What you need to know about Deferiprone?

Deferiprone (1,2-dimethyl-3-hydroxypyridin-4- one, or L1, DMHP, Kelfer, CP20, Ferriprox®) is an oral iron chelator from the bidentate hydroxypyridones family. It was synthesized in the eighties and early applied to humans, with a long but not systematic development as a drug. Results of large and controlled studies in humans became available in the 1990s, allowing the approval of deferiprone in Europe and in a number of countries outside United States and Canada often as a second-line treatment for iron overload when DFO therapy is contraindicated or inadequate [1]. 

Therapeutic Uses

Ferriprox (deferiprone) is indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate[2].

Mechanism of action

Deferiprone is an iron chelator that binds to ferric ions (iron III) and forms a 3:1 (deferiprone: iron) stable complex and is then eliminated in the urine. Deferiprone is more selective for iron in which other metals such as zinc, copper, and aluminum have a lower affinity for deferiprone.

Absorption

Deferiprone is absorbed in the upper gastrointestinal tract. Absorption is rapid with maximum plasma concentrations occurring after 1 hour in the fasted state and after 2 hours in the fed state.

Toxicity

Agranulocytosis and neutropenia may occur, which can lead to fatal infections. Hepatoxicity is also possible. Most common side effects that lead to discontinuation of therapy were the gastrointestinal adverse effects (diarrhea, ulcer, nausea, gastrointestinal disturbances) [3].

Important Information

1)  Before taking this medicine, you should not use deferiprone if you are allergic to it.

2)  Tell your doctor if you have ever had liver disease or a weak immune system.

3)  It is not known whether this medicine will harm an unborn baby. Both men and women using this medicine should use effective birth control to prevent pregnancy. 

4)  If you take any of the following medicines, take your deferiprone dose 4 hours before or 4 hours after you take the other medicine:

•  an antiacid that contains aluminum;
•  a medicine or supplement that contains iron (including ferric citrate, Feosol, Fergon, Ferrocite, Hemocyte, and others; or
•  vitamin or mineral supplements that contain iron or zinc.

5)  Avoid taking an herbal supplement containing milk thistle.

6)  Other drugs may affect deferiprone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using [4]. 

Reference

[1] Antonio Piga, Simona Roggero, Ilaria Salussolia, Davide Massano, Melania Serra, & Filomena Longo. (2010). Deferiprone. Annals of the New York Academy of Sciences, 1202.
[2] https://pubchem.ncbi.nlm.nih.gov/compound/Deferiprone#section=Manufacturer
[3] https://www.drugbank.ca/drugs/DB08826
[4] https://www.drugs.com/mtm/deferiprone.htm