[Translation] A multicenter, randomized, double-blind, placebo-controlled, parallel-controlled Phase II clinical study to evaluate the efficacy and safety of 101BHG-D01 nasal spray in the treatment of runny nose caused by colds

主要目的：评价101BHG-D01鼻喷雾剂治疗感冒引起的流涕的有效性。次要目的：（1）评价101BHG-D01鼻喷雾剂治疗感冒引起的流涕、鼻塞、喷嚏的安全性。（2）评价101BHG-D01鼻喷雾剂对感冒引起的鼻塞、喷嚏的改善情况。

[Translation]

Primary objective: To evaluate the effectiveness of 101BHG-D01 nasal spray in treating runny nose caused by cold. Secondary objectives: (1) To evaluate the safety of 101BHG-D01 nasal spray in treating runny nose, nasal congestion and sneezing caused by cold. (2) To evaluate the improvement of 101BHG-D01 nasal spray in treating nasal congestion and sneezing caused by cold.

Start Date22 Nov 2022

Sponsor / Collaborator

Beijing Showby Pharmaceutical Co Ltd

ChiCTR2200065138 / SuspendedPhase 2IIT

A multicenter, randomized, double-blind, placebo, parallel controlled phase II clinical study to evaluate the efficacy and safety of 101BHG-D01 nasal spray in patients with runny nose caused by colds

Start Date31 Oct 2022

Sponsor / Collaborator

Peking University Third Hospital

CTR20222288 / CompletedPhase 2

一项评价101BHG-D01鼻喷雾剂治疗季节性变应性鼻炎的有效性和安全性的多中心、随机、双盲、安慰剂对照II期临床研究

[Translation] A multicenter, randomized, double-blind, placebo-controlled phase II clinical study to evaluate the efficacy and safety of 101BHG-D01 nasal spray in the treatment of seasonal allergic rhinitis

主要目的：评价101BHG-D01鼻喷雾剂治疗季节性变应性鼻炎的初步疗效及剂量与疗效之间的关系。次要目的： 1.评价101BHG-D01鼻喷雾剂治疗季节性变应性鼻炎的安全性； 2.评价101BHG-D01鼻喷雾剂对眼部症状的改善情况； 3.评价101BHG-D01鼻喷雾剂对受试者生活质量的改善情况。

[Translation]

Main purpose: To evaluate the preliminary efficacy of 101BHG-D01 nasal spray in the treatment of seasonal allergic rhinitis and the relationship between dose and efficacy. Secondary objectives: 1. To evaluate the safety of 101BHG-D01 nasal spray in the treatment of seasonal allergic rhinitis; 2. To evaluate the improvement of eye symptoms by 101BHG-D01 nasal spray; 3. To evaluate the improvement of the quality of life of subjects by 101BHG-D01 nasal spray.

Start Date21 Sep 2022

Sponsor / Collaborator

Beijing Showby Pharmaceutical Co Ltd

100 Clinical Results associated with 101BHG-D01

100 Translational Medicine associated with 101BHG-D01

100 Patents (Medical) associated with 101BHG-D01

Literatures (Medical) associated with 101BHG-D01

01 Nov 2023·Current Drug Metabolism

Pharmacokinetics, Mass Balance, Tissue Distribution and Metabolism of [14C]101BHG-D01, a Novel Muscarinic Receptor Antagonist, in Rats

Article

Author: Gao, Huaye ; Shu, Chang ; Diao, Xingxing ; Ding, Li ; Hu, Wenhui ; Zheng, Yuandong ; Ding, Juefang ; Yang, Cheng

Background::101BHG-D01, a novel long-acting and selective muscarinic receptor antagonist for the treatment of chronic obstructive pulmonary disease (COPD), is undergoing Phase Ib clinical trial in patients and has shown its potential efficacy. Its preparation method and medical use thereof have been patented in the United States (Patent No.US9751875B2).Objective::In this study, the pharmacokinetics, mass balance, tissue distribution and metabolism of radioactive 101BHG-D01 were investigated in rats after an intravenous dose of 1 mg/kg [14C]101BHG-D01 (100 μCi/kg).Methods::Radioactivity in rat plasma, urine, feces, and tissues was measured by liquid scintillation counting (LSC), and metabolite profiling and identification were conducted by UHPLC-β-RAM and UHPLC-Q-Exactive Plus MS.Results::The total radioactivity of the study drug in rat plasma rapidly declined with an average terminal elimination half-life of 0.35 h. The radioactivity in most tissues reached the maximum concentration at 0.25 h post-- dosing. The radioactivity mainly concentrated in the kidney and pancreas. The drug-related substances tended to be distributed into the blood cells in the circulation. At 168 h post dosing, the mean recovery of the total radioactivity in urine and feces was 78.82%. Fecal excretion was the major excretion route, accounting for approximately 61% of the radioactive dose. The study drug was metabolized extensively, and a total of 17 metabolites were identified in rat plasma, urine, and feces. The major metabolic pathways involved oxidation, oxidation and dehydrogenation, and O-dephenylation.Conclusion::In conclusion, the study results are useful for better understanding the pharmacokinetic profiles of 101BHG-D01 and provide a robust foundation for subsequent clinical studies.

