Characterization and Detection of Prolonged Endothelin Receptors Antagonists Administration

NCT01352065 | Completed Phase 2 DMC

• 1 other identifier: CHS-ERA-2011
• Study Type: interventional
• Target: 30
• Locations: 1 country
• Sites: 1

Brief Summary

Endothelin receptors antagonists (ERA), such as bosentan and ambrisentan, are a class of vasoactive drugs that have been developed for the treatment of pulmonary arterial hypertension. It has been anecdotally reported that ERA is frequently used among top-level athletes to counteract exercise-induced rise in pulmonary vascular pressures and increase exercise performance. Yet, the effects of ERA on exercise capacity in healthy humans are puzzling, with the drugs not included in the current Prohibited List, since the ergogenic potential is yet to be fully understood and determined. Furthermore, the urinary excretion of ERA metabolites following administration has not been studied systematically at rest and during exercise in athletes, as a way to detect its intake if performance-enhancing potential is confirmed. In the planned study ERA will be administered in newly approved doses for 8 weeks in order to assess the presumed doping potential for both male and female athletes, and to monitor serum and urinary ERA excretion dynamics after single- and multiple-dose administration. The possible effects of prolonged ERA administration in higher doses on exercise performance may be relevant, if further confirmed, in terms of their possible fraudulent utilization to influence exercise performance in sports, raising the difficult question of whether, particularly in some circumstances, the ERA might be considered as prohibited substances in athletes.

Conditions

Pulmonary Hypertension

Keywords

Pharmacokinetics; Exercise performance; Athletes

Outcome Measures

Primary Outcomes (1)

• Maximal oxygen uptake

  Maximal oxygen uptake is the maximum capacity of an individual's body to transport and use oxygen during incremental exercise, which reflects the physical fitness of the individual.

  Change from Baseline in Maximal oxygen uptake at 8 weeks

Secondary Outcomes (1)

• Plasma concentration of bosentan

  Regular sampling will be performed during administration at 0, 1, 2, 4, 6, and 8 weeks, and after 2 and 4 weeks post-administration

Study Arms (3)

BOSENTAN

EXPERIMENTAL

Drug: Bosentan

AMBRISENTAN

EXPERIMENTAL

Drug: Ambrisentan

PLACEBO

PLACEBO COMPARATOR

Drug: Placebo

Interventions

Bosentan DRUG

tablet, 250 mg per day, twice per day, 8 weeks

BOSENTAN

Ambrisentan DRUG

tablet, 10 mg per day, single per day, 8 weeks

AMBRISENTAN

Placebo DRUG

Tablet, 10 mg per day, single per day, 8 weeks

PLACEBO

Eligibility Criteria

• Age: 20 Years - 30 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• male and female volunteers
• experienced in athletic training (\> 5 years of experience)
• aged 20 to 30 years
• free from musculoskeletal dysfunctions
• free from metabolic and heart diseases

You may not qualify if:

• pregnancy
• use of hormonal contraceptives
• use of dietary supplement that contains any ergogenic agent

Sponsors & Collaborators

• Center for Health Sciences, Serbia: lead

Study Sites (1)

Center for Health, Exercise and Sport Sciences

Belgrade, 11000, Serbia

Location

Related Publications (1)

• Ostojic SM, Stojanovic M, Calleja-Gonzalez J, Olcina G, Sekulic D, Hoffman JR. Performance-enhancing effects of non-selective endothelin receptor antagonist. Int J Cardiol. 2014 Feb 1;171(2):294-7. doi: 10.1016/j.ijcard.2013.11.077. Epub 2013 Dec 4. No abstract available.

  PMID: 24342407 DERIVED

MeSH Terms

Conditions

Hypertension, Pulmonary

Interventions

Bosentan; ambrisentan

Condition Hierarchy (Ancestors)

Lung Diseases; Respiratory Tract Diseases; Hypertension; Vascular Diseases; Cardiovascular Diseases

Intervention Hierarchy (Ancestors)

Benzenesulfonamides; Sulfonamides; Amides; Organic Chemicals; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons; Sulfones; Sulfur Compounds; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Sergej M Ostojic, MD, PhD

  Center for Health, Exercise and Sport Sciences

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 2
• Allocation: RANDOMIZED
• Masking: QUADRUPLE
• Who Masked: PARTICIPANT, CARE PROVIDER, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: OTHER

Study Record Dates

• First Submitted: May 9, 2011
• First Posted: May 11, 2011
• Study Start: January 1, 2011
• Primary Completion: December 1, 2012
• Study Completion: May 1, 2013
• Last Updated: May 8, 2013

Record last verified: 2013-05

Locations

SE (1)