Drug intelligence / Profile preview

docetaxel + leuprolide + testosterone

Development stage
Discontinued
Lead developer
Memorial Sloan Kettering Cancer Center
Modality
Small Molecules, Peptides
Administration
Intravenous, Topical, Subcutaneous
01

Overview

This investigational combination therapy, evaluated by Memorial Sloan Kettering Cancer Center (MSKCC), consists of the taxane chemotherapy docetaxel administered alongside a "rapid hormonal cycling" regimen of leuprolide and topical testosterone. Docetaxel acts as a microtubule stabilizer, binding to the interior surface of microtubules to prevent mitotic spindle assembly, thereby inducing cell cycle arrest and apoptosis. Leuprolide, a GnRH agonist, is used to deplete endogenous testosterone levels, while topical testosterone gel is used for periodic repletion. This approach aims to exploit the sensitivity of prostate cancer cells to fluctuating androgen levels to enhance the apoptotic effect of chemotherapy. The regimen was specifically studied in patients with progressive non-castrate prostate adenocarcinoma.

Other names
Docetaxel With Rapid Hormonal CyclingDocetaxel with rapid androgen cycling
02

Targets

AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)TUBB (Tubulin (alpha and beta subunits))

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