Two encouraging trials commenced at the start of 2015 for anti-cancer therapy Mocetinostat. Both studies, sponsored by Mirati Therapeutics, focus on this powerful and selective inhibitor of HDAC 1, 2, 3 and 11, which all are major players in the regulation of cancer gene expression. As an orally-bioavailable therapy, Mocetinostat has been at the forefront of over a dozen clinical trials worldwide, involving more than 400 patients with both solid tumors and hematologic malignancies.
Mocetinostat therapy is currently involved in an investigator sponsored Phase 2 study for patients with non-Hodgkin’s lymphoma. This study began on January 6, 2015 and is focused on specific deletions and mutations of the EP300 and CREBBP genes in lymphomas. These mutations and deletions are implicated in both refractory and relapsed follicular lymphoma and diffuse large B-cell lymphoma. Utilizing targeted treatment alongside genetic sequencing has led to an exciting endeavor for researchers seeking to find potential predictive responses in patients with the aforementioned genetic mutations who are administered Mocetinostat. Approximately 25 percent of patients who are diagnosed with diffuse large B-cell lymphoma and follicular lymphoma have the EP300 and CREBBP mutations. This open-label Phase 2 study thus far has 54 patients with refractory non-Hodgkin’s lymphoma enrolled, as well as 27 patients with follicular lymphoma and 27 patients diffuse large B-cell lymphoma. The clinical trial participants will receive a dosage of 90 milligrams of Mocetinostat three times a week on a 28 day schedule. The FDA has granted an Orphan Drug Designation to Mocetinostat as a treatment for patients with diffuse large B-cell lymphoma.
Another Mocetinostat study has begun for patients with bladder cancer who have histone acetyltransferase gene CREBBP and EP300 mutations. This Phase 2 clinical trial will evaluate the safety and efficacy of Mocetinostat in this patient population. Roughly one-quarter of patients diagnosed with bladder cancer have the EP300 and CREBBP mutations. The use of Mocetinostat as a pointed HDAC inhibitors leads researchers to believe a targeted dysregulation in histone and DNA acetylation will occur in the patients with these types of bladder cancer. Participants in this trial will receive an oral capsule of Mocetinostat three times a week on a 28 day cycle. Many years have elapsed without new therapies to treat bladder cancer, which becomes metastatic in more than 50 percent of patients. The use of a potent treatment like Mocetinostat is an exciting development in the fight against refractory cancer of the bladder. The most frequently reported grade 3 and 4 adverse effects from treatment with Mocetinostat have been fatigue and neutropenia.
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