Constellation begins Phase I trial of CPI-1205 in lymphoma patients

The company said that this first-in-human trial is currently open at Horizon Oncology in Lafayette, Indiana, Sarah Cannon Research Institute in Nashville, Tennessee, the John Theurer Cancer Center in Hackensack, New Jersey and the Massachusetts General Hospital in Boston, Massachusetts.

Constellation histone methyltransferase program lead biologist Patrick Trojer said: "CPI-1205 allows us to target a pathway that cancer cells utilize to silence certain genes and thereby gain a growth advantage. Our preclinical data and that of other investigators suggest that EZH2 inhibition may have broad activity in lymphoma as well as activity in solid tumors.

"CPI-1205 has a number of favorable attributes that make us optimistic that its preclinical activity will translate into anti-tumor activity for patients."

EZH2 is part of a multi-protein complex called the polycomb repressive complex 2 (PRC2), whose function is to selectively suppress gene expression.

Under the PRC2 complex, EZH2 catalyzes the transfer of methyl groups to a distinct lysine residue of a histone protein (H3) that is associated with DNA.