Combinations for the treatment of neoplasms using quiescent cell targeting and inhibitors of mitosis
AssigneeFelicitex Therapeutics, Inc.
InventorsMaria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
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Abstract
The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with therapeutic agents that are inhibitors of mitosis (a mitotic inhibitor).
Claims32
A method for treating a subject having a neoplasm, the method comprising administering to the subject, sequentially or concomitantly,
- (a) a DYRK1 inhibitor which inhibits DYRK1A or DYRK1B kinase activity with an IC50 of 100 nM or lower in biochemical assays, and reduces the fraction of quiescent cancer cells (in vitro or in vivo) that would otherwise be found in the absence of such inhibitor by at least 10%;
- and
- (b) administering to the subject an inhibitor of mitosis.
A method for treating a subject having a neoplasm, the method comprising administering to the subject, sequentially or concomitantly, a DYRK1 inhibitor and administering to the subject an inhibitor of mitosis, wherein the EC50 value of the inhibitor of mitosis is at least 20% lower in the combination treatment when compared to the same treatment with the inhibitor of mitosis alone, as determined in cell-based assays.
A method for treating a subject having a neoplasm, the method comprising administering to the subject, sequentially or concomitantly, a DYRK1 inhibitor and administering to the subject an inhibitor of mitosis, wherein the combination treatment increases fraction of apoptotic cells in a treated population as compared to either agent alone by at least by 2-fold, as determined by fraction of sub-G0 cells by a FACS assay.
Dependencies are inferred from the claim text.