Drug intelligence / Profile preview

FCN-437c + letrozole + goserelin

Development stage
Unknown
Lead developer
Jinzhou Ahon Pharmaceutical
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

FCN-437c + letrozole + goserelin is a combination therapy under investigation for the treatment of hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, particularly in premenopausal women. **FCN-437c** (also known as Fovinaciclib) is a novel, potent, and selective oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), developed to block cell cycle progression by inhibiting phosphorylation of the retinoblastoma protein (Rb), thereby arresting tumor cell growth[1][3][5][7]. It has demonstrated good blood-brain barrier penetration and improved potency compared to currently approved CDK4/6 inhibitors[1][5]. **Letrozole** is an aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme, reducing estrogen-driven tumor growth. **Goserelin** is a luteinizing hormone-releasing hormone (LHRH) agonist that suppresses ovarian function and lowers circulating estrogen levels in premenopausal women. The combination aims to maximize endocrine suppression while targeting cell cycle progression pathways. Clinical studies have shown efficacy for combinations of CDK4/6 inhibitors with endocrine therapies like letrozole plus ovarian suppression with goserelin in advanced breast cancer settings[3][6][8][10].

Other names
Fovinaciclib + letrozole + goserelin
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)CDK4 (Cyclin-dependent kinase 4)CYP19A1 (Aromatase)

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