Pulmonary Arterial HypertensionPhase 1NCT07173738
Pharmacokinetics, Safety and Tolerability of Concurrent Doses of BIA 5-1058 and Furosemide
A Phase 1 study testing BIA 5-1058, Furosemide and BIA 5-1058 and Furosemide in people with Pulmonary Arterial Hypertension, run by Bial - Portela C S.A. at 1 site in United Kingdom.
Trial summary
The purpose of this study is: To assess the effect of BIA 5 1058 400 mg on furosemide pharmacokinetics (PK). To assess the effect of furosemide 40 mg on the PK of BIA 5 1058. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Pulmonary Arterial Hypertension
- What is being tested?
- BIA 5-1058, Furosemide and BIA 5-1058 and Furosemide
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 44 participants
- Where
- 1 siteUnited Kingdom
- Study dates
- 11 Jun 2018to 7 Sep 2018
- Phase
- Phase 1
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- A signed and dated informed consent form before any study-specific screening procedure is performed;
- Males and Females subjects aged 18 to 55 years, inclusive;
- Non-smoker or ex-smokers for at least 3 months prior to screening;
- Body mass index (BMI) between 18 and 30 kg/m2, inclusive;
- Subject with no clinically significant history of previous allergy / sensitivity to BIA 5-1058/furosemide or any of the excipients contained within the IMP(s);
- 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;
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- Negative screen for alcohol and drugs of abuse at screening and admission to each treatment period;
- Healthy as determined by the Investigator based on medical history, physical examination, , vital signs (systolic blood pressure (SBP) ≥ 90 mmHg and ≤ 140 mmHg, diastolic blood pressure (DBP) ≥ 50 mmHg and ≤ 90 mmHg) and digital 12-lead electrocardiogram (ECG));
- Clinical laboratory test results clinically acceptable at screening and admission to each treatment period;
- If male:
- Male subjects and female partner willing to use 2 effective methods of contraception, i.e., established method of contraception + condom, if applicable (unless anatomically sterile or where abstaining from sexual intercourse is in line with the preferred and usual lifestyle of the subject) from first dose until 3 months after last dose of IMP.
- Refraining from donating sperm throughout the study and for 3 months after the last dose of IMP;
- If female:
- No childbearing potential by reason of surgery or at least 1 year post-menopause (i.e., 12 months post last menstrual period), or menopause confirmed by follicle-stimulating hormone (FSH) testing;
- If of childbearing potential, using an effective non-hormonal method of contraception [intrauterine device; 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 and for 3 months after the last dose of IMP;
- Negative serum pregnancy test at screening and negative urine pregnancy test on admission of each treatment period).
Who cannot join
- Any personal or family history of haemostatic disorder;
- Consumption of more than 21 units (14 units for female subjects) of alcohol a week [1 unit corresponds to 1 glass of 12% wine (10 cl), 1 glass of 45% pastis (2.5 cl), 1 glass of 40% whisky (2.5 cl), 1 glass of 12% champagne (10 cl), 1 glass of 18% aperitif drink (7 cl) or one 25-cl glass of 5% beer];
- Use of nicotine replacement products such as patches, gum and/or electronic cigarettes within 3 months prior to the screening visit;
- Significant infection or known inflammatory process at screening or admission to each treatment period;
- Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
- Symptomatic orthostatic hypotension [drop of > 20 mmHg in SBP and/or > 10 mmHg] in DBP when moving from supine to standing position, together with other symptoms, e.g. dizziness
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- Previous use of BIA 5-1058;
- Use of any investigational drug or participation in any clinical trial within 90 days or 5 half-life times, whichever is longer,
- Participation in more than 4 clinical trials within the 12 months prior to screening;
- Donation or reception of any blood or blood products within the 3 months prior to screening;
- Vegetarians, vegans or other medical dietary restrictions;
- Not able to communicate reliably with the Investigator;
- Unlikely to co-operate with the requirements of the study;
- Use of medicines within 28 days of initiation of treatment that may affect the safety or other study assessments, in the Investigator's opinion or intake of any of the prohibited medications.
- Clinically relevant history or presence of respiratory, gastrointestinal, hepatic, renal, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, endocrine, connective tissue diseases or disorders;
- Clinically relevant surgical history that could interfere with the pharmacokinetics of the trial medications;
- No medication will be permitted throughout the study, except for medications to treat adverse events (AEs).
- Subject has an abnormal hepatic function based on an overall assessment by the Investigator regarding medical history, physical examination and laboratory tests of hepatic function (ALT > 1times the upper limit of normal (ULN), aspartate transaminase (AST) > 1times the ULN and total bilirubin > 1times the ULN [confirmed by subsequent repeat]), as judged by the Principal Investigator. If a laboratory assessment is outside of the reference range at the local laboratory at the Screening Visit or baseline, the assessment may be repeated once as soon as possible and in any cases before enrolment to rule out laboratory error.
