Archexin® is a first-in-class, potent inhibitor of Akt-1 protein kinase which is involved in the proliferation of cancer cells. Archexin is in Phase II trials for the treatment of pancreatic cancer and has US FDA orphan drug designation for five cancers (RCC, glioblastoma, and cancers of the ovary, stomach and pancreas). Multiple indications for other solid tumors may also be pursued.
Archexin is an antisense oligonucleotide (ASO) compound that is complementary to Akt mRNA, and highly selective for inhibiting mRNA expression and production of Akt protein. Akt activation leads to cancer cell survival, proliferation, angiogenesis and drug resistance. Both native and activated forms of Akt are involved in cancer cell signaling.
Archexin is the first anticancer drug that inhibits both native and activated forms of Akt, with the potential to inhibit cancer survival and proliferation, angiogenesis and drug resistance. In the Archexin Phase I clinical study, grade 3 (G3) fatigue was the only dose limiting toxicity observed.
The goal of the ongoing Phase II trial is to assess efficacy and safety in treating metastatic pancreatic cancer. The primary study endpoints are tolerability and survival. Other endpoints include AKT-1 and VEGF biomarkers evaluation and tumor response using RECIST criteria.
