Randomized, Multicenter Clinical Study of Tratinterol Hydrochloride Tablets for the Treatment of Bronchial Asthma

Recent Advances in β2-Agonists for Treatment of Chronic Respiratory Diseases and Heart Failure

“…There were also no significant differences between the groups in other parameters including days with rescue medication use, symptom score, lung function, vital signs, and adverse effects. The results demonstrate that the use of trantinterol hydrochloride tablets for asthma control is safe and effective . Biological studies have shown that trantinterol ( 10 ) is a highly selective β 2 -agonist with strong tracheal relaxant activities in guinea pigs and rabbits .…”

“…Trantinterol ( 10 ) with a nonclassical 2-amino-2-phenylethanol core structure (Figure ) is a potential drug candidate for asthma . In a randomized, multicenter clinical study conducted in China, the treatment effects of trantinterol hydrochloride and procaterol hydrochloride in 223 eligible participants were compared . After a run-in period of 3 days, patients in the treatment group and the control group were given 50 μg of the tablet drugs twice daily for 10 days.…”

“…The results demonstrate that the use of trantinterol hydrochloride tablets for asthma control is safe and effective. 190 Biological studies have shown that trantinterol (10) is a highly selective β 2 -agonist with strong tracheal relaxant activities in guinea pigs and rabbits. 189 Trantinterol (10) at 0.01 (equivalent to 50 μg or maximum recommended dose in human), 0.1, and 1 ng/mL did not cause significant inhibition of cytochrome P450 enzymes in human liver microsomes in vitro, demonstrating a low potential for drug−drug interactions.…”

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.…”