GLPG0492 Pharmacodynamics

Assessment of the Muscle Protein Fractional Synthesis Rate Induced by Repeated Administrations of GLPG0492 to Healthy Male Subjects and Assessment of the Safety, Tolerability and Pharmacokinetics of Repeated Administrations of GLPG0492 to Healthy Postmenopausal Women.

GLPG0492 is a selective androgen receptor modulator: the compound should help protect against (or help restore) muscle loss in case of immobilization (e.g. after orthopedic surgery) or due to aging (androgenic effect), but without anabolic effects (e.g. effect on testosterone). In the first part of the current study it will be tested whether GLPG0492 given orally to healthy male volunteers increases the protein synthesis in muscle, as measured by the uptake into the muscle of intravenously infused phenylalanine.

In the second part of the study, the effect of the compound on the "hormone household" in healthy, postmenopausal women will be assessed.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: GLPG0492

• Study Type: Interventional
• Enrollment (Actual): 26
• Phase: Phase 1

Contacts and Locations

Study Locations

• Belgium
  • Antwerp, Belgium
    • SGS Stuivenberg

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy male, age 18-50 years (for part 1), and postmenopausal subjects age 35-65 years (for part 2)
• Body mass index (BMI) between 18-30 kg/m², inclusive.
• For men: normal values of testosterone (175-781 ng/dL) and LH (1.24-8.62 U/L).
• Women must be postmenopausal for at least 2 years with postmenopausal FSH level according to the local lab (+negative pregnancy test at screening & admission).

Exclusion Criteria:

• smoking
• drug or alcohol abuse
• hypersensitivity to any of the ingredients of the study drug

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Parallel Assignment
• Masking: Quadruple

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: GLPG0492 oral solution; Multiple ascending doses once daily for 7 days (part 1) or 14 days (part 2), starting at 0.5 mg/day	Drug: GLPG0492; Oral solution
Placebo Comparator: Placebo; Placebo oral solution, once daily for 7 days (part 1) or 14 days (part 2).	Drug: Placebo; Placebo oral solution

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
To evaluate the safety and tolerability of GLPG0492 in terms of adverse events, vital signs, ECG and abnormal lab tests in comparison with placebo	Occurrence of adverse events, vital signs, ECG and abnormal lab tests as a measure of safety and tolerability	Up to 7 to 10 days after last treatment
In male volunteers: effect on protein synthesis in muscle, as measured by the uptake into the muscle of intravenously infused phenylalanine	During a 5-hour infusion of phenylalanine two muscle biopsies will be taken; this procedure is performed before and after one week of treatment with GLPG0492, to determine the effect of the compound.	One week

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
To determine the pharmacokinetic profile and metabolism after single and multiple oral doses of GLPG0492	The plasma levels of GLPG0492 will be determined as a measure of pharmacokinetics, and the plasma and urine samples will be used for metabolism investigation	Up to 24h hours after last treatment
In female volunteers: effects on hormone household.	In female volunteers the effect of two weeks treatment on hormone levels in the blood will be assessed.	up to 7 to 10 days after treatment.

Collaborators and Investigators

• Sponsor: Galapagos NV
• Investigators: Study Director: Florence Namour, MSc, Galapagos SASU

Study record dates

Study Major Dates

• Study Start: January 1, 2012
• Primary Completion (Actual): March 1, 2012
• Study Completion (Actual): April 1, 2012

Study Registration Dates

• First Submitted: February 20, 2012
• First Submitted That Met QC Criteria: February 23, 2012
• First Posted (Estimate): February 24, 2012

Study Record Updates

• Last Update Posted (Estimate): April 19, 2012
• Last Update Submitted That Met QC Criteria: April 18, 2012
• Last Verified: April 1, 2012

More Information

Terms related to this study

• Keywords: Safety; Pharmacokinetics; Tolerability; Pharmacodynamics
• Other Study ID Numbers: GLPG0492-CL-103; 2011-004743-41 (EudraCT Number)