vodobatinib

Vodobatinib is a third-generation, orally bioavailable small molecule inhibitor of Bcr-Abl (c-Abl) tyrosine kinase. It is structurally related to dasatinib and ponatinib and was developed as a more potent c-Abl inhibitor, with an IC50 of 0.9 nM for c-Abl, surpassing nilotinib in potency. Vodobatinib selectively targets the Bcr-Abl fusion oncoprotein—including forms with resistance mutations such as T315I—thereby inhibiting proliferation of Bcr-Abl-expressing tumor cells. The drug has been investigated for its antineoplastic activity in chronic myeloid leukemia (CML) and precursor B-cell lymphoblastic leukemia/lymphoma, as well as for neuroprotective effects in Parkinson’s disease and dementia with Lewy bodies due to its ability to penetrate the brain and inhibit c-Abl-mediated pathogenic processes such as α-synuclein aggregation. Development for neurodegenerative indications has been discontinued; clinical trials in hematologic malignancies are ongoing[2][3][4][6].

Other names

1388803-90-4