Safety, Tolerability, and Pharmacokinetic Study of 101BHG-D01 Nasal Spray, a Novel Long-Acting and Selective Cholinergic M Receptor Antagonist, in Healthy Chinese Volunteers: A Randomized, Double-Blind, Placebo-Controlled, Single-Dose Escalation, First-In-Human Study

Autor: Nan-Nan, Chu, Kai, Huang, Lin-Ling, Que, Ying, Ding, Xiang-Hong, Gu, Lin, Zhang, Jia-Kun, Wang, Xiao-Ping, Chen, Zhan-Guo, Sun, Qing, He
Rok vydání: 2022
Předmět:
Zdroj: European Journal of Drug Metabolism and Pharmacokinetics. 47:509-521
ISSN: 2107-0180
0378-7966
DOI: 10.1007/s13318-022-00769-6
Popis: 101BHG-D01 nasal spray is the first novel long-acting cholinergic M receptor antagonist under development to treat rhinorrhea in rhinitis. This first-in-human study aimed to evaluate the safety, tolerability, and pharmacokinetics of 101BHG-D01 nasal spray following single intranasal doses in healthy Chinese subjects.A randomized, double-blind, placebo-controlled, single-dose escalation study was conducted in healthy Chinese volunteers after intranasal doses of 101BHG-D01 nasal spray or placebo ranging from 40 µg to 960 µg (total of six doses). Blood samples were collected at scheduled time points, and plasma concentrations were determined using a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. A non-compartmental method was used to calculate the main pharmacokinetic parameters, including the area under the plasma concentration-time curve from time zero to the time of the last measurable concentration (AUCFollowing single intranasal dosing, 101BHG-D01 was rapidly absorbed with a median T101BHG-D01 nasal spray was safe and well tolerated in healthy Chinese subjects when administered intranasally in single escalating doses. The mean C
Databáze: OpenAIRE
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