Drug intelligence / Profile preview

enzalutamide + taselisib

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Enzalutamide + taselisib is an investigational combination therapy consisting of two small molecule drugs. Enzalutamide is an androgen receptor (AR) antagonist that inhibits AR signaling, thereby blocking the growth-promoting effects of androgens in AR-positive tumor cells. Taselisib is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K), specifically targeting the PI3K pathway involved in cancer cell proliferation and survival. This combination has been studied primarily in patients with metastatic triple-negative breast cancer (TNBC) that expresses androgen receptor (AR+ TNBC). Clinical trials have shown that this combination can increase clinical benefit rates compared to enzalutamide alone, particularly in patients with luminal AR subtype tumors. The rationale for combining these agents stems from preclinical evidence suggesting synergy between AR antagonism and PI3K inhibition in certain breast cancer subtypes[1][2][3][4][6][8].

Brand names
GDC-0032GDC0032GDC 0032
02

Targets

AR (Adrenergic receptors)PIK3CA (Phosphoinositide 3-kinase alpha)

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