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xentuzumab + abemaciclib + anastrozole
- Development stage
- Unknown
- Lead developer
- Boehringer Ingelheim
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
**xentuzumab + abemaciclib + anastrozole** is an investigational combination therapy, primarily studied in hormone receptor-positive, HER2-negative metastatic breast cancer. - **Xentuzumab** is a monoclonal antibody that neutralizes insulin-like growth factors IGF-1 and IGF-2, blocking their activation of IGF-1R and thus impeding tumor cell growth signaling. - **Abemaciclib** is a small molecule inhibitor of cyclin-dependent kinases CDK4 and CDK6, causing cell cycle arrest through inhibition of Rb1 protein phosphorylation, restricting cancer cell proliferation. - **Anastrozole** is an aromatase inhibitor, lowering circulating estrogen by blocking aromatase enzyme activity, used in hormone receptor-positive breast cancer treatment, especially postmenopausal women. The combination aims to synergistically target hormone signaling, cell cycle progression, and IGF-mediated survival pathways to improve antitumor efficacy in advanced breast cancer[5][1][3].
- Other names
- xentuzumab + abemaciclib + anastrozole
02
Targets
IGF2 (Insulin-like growth factor 2)CDK4 (Cyclin-dependent kinase 4)IGF-1 (Insulin-like growth factor 1)CYP19A1 (Aromatase)CDK9 (Cyclin-dependent kinase 9)CDK6 (Cyclin-dependent kinase 6)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)
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