A Potential Best-in-Class Anti-Cancer Akt-1 Inhibitor

RX-0301 is a potential best-in-class, potent inhibitor of the protein kinase Akt-1, which we believe plays a critical role in cancer cell proliferation, survival, angiogenesis, metastasis, and drug resistance. RX-0301 works by specifically inhibiting the cancer cell signaling protein Akt-1, which is highly over-expressed in cancer cells. We believe RX-0301 is different from other Akt-1 inhibitors by its ability to inhibit both activated and inactivated forms of Akt-1, and as a result, it is not expected to lead to drug resistance. RX-0301 has received orphan drug designation from the FDA for renal cell carcinoma (RCC), glioblastoma, ovarian cancer, stomach cancer, and pancreatic cancer.

Inhibiting both Activated and Inactivated Forms of Akt-1

Akt-1 is over-activated in patients with multiple forms of cancer, including breast, colorectal, gastric, pancreatic, prostate, and melanoma cancers. Akt-1 activity may be inhibited by signaling molecules upstream of Akt-1 in cancer cells through the use of vascular endothelial growth factor and epidermal growth factor receptor inhibitors, but this treatment only indirectly affects the activity of native Akt-1. Because signal transmission for cancer progression and resistance occurs when Akt-1 is activated, inhibition of activated Akt-1 has the potential to prevent cancer progression.