Indole is a compound of pyrrole and benzene in parallel, also known as benzopyrrole. There are two combinations of pyrrole and benzene, called indole and isoindole, respectively. Many derivatives of indole have physiological and pharmacological activities, and can synthesize vasodilators, antihistamines, antipyretic analgesics, etc. in medicine, so indole is also a very important heterocyclic compound.
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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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