Emerging evidence supports synergistic potential of new-generation PLK1 inhibitors, such as Onvansertib, with chemo- and immune-therapies. This mini-review and perspective present current insights on PLK1 overexpression and its mechanistic impact on cancer aggressiveness and therapy resistance. We highlight the need for refined patient stratification and innovative combination regimens to exploit PLK1 inhibition in cancer treatment.
BAL0891 combined with paclitaxel in vivo showed strong reproducible synergy in the TNBC BR1282 model, with a high percentage of complete cures. Synergistic anti-tumor effects were also observed with carboplatin in the ovarian SKOV-3 model. Strong BAL0891 single agent activity was previously reported; the current data support BAL0891 combination strategies in the clinic.
BAL0891 is a novel dual TTK/PLK1 mitotic checkpoint inhibitor with potent anti-cancer activity in TNBC models. Intermittent IV administration is well tolerated and associated with prolonged tumor drug exposure, prolonged TTK inhibition and notable anti-tumor efficacy. These data support further investigation of BAL0891 for the treatment of cancer patients (incl.
BAL0891 is a novel, dual TTK/PLK1 mitotic checkpoint inhibitor. In tumor cells, a prolonged effect on TTK combined with a transient effect on PLK1 contributes to rapid SAC disruption and aberrant mitotic exit, associated with potent single agent activity in mouse models of human cancer.