Drug intelligence / Profile preview

tuspetinib + venetoclax

Development stage
Unknown
Lead developer
Aptose Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

Tuspetinib + venetoclax is an investigational combination therapy under development for the treatment of newly diagnosed acute myeloid leukemia (AML). Tuspetinib (HM43239) is a small molecule kinase inhibitor that targets key driver mutations in AML, including FLT3, SYK, and JAK kinases, while venetoclax (Venclexta) is a small molecule BCL-2 inhibitor that induces apoptosis in malignant cells. The combination is being studied as part of multi-drug regimens, including with azacitidine, aimed at improving response rates and minimal residual disease (MRD) negativity for AML patients, including those with high-risk genetic mutations such as TP53, RAS, and FLT3-ITD. Clinical data from the ongoing TUSCANY phase 1/2 trial show high rates of complete response and MRD-negativity with a favorable safety profile, supporting its potential as a frontline therapy for AML[1][2][3][4].

Other names
TUS+VENTUSVEN
02

Targets

JAK2 (Janus kinase 2)Bcl-w (B-cell lymphoma 2-like 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)JAK1 (Janus kinase 1)BCL2L1 (B-cell lymphoma-extra large protein)SYK (Spleen Tyrosine Kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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