Spirita Oncology, LLC Initiates a Phase 1 Clinical Trial of the Anti-Cancer Agent E6201 in Combination with Dabrafenib in Patients with Central Nervous System Metastases from BRAF V600 Mutated Metastatic Melanoma

Spirita Oncology, LLC, has initiated a Phase 1 clinical trial of anti-cancer agent E6201 in combination with dabrafenib in patients with BRAF V600-mutated metastatic melanoma that has spread to the central nervous system.

There are approximately 47,000 new cases of metastatic melanoma in the U.S. each year, with approximately 10,000 deaths. More than 15,000 of these patients develop brain metastases. The median overall survival for patients with brain metastases is four months. Approximately 50% of patients harbor BRAF- or MEK-mutated melanoma, with limited treatment options available. Targeted therapies and immune checkpoint inhibitors have improved overall survival for metastatic melanoma patients with brain metastases. However, responses are usually of short duration, and new agents that effectively penetrate the blood-brain-barrier (BBB) are needed.

E6201 is an ATP-competitive MEK1 inhibitor that has demonstrated preclinical activity in BRAF V600-mutant melanoma cell lines. E6201 has shown excellent brain distribution characteristics and minimal CNS efflux by transporters at the BBB. A Phase 1 trial (NCT00794781) evaluating E6201 in patients with advanced solid tumors demonstrated activity in metastatic melanoma patients, including two patients with brain metastases, one of whom maintained an exceptional ongoing durable response lasting for more than 10 years.

"E6201 is a potent MEK1 inhibitor. Exceptional responses were seen with E6201 monotherapy in patients with melanoma brain metastases in our prior Phase 1 studies. By utilizing a targeted drug against BRAF- or MEK-mutated melanoma CNS metastases with excellent brain penetration and retention, we hope to provide a more effective therapeutic in combination with dabrafenib than achieved with the currently available targeted agents and immunotherapies," said Dr. Linda Paradiso, Chief Development Officer for Spirita Oncology. "We are fully committed to deliver breakthrough therapies using innovative approaches for patients with devastating metastatic brain melanoma."

About Spirita Oncology, LLC: Spirita Oncology is an integrated oncology research and development company with experience in developing, managing, and optimizing global pharmaceutical drug development programs from late discovery, translational research and clinical development through market authorization and post-marketing life-cycle management.