Idronoxil has been the subject of more than 50 peer-reviewed publications over the last
two decades. This isoflavone is an intriguing regulator of multiple signal transduction pathways, capable
of causing a range of biological effects, including cell cycle arrest, apoptosis, an ability to
stimulate the immune system, and inhibition of angiogenesis. These multifaceted actions suggest
that idronoxil has the potential to synergize with, or complement, a wide range of cancer therapies.
Whilst clinically tested in the past, idronoxil’s journey was discontinued as a result of its low
bioavailability in humans when administered either intravenously or orally, though strategies to
overcome this issue are currently being explored. Here, we summarize the current literature regarding
the key cellular targets of idronoxil and the mechanisms by which idronoxil exerts its anticancer
effects, laying a new foundation toward giving this unique molecule a second chance of contributing
to the future of cancer treatment.