March, 2016
ENB Therapeutics presents poster entitled “Development of ENB-001 for the Treatment of Melanoma Brain Metastasis” at the 2016 HemOnc Today Melanoma and Cutaneous Malignancies Meeting in NYC. The meeting draws more than 250 colleagues and renowned speakers with a program designed for oncologists, dermatologists, researchers and students. The poster abstract is below:
As systemic therapy improves, patients with melanoma are living longer. As a result, 44% – 76% of all those diagnosed with advanced melanoma are developing, and dying from, melanoma that metastasizes to the central nervous system (CNS), specifically the brain. This catastrophic event is the most common cause of death in patients with melanoma and there are no approved therapies specifically for melanoma with CNS involvement. A common cause of resistance to melanoma treatment is upregulation of the endothelin B receptor (ETBR). ENB-001 is a small molecule that precisely targets the ETBR, inhibiting downstream RAF, MEK and AKT activity. ENB-001 has achieved proof of concept in animal models of CNS melanoma as well as extra-CNS melanoma metastases. Efficacy in preclinical studies for glioblastoma and squamous cell carcinoma has also been demonstrated. ENB-001, in contrast to approved MEK inhibitors, also has immunostimulatory effects, enhancing T-cell homing and adhesion to cancer cell vasculature. We have partnered with a drug formulation company that has a proprietary nanoparticle intranasal delivery system that bypasses the blood brain barrier, and will be used to deliver ENB-001 directly to the central nervous system. The development of ENB-001 will have a significant impact for patients with CNS melanoma. Further opportunities include the treatment of non-CNS melanoma metastatic disease, other malignancies, and the development of a companion diagnostic.