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tesmilifene
- Development stage
- Discontinued
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
Tesmilifene is a small molecule chemosensitizer and a diphenylmethane derivative. It acts as a high-affinity ligand for the anti-estrogen binding site (AEBS), which is an intracellular protein complex associated with the microsomal histamine receptor and identified as cholestenol delta-isomerase (EBP). By binding to this site, tesmilifene modulates cell proliferation and enhances the cytotoxic effects of various chemotherapeutic agents, such as anthracyclines and taxanes, without increasing their systemic toxicity. It was primarily developed by YM BioSciences for the treatment of metastatic breast cancer and other solid tumors. Despite showing promise in early trials, a pivotal Phase 3 trial (DECIDE) in metastatic breast cancer failed to meet its primary endpoint of improving overall survival, leading to the discontinuation of its development for that indication.
- Other names
- N,N-diethyl-2-[4-(phenylmethyl)phenoxy]ethanamine2-(4-benzylphenoxy)-N,N-diethylethanamine
02
Targets
ABCB1 (P-glycoprotein)ABCC1 (MRP1)ABCG2 (Breast cancer resistance protein)
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