Phase I study of procaspase-activating compound-1 (PAC-1) in the treatment of advanced malignancies

• Published in: British journal of cancer Vol. 128; no. 5; pp. 783 - 792
• Main Authors: Danciu, Oana C., Holdhoff, Matthias, Peterson, Richard A., Fischer, James H., Liu, Li C., Wang, Heng, Venepalli, Neeta K., Chowdhery, Rozina, Nicholas, M. Kelly, Russell, Meredith J., Fan, Timothy M., Hergenrother, Paul J., Tarasow, Theodore M., Dudek, Arkadiusz Z.
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 23.03.2023; Nature Publishing Group
• Subjects: 692/4028; 692/4028/67/1059/153; Antineoplastic Agents - therapeutic use; Apoptosis; Biomedical and Life Sciences; Biomedicine; Cancer Research; Caspase 1; Caspase-3; Clinical trials; Cognition; Cognitive ability; Dosage; Drug Resistance; Epidemiology; Humans; Malignancy; Maximum Tolerated Dose; Molecular Medicine; Neoplasms - drug therapy; Neuroendocrine tumors; Oncology; Oral administration; PAC1 protein; Patients; Pharmacokinetics; Toxicity

Background Procaspase-3 (PC-3) is overexpressed in multiple tumour types and procaspase-activating compound 1 (PAC-1) directly activates PC-3 and induces apoptosis in cancer cells. This report describes the first-in-human, phase I study of PAC-1 assessing maximum tolerated dose, safety, and pharmaco...