Pacylex Pharmaceutical Explores N-myristoyltransferase Inhibitors as Promising ADC Payloads
TL;DR
Pacylex Pharmaceuticals leads in developing NMTis for cancer, presenting at ADC Payload Summit for potential partnership advantage.
Zelenirstat, an NMTi, inhibits myristoylation affecting cancer cell growth, validated targets, and oxidative phosphorylation mechanisms.
Pacylex's NMTis show promise as effective ADC payloads, offering hope for improved cancer treatment outcomes and survival rates.
Zelenirstat's mechanism of action in killing cancer cells through multiple processes makes it a novel and intriguing potential treatment option.
Found this article helpful?
Share it with your network and spread the knowledge!

Pacylex Pharmaceuticals is advancing a novel approach to cancer treatment through its exploration of N-myristoyltransferase inhibitors (NMTis) as potential payloads for antibody drug conjugates (ADCs). The company's CEO, Michael Weickert, will present research at the 2nd Annual ADC Payload Summit highlighting the potential of these innovative therapeutic compounds.
The pharmaceutical company has developed 28 NMTis with single-digit nanomolar IC50s against human NMT1, with zelenirstat emerging as a first-in-class myristoylation inhibitor currently in clinical studies. Preliminary research demonstrates that these compounds can simultaneously disrupt multiple critical processes in cancer cell growth and survival.
Early clinical trials of zelenirstat have shown promising results, with 57% of patients experiencing stable disease or better over 6-16 months. The drug was well-tolerated in Phase 1 trials involving patients with refractory lymphoma and solid tumors, with no dose-limiting toxicities observed.
NMTis represent a potentially transformative approach to cancer treatment by targeting multiple cellular mechanisms. They can inhibit critical protein assembly, block mitochondrial function, and interrupt signaling pathways essential for cancer cell survival. This multi-pronged approach could offer more comprehensive cancer cell elimination compared to traditional targeted therapies.
Weickert emphasized the company's commitment to exploring these compounds, stating that the correlation between genes predicting sensitivity to zelenirstat and ADC targets is particularly promising. Pacylex is actively seeking partnerships to further develop these NMTis as novel ADC payloads across various cancer types.
Curated from Reportable

