zelenirstat + immune checkpoint inhibitors

Zelenirstat + immune checkpoint inhibitors is an investigational combination therapy program being developed by Pacylex Pharmaceuticals. The combination pairs zelenirstat (also known as PCLX-001), a first-in-class, orally bioavailable small molecule inhibitor of N-myristoyltransferase 1 (NMT1) and N-myristoyltransferase 2 (NMT2), with immune checkpoint inhibitors (such as the anti-PD-1 monoclonal antibody pembrolizumab). NMT1 and NMT2 catalyze the myristoylation of proteins essential for cancer cell survival and proliferation. Preclinical studies suggest that inhibiting myristoylation with zelenirstat disrupts the membrane localization of PD-L1 and restores sensitivity to immunotherapy in resistant tumor models. The program is currently in the IND-enabling stage of development for the treatment of head and neck cancer, cervical cancer, and lung cancer.

Other names

PCLX-001 + ICIsPCLX-001 + immune checkpoint inhibitorsPCLX-001 + pembrolizumabzelenirstat + ICIszelenirstat + pembrolizumab