Efficacy and Tolerability of Tratinterol Hydrochloride Tablets in Bronchial Asthma: A Multicenter, Randomized, Double-blind, Dose-finding Clinical Trial

Discovery of a Highly Selective β2-Adrenoceptor Agonist with a 2-Amino-2-phenylethanol Scaffold as an Oral Antiasthmatic Agent

“…Highly specific β 2 -AR agonists may be formulated as oral drugs for maintenance treatment of asthma and consequently reduce the cost of treating this chronic disease. This possibility could be offered by trantinterol 1a as the safety and efficacy of trantinterol hydrochloride tablets in asthma patients have been demonstrated in clinical studies. − In a recent clinical study comparing trantinterol hydrochloride tablets and procaterol hydrochloride tablets in adult patients with bronchial asthma, the incidences of adverse effects associated with β 2 -AR agonists, namely, palpitation and tremor, were lower in the trantinterol group . This might be due to the higher selectivity of trantinterol for the β 2 -AR.…”

“…Compound 1a has demonstrated good biological activities in subsequent experiments and a potential to become a bronchodilator β 2 -AR agonist . Later, compound 1a was proceeded to a series of clinical testing. , A recent phase III clinical study has shown that trantinterol hydrochloride given 50 μg/d orally twice a day was safe and effective and noninferior to procaterol hydrochloride in the studied population of adult Chinese patients with asthma . However, previous biological studies on compound 1a ,, are either short of a systemic structure–activity relationship study or lack of perspectives on the evaluation of the oral bioavailability of the compound and a comparison with existing selective β 2 -AR agonists on β 2 /β 1 -selectivity.…”