|1-(2-(4-((4-氨甲酰基哌嗪-1-基)甲基)-N-甲基苯甲酰氨基)乙基)哌啶-4-基[1,1'-联苯]-2-基氨基甲酸酯|CsnPharm

CAS No.: 864750-70-9

Revefenacin Catalog No. CSN21285

Synonyms: TD-4208;GSK1160724;Yupelri

TD-4208 is a long-actingmuscarinic cholinergic receptor (mAChR) antagonist and may be potentially useful for the treatment of respiratory disease.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TD-4208 (Revefenacin) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM. At human recombinant mAChRs, revefenacin displayed high affinity (pKI = 8.2-9.8) and behaved as a competitive antagonist (pKI, apparent = 9.4-10.9) at the five human recombinant mAChRs. In isolated tracheal tissues from rat and guinea pig and isolated bronchial tissues from humans, revefenacin potently antagonized mAChR-mediated contractile responses. Furthermore, the antagonistic effects of revefenacin in rat, guinea pig, and human airway tissues were slowly reversible (t1/2 of 13.3, >16, and >10 hours, respectively) ^[1]. In anesthetized dogs, TD-4208, along with tiotropium and glycopyrronium, produced sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled TD-4208 exhibited dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The calculated lung selectivity index (i.e., ratio of antisialagogue and bronchoprotective potency) of TD-4208 was superior to glycopyrronium after both single and repeat dosing regimens and was superior to tiotropium after repeat dosing^[2]. 88 and 175 μg revefenacin are appropriate doses for use in longer-term safety and efficacy trials. Revefenacin offers the potential for the first once-daily LAMA (long-acting muscarinic antagonist) for nebulization in patients with COPD (chronic obstructive pulmonary disease) who require or prefer a nebulized drug delivery option^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03095456	Chronic Obstructive Pulmonary ... more >>Disease, COPD Low Peak Inspiratory Flow Rate (PIFR) Collapse <<	Phase 3	Completed	-	United States, South Carolina ... more >> Clinical Research of Rock Hill Rock Hill, South Carolina, United States, 29732 Collapse <<
NCT03573817	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 3	Completed	-	United States, Oregon ... more >> Theravance Biopharma Call Center Medford, Oregon, United States, 97504 Collapse <<
NCT01704404	-	-	Completed	-	-

更多
参考文献

[1] Hegde SS, Pulido-Rios MT, Luttmann MA, et al. Pharmacological properties of revefenacin (TD-4208), a novel, nebulized long-acting, and lung selective muscarinic antagonist, at human recombinant muscarinic receptors and in rat, guinea pig, and human isolated airway tissues. Pharmacol Res Perspect. 2018;6(3):e00400.
[2] Pulido-Rios MT, McNamara A, Obedencio GP, et al. In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. J Pharmacol Exp Ther. 2013;346(2):241-250
[3] Pudi KK, Barnes CN, Moran EJ, Haumann B, Kerwin E. A 28-day, randomized, double-blind, placebo-controlled, parallel group study of nebulized revefenacin in patients with chronic obstructive pulmonary disease. Respir Res. 2017;18(1):182.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6729 mL
- 8.3647 mL
- 16.7295 mL
- 5 mM
- 0.3346 mL
- 1.6729 mL
- 3.3459 mL
- 10 mM
- 0.1673 mL
- 0.8365 mL
- 1.6729 mL

技术信息

CAS号

864750-70-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C35H43N5O4

运输

蓝冰

分子量

597.75

别名

TD-4208;GSK1160724;Yupelri

溶解度

DMSO	420.0 mg/mL (702.6 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03095456	Chronic Obstructive Pulmonary ... more >>Disease, COPD Low Peak Inspiratory Flow Rate (PIFR) Collapse <<	Phase 3	Completed	-	United States, South Carolina ... more >> Clinical Research of Rock Hill Rock Hill, South Carolina, United States, 29732 Collapse <<
NCT03573817	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 3	Completed	-	United States, Oregon ... more >> Theravance Biopharma Call Center Medford, Oregon, United States, 97504 Collapse <<
NCT01704404	-	-	Completed	-	-
NCT02040792	COPD	Phase 2	Completed	-	United States, South Carolina ... more >> Upstate Pharmaceutical Research Greenville, South Carolina, United States, 29615 Collapse <<
NCT02820311	Cardiac Repolarization in Heal... more >>thy Subjects Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Celerion Tempe, Arizona, United States, 85283 Collapse <<
NCT02459080	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 3	Completed	-	United States, Oregon ... more >> Allergy Associates Research Center (AARC) Portland, Oregon, United States, 97202 Collapse <<
NCT01704404	COPD	Phase 2	Completed	-	New Zealand ... more >> P3 Research Ltd Wellington, New Zealand Collapse <<
NCT02512510	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 3	Completed	-	United States, South Carolina ... more >> Palmetto Medical Research Associates L.L.C. Easley, South Carolina, United States, 29640 Collapse <<
NCT02518139	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 3	Completed	-	United States, South Carolina ... more >> Palmetto Medical Research Associates L.L.C Easley, South Carolina, United States, 29640 Collapse <<
NCT03064113	Chronic Obstructive Pulmonary ... more >>Disease, COPD Collapse <<	Phase 2	Completed	-	New Zealand ... more >> P3 Research Wellington, New Zealand, 6021 Collapse <<
NCT02040792	-	-	Completed	-	-
NCT02772159	Chronic Obstructive Pulmonary ... more >>Disease (COPD) Collapse <<	Phase 1	Completed	-	United States, Nebraska ... more >> Celerion Lincoln, Nebraska, United States, 68502 Collapse <<
NCT02578082	Renal Impairment	Phase 1	Completed	-	United States, Florida ... more >> Orlando Clinical Research Center (OCRC) Orlando, Florida, United States, 32809 Collapse <<
NCT02109172	-	-	Completed	-	-
NCT02581592	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Orlando Clinical Research Center (OCRD) Orlando, Florida, United States, 32809 Collapse <<
NCT02109172	Chronic Obstructive Pulmonary ... more >>Disease COPD Collapse <<	Phase 2	Completed	-	United States, North Carolina ... more >> American Health Research Charlotte, North Carolina, United States, 28207 Collapse <<

Revefenacin Catalog No. CSN21285

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