Drug intelligence / Profile preview

goserelin acetate extended-release microspheres LY01022

Development stage
Phase 1
Lead developer
Luye Pharma
Modality
Peptides, Small Molecules
Administration
Intramuscular
01

Overview

LY01022 is a 3‑month long-acting intramuscular depot formulation of goserelin acetate, developed as extended‑release microspheres to provide sustained gonadotropin-releasing hormone (GnRH) receptor agonism and medical castration in hormone‑sensitive cancers. By continuously stimulating pituitary GnRH receptors, goserelin initially causes a transient surge in luteinizing hormone (LH), follicle‑stimulating hormone (FSH), and downstream sex steroids, followed by receptor desensitization and down‑regulation, leading to profound suppression of testosterone or estrogen and regression of sex hormone‑dependent tumors such as prostate and certain breast cancers.[2][12][13] LY01022 is being developed by Luye Pharma as a 3‑month dosing-cycle microsphere formulation intended to offer more stable drug release, higher entrapment efficiency, and reduced injection frequency compared with monthly goserelin depot products, with clinical development focused on prostate cancer and breast cancer that are amenable to hormone therapy.[2][6][12]

Other names
goserelin acetate extended-release microspheres LY010223-month long-acting goserelin acetate extended-release microspheres for injection
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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