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CREBBP and EP300

Mutations and deletions of CREBBP and EP300 are implicated in the growth and progression of bladder/urothelial cancers. These genes have been found to be altered in up to 30% of bladder cancer patients. The loss of function of the CREBBP and EP300 genes results in impaired regulation of histone acetylation and dysregulation of gene expression leading to tumor progression. By countering the effect of CREBBP and EP300 mutations, mocetinostat may be able to restore normal gene expression patterns, block tumor growth and result in tumor cell death resulting in better clinical outcomes.

Trials targeting CREBBP and EP300

Indications: Bladder Cancer
 
Drug Candidate: Mocetinostat
 
Driver Mutations: CREBBP, EP300

Mirati Therapeutics is enrolling a Phase 2 study evaluating the effects of mocetinostat as a treatment for patients with previously treated, locally advanced, unresectable or metastatic urothelial bladder cancer whose tumors carry genetic alterations of CREBBP and EP300. Participating trial sites will analyze the genetic sequence of the tumors of eligible patients to determine if those mutations are present before enrolling in the clinical trial.



Indications: Diffuse Large B-Cell Lymphoma and Follicular Lymphoma
 
Drug Candidate: Mocetinostat
 
Driver Mutations: CREBBP, EP300

Mocetinostat is being evaluated in a Phase 2 study as a treatment for patients with Diffuse Large B-cell Lymphoma and Follicular Lymphoma whose tumors carry genetic alterations of CREBBP and EP300 genes. This study is being led by Dr. Anas Younes, Chief of Memorial Sloan Kettering's Lymphoma Service. Memorial Sloan Kettering will analyze the genetic sequence of the tumors of eligible patients to determine if those mutations are present before enrolling in the clinical trial.

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