Table 3.
Novel agents targeting the AR axis: early-phase trials and future directions
| Agent | Phase | Population | Notes | References/clinicaltrial.gov | |
|---|---|---|---|---|---|
|
AR- targeted |
|||||
| AZD3514 | I | mCRPC |
NCT01162395 (active, not recruiting) |
||
| AZD3514 | II | solid tumor with AR+ |
NCT02144051 (recruiting) | ||
|
Combination trials |
|||||
| ARN-509 + AA |
I | mCRPC | AR targeting | NCT02123758 (recruiting) | |
| BEZ235 or BKM120 + AA |
I | mCRPC | Pan class PI3K inhibitor |
NCT01634061 (active, not recruiting) |
|
| BMK120 + AA |
I | mCRPC | Pan class PI3K inhibitor |
NCT01741753 (recruiting) | |
| GDC-0068 or GDC- 0980 + AA |
I | mCRPC | Pan-Akt | NCT01485861 (recruiting) | |
| Dasatinib or sunitinib + AA |
I | mCRPC | ABL, SRC or VEGFR, EGFR tyrosine kinase inhibitor |
NCT01254864 (recruiting) | |
| Alisertib + AA |
I/II | mCRPC | Small molecule inhibitor of serine/threonine protein kinase, aurora A kinase |
NCT01848067(recruiting) | |
| Tivozanib + enzalutamide |
I | mCRPC | Antisense to clusterin |
NCT01885949 (recruiting) | |
| Temsirolimus + ARN- 509 |
Ib | mCRPC | mTOR inhibitor |
NCT02106507 (recruiting) |
AR, androgen receptor; mCRPC, metastatic castration-resistant prostate cancer; AA, abiraterone acetate; HSP, heat shock protein; PI3K, phosphatidylinositol 3-kinase; VEGFR, vascular endothelial growth factor receptor; EGFR, epidermal growth factor receptor; mTOR, mammalian target of rapamycin.