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entinostat + lapatinib + trastuzumab
- Development stage
- Unknown
- Lead developer
- Syndax Pharmaceuticals
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
A combination therapy consisting of entinostat (an HDAC inhibitor), lapatinib (a tyrosine kinase inhibitor), and trastuzumab (a monoclonal antibody). This regimen has been studied in clinical trials for patients with HER2-positive metastatic breast cancer who have progressed during treatment with trastuzumab-containing regimens. Preclinical studies showed that entinostat can epigenetically reverse resistance to anti-HER2 agents and shows synergistic efficacy with lapatinib in inhibiting growth of trastuzumab-resistant HER2-positive breast cancer. The combination works by downregulating phosphorylated Akt, activating FOXO3 transcriptional activity, and inducing the pro-apoptotic protein Bim1.
- Other names
- entinostat + lapatinib ditosylate + trastuzumabentinostat, lapatinib, and trastuzumab combination
02
Targets
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