Efficacy and safety of tratinterol hydrochloride tablets in bronchial asthma: a randomized double-blind and multicenter clinical trial

Kong, Lingfei; Zhao, Yang; Wang, Yan; Chang, Xiaolin; Gu, Guozhong; Ma, Zhuang; Lu, Qiang; Zhou, Lei; Lianming, Ding; Wang, Zhenshan; Shao, Yi; Tang, Huaping; Zhang, Chunyu; Hui, Fuxin; Mei, Xiaodong; Xin, Jian-Bao; Huo, Jianmin; Sun, Shenghua; Zhu, Sai-Nan; Yao, Chen; Du, Guijie; Cheng, Maosheng; Kang, Jian

doi:10.1080/02770903.2019.1663427

Cited by 2 publications

(3 citation statements)

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“…38−40 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. 40 This might be due to the higher selectivity of trantinterol for the β 2 -AR.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

“…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.…”

Section: Resultsmentioning

confidence: 99%

“…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.…”

Section: Introductionmentioning

confidence: 99%

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

Xing

Woo

et al. 2022

J. Med. Chem.

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Asthma patients in resource-poor countries cannot obtain adequate basic asthma medications because most asthma medications are supplied as inhalants. An alternative approach is to create oral antiasthmatic drugs with high β2/β1-selectivity, which should reduce treatment costs. In this study, we designed a cohort of compounds 1 using 2-(4-amino-3-chloro-5-(trifluoromethyl)phenyl)-2-(tert-butylamino)ethan-1-ol hydrogen chloride (1a) as the lead compound with an aim to expand the library of compounds possessing the 2-amino-2-phenylethanol scaffold. Structure–activity relationship studies on these compounds revealed that compounds created showed remarkable β2 selectivity compared to isoproterenol and gave additional insights on the rational design of β2-adrenoceptor agonists. Moreover, 1a was found as the best candidate compound showing the greatest potential for drug development. Cell-based assays showed that 1a was about 10 times more selective than salbutamol toward the β2-adrenoceptor. Moreover, 1a exhibited good oral bioavailability and low acute oral toxicity. These data reveal 1a as an oral antiasthmatic agent.

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Section: ■ Results and Discussionmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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

Xing

Woo

et al. 2022

J. Med. Chem.

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Role of dispersion enhancer selection in the development of novel tratinterol hydrochloride dry powder inhalation formulations

Liu

Tong

Liao

et al. 2023

International Journal of Pharmaceutics

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Efficacy and safety of tratinterol hydrochloride tablets in bronchial asthma: a randomized double-blind and multicenter clinical trial

Cited by 2 publications

References 9 publications

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

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

Role of dispersion enhancer selection in the development of novel tratinterol hydrochloride dry powder inhalation formulations

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Efficacy and safety of tratinterol hydrochloride tablets in bronchial asthma: a randomized double-blind and multicenter clinical trial

Cited by 2 publications

References 9 publications

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

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

Role of dispersion enhancer selection in the development of novel tratinterol hydrochloride dry powder inhalation formulations

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

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