Pyrimethamine

CHEMBL36 Phase 4 Approved Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
248.7 g/mol
LogP
2.7
Phase
4

Pyrimethamine is a diaminopyrimidine antiparasitic agent that selectively inhibits plasmodial and toxoplasmal dihydrofolate reductase (DHFR) with much greater affinity than the mammalian enzyme, thereby blocking folate metabolism and inhibiting nucleic acid synthesis in the parasite. It is used in combination with sulfadiazine or dapsone for the treatment and secondary prophylaxis of toxoplasmosis, and with sulfadoxine as the combination Fansidar for treatment of chloroquine-resistant malaria.

Molecular Weight

248.7100 g/mol

LogP

2.70

TPSA

77.80 Ų

Lipinski RO5

Pass

Therapeutic Areas

Mechanism of Action

Disrupts essential metabolic pathways or structural components of parasitic organisms, leading to paralysis, starvation, or death of the parasite.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Disrupts essential metabolic pathways or structural components of parasitic organisms, leading to paralysis, starvation, or death of the parasite.

2D Structure

SVG PNG

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SMILES

CCc1nc(N)nc(N)c1-c1ccc(Cl)cc1

InChI

InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)

Molecular Formula

C12H13ClN4

HBD / HBA

2 / 4

Rotatable Bonds

2

Heavy Atoms

17

No targets recorded

Target interaction data is not yet available for this drug.

No interactions recorded

Drug interaction data is not yet available for this compound.

No side effects recorded

Side effect data is not yet available for this drug.

Frequently Asked Questions

Pyrimethamine is a diaminopyrimidine antiparasitic agent that selectively inhibits plasmodial and toxoplasmal dihydrofolate reductase (DHFR) with much greater affinity than the mammalian enzyme, thereby blocking folate metabolism and inhibiting nucleic acid synthesis in the parasite. It is used in combination with sulfadiazine or dapsone for the treatment and secondary prophylaxis of toxoplasmosis, and with sulfadoxine as the combination Fansidar for treatment of chloroquine-resistant malaria.

Disrupts essential metabolic pathways or structural components of parasitic organisms, leading to paralysis, starvation, or death of the parasite.

Yes, Pyrimethamine is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

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References & Data Sources

  • ChEMBL — European Bioinformatics Institute (EBI). CHEMBL36. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 4993. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

Medical Disclaimer

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.