piperaquine
Piperaquine is an antiparasitic drug used in combination with dihydroartemisinin to treat malaria. Piperaquine was developed under the Chinese National Malaria Elimination Programme in the 1960s and was adopted throughout China as a replacement for the structurally similar antimalarial drug chloroquine. Due to widespread parasite resistance to piperaquine, the drug fell out of use as a monotherapy, and is instead used as a partner drug for artemisinin combination therapy. Piperaquine kills parasites by disrupting the detoxification of host heme. — Wikipedia
Clinical trial activity
155 trials · 195 clinical orgs · 0 marketing orgs
Earliest trial started May 1, 2003 (NCT00313872)
Timeline
Indications
Approved for
Studied for
- Anemia · Phase 4
- Anemia, Sickle Cell · Phase 2/Phase 3
- Cardiotoxicity · Phase 2
- Drug Combinations · Phase 1
- Drug Interactions · Phase 4
- Drugs, Investigational · Phase 2/Phase 3
- Elephantiasis, Filarial · Phase 3
- Fever · Phase 3
- Glucosephosphate Dehydrogenase Deficiency · Phase 4
- Healthy Volunteers · Phase 4
- Helminthiasis · Phase 3
- HIV · Phase 3
- HIV Infections · Phase 4
- Hookworm Infections · Phase 3
- Infections · Phase 2
- Malaria · Phase 4
- Malaria, Falciparum · Phase 4
- Malaria Vaccines · Phase 2
- Malaria, Vivax · Phase 4
- Neoplasm Metastasis · Phase 3
- Parasitemia · Phase 2
- Parasitic Diseases · Phase 4
- Pharmacokinetics · Phase 4
- Pharmacological and Toxicological Phenomena · Phase 2
- Plasmodium · Phase 4
- Plasmodium falciparum · Phase 4
- Plasmodium vivax · Phase 1/Phase 2
- Pregnancy · Phase 4
- Pregnancy Complications · Phase 4
- Scabies · Phase 3
- Stomach Neoplasms · Phase 3
- Strongyloidiasis · Phase 3
- Therapeutics · Phase 3
- Treatment Adherence and Compliance · Phase 4
- Treatment Outcome · Phase 4
- Trichomonas Vaginitis · Phase 3
- Tropical Medicine · Phase 3
- Vaginosis, Bacterial · Phase 3
Mechanism of action
- Ferriprotoporphyrin IXINHIBITOR
Ferriprotoporphyrin IX inhibitor
Mechanism not fully elucidated.
- UnclearUnclear
Unclear unclear
Chemistry & pharmacology
SMILES
Clc1ccc2c(N3CCN(CCCN4CCN(c5ccnc6cc(Cl)ccc56)CC4)CC3)ccnc2c1.O=P(O)(O)O.O=P(O)(O)O.O=P(O)(O)O.O=P(O)(O)O- Mol. weight
- 927.5 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPiperaquine ↗
- ChEMBLCHEMBL539666 ↗
- ChEMBLCHEMBL303933 ↗
- ChEMBLCHEMBL1652442 ↗
Also known as
- 1,3-bis(1-(7-chloro-4'-quinolyl)-4'-piperazinyl)propane
- 1,3-bis(4-(7'-chloro-4'-quinoline)-1-piperazine)
- dihydroartemisinin mixture with piperaquine tetraphosphate
- piperaquine
- piperaquine
- piperaquine
- piperaquine
- piperaquine
- piperaquine
- piperaquine phosphate
- piperaquine phosphate
- piperaquine phosphate
- piperaquine phosphate
- piperaquine phosphate hydrate
- piperaquine tetraphosphate
- piperaquine tetraphosphate
- piperaquine tetraphosphate
- piperaquine tetraphosphate /artenimol
- piperaquinoline
- quinoline, 4,4'-(1,3-propanediyldi-4,1-piperazinediyl)bis(7-chloro-)
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07246525 | Phase 4 | Dec 1, 2025 | Government of Uganda, Infectious Disease Institute, Kampala, Uganda, National Institute of Allergy and Infectious Diseases (NIAID), University of California, San Francisco |
| NCT07021430 | Early Phase 1 (Phase 1) | Oct 31, 2025 | National Institute of Allergy and Infectious Diseases (NIAID), University of North Carolina at Chapel Hill |
| NCT06962319 | Phase 3 | Sep 30, 2025 | Medicines for Malaria Venture, University of Liverpool |
| NCT07082205 | Phase 3 | May 2, 2025 | Centers for Disease Control and Prevention (CDC), National Institute of Allergy and Infectious Diseases (NIAID), University of Liverpool |
| NCT06870344 | N/A | Mar 12, 2025 | Mbarara University of Science and Technology, National Institute of Allergy and Infectious Diseases (NIAID), North Carolina State University, University of North Carolina at Chapel Hill |
| NCT06083688 | Phase 4 | Oct 31, 2024 | Kamuzu University of Health Sciences, University of Liverpool |
| NCT07281443 | N/A | Sep 23, 2024 | Cheikh Anta Diop University, Senegal, Government of France, Government of Senegal |
| NCT06516042 | Phase 3 | Aug 21, 2024 | Government of Ethiopia, PATH |
| NCT06347471 | Phase 4 | May 28, 2024 | Infectious Disease Institute, Kampala, Uganda, Radboud University, University of London |
| NCT06172686 | Phase 1 | Jan 9, 2024 | Ifakara Health Institute, University of Oxford |
| NCT06068530 | Phase 4 | Nov 1, 2023 | Mahidol University, University of Oxford |
| NCT05930782 | Phase 1 | Aug 14, 2023 | Ifakara Health Institute, Medicines for Malaria Venture |
| NCT05946642 | Phase 3 | Jul 15, 2023 | Malaria Consortium |
| NCT05788094 | Phase 4 | Jun 26, 2023 | Mahidol University |
| NCT05980156 | Phase 4 | Feb 13, 2023 | Doris Duke Charitable Foundation, Kamuzu University of Health Sciences, University of Maryland |
| NCT05829187 | Phase 2 | Nov 1, 2022 | Pancasila University |
| NCT05426434 | Phase 3 | Aug 31, 2022 | Curtin University, Government of Papua New Guinea, Menzies School of Health Research, University of Liverpool, University of Melbourne |
| NCT05252845 | Phase 2 | Jul 31, 2022 | Mahidol University, University of Oxford |
| NCT05323721 | Phase 4 | Jun 1, 2022 | Government of Uganda, Malaria Consortium |
| NCT05340153 | Phase 4 | Apr 11, 2022 | Association Camerounaise pour le Marketing Social (ACMS), Cameroon, Government of Cameroon, Impact Malaria, Cameroon, University of Yaounde |