01 Sep 2023·Journal of Pharmaceutical and Biomedical Analysis

Development and validation of LC-MS/MS methods for the quantification of 101BHG-D01, a novel, long-acting and selective muscarinic receptor antagonist, and its main metabolite M6 in human plasma, urine and feces: Application to a clinical study in healthy Chinese subjects

Article

Author: Gao, Huaye ; Ding, Li ; Liu, Haijun ; Cheng, Minlu

101BHG-D01 is a novel, long-acting and selective muscarinic receptor antagonist for the treatment of chronic obstructive pulmonary disease (COPD) and rhinorrhea in rhinitis. To support its clinical study, several liquid chromatography tandem mass spectrometry (LC-MS/MS) methods for the quantification of 101BHG-D01 and its main metabolite M6 in human plasma, urine and feces were developed. The plasma samples were prepared by protein precipitation, and the urine and fecal homogenate samples were pretreated by direct dilution, respectively. The chromatographic separation was performed on an Agilent InfinityLab Poroshell 120 C18 column with 0.1% formic acid and 10.0 mM ammonium acetate buffer solution in water and methanol as the mobile phase. The MS/MS analysis was performed by using multiple reaction monitoring (MRM) under a positive ion electrospray ionization mode. The methods were validated with regards to selectivity, linearity, lower limit of quantitation (LLOQ), accuracy and precision, matrix effect, extraction recovery, dilution integrity, batch size, carryover and stability. The calibration ranges were as follows: 1.00-800 pg/mL for 101BHG-D01 and 1.00-20.0 pg/mL for M6 in plasma; 0.0500-20.0 ng/mL for 101BHG-D01 and M6 in urine; 0.400-400 ng/mL for 101BHG-D01 and 0.100-100 ng/mL for M6 in feces. There was no endogenous or cross interference observed at the retention time of the analytes and internal standard in various biological matrices. Across these matrices, for the lower limit of quantitation quality control (LLOQ QC) samples, the intra- and inter-batch coefficients of variation were within 15.7%. For other QC samples, the intra- and inter-batch coefficients of variation were within 8.9%. The intra- and inter-batch accuracy deviations for all QC samples were within the range of - 6.2-12.0%. No significant matrix effect was observed from the matrices. The extraction recoveries of these methods at different concentrations were consistent and reproducible. The analytes were stable in different matrices under various storage conditions. The other bioanalytical parameters were also fully validated and met the criteria given in the FDA guidance. These methods were successfully applied to a clinical study in healthy Chinese subjects after a single dose administration of 101BHG-D01 inhalation aerosol. After inhalation, 101BHG-D01 was absorbed into plasma rapidly with the time to reach the maximum drug concentration (T_max) of 5 min and eliminated slowly with a half-life time about 30 h. The cumulative urinary and fecal excretion rates revealed 101BHG-D01 was mainly excreted in feces, rather than urine. The pharmacokinetic results of the study drug laid a foundation for its further clinical development.

01 Sep 2023·European Journal of Pharmacology

Effects of 101BHG-D01, a novel M receptor antagonism, on allergic rhinitis in animal models and its mechanism

Article

Author: Shen, Huijuan ; Jiang, Junxia ; Shen, Jian ; Xie, Qiangmin ; Wei, Hao ; Dai, Haibin ; Li, Yanyou ; Jia, Yongliang ; Chen, Xiaoping ; Xie, Yicheng ; Yao, Hongyi

Allergic rhinitis (AR) is a nasal mucosal disease with sneezing and nasal itching as the main symptoms. Although AR treatment continues to improve, there remains a lack of effective drugs. There are still controversies regarding whether anticholinergic drugs can effectively and safely relieve the symptoms of AR and reduce inflammation in the nasal mucosa. Here, we synthesized 101BHG-D01, which is a novel anticholinergic drug that mainly targets the M3 receptor and may reduce the adverse effects of other anticholinergic drugs on the heart. We evaluated the effects of 101BHG-D01 on AR and investigated the potential molecular mechanism of anticholinergic therapy for AR. We found that 101BHG-D01 effectively alleviated AR symptoms, reduced the infiltration of inflammatory cells and attenuated the expression of inflammatory factors (IL-4, IL-5, IL-13, etc.) in various AR animal models. In addition, 101BHG-D01 reduced the activation of mast cells and the release of histamine from rat peritoneal mesothelial cells (RPMCs) challenged by IgE. Moreover, 101BHG-D01 reduced the expression of MUC5AC in IL-13-challenged rat nasal epithelial cells (RNECs) and human nasal epithelial cells (HNEpCs). Furthermore, IL-13 stimulation significantly increased JAK1 and STAT6 phosphorylation, which was suppressed by 101BHG-D01. We demonstrated that 101BHG-D01 reduced mucus secretion and inflammatory cell infiltration in the nasal mucosa, which may occur through a reduction in activation of the JAK1-STAT6 signaling pathway, indicating that 101BHG-D01 is a potent and safe anticholinergic therapy for AR.

100 Deals associated with 101BHG-D01

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Common Cold	Phase 2	CN	Beijing Showby Pharmaceutical Co Ltd	22 Nov 2022
Rhinitis, Allergic, Seasonal	Phase 2	CN	Beijing Showby Pharmaceutical Co Ltd	21 Sep 2022
Pulmonary Disease, Chronic Obstructive	Phase 1	CN	Beijing Showby Pharmaceutical Co Ltd	15 Oct 2019
Chronic rhinitis	Discovery	CN	Beijing Showby Pharmaceutical Co Ltd	28 Oct 2021
Asthma	Discovery	CN	Beijing Showby Pharmaceutical Co Ltd	15 Oct 2019

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