Basilea Pharmaceutica Ltd. has reported that preclinical data on the single agent anti-cancer activity of the drug candidate BAL0891 have been presented at the Targeted Anticancer Therapies congress 2022 of the European Society of Medical Oncology (ESMO TAT 2022), which is taking place online March 7-8, 2022. BAL0891 is a potential first-in-class mitotic checkpoint inhibitor (MCI) that drives aberrant tumor cell division, leading to tumor cell death.
The company said that BAL0891 is a novel dual inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1).1 TTK and PLK1 collaborate in activating the mitotic spindle assembly checkpoint (SAC), a mechanism regulating correct chromosome alignment and segregation during cell division. The preclinical data presented at ESMO TAT 2022 have been generated in collaboration with the Dutch precision medicine company, NTRC, from which Basilea in-licensed the drug candidate. The results confirm the mode of action by demonstrating that BAL0891 causes rapid disruption of the SAC, driving tumor cells through mitosis before the chromosomes are properly aligned, leading to premature cell division and tumor cell death. Confirmation of the unique dual activity of BAL0891 supports the differentiation over TTK- and PLK1-specific inhibitors. Moreover, potent activity on the SAC translates into strong anti-cancer activity in a broad panel of cancer cell lines, as well as tumor shrinkage and confirmed complete regressions in a preclinical in-vivo model of breast cancer.
Dr. Laurenz Kellenberger, Chief Scientific Officer of Basilea, said: “We are very pleased with the strong single agent anti-cancer activity observed in preclinical models. Following the approval of our IND application by the U.S. Food and Drug Administration in December 2021, we are continuing the preparations to enable the start of a phase 1 study with BAL0891 by mid-year.”
More preclinical data, including in-vivo data on the anti-cancer activity of BAL0891 in additional models of human cancers are planned to be presented at upcoming scientific conferences, the company said.