Target intelligence / Profile preview

Plasmodium falciparum heme

Molecular classification
Other (prosthetic group/cofactor), Enzyme (when referring to associated proteins such as heme detoxification protein, falcipains, plasmepsins, heme polymerase), Protein (in the context of heme-binding proteins)
01

Overview

Plasmodium falciparum heme refers to the iron-containing prosthetic group released during the parasite’s digestion of host hemoglobin in red blood cells. The parasite uses hemoglobin as its main nutrient source, breaking it down in the acidic food vacuole and releasing heme, which is toxic unless detoxified. To prevent heme toxicity, Plasmodium falciparum polymerizes free heme into inert crystals known as hemozoin, using proteins such as heme detoxification protein (HDP), histidine-rich protein II (HRP II), and other enzymes[1][6]. The unique abundance and biochemical activity of heme inside the parasite are exploited by antimalarial drugs containing an endoperoxide bridge, such as artemisinin and its derivatives. These drugs are activated by heme iron, resulting in cleavage of the endoperoxide bridge and formation of highly reactive radicals. The radicals cause rapid molecular and membrane damage, leading to parasite death[2][4][6]. Heme and heme-related metabolic enzymes are therefore validated therapeutic targets for the selective killing of Plasmodium falciparum by the endoperoxide class of antimalarials.

Other names
Ferriprotoporphyrin IX (heme)Malaria parasite hemeHeminHaem iron
02

Mechanism of action

Bioactivation of endoperoxide bridge in antimalarial drugs in the presence of heme iron (Fe2+), forming cytotoxic radicals[2][4][6]; Induction of parasite membrane damage, alkylation, oxidative stress, and cell death; Alkylation of heme and proteins, inhibition of enzymes and nucleic acid synthesis

03

Biological functions

Metabolic cofactorComponent of heme detoxificationIron activation and redox chemistrySubstrate for hemozoin formationMediation of parasite death via drug activation[1][6]
04

Disease associations

Infection (malaria)Other (drug activation)
05

Safety considerations

Host toxicity due to off-target radical generation and oxidative stressDrug resistance via altered heme metabolism and detoxification pathwaysPotential hemolysis in patients with underlying red blood cell disorders
06

Interacting drugs

Artemisinin and derivatives (artesunate, artemether, dihydroartemisinin, etc.)[2][4][6]

1 more in the full profile.

07

Biomarkers

Hemozoin (the product of heme detoxification/polymerization; can be monitored microscopically or by detection techniques)Parasite clearance rate (indirect biomarker for efficacy of endoperoxide drugs)

Beyond the preview

Go deeper on Plasmodium falciparum heme.

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Plasmodium falciparum heme.

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call