Drug intelligence / Profile preview

enzastaurin + docetaxel + prednisone

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Enzastaurin + docetaxel + prednisone is an experimental combination therapy evaluated primarily in clinical trials for **castration-resistant metastatic prostate cancer**. Enzastaurin is an oral **serine/threonine kinase inhibitor** targeting the beta isoform of **protein kinase C** (PKCβ), and it also modulates the PI3K/AKT signaling pathway. Docetaxel is a taxane-based **chemotherapeutic agent** that inhibits cell division by stabilizing microtubules, and prednisone is a **synthetic glucocorticoid corticosteroid** used to reduce inflammation and as part of standard prostate cancer therapy. The combination was tested to determine if enzastaurin adds benefit to the standard docetaxel/prednisone regimen. Clinical results indicated no statistically significant improvement in objective response rate or survival, and the combination was more myelosuppressive than docetaxel/prednisone alone, without clear added efficacy[1][4].

02

Targets

GR (Glucocorticoid receptor)PRKCB (Protein kinase C beta)TUBB (Tubulin (alpha and beta subunits))PIKFYVE (Phosphoinositide kinase, FYVE-type zinc finger containing enzyme)PDE3B (Phosphodiesterase 3B)

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