Product
BTG6228
Indication
Solid tumours
Phase
Preclinical
Description
BTG6228 is a novel, targeted, broad spectrum cancer therapeutic whose primary target is Na/K ATPase with effects on downstream pathways including the Hif pathway.
Further information
The Na/K ATPase pathway has been studied in man for over 30 years. Other compounds modulate the Hif pathway, but only a few target Hif directly.
Most solid tumours are hypoxic (lacking oxygen) and become more hypoxic on treatment with conventional cytotoxics which in turn reduces the effectiveness of those drugs. Hif-1 (hypoxia-inducible factor-1) is a transcription factor that enables solid tumours to adapt to oxygen deprivation or hypoxic stress, thereby circumventing cytotoxic therapy. Hif-1 is composed of Hif-1α and Hif-1β subunits, with Hif-1α over-expression related to increased patient mortality in several cancer types. Inhibiting Hif-1 may make solid tumours more susceptible to cytotoxic drugs.
BTG6228 is a Na/K ATPase inhibitor that has demonstrated in vivo efficacy in renal, pancreatic and chondrosarcoma xenograft models.
Due to the mechanism of action, BTG6228 has single agent potential, as well as potential to be added to many existing cytotoxic drug regimens to improve efficacy.
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