Metabolism and Pharmacokinetics of [14C]- BIBW 2992 MA2 in Healthy Male Volunteers

Boehringer Ingelheim

Status and phase

Completed

Phase 1

Conditions

Healthy

Treatments

Drug: [14C]- BIBW 2992 MA2

Study type

Interventional

Funder types

Industry

Identifiers

NCT02171689

1200.25

Details and patient eligibility

About

The aim of the study was to investigate the metabolism and pharmacokinetics of BIBW 2992 MA2 after a single oral dose of [14C]-radiolabelled BIBW 2992 MA2 in healthy male volunteers. Metabolites in human plasma and excretions were measured, the structures of the metabolites analysed and compared with metabolites in animals. In addition, the mass-balance of excretion, the protein binding of [14C]-radioactivity, the plasma concentrations of BIBW 2992 MA2, and the [14C]-radioactivity in blood cells, plasma, urine and faeces were measured. The safety and tolerability of BIBW 2992 were also investigated.

Enrollment

8 patients

Sex

Male

Ages

35 to 60 years old

Volunteers

Accepts Healthy Volunteers

Inclusion criteria

Healthy male subjects as determined by results of screening
Signed written informed consent in accordance with Good Clinical Practice and local legislation
Age ≥35 and ≤60 years
Body Mass Index ≥18.5 kg/m2 and ≤29.9 kg/m2

Exclusion criteria

Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance
History or current gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunologic, hormonal disorders
History of any major surgery within the last four weeks before participation in this study or any bone fracture within the last two months
History of orthostatic hypotension, fainting spells and blackouts
Diseases of the central nervous system (such as epilepsy) or psychiatric disorders
Chronic or relevant acute infections
History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator
Intake of drugs with a long half-life (> 24 hours) within 1 month prior to administration
Planned use of any drugs which might influence the results of the trial within 10 days prior to administration or during the trial
Participation in another trial with an investigational drug within 2 months prior to administration or during trial
Smoker (> 10 cigarettes or 3 cigars or 3 pipes/day) or inability to refrain from smoking on study days
Alcohol abuse (> 60 g/day)
Drug abuse
Blood donation within 1 month prior to administration or during the trial
Excessive physical activities within 5 days prior to administration or during the trial
Any laboratory value outside the reference range, unless considered to lack clinical reference
Male subjects must agree to minimize the risk of female partners becoming pregnant from the dosing day until 3 months after the completion of the study. Acceptable methods of contraception for male volunteers include a vasectomy no less than 3 months prior to dosing, barrier contraception or a medically accepted contraceptive method. For female partners of male volunteers, acceptable methods of contraception include intra-uterine device, tubal ligation, hormonal contraceptive since at least two months and diaphragm with spermicide