Drug intelligence / Profile preview

ASP1707 + itraconazole

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

ASP1707 + itraconazole is a combination of two drugs: **ASP1707**, an orally administered small molecule gonadotropin-releasing hormone (GnRH) antagonist developed for the treatment of endometriosis-associated pelvic pain and investigated for rheumatoid arthritis, and **itraconazole**, a triazole antifungal agent widely used to treat various serious fungal infections. ASP1707 works by inhibiting GnRH receptors, leading to a reduction in luteinizing hormone and follicle-stimulating hormone, ultimately decreasing estrogen production and alleviating pain symptoms related to endometriosis. Itraconazole acts by inhibiting synthesis of ergosterol, an essential component of fungal cell membranes, through the inhibition of cytochrome P450 14α-demethylase, leading to cell membrane disruption and fungal death[2][3][5][6][7]. ASP1707 was developed by Astellas for gynecological diseases, and itraconazole is a widely available antifungal with generic manufacturers.

02

Targets

CYP51A1 (Sterol 14α-demethylase)GnRHR (Gonadotropin-releasing hormone receptor)

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