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Griseofulvin, an orally active antifungal drug used to treat dermatophyte infections, has a secondary effect of inducing cytochrome P450-mediated production of  N -methyl protoporphyrin IX ( N -MPP).  N- MPP is a potent competitive inhibitor of the heme biosynthetic-enzyme ferrochelatase, and inhibits the growth of cultured erythrocyte stage  Plasmodium falciparum . Novel drugs against  Plasmodium  are needed to achieve malaria elimination. Thus, we investigated whether griseofulvin shows anti-plasmodial activity. We observed that the intraerythrocytic growth of  P. falciparum  is inhibited in red blood cells pretreated with griseofulvin  in vitro . Treatment with 100 μM griseofulvin was sufficient to prevent parasite growth and induce the production of  N -MPP. Inclusion of the ferrochelatase substrate PPIX blocked the inhibitory activity of griseofulvin, suggesting that griseofulvin exerts its activity through the  N -MPP-dependent inhibition of ferrochelatase. In an  ex-vivo  study, red blood cells from griseofulvin-treated subjects were refractory to the growth of cultured  P. falciparum . However, in a clinical trial griseofulvin failed to show either therapeutic or prophylactic effect in subjects infected with blood stage  P. falciparum . Although the development of griseofulvin as an antimalarial is not warranted, it represents a novel inhibitor of  P. falciparum  growth and acts via the  N -MPP-dependent inhibition of ferrochelatase.

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Griseofulvin impairs intraerythrocytic growth of Plasmodium falciparum through ferrochelatase inhibition but lacks activity in an experimental human infection study