Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines are known to be the backbone of many bulk compounds and important core structures for approved drugs; studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity.
Venetoclax (VEN) combined with a hypomethylating agent (HMA) has proven effective for treating acute myeloid leukemia (AML) patients who are ineligible for intensive chemotherapy. However, this combination therapy still faces issues such as low response rates, limited survival, and potential resistance to VEN.
Aptose’s Tuspetinib (TUS) is a multi-kinase inhibitor selectively targeting SYK, RSK, FLT3 , JAK1/2, KIT, which drive proliferation in AML. The addition of Tuspetinib into VEN and HMA therapy improves medical efficacy and and may help prevent resistance to both agents. TUS+VEN+HMA triplet protocol in frontline therapy for newly diagnosed (ND) AML is currently being tested in a global phase 1/2 trial.
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