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zelenirstat + venetoclax
- Development stage
- Preclinical
- Lead developer
- Pacylex Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Zelenirstat + venetoclax is a small molecule combination therapy being developed by Pacylex Pharmaceuticals for the treatment of acute myeloid leukemia (AML). Zelenirstat (formerly PCLX-001) is a first-in-class, dual inhibitor of N-myristoyltransferase 1 and 2 (NMT1 and NMT2), enzymes that catalyze the N-myristoylation of proteins essential for oncogenic signaling and cell survival. Venetoclax is a selective inhibitor of the anti-apoptotic protein BCL-2, which is frequently overexpressed in hematologic malignancies. The combination is designed to leverage the synergistic effects of NMT inhibition and BCL-2 inhibition to induce apoptosis and overcome resistance mechanisms in leukemia cells. As of 2024, the program is in IND-enabling studies, with a Phase 1 clinical trial planned for 2025.
- Other names
- PCLX-001 + venetoclaxzelenirstat + ABT-199
02
Targets
BCL-2 (BCL-2 family)NMT1 (N-myristoyltransferase 1)NMT2 (N-myristoyltransferase 2)
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