|Class I & IV HDAC Inhibitor|
|NSCLC and other solid tumors|
Mocetinostat (MGCD103) is an orally-bioavailable, spectrum-selective Class I & IV HDAC inhibitor currently being studied in a Phase 2 trial as a combination therapy with durvalumab, targeting the programmed death ligand 1 (PD-L1) pathway, which has been implicated in advanced lung cancers. In preclinical models, mocetinostat with durvalumab demonstrated significant reduction in tumor volume compared to either agent alone.
Mirati retains worldwide rights to mocetinostat (MGCD103) with the exception of certain Asian territories where the program is partnered with Taiho.
IASLC 2016 TiP Poster #5521
AACR 2016 Poster #4021
Click to view “The class I HDAC inhibitor, mocetinostat, induces expression of PD-L1 and tumor antigen presentation machinery and modifies tumor immune cellular subsets providing a rationale for immune checkpoint inhibitor combinations”
NON-SMALL CELL LUNG CANCER (NSCLC)
The overall five year survival rate for patients with NSCLC is only 16.8% and NSCLC results in the greatest number of cancer deaths in the United States. Over recent years, new therapies have been approved that target gene pathways implicated in progression of NSCLC, including EGFR kinase inhibitors, EML4-ALK inhibitors, and immune checkpoint inhibitors. However, these targets represent only a fraction of the growing list of cancer genes that play a role in NSCLC. There remains a significant unmet medical need to develop new therapies that inhibit multiple targets, particularly those that also inhibit novel targets for which no therapy exists. Backed by a strong scientific rationale, we believe that Mocetinostat (MGCD103), combined with durvalumab (an investigational anti-PD-L1 immune checkpoint inhibitor), may result in synergistic and immune enhancing anti-tumor effect.