- Any clinically relevant findings in the laboratory tests, including any abnormality in the coagulation tests;
- History of alcoholism or drug abuse;
- Females who are currently breast feeding.
Trial locations and contacts
1 site in 1 country.
United Kingdom1 site
Simbec Research Ltd (Simbec)
Merthyr Tydfil, CF48 4DR
About this study
Official title: An Open Label, Three Period, Fixed Sequence Study to Assess the Pharmacokinetics, Safety and Tolerability of Concurrent Doses of BIA 5-1058 and Furosemide in Healthy Subjects Under Fasting Conditions.
The purpose of this study is:
- To assess the effect of BIA 5 1058 400 mg on furosemide pharmacokinetics (PK).
- To assess the effect of furosemide 40 mg on the PK of BIA 5 1058.
Read the detailed description
This was an open-label, single-dose, fasted, 3-periods, fixed-sequence study separated by a washout period of 10 days or more in healthy volunteers.
Each healthy subject will participate in the study for approximately 3 months, including a 28-day screening period, 3 periods of 3.5 days and 4 nights (inpatient) with each dosage separated by a 10 day washout period and a follow-up visit. The inpatient period will be from Day -1 to Day 4 morning. Dosing will occur on Day 1 and subjects will remain in the clinic until 72 hours (h) after administration.
A Follow up visit will be performed 14 ± 2 days after discharge of the last period.
- Conditions
- Pulmonary Arterial Hypertension
- Being tested
- BIA 5-1058, Furosemide, BIA 5-1058 and Furosemide
- Keywords
- Pulmonary Arterial Hypertension (PAH), BIA 5-1058, Zamicastat, Furosemide, Dopamine ß-hydroxylase (DßH) inhibitor, BIAL
- Medical subject headings
- Pulmonary Arterial Hypertension
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
BIA 5-1058Drug
Also called Period 1
During treatment period 1, a single oral dose of BIA 5-1058 (400 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h.
FurosemideDrug
Also called Period 2
During treatment period 2, a single oral dose of furosemide (40 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h.
BIA 5-1058 and FurosemideDrug
Also called Period 3
During treatment period 3, a single oral dose of both investigational medicinal product (IMPs) BIA 5-1058 (400 mg) concomitantly with furosemide (40 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h.
| Study group | Role | What they receive |
|---|---|---|
| BIA 5-1058 | Experimental | Period 1: Single oral dose of BIA 5-1058 400 mg Receives: Drug: BIA 5-1058 |
| Furosemide | Experimental | Period 2: 40 mg furosemide (single oral dose) Receives: Drug: Furosemide |
| BIA 5-1058 and Furosemide | Experimental | Period 3: 40 mg furosemide (single oral dose) concomitant with a single oral dose of BIA 5-1058 400 mg Receives: Drug: BIA 5-1058 and Furosemide |
What is being measured
The primary outcome is the main question the study is designed to answer.
Maximum observed concentration (Cmax)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Time to Cmax (Tmax)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Elimination rate constant (kel)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Terminal elimination half-life (t1/2)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Area under the concentration-time curve (AUC) from time of dosing to last measurable concentration (AUC0-t)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
AUC extrapolated to infinity (AUC0-inf)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Clearance (CL/F)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Volume of distribution (Vz/F)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
AUC% extrapolated (residual area)
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Measured: Up to 3 months
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted15 Sep 2025
- Study start11 Jun 2018
- Primary completion7 Sep 2018
- Study completion7 Sep 2018
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Other trials for Pulmonary Arterial HypertensionStudies of the same condition, open and under way.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 1
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Sequential
- Masking
- None (open label)
- Enrolment
- 44 participants (actual)
Sponsor and investigators
- Lead sponsor
- Bial - Portela C S.A.
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Annelize Koch, Dr, Principal investigator, Simbec Research
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT07173738
- Sponsor's protocol ID
- BIA-51058-111
- Other IDs
- 2017-002807-93, 2017
- Status last verified
- Sep 2025
- First submitted
- 8 Sep 2025
- Last updated
- 15 Sep 2025
- Results posted
- No
- Data monitoring committee
- No
- FDA-regulated drug
- No
- FDA-regulated device
- No
Study at a glance
From the registry record, last updated by the sponsor on 15 Sep 2025. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- An Open Label, Three Period, Fixed Sequence Study to Assess the Pharmacokinetics, Safety and Tolerability of Concurrent Doses of BIA 5-1058 and Furosemide in Healthy Subjects Under Fasting Conditions.
