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  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Zelenirstat Nmt Inhibitor in Patients with Relapsed/Refractory B-Cell Lymphoma and Acute Myelogenous Leukemia: Mechanistic Insights and Clinical Outcomes () -  Dec 7, 2024 - Abstract #ASH2024ASH_7871;    
    Zelenirstat is safe and well tolerated at the 210 mg OD dose in patients with R/R DLBCL, and objective responses of significant duration have been observed in heavily pre-treated patients. The absence of severe toxicities to date, the attainment of plasma concentrations highly active in preclinical models, and pre-clinical and clinical evidence of anticancer activity support the ongoing development of zelenirstat as an oral, daily therapy for patients with R/R B-cell lymphoma and R/R AML.
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Journal:  HIV-1 N-myristoylation-dependent hijacking of late endosomes/lysosomes to drive Gag assembly in macrophages. (Pubmed Central) -  Oct 23, 2024   
    Additionally, myristoylation inhibition by PCLX-001 decreased Gag presence on endosomes and inhibited VCCs formation, in both cell-line- and primary macrophages. In conclusion, we presented evidence supporting the idea that HIV-1 manipulates the LEL trajectory to guide Gag to VCCs in an N-myristoylation-dependent manner.
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Trial primary completion date, Metastases:  Study of PCLX-001 in R/R Advanced Solid Malignancies and B-cell Lymphoma (clinicaltrials.gov) -  Apr 4, 2024   
    P1,  N=60, Recruiting, 
    NMT inhibition represents a new target for ongoing research efforts and further clinical development of zelenirstat is warranted. Trial primary completion date: Feb 2024 --> Oct 2024
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Trial completion date, Trial primary completion date, Metastases:  Study of PCLX-001 in R/R Advanced Solid Malignancies and B-cell Lymphoma (clinicaltrials.gov) -  Nov 18, 2023   
    P1,  N=60, Recruiting, 
    Updated data will be presented. Trial completion date: Jul 2024 --> Oct 2024 | Trial primary completion date: Jun 2023 --> Feb 2024
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Trial completion date, Trial primary completion date, Metastases:  Study of PCLX-001 in R/R Advanced Solid Malignancies and B-cell Lymphoma (clinicaltrials.gov) -  May 30, 2023   
    P1,  N=60, Recruiting, 
    Trial completion date: Jul 2024 --> Oct 2024 | Trial primary completion date: Jun 2023 --> Feb 2024 Trial completion date: Jul 2023 --> Jul 2024 | Trial primary completion date: Feb 2023 --> Jun 2023
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    N-MYRISTOYLATION INHIBITION ABROGATES OXIDATIVE PHOSPHORYLATION TO TARGET ACUTE MYELOID LEUKEMIA STEM CELLS (Poster area) -  May 12, 2023 - Abstract #EHA2023EHA_1829;    
    We demonstrate PCLX-001 kills bulk leukemic cells and LSCs in vitro and in vivo by disrupting the function of key myristoylated proteins. While PCLX-001 is currently undergoing clinical evaluation in B-cell lymphoma and solid tumours, these results warrant clinical evaluation in AML with trials scheduled to start spring 2023.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals, Sutent (sunitinib) / Pfizer
    N-myristoylation inhibition reduces angiogenesis and cancer cell migration (Section 4; Poster Board #26) -  Mar 14, 2023 - Abstract #AACR2023AACR_6611;    
    Overall, by lowering SFK levels, PCLX-001 reduces angiogenesis, cell migration/invasion, and thus potentially cancer metastasis. Reducing these classical cancer hallmarks in malignant cells may benefit a wide array of cancer patients and ultimately improve cancer treatment outcomes.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    Understanding the sensitivity of cancer cells to myristoylation inhibitors for oncology applications (Section 18; Poster Board #19) -  Mar 14, 2023 - Abstract #AACR2023AACR_3905;    
