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news.Mirati Therapeutics has dosed the first patient in a Phase II clinical trial of mocetinostat, an orally-bioavailable, spectrum-selective HDAC inhibitor, as treatment for a select group of patients with bladder cancer.
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The trial, which is designed to evaluate the efficacy, safety and pharmacokinetics of mocetinostat, will enroll patients whose tumors have mutations or deletions of the CREBBP and/or EP300 genes.
Mocetinostat is a potent spectrum selective inhibitor of HDAC 1, 2, 3 and 11, and is being developed as a single agent treatment targeting mutations and deletions of the histone acetyltransferase (HAT) genes CREBBP and EP300.
The company said that these genetic alterations are implicated in the pathogenesis and progression of bladder cancer and other solid tumor types, as well as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL).
Mirati president and CEO Charles Baum said: "Published research suggests that genetic alterations of CREBBP and EP300 appear in up to 25% of bladder cancer cases.
"This represents a promising patient enrichment strategy for clinical development and, if successful, may lead to an accelerated development path for a highly underserved population of patients with advanced bladder cancer."
The trial’s primary objective is to determine the efficacy of mocetinostat in patients with previously treated, locally advanced, unresectable or metastatic urothelial carcinoma harboring inactivating mutations or deletions of the HAT genes CREBBP and/or EP300.
Secondary objectives of the trial include evaluation of safety, secondary efficacy endpoints and pharmacokinetics.