Stedivaze (apadenoson) - A2A receptor agonist in trials as stress agent for patients with asthma and COPD

Stedivaze (Apadenoson) Demonstrated Safety and Tolerability in Patients with Asthma and COPD in Phase I Trial.

Stedivaze is a potent and highly selective agonist of the adenosine A2A receptor subtype in development as a pharmacologic stress agent for myocardial perfusion imaging (MPI). Currently available adenosine agonists must be used with caution or are contraindicated in patients with asthma and COPD.

Adenosine and dipyridamole are the currently available vasodilators for myocardial perfusion imaging and they produce hyperemic coronary flow by stimulating A(2A) adenosine receptors on arteriolar vascular smooth muscle cells. However, both vasodilators are nonselective activators of the adenosine receptors A(1), A(2B), and A(3), which contributes to common undesirable effects.

Regadenoson is a new highly selective, low-affinity A(2A) adenosine agonist that is a coronary vasodilator. It was approved by the United States Food and Drug Administration on April 10, 2008 and is marketed under the tradename Lexiscan.

References:

Clinical Data, Inc. Reports Results of Phase I Studies of Stedivaze(TM) Demonstrating Safety and Tolerability in Patients with Asthma and COPD. MarketWatch.

The future of pharmacologic stress testing: selective A2A adenosine receptor agonist regadenoson (Lexiscan)?

Image source: Heart, Gray's Anatomy, 1918, public domain.