Relative Bioavailability of BI 207127 Trial Formulation II Prototypes Versus BI 207127 Trial Formulation I in Healthy Volunteers

Boehringer Ingelheim

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: BI 207127 NA delayed release; Drug: BI 207127 NA (TF-I); Drug: BI 207127 NA extended release (20% HPMC); Drug: BI 207127 NA (TF-II); Drug: BI 207127 NA extended release (15% PEO); Drug: BI 207127 NA extended release (10% HPMC)

Study type: Interventional

Funder types: Industry

Identifiers

NCT02182414

1241.9

Details and patient eligibility

About

Study to investigate the relative bioavailability of 5 new 400 mg tablet formulations (trial formulation II prototypes) of BI 207127 compared to the current 200 mg BI 207127 tablet formulation (trial formulation I) in healthy male volunteers with the aim to identify the best formulation for further drug development (formulation finding part / trial part 1) and to investigate the effect of food on the relative bioavailability of the most promising one of these trial formulation II prototypes (food-effect part / trial part 2).

Enrollment: 42 patients

Sex: Male

Ages: 18 to 50 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Healthy males according to a complete medical history, including a physical examination,vital signs (blood pressure (BP), pulse rate (PR)), 12-lead Electrocardiogram (ECG), and clinical laboratory tests
• Age 18 to 50 years, inclusive
• Body mass index 18.5 to 29.9 kg/m2, inclusive
• Signed and dated written informed consent prior to admission to the study in accordance with Good Clinical Practice and the local legislation

Exclusion criteria

• Any finding of the medical examination (including BP, PR and ECG) deviating from normal and of clinical relevance
• Any evidence of a clinically relevant concomitant disease
• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
• Surgery of the gastrointestinal tract (except appendectomy)
• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
• History of relevant orthostatic hypotension, fainting spells or blackouts
• Chronic or relevant acute infections
• History of relevant allergy/hypersensitivity (including allergy to drug or its excipients)
• Intake of drugs with a long half-life (> 24 hours) within at least one month prior to administration of the trial drug or during the trial
• Use of any drugs (including herbal preparations, vitamins and nutrient supplements) within 14 days prior to first administration of the trial drug or during the trial
• Participation in another trial with an investigational drug within two months prior to administration of the trial drug or during the trial
• Smoker (> 10 cigarettes or > 3 cigars or > 3 pipes/day)
• Alcohol abuse (more than 40 g/day)
• Drug abuse
• Blood donation (more than 100 mL within four weeks prior to first administration of the trial drug or during the trial)
• Excessive physical activities (within one week prior to first administration of the trial drug of the trial drug or during the trial)
• Any laboratory value outside the reference range that is of clinical relevance
• Inability to comply with dietary regimen of trial site
• A marked baseline prolongation of QT/QTc interval (e.g., repeated demonstration of a QTc interval >450 MS)
• A history of additional risk factors for Torsade de Points (TdP) (e.g., heart failure, hypokalemia, family history of Long QT Syndrome)
• History of photosensitivity or recurrent rash

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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42 participants in 8 patient groups

BI 207127 NA (TF-I)

Active Comparator group

Description:

trial part 1: 800 mg BI 207127 NA Trial formulation I (TF-I)

Treatment:

Drug: BI 207127 NA (TF-I)

BI 207127 NA (TF-II)

Experimental group

Description:

trial part 1: 800 mg BI 207127 NA Trial formulation II (TF-II)

Treatment:

Drug: BI 207127 NA (TF-II)

BI 207127 NA delayed release

Experimental group

Description:

trial part 1: 800 mg BI 207127 NA TF-II, delayed release

Treatment:

Drug: BI 207127 NA delayed release

BI 207127 NA extended release (10% HPMC)

Experimental group

Description:

trial part 1: 800 mg BI 207127 NA TF-II, extended release (10% Hydroxypropyl methyl cellulose (HPMC))

Treatment:

Drug: BI 207127 NA extended release (10% HPMC)

BI 207127 NA extended release (15% PEO)

Experimental group

Description:

trial part 1: 800 mg BI 207127 NA TF-II, extended release (15% Polyethylene oxide (PEO))

Treatment:

Drug: BI 207127 NA extended release (15% PEO)

BI 207127 NA extended release (20% HPMC)

Experimental group

Description:

trial part 1: 800 mg BI 207127 NA TF-II, extended release (20% HPMC)

Treatment:

Drug: BI 207127 NA extended release (20% HPMC)

BI 207127 (TF-II), fed

Experimental group

Description:

trial part 2

Treatment:

Drug: BI 207127 NA delayed release

Drug: BI 207127 NA extended release (15% PEO)

Drug: BI 207127 NA extended release (20% HPMC)

Drug: BI 207127 NA (TF-II)

Drug: BI 207127 NA extended release (10% HPMC)

BI 207127 (TF-II), fasted

Experimental group

Description:

trial part 2

Treatment:

Drug: BI 207127 NA delayed release

Drug: BI 207127 NA extended release (15% PEO)

Drug: BI 207127 NA extended release (20% HPMC)

Drug: BI 207127 NA (TF-II)

Drug: BI 207127 NA extended release (10% HPMC)