Tolerability, Pharmacokinetics and Pharmacodynamics of Six Multiple Rising Dose Regimens of BIA 5-453

NCT02840565 | Completed Phase 1

• 2 other identifiers: BIA-5453-1022007-004142-33
• Study Type: interventional
• Target: 57
• Locations: 0 countries
• Sites: N/A

Brief Summary

The purpose of this study is to assess the tolerability of BIA 5-453 after six multiple rising dose regimens of BIA 5-453.

Conditions

Hypertension; Chronic Heart Failure

Outcome Measures

Primary Outcomes (2)

• Percent of subjects with at least one adverse event

  through study completion, an average of 10 days

• Percent of subjects by dose group with at least one treatment-emergent adverse event (TEAEs)

  Treatment-emergent adverse events are adverse events that occurred either in the 72 hours after dosing or that was present prior to dosing but exacerbated within 72 hours after dosing.

  through study completion, an average of 10 days

Study Arms (6)

BIA 5-453 25 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 25 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

BIA 5-453 50 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 50 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

BIA 5-453 100 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 100 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

BIA 5-453 200 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 200 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

BIA 5-453 400 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 400 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

BIA 5-453 600 mg or placebo

EXPERIMENTAL

Multiple oral doses of BIA 5-453 600 mg or placebo were administered once daily for 10 days to subjects in fasting conditions.

Drug: BIA 5-453; Drug: Placebo

Interventions

BIA 5-453 DRUG

Presented as blue hard gelatine capsules (size 2) of 1 mg, 10 mg and 50 mg for oral administration

Also known as: Etamicastat

BIA 5-453 100 mg or placebo; BIA 5-453 200 mg or placebo; BIA 5-453 25 mg or placebo; BIA 5-453 400 mg or placebo; BIA 5-453 50 mg or placebo; BIA 5-453 600 mg or placebo

Placebo DRUG

The composition of the placebo is qualitatively the same but without BIA 5-453 pharmaceutical active ingredient.

BIA 5-453 100 mg or placebo; BIA 5-453 200 mg or placebo; BIA 5-453 25 mg or placebo; BIA 5-453 400 mg or placebo; BIA 5-453 50 mg or placebo; BIA 5-453 600 mg or placebo

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• A signed and dated informed consent form before any study-specific screening procedure was performed.
• Aged between 18 and 45 years, inclusive.
• Healthy as determined by the investigator on the basis of medical history, physical examination, clinical laboratory test results, vital signs and digital 12-lead ECG.
• Nonsmoker or smoker of fewer than 10 cigarettes per day as determined by history. Must have been able to abstain from smoking during the inpatient stay.
• Have a high probability for compliance with and completion of the study.

You may not qualify if:

• Medical History
• Any significant cardiovascular (e.g. hypertension), hepatic, renal, respiratory (e.g. childhood asthma), gastrointestinal, endocrine (e.g. diabetes, dyslipidemia), immunologic, dermatological, haematological, neurologic, or psychiatric disease.
• Acute disease state (e.g., nausea, vomiting, fever, diarrhoea) within 7 days before study Day1.
• History of drug abuse within 1 year before study Day1.
• History of alcoholism within 1 year before Day1. Consumption of more than 50 g of ethanol per day (12.5 cL glass of 10° \[10%\] wine = 12 g; 4 cL of aperitif, 42° \[42%\] whiskey = 17 g; 25 cL glass of 3° \[3%\] beer = 7.5 g; 25 cL glass of 6° \[6%\] beer = 15 g
• History of any clinically important drug allergy.
• Physical and Laboratory Findings
• An automatic ECG QTc interval reading at screening or enrolment \>450 ms.
• Positive serologic findings for human immunodeficiency virus (HIV) antibodies, hepatitis B surface antigen (HBsAg), and/or hepatitis C virus (HCV) antibodies.
• Positive findings of urine drug screen (eg, amphetamines, barbiturates, benzodiazepines, cannabinoids, cocaine, methadone, opiates, MDMA \[3,4-methylenedioxy-methamphetamine; ecstasy\]).
• Prohibited treatments
• Prohibited Treatments: use of any investigational drug within 90 days or prescription drug within 30 days before investigational medical product (IMP) administration.
• Consumption of any caffeine-containing products (e.g., coffee, tea, chocolate, or soda) in excess of 6 cups per day (or equivalent), of grapefruit, grapefruit-containing products, or alcoholic beverages within 72 before study day -1.
• Use of any over-the-counter drugs including herbal supplements (except for the occasional use of acetaminophen \[paracetamol\], aspirin and vitamins ≤100% recommended daily allowance) within 7 days before IMP administration.
• Donation of blood (ie 450 ml) within 90 days before study Day1.

Sponsors & Collaborators

• Bial - Portela C S.A.: lead

MeSH Terms

Conditions

Hypertension

Interventions

etamicastat

Condition Hierarchy (Ancestors)

Vascular Diseases; Cardiovascular Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 19, 2016
• First Posted: July 21, 2016
• Study Start: September 1, 2007
• Primary Completion: July 1, 2008
• Study Completion: July 1, 2008
• Last Updated: July 21, 2016

Record last verified: 2016-07