Open label, single-center, cross-over randomized, relative bioavailability study comparing 4 new BF2.649 (pitolisant) tablet formulations versus the reference pitolisant (Wakix®) tablet formulation after single oral administrations in healthy male subjects.

Trial details

Who runs it

Bioprojet Pharma

Trial code

EU 2023-505769-98-00

Record updated

10 October 2023

Original description

To compare the pharmacokinetic (PK) parameters of pitolisant, its main identified metabolites (BP2.951, BP1.8054, BP1.9733, BP1.3484, BP1.3473, BP1.10556 and BP1.10749), after a single oral administration of 40 mg pitolisant hydrochloride of each of the new formulated tablets versus the reference formulation (Wakix®), in fasting conditions, in healthy male subjects.Read full original descriptionShow less

To compare the pharmacokinetic (PK) parameters of pitolisant, its main identified metabolites (BP2.951, BP1.8054, BP1.9733, BP1.3484, BP1.3473, BP1.10556 and BP1.10749), after a single oral administration of 40 mg pitolisant hydrochloride of each of the new formulated tablets versus the reference formulation (Wakix®), in fasting conditions, in healthy male subjects.

Inclusion: Has given written informed consent; Male subject ≥ 18 and ≤ 50 years old,; Healthy subject ascertained by detailed medical history and physical examination, including subject presenting a history of seasonal and/or contact allergy; Body mass index (BMI) ≥ 18 and ≤ 30 kg/m2; Normal laboratory tests or if abnormal, judged as not clinically significant by the Investigator,; Subject should agree to use an efficient contraceptive mean i.e., barrier method or abstinence during the whole study duration and up to 5 times the drug half-life,; Normal arterial BP and pulse rate or, if abnormal, judged as not clinically significant by the Investigator. Normal BP values are defined by: (i) Systolic BP (SBP) > 90 millimeters of mercury (mmHg) and < 145 mmHg after 5 minutes (min) in supine position, (ii) Diastolic BP (DBP) > 45 mmHg and < 90 mmHg after 5 min in supine position, (iii) HR > 40 beats per minute (bpm) and =< 90 bpm after 5 min in supine position; Normal 12-lead ECG recording or, if abnormal, judged as not clinically significant by the Investigator. Normal ECGs are defined by: (i) HR [40-90 bpm], (ii) PR [120 -200 milliseconds (ms)], (iii) QRS < 120 ms, (iiii) QTcF < 450 ms, (iiiii) No clinically significant conduction disorders or significant arrhythmia.

Exclusion: Intake of any food or any beverage containing grapefruit or grapefruit juice within 48 h prior to the first dosing and the inability to stop such intake during the study,; Blood donation or loss of significant amount of blood within 2 months prior to the first dosing,; Positive drug screen (amphetamines, benzodiazepines, cocaine, opiate class, barbiturates, and cannabinoids) at screening or at the determination performed before the first dosing,; Receiving any immune suppressive treatment within 6 weeks before the study,; Viral, systemic, fungal, bacterial or protozoal infection (flu like symptoms (cough, fever)) within 4 weeks before the study,; Subject in the 2-month period of a previous study or currently participating in, or plan to participate, in an investigational drug or medical device study during the 2 months following study completion; Any condition requiring regular concomitant medication, including herbal products and over-the-counter (OTC) medication or predicted need of any concomitant medication during the study,; Intake of any medication (except paracetamol), including OTC medications and herbal products that could affect the outcome of the study, within 2 weeks prior to the first drug administration or less than 5 times the t1/2 of that drug, whichever is longer,; Current drug or alcohol abuse [including regular alcohol drinking of more than 21 units per week (1 unit = 4 cL spirits or equivalent)] or a history of drug or alcohol abuse within 1 year before screening,; Positive serology to HIV (HIV1 and HIV2) and/or HCV antibodies, and/or hepatitis B surface antigen (HBsAg),; Presenting any suggestive clinical evidence of active or latent tuberculosis,; Any other condition that in the opinion of the Investigator would interfere with the evaluation of the results or constitute a health risk for the subject,; Evidence of clinically relevant cardiovascular, renal, hepatic, hematological, gastrointestinal, pulmonary, metabolic-endocrine, neurological, urogenital or psychiatric diseases as judged by the Investigator,; History of asthma of allergic origin, history of drug and/or food allergy,; Evidence of any clinically significant acute or chronic disease on direct questioning and physical examination, including known or suspected human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV) infection,; Known hypersensitivity to any of the test materials or related compounds,; History of additional risk factors for “Torsades de Pointe” (e.g., heart failure, hypokalemia, family history of Long QT Syndrome,; Predictable poor compliance or inability to communicate well with the Investigator,; Current use of nicotine containing products, i.e., more than 5 cigarettes or equivalent/day and the inability to stop using nicotine containing products during confinement in the clinical center,; Use of caffeine containing beverages exceeding 500 mg caffeine/day (5 cups of coffee) and the inability to refrain from the use of caffeine containing beverages during confinement in the clinical center,; Positive alcohol breath test at screening or at determination performed before the first dosing,; Unsuitable veins for repeated venipuncture; Having any vaccination during the 2 weeks preceding the study screening,.

EU CTIS 2023-505769-98-00