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eribulin mesylate + cetuximab
- Development stage
- Unknown
- Lead developer
- Howard Safran
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Eribulin mesylate + cetuximab is a combination therapy investigated for the treatment of advanced malignancies, specifically head and neck squamous cell carcinoma (HNSCC) and colorectal cancer. Eribulin mesylate is a synthetic analog of halichondrin B, a small molecule that acts as a non-taxane microtubule dynamics inhibitor. It binds to the plus ends of microtubules, inhibiting the growth phase without affecting the shortening phase, which leads to irreversible mitotic blockade and apoptosis. Cetuximab is a recombinant human/mouse chimeric monoclonal antibody that binds specifically to the extracellular domain of the epidermal growth factor receptor (EGFR). By binding to EGFR, cetuximab inhibits the activation of the receptor and subsequent downstream signaling pathways, such as MAPK and PI3K/Akt, which are involved in cell proliferation, survival, and angiogenesis. The combination was evaluated in a Phase 1/2 study (NCT01266070) led by Dr. Howard Safran to determine safety and efficacy in patients who had progressed on prior therapies.
- Brand names
- HalavenErbitux
- Other names
- Eribulin and CetuximabEribulin mesylate and Cetuximab
02
Targets
CYP3A4 (Cytochrome P450 3A4)TUBB (Tubulin (alpha and beta subunits))EGFR (Epidermal growth factor receptor)
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