Combretastatin A-1 Explained

Combretastatin A-1 is a combretastatin and a stilbenoid. It can be found in Combretum afrum, the Eastern Cape South African Bushwillow tree.^[1]

Biological effects in mammals

It is an antiangiogenic agent acting by destabilizing tubulin, which induces cell apoptosis of proliferating endothelial cells.^[1]

Derivatives as drugs

Currently designated an orphan drug by the FDA, combretastatin A1 diphosphate (OXi4503 or CA1P) is in Phase I clinical trials for relapsed and refractory acute myeloid leukemia and myelodysplastic syndrome.^[2]

Notes and References

1. Pettit . G. R. . Singh . S. B. . Niven . M. L. . Hamel . E. . Schmidt . J. M. . Isolation, Structure, and Synthesis of Combretastatins A-1 and B-1, Potent New Inhibitors of Microtubule Assembly, Derived from Combretum caffrum . 10.1021/np50049a016 . Journal of Natural Products . 50 . 1 . 119–131 . 1987 . 3598594.
2. Web site: A Phase I Clinical Trial of OXi4503 for Relapsed and Refractory Acute Myelogenous Leukemia (AML) and Myelodysplastic Syndromes (MDS). 7 August 2017.