    Using differential proteomics in the CRISPR/Cas9 NMT1 KO HAP1 near-haploid cell line derived from the chronic myelogenous leukemia versus WT HAP1 cells, we surprisingly found that few signaling proteins were downregulated, rather, 36 mitochondrial protein levels were decreased and 18 of these belonged to respiratory complex I. Myristoylated mitochondrial protein NDUFAF4, a major complex I assembly factor, was the most downregulated and PCLX-001 reduced its levels leading to decreased complex I activity. This seemingly ordinary observation could have transformational implications for cancer treatment since oxidative phosphorylation is essential for both cancer stem cell survival and metastasis.In addition, gene set enrichment analyses performed on RNASeq data obtained from 1200 cell lines treated with myristoylation inhibitors allowed us to derive an NMT inhibition sensitivity gene set that could be used to identify patients which would most benefit from NMT inhibition therapy.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    A First in Class, Open-Label, First-in-Human, Phase I Trial of Daily Oral Pclx-001 () -  Nov 29, 2022 - Abstract #ASH2022ASH_7441;    
    Conclusion s : Our results support the ongoing development of PCLX-001 as an oral, daily anticancer therapy. Updated study results will be presented, summarizing the safety and efficacy outcomes in PCLX-001 treated patients.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    Targeting N-Myristoylation for Adult Acute Myeloid Leukemia Therapy (ENMCC - Hall D) -  Nov 4, 2022 - Abstract #ASH2022ASH_2165;    
    In aggregate, our preclinical observations suggest that PCLX-001 is highly potent against AML cells in vitro and in vivo (both circulating and in the bone marrow), and, that LSCs are also more sensitive to PCLX-001 than non-leukemic stem cells. This further supports the initiation of PCLX-001evaluation in AML clinical trials scheduled to start in late 2022.
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Trial completion date, Trial primary completion date, Metastases:  Study of PCLX-001 in R/R Advanced Solid Malignancies and B-cell Lymphoma (clinicaltrials.gov) -  Sep 27, 2022   
    P1,  N=60, Recruiting, 
    This further supports the initiation of PCLX-001evaluation in AML clinical trials scheduled to start in late 2022. Trial completion date: Mar 2023 --> Jul 2023 | Trial primary completion date: May 2022 --> Feb 2023
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    P1 data, Journal:  Novel, First-in-Human, Oral PCLX-001 Treatment in a Patient with Relapsed Diffuse Large B-Cell Lymphoma. (Pubmed Central) -  Apr 15, 2022   
    We conclude that PCLX-001 oral monotherapy has suitable pharmacokinetic parameters for dose escalation, and that higher doses are required to achieve pharmacodynamic evidence of on-target activity in normal tissues. The current protocol is appropriately designed to achieve these ends, and the study proceeds without modification.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    Targeting N-myristoylation for therapy of adult acute myeloid leukemia (E-Poster Website) -  Mar 9, 2022 - Abstract #AACR2022AACR_7163;    
    PCLX-001 preferentially targeted AML cells inducing apoptosis and reducing leukemic burden. These findings validate NMT inhibition as a novel therapeutic strategy for AML and warrant the evaluation of PCLX-001 in clinical trials for adult AML.
  • ||||||||||  PCLX-001 / Pacylex Pharmaceuticals
    An Open-Label, First-in-Human, Phase I Trial of Daily Pclx-001 (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_2932;    
    PCLX-001 induced apoptosis in AML cell lines and patient blasts at concentrations which spared a large proportion of peripheral blood lymphocytes and monocytes from healthy individuals. Updated study results will be presented, summarizing the outcomes in the preliminary dose cohorts.
  • ||||||||||  zelenirstat (PCLX-001) / Pacylex Pharmaceuticals
    Trial completion date, Metastases:  Study of PCLX-001 in R/R Advanced Solid Malignancies and B-cell Lymphoma (clinicaltrials.gov) -  Sep 16, 2021   
    P1,  N=60, Recruiting, 
    Updated study results will be presented, summarizing the outcomes in the preliminary dose cohorts. Trial completion date: Dec 2022 --> Mar 2023