- ClinicalTrials.gov ID
- NCT07173738
- Acronym / sponsor ID
- BIA-51058-111
- Conditions
- Pulmonary Arterial Hypertension
- Keywords
- Pulmonary Arterial Hypertension (PAH), BIA 5-1058, Zamicastat, Furosemide, Dopamine ß-hydroxylase (DßH) inhibitor, BIAL
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 44 participants (actual)
- Lead sponsor
- Bial - Portela C S.A.Industry (pharma, biotech, devices)
- Study start
- 11 Jun 2018 (actual)
- Primary completion
- 7 Sep 2018 (actual)
- Study completion
- 7 Sep 2018 (actual)
- First posted
- 15 Sep 2025 (actual)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is:
- To assess the effect of BIA 5 1058 400 mg on furosemide pharmacokinetics (PK).
- To assess the effect of furosemide 40 mg on the PK of BIA 5 1058.
Detailed description
This was an open-label, single-dose, fasted, 3-periods, fixed-sequence study separated by a washout period of 10 days or more in healthy volunteers.
Each healthy subject will participate in the study for approximately 3 months, including a 28-day screening period, 3 periods of 3.5 days and 4 nights (inpatient) with each dosage separated by a 10 day washout period and a follow-up visit. The inpatient period will be from Day -1 to Day 4 morning. Dosing will occur on Day 1 and subjects will remain in the clinic until 72 hours (h) after administration.
A Follow up visit will be performed 14 ± 2 days after discharge of the last period.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Sequential
- Masking
- None (open label)
- Number of arms
- 3
| Arm | Type | Receives |
|---|---|---|
| BIA 5-1058 | Experimental | Drug: BIA 5-1058Period 1: Single oral dose of BIA 5-1058 400 mg |
| Furosemide | Experimental | Drug: FurosemidePeriod 2: 40 mg furosemide (single oral dose) |
| BIA 5-1058 and Furosemide | Experimental | Drug: BIA 5-1058 and FurosemidePeriod 3: 40 mg furosemide (single oral dose) concomitant with a single oral dose of BIA 5-1058 400 mg |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (16 listed)
- A signed and dated informed consent form before any study-specific screening procedure is performed;
- Males and Females subjects aged 18 to 55 years, inclusive;
- Non-smoker or ex-smokers for at least 3 months prior to screening;
- Body mass index (BMI) between 18 and 30 kg/m2, inclusive;
- Subject with no clinically significant history of previous allergy / sensitivity to BIA 5-1058/furosemide or any of the excipients contained within the IMP(s);
Key exclusion criteria (21 listed)
- Any personal or family history of haemostatic disorder;
- Consumption of more than 21 units (14 units for female subjects) of alcohol a week [1 unit corresponds to 1 glass of 12% wine (10 cl), 1 glass of 45% pastis (2.5 cl), 1 glass of 40% whisky (2.5 cl), 1 glass of 12% champagne (10 cl), 1 glass of 18% aperitif drink (7 cl) or one 25-cl glass of 5% beer];
- Use of nicotine replacement products such as patches, gum and/or electronic cigarettes within 3 months prior to the screening visit;
- Significant infection or known inflammatory process at screening or admission to each treatment period;
- Acute gastrointestinal symptoms (e.g., nausea, vomiting, diarrhoea, heartburn) at the time of screening or admission to each treatment period;
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| BIA 5-1058Also: Period 1During treatment period 1, a single oral dose of BIA 5-1058 (400 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h. | Drug | BIA 5-1058 |
| FurosemideAlso: Period 2During treatment period 2, a single oral dose of furosemide (40 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h. | Drug | Furosemide |
| BIA 5-1058 and FurosemideAlso: Period 3During treatment period 3, a single oral dose of both investigational medicinal product (IMPs) BIA 5-1058 (400 mg) concomitantly with furosemide (40 mg) will be administered on the morning of day 1, following an overnight fast of at least 10 h. | Drug | BIA 5-1058 and Furosemide |
Primary outcome
Maximum observed concentration (Cmax)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Time to Cmax (Tmax)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Elimination rate constant (kel)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Terminal elimination half-life (t1/2)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Area under the concentration-time curve (AUC) from time of dosing to last measurable concentration (AUC0-t)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
AUC extrapolated to infinity (AUC0-inf)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Clearance (CL/F)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Volume of distribution (Vz/F)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
AUC% extrapolated (residual area)
Time frame: Up to 3 months
Will be calculated from the treatment periods 1, 2 and 3, days 1 to 4, BIA 5-1058 and furosemide concentration-time data
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 15 Sep 2025.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Annelize Koch, Dr principal investigator
Simbec Research
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing BIA 5-1058, Furosemide and BIA 5-1058 and Furosemide in people with Pulmonary Arterial Hypertension, run by Bial - Portela C S.A. at 1 site in United Kingdom.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 16 inclusion and 21 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 15 Sep 2025. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United Kingdom. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Maximum observed concentration (Cmax) (time frame: Up to 3 months). The study lists 9 primary outcomes in all. It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 15 Sep 2025.