Drug intelligence / Profile preview

tesmilifene + docetaxel

Development stage
Discontinued
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Intravenous
01

Overview

Tesmilifene + docetaxel is an investigational combination therapy evaluated primarily for the treatment of metastatic breast cancer and other solid tumors. **Tesmilifene** is a small molecule chemopotentiator and phenyl ether that has been studied for its ability to enhance the cytotoxic effects of chemotherapeutic agents such as docetaxel. Its mechanism includes antagonism of estrogen receptors and histamine receptors, as well as proposed activity in targeting multi-drug resistant cells through modulation of ATP-binding cassette transporters and p-glycoprotein activity, possibly increasing reactive oxygen species-induced cell death in cancer cells. **Docetaxel** is a second-generation taxane, a widely-used cytotoxic agent that stabilizes microtubules, inhibiting cell division and inducing apoptosis in cancer cells. The combination was intended to improve response rates and survival outcomes compared to docetaxel alone, but development has been discontinued for these indications[1][2][3][4][5].

Other names
tesmilifene + docetaxeltesmilifene + Taxotere
02

Targets

ABCB1 (P-glycoprotein)TUBB (Tubulin (alpha and beta subunits))HRH1 (Histamine H1 Receptor)

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