Chemotherapy-induced nausea and vomiting is mediated via centrally-acting NK1 receptors and, therefore, any drug for this indication must have good penetration of the CNS. MPC-4505 achieves good penetration of the central nervous system, with a sustained brain concentration of compound over an extended period, as tested in the rat. MPC-4505 is also highly selective; it has an affinity for the NK-1 receptor subtype in the <1 nanomolar range. "We are excited about the potential for this compound to treat both acute and delayed emesis in patients receiving highly emetogenic chemotherapies such as cisplatin," said Adrian Hobden, Ph.D., President of Myriad Pharmaceuticals, Inc. "Improving tolerance to chemotherapy greatly enhances patient acceptance of cancer chemotherapy and may increase their compliance with the full prescribed course of chemotherapy.
This compound adds to Myriad's portfolio of drugs for the treatment of cancer, which includes late stage preclinical drug candidates MPC-176716 for ovarian cancer and MPC-6827 for pancreatic and other cancers."