Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ESR 1150 CL in Healthy Subjects

Healthy Clinical Trial

Official title:

Administration of ESR 1150 CL in Ascending Doses of 0.5, 1, 2, 4 and 8 mg in an Open, Group Comparison and Placebo-controlled Design (Placebo Randomised Double Blind in the Dose Groups) for the Assessment of Safety, Tolerability (Maximum Tolerated Dose, MTD), Pharmacokinetics and Pharmacodynamics in 5 Groups of 8 Female and 5 Male Healthy Subjects, and 4 mg Additionally in Fed State, in a Cross Over Design. Safety, Tolerability and Pharmacokinetics of MTD/4, MTD/2 and MTD in 6 Healthy Male Subjects, Identified as CYP2D6 and/or "Spartein" Poor Metabolizers, in a 3-fold Cross Over, Open Study.

Clinical Trial Details — Status: Terminated

Administrative data

• NCT number: NCT02209688
• Other study ID #: 1172.2
• Status: Terminated
• Phase: Phase 1
• First received: August 5, 2014
• Last updated: August 5, 2014
• Start date: February 2000

Study information

• Verified date: August 2014
• Source: Boehringer Ingelheim
• Contact: n/a
• Is FDA regulated: No
• Health authority: Germany: Federal Institute for Drugs and Medical Devices
• Study type: Interventional

Clinical Trial Summary

The objective of this study was to obtain safety and tolerability data and first pharmacokinetic and pharmacodynamic data of escalating doses of ESR 1150 CL.

Recruitment information / eligibility

• Status: Terminated
• Enrollment: 39
• Est. primary completion date: March 2000
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Both
• Age group: 18 Years to 50 Years

Eligibility

Inclusion Criteria:

• Healthy male and female Caucasian subjects as determined by results of screening

• Written informed consent in accordance with Good Clinical Practice and local legislation given

• Age = 18 and = 50 years

• Broca = - 20 % and = + 20 %

• for first part of study: extensive metabolizers of CYP2D6 and/or "spartein" type; for second part of study: poor metabolizers of CYP2D6 and/or "spartein"

Exclusion Criteria:

• Any finding of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance

• Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders

• Surgery of gastrointestinal tract (except appendectomy)

• Diseases of the central nervous system (such as epilepsy) or psychiatric disorders of neurological disorders

• History of orthostatic hypotension, fainting spells or blackouts

• 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) (= 1 month prior to administration or during the trial, except for oral contraceptives)

• Use of any drugs which might influence the results of the trial (= 10 days prior to administration or during the trial except for oral contraceptives)

• Participation in another trial with an investigational drug (= 2 months prior to administration or during the trial)

• Smoker (> 10 cigarettes or > 3 cigars or > 3 pipes/day)

• Inability to refrain from smoking on trial days

• Alcohol abuse (> 60 g/days)

• Drug abuse

• Blood donation > 100 ml (= 4 weeks prior to administration or during the trial)

• Excessive physical activities (= 10 days prior to administration or during the trial)

• Any laboratory value outside the reference range of clinical relevance

• Females only:

• No reliable contraception (examples of reliable contraception: oral contraceptives, 3-month injection, intrauterine device, sterilisation, condoms + spermicide)

• pregnancy or breast feeding period

Study Design

Allocation: Randomized, Intervention Model: Crossover Assignment, Masking: Open Label, Primary Purpose: Treatment

Related Conditions & MeSH terms

• Healthy

Intervention

Drug:
• ESR 1150 CL

• Placebo

Locations

Country	Name	City	State
n/a

Sponsors (1)

Lead Sponsor	Collaborator
Boehringer Ingelheim

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Number of patients with adverse events		up to 30 days	No
Primary	Area under the curve (AUC)		up to 24 hours after administration	No
Primary	Maximum concentration (Cmax)		up to 24 hours after administration	No
Primary	Time to maximum concentration (tmax)		up to 24 hours after administration	No
Primary	Apparent total plasma clearance (CLtot/f)		up to 24 hours after administration	No
Primary	Apparent volume of distribution (Vz/f)		up to 24 hours after administration	No
Primary	Elimination half-life (t1/2)		up to 24 hours after administration	No
Primary	Amount excreted in urine (Ae)		up to 24 hours after administration	No
Primary	Maximum flow rate (Qmax)	assessed by free uroflowmetry	up to 8 hours after administration	No
Primary	Average flow rate (Qave)	assessed by free uroflowmetry	up to 8 hours after administration	No
Primary	Voided volume (Vcomp)	assessed by free uroflowmetry	up to 8 hours after administration	No
Primary	Voiding time (T100)	assessed by free uroflowmetry	up to 8 hours after administration	No
Primary	Time to maximum flow (TQmax)	assessed by free uroflowmetry	up to 8 hours after administration	No
Primary	Residual urinary volume	assessed by means of transabdominal ultrasound evaluation	up to 8 hours after administration	No
Primary	Assessment of micturition pattern	evaluated by Independent reviewer	up to 8 hours after administration	No
Primary	Amount of inhibition constants (Ki) at a1A, adrenoreceptor subtype level	assessed by ex vivo radioreceptor assay	up to 8 hours after administration	No

External Links

•   Link