Tafenoquine

CHEMBL298470 Phase 4 Approved Small molecule

Half-Life

—

Bioavailability

—

Protein Binding

—

Molecular Weight

463.5 g/mol

LogP

5.4

Phase

4

Tafenoquine is a long-acting 8-aminoquinoline antimalarial drug used for radical cure of Plasmodium vivax malaria (preventing relapse from hypnozoites) and for malaria chemoprophylaxis, with a half-life of approximately 14 days allowing single-dose treatment for vivax radical cure. Its mechanism involves generation of reactive oxygen species that are selectively toxic to Plasmodium parasites, particularly the dormant liver-stage hypnozoites responsible for P. vivax relapse. Like primaquine, it can cause hemolytic anemia in patients with G6PD deficiency.

Molecular Weight

463.5000 g/mol

LogP

5.40

TPSA

78.60 Å²

Lipinski RO5

Pass

Therapeutic Areas

Infectious Disease Malaria

Pharmacokinetics (PK)

Pharmacodynamics (PD)

2D Structure

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SMILES

COc1cc(C)c2c(Oc3cccc(C(F)(F)F)c3)c(OC)cc(NC(C)CCCN)c2n1

InChI

InChI=1S/C24H28F3N3O3/c1-14-11-20(32-4)30-22-18(29-15(2)7-6-10-28)13-19(31-3)23(21(14)22)33-17-9-5-8-16(12-17)24(25,26)27/h5,8-9,11-13,15,29H,6-7,10,28H2,1-4H3

Molecular Formula

C24H28F3N3O3

HBD / HBA

2 / 9

Rotatable Bonds

9

Heavy Atoms

33

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

Tafenoquine is a long-acting 8-aminoquinoline antimalarial drug used for radical cure of Plasmodium vivax malaria (preventing relapse from hypnozoites) and for malaria chemoprophylaxis, with a half-life of approximately 14 days allowing single-dose treatment for vivax radical cure. Its mechanism involves generation of reactive oxygen species that are selectively toxic to Plasmodium parasites, particularly the dormant liver-stage hypnozoites responsible for P. vivax relapse. Like primaquine, it can cause hemolytic anemia in patients with G6PD deficiency.

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

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

ChEMBL — European Bioinformatics Institute (EBI). CHEMBL298470. Open-access bioactivity database.
PubChem — National Center for Biotechnology Information (NCBI). CID 115358. Chemical information database.

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

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Structure

Quick Data

Formula: C24H28F3N3O3
Synonyms: 3

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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.