketed, TBM); Other Name: OPC, Opicapone

Outcome Measures

Primary Outcome Measures :

1. Cmax - Maximum Observed Plasma Concentration [ Time Frame: before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose ]

Secondary Outcome Measures :

1. AUC0-t - Area Under the Plasma Concentration-time Curve for BIA 9-1067 [ Time Frame: before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose ]
   Area Under the plasma concentration-time Curve from time 0 to the time of last quantifiable concentration
2. Tmax - Time of Occurrence of Cmax [ Time Frame: before OPC dosing, and ½, 1, 2, 3, 4, 6, 8, 12, 16, 24, 36 and 48 hours post-OPC dose ]

Eligibility Criteria

• Ages Eligible for Study: Child, Adult, Older Adult
• Sexes Eligible for Study: All
• Accepts Healthy Volunteers: Yes

Criteria

Inclusion Criteria:

• A signed and dated informed consent form before any study-specific screening procedure was performed;
• Male or female subjects aged 18 to 45 years, inclusive;
• Body mass index (BMI) between 18 and 30 kg/m2 inclusive;
• Healthy as determined by pre-study medical history, physical examination, vital signs, complete neurological examination and 12-lead electrocardiogram (ECG);
• Negative tests for hepatitis B surface antigen (HBsAg), anti- hepatitis C virus antibodies (HCV Ab) and anti-human immunodeficiency virus antibodies (HIV-1 and HIV-2 Ab) at screening;
• Clinical laboratory test results clinically acceptable at screening and admission to each treatment period;
• Negative screen for alcohol and drugs of abuse at screening and admission to each treatment period;
• Non-smokers or ex-smokers for at least 3 months;
• Able to participate, and willing to give written informed consent and comply with the study restrictions.
• If female:
• She was not of childbearing potential by reason of surgery or, if of childbearing potential, she used 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 was the sole partner of that subject] for all the duration of the study;
• She had a negative serum pregnancy test at screening and a negative urine pregnancy test at admission to each treatment period.

Exclusion Criteria:

• 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, or had a clinically relevant surgical history;
• Had clinically relevant findings in laboratory tests, particularly any abnormality in the coagulation tests, or any abnormality in the liver function tests;
• Had a history of relevant atopy or drug hypersensitivity;
• Had a history of alcoholism and/or drug abuse;
• Consumed more than 14 units of alcohol per week [1 unit of alcohol = 280 mL beer (3-4°) = 100 mL wine (10-12°) = 30 mL spirits (40°)];
• Had a significant infection or known inflammatory process on screening or admission to each treatment period;
• Had acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
• Had used medicines within 2 weeks of admission to first period that could affect the safety or other study assessments, in the Investigator's opinion;
• Had previously received opicapone;
• Had used any investigational drug or participated in any clinical trial within 90 days prior to screening;
• Had participated in more than 2 clinical trials within the 12 months prior to screening;
• Had donated or received any blood or blood products within the 3 months prior to screening;
• Were vegetarians, vegans or had medical dietary restrictions;
• Could not communicate reliably with the Investigator;
• Were unlikely to co-operate with the requirements of the study;
• Were unwilling or unable to give written informed consent;

If female:

• She was pregnant or breast-feeding.

Contacts and Locations

No Contacts or Locations Provided

More Information

• Responsible Party: Bial - Portela C S.A.
• ClinicalTrials.gov Identifier: NCT02305277
• Other Study ID Numbers: BIA-91067-119
• First Posted: December 2, 2014
• Results First Posted: November 17, 2015
• Last Update Posted: November 17, 2015
• Last Verified: October 2015

Additional relevant MeSH terms:

Opicapone; Catechol O-Methyltransferase Inhibitors; Enzyme Inhibitors; Molecular Mechanisms of Pharmacological Action; Antiparkinson Agents; Anti-Dyskinesia Agents