Safety and Tolerability Study of BIBF 1120 as Intravenous Infusion and Absolute Bioavailability of BIBF 1120 as Soft Gelatine Capsule in Healthy Subjects

Boehringer Ingelheim

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: BIBF 1120 intravenous solution; Drug: BIBF 1120 soft gelatine capsule; Drug: Placebo ampoule

Study type: Interventional

Funder types: Industry

Identifiers

NCT02182258

1199.75

Details and patient eligibility

About

The primary objective of this trial was to assess the safety and tolerability of BIBF 1120 administered as intravenous (iv) infusions of 1, 3, 10, and 20 mg, and to assess the absolute bioavailability of orally administered 100 mg BIBF 1120 as soft gelatine capsules. A secondary objective was the exploration of the pharmacokinetic (PK) of BIBF 1120 after single iv dosing, including dose proportionality.

Enrollment: 30 patients

Sex: Male

Ages: 18 to 50 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

Healthy males according to the following criteria:

1. Based upon a complete medical history, including the physical examination, vital signs (blood pressure, pulse rate), 12-lead ECG, and clinical laboratory tests
2. Age ≥18 years and ≤50 years
3. Body mass index (BMI) ≥18.5 and ≤29.9 kg/m2
4. Signed and dated written informed consent prior to admission to the study, in accordance with GCP and local legislation

Exclusion criteria

1. Any finding from medical examination (including blood pressure, pulse rate, ECG) deviating from normal and of clinical relevance
2. History of or current gastrointestinal, hepatic (including Gilbert's syndrome and history of bilirubin increases) renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders
3. History of relevant orthostatic hypotension, fainting spells, and blackouts
4. Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders
5. Chronic or relevant acute infections
6. History of allergy/hypersensitivity (including drug allergy or its excipients) which is deemed relevant to the trial as judged by the investigator
7. History of any bleeding disorder including prolonged or habitual bleeding, other haematologic disease or cerebral bleeding (e.g. after a car accident) or commotio cerebri
8. Intake of drugs with a long half-life (>24 h) within 1 month prior to administration or during the trial
9. Use of any drugs which might influence the results of the trial within 14 days prior to administration or during the trial
10. Participation in another trial with an investigational drug within 2 months prior to administration or during the trial
11. Smoker (>10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
12. Alcohol abuse (>30 g/day)
13. Drug abuse
14. Blood donation (>150 mL within 4 weeks prior to administration or during the trial)
15. Excessive physical activities within 5 days prior to administration or during the trial
16. Any laboratory value outside the reference range that is of clinical relevance
17. Male subjects refusing to minimise the risk of female partners becoming pregnant from the first dosing day until 3 months after completion of the study. Acceptable methods of contraception for male volunteers include vasectomy no less than 3 months prior to administration, barrier contraception, or a medically accepted contraceptive method. Acceptable methods of contraception for female partners of male volunteers include intra-uterine device, tubal ligation, hormonal contraceptive for at least 2 months and diaphragm with spermicide.
18. Homozygous genotype status for UGT1A1*28, *60 (Gilbert polymorphisms)

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: Single Blind

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30 participants in 3 patient groups, including a placebo group

Placebo

Placebo Comparator group

Treatment:

Drug: Placebo ampoule

BIBF 1120 intravenous

Active Comparator group

Treatment:

Drug: BIBF 1120 intravenous solution

BIBF 1120 capsule

Experimental group

Treatment:

Drug: BIBF 1120 soft gelatine capsule