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NCT Number: NCT01352065

Characterization and Detection of Prolonged Endothelin Receptors Antagonists Administration

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.

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Key information

Conditions

Pulmonary Hypertension Cardiovascular Diseases Hypertension Hypertension, Pulmonary Lung Diseases Respiratory Tract Diseases Vascular Diseases

Age range

20 year–30 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 2 / Phase 3

Primary location

Center for Health, Exercise and Sport Sciences

Belgrade, 11000, Serbia

About this study

Preliminary findings of our research group indicated that ERA enhances exercise performance (particularly aerobic) after 7-day intake of higher doses of non-selective ERA bosentan (doses used were approved for pulmonary arterial hypertension treatment). This is in part in accordance with results of previous research (Faoro et al. 2009), although authors administered regular single dose (62.5 mg) of bosentan in hypoxic healthy subjects. Our study should examine metabolic profiles of athletes after receiving significantly higher doses of two oral ERA as compared to previous research, along with assessment of ergogenic potential with 8 weeks of administration in placebo-control and randomized design. We expect that ERA will increase time to exhaustion during endurance test, increase the maximal oxygen uptake and rate of ultra-short term heart rate recovery after exercise, and affecting blood and urine cortisol, testosterone and dehydroepiandrosterone following administration. Moreover, we will clearly evaluate 24-h pharmacokinetic profile of ERA in blood and urine and collect data for concentration-time profiles of ERA and main active metabolites, in aim to provide more rationale basis for identification and detection for doping control.

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • 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

Exclusion criteria

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

Treatment and study plan

Bosentan

Drug

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

Ambrisentan

Drug

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

Placebo

Drug

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

Primary outcomes

  1. Maximal oxygen uptake

    Time frame: Change from Baseline in Maximal oxygen uptake at 8 weeks

    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.

Secondary outcomes

  1. Plasma concentration of bosentan

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

Sponsors and collaborators

Lead sponsor

Center for Health Sciences, Serbia

Other

Registry information

Official study title

Phase 3 Characterization and Detection of Prolonged Endothelin Receptors Antagonists Administration

Acronym: ERAATH

Important dates

Study start
2011
Primary completion
2012
Study completion
2013
First posted
May 11, 2011
Registry last updated
May 8, 2013

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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