Drug intelligence / Profile preview

ozarelix

Development stage
Phase 2
Lead developer
Ceapro
Modality
Small Molecules, Peptides
Administration
Injection (parenteral)
01

Overview

Ozarelix is a synthetic, highly modified fourth-generation linear decapeptide that acts as a gonadotropin-releasing hormone (GnRH) antagonist. It competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, leading to rapid inhibition of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. In males, this results in decreased testosterone production, which can be beneficial for treating hormonally dependent diseases such as prostate cancer and benign prostatic hyperplasia (BPH). Ozarelix was developed as a long-lasting injectable formulation primarily for prostate cancer but was also investigated for BPH, endometriosis, Alzheimer's disease, and ovarian cancer. Development has been discontinued or terminated for most indications[1][2][3][4][5].

Other names
ozarelixumOzarélixOzarelix [INN]Q1IF8M2YL3Q-1IF8M2YL3Q 1IF8M2YL3UNII-Q1IF8M2YL3UNII-Q-1IF8M2YL3UNII-Q 1IF8M2YL3Ac-D-Nal(2)-D-Phe(4Cl)-D-Pal(3)-Ser-NMe-Tyr-D-Hcit-Nle-Arg-Pro-D-Ala-NH2
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)

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