Drug intelligence / Profile preview

abemaciclib + goserelin + letrozole + trastuzumab

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Subcutaneous, Intravenous
01

Overview

This is a four-drug combination regimen consisting of abemaciclib, goserelin, letrozole, and trastuzumab. It is used as a non-chemotherapy treatment strategy for patients with HER2-positive and hormone receptor (HR)-positive metastatic breast cancer, particularly in premenopausal women. - **Abemaciclib** is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. - **Goserelin** is a luteinizing hormone-releasing hormone (LHRH) agonist that suppresses ovarian function to reduce estrogen production. - **Letrozole** is an aromatase inhibitor that further reduces estrogen synthesis by blocking the conversion of androgens to estrogens. - **Trastuzumab** is a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2), inhibiting proliferation of HER2-overexpressing tumor cells. This combination aims to simultaneously block cell cycle progression, suppress estrogen-driven signaling, and inhibit HER2-mediated pathways. Clinical evidence suggests it can provide durable responses with manageable toxicity profiles in selected patient populations[1][6][7].

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)LHCGR (Luteinizing hormone/choriogonadotropin receptor)CDK4 (Cyclin-dependent kinase 4)CDK9 (Cyclin-dependent kinase 9)GnRHR (Gonadotropin-releasing hormone receptor)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)

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