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DRUG:

IODVA1

i
Other names: IODVA1
Company:
University of Cincinnati
Drug class:
RAS inhibitor, Vav3 inhibitor
3years
Inhibition of the RacGEF VAV3 by the small molecule IODVA1 impedes RAC signaling and overcomes resistance to tyrosine kinase inhibition in acute lymphoblastic leukemia. (PubMed, Leukemia)
Importantly, IODVA1 suppresses the leukemic burden in the treatment refractory pediatric Ph and TKI-resistant Ph B-ALL patient-derived xenograft models better than standard-of-care dasatinib or ponatinib and provides a more durable response after treatment withdrawal. Pediatric leukemia samples with diverse genetic lesions show high sensitivity to IODVA1 ex vivo and this sensitivity is VAV3 dependent. IODVA1 thus spearheads a novel class of drugs that inhibits a RacGEF and holds promise as an anti-tumor therapy.
Journal
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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BCR-ABL1 T315I • ABL1 T315I
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dasatinib • Iclusig (ponatinib) • IODVA1