Pharmacological and toxicological studies of a novel goserelin acetate extended-release microspheres in rats.

ABSTRACT: LY01005 is an investigational new drug product of goserelin acetate which is formulated as extended-release microspheres for intramuscular injection. To support the proposed clinical trials and marketing application of LY01005, pharmacodynamics, pharmacokinetics and toxicity studies were performed in rats. In the pharmacological study in rats, LY01005 induced an initial supra-physiological level increase of testosterone at 24 h post-dosing which then rapidly fell to castration level. The potency of LY01005 was comparable to the comparator Zoladex^® but its effect lasted longer and more stable. A single-dose pharmacokinetics study in rats demonstrated that the C_max and AUC_last of LY01005 increased in a dose-proportional manner in the range of 0.45-1.80 mg/kg

SUBMITTER: Yutong M 

PROVIDER: S-EPMC9989164 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature