Phase I, open-label, dose-finding study of GSK2636771, a phosphoinositide 3-kinase (PI3K)β inhibitor, in combination with enzalutamide in male subjects with metastatic castration-resistant prostate cancer (mCRPC)

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Abstract
Background: GSK2636771 is a potent, adenosine triphosphate (ATP) competitive, selective, oral inhibitor of the PI3Kβ isoform that inhibits the growth of phosphatase and tensin homolog (PTEN) deficient tumor cells in preclinical models. Resistance to the androgen receptor (AR) inhibitor enzalutamide (Xtandi®) may be mediated through upregulation of the PI3K pathway. Thus, GSK2636771 may enhance PTEN deleted prostate cancer cell kill.