Halofantrine
Halfan (halofantrine) is a small molecule pharmaceutical. Halofantrine was first approved as Halfan on 1992-07-24. It is used to treat falciparum malaria, malaria, and vivax malaria in the USA. It is known to target voltage-gated inwardly rectifying potassium channel KCNH2; potassium voltage-gated channel subfamily H member 2.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| infections | D007239 |
Trade Name
FDA
EMA
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Labels
FDA
EMA
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Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| malaria | EFO_0001068 | D008288 | B54 |
| vivax malaria | EFO_0007445 | D016780 | B51 |
| falciparum malaria | EFO_0007444 | D016778 | B50 |
Agency Specific
FDA
EMA
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Patent Expiration
No data
HCPCS
No data
Clinical
Clinical Trials
76 clinical trials
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Indications Phases 4
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hepatitis b | D006509 | — | — | 2 | 2 | 8 | 1 | 1 | 13 |
| Depression | D003863 | — | F33.9 | 2 | — | — | 2 | — | 4 |
| Hiv infections | D015658 | EFO_0000764 | B20 | — | 1 | — | 2 | — | 3 |
| Hepatocellular carcinoma | D006528 | — | C22.0 | — | 2 | 1 | 1 | — | 3 |
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | — | 2 | 1 | 1 | — | 3 |
| Hiv | D006678 | — | O98.7 | — | — | 1 | 1 | — | 2 |
| Neoplasms | D009369 | — | C80 | — | 1 | 1 | 1 | — | 2 |
| Immunity | D007109 | — | — | — | — | — | 2 | — | 2 |
| Human influenza | D007251 | EFO_0007328 | J11.1 | — | 1 | — | 1 | — | 2 |
| Acquired immunodeficiency syndrome | D000163 | EFO_0000765 | B20 | — | — | — | 1 | — | 1 |
Show 26 more
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Hepatitis | D006505 | — | K75.9 | 1 | 1 | 6 | — | — | 8 |
| Hepatitis a | D006506 | EFO_0007305 | B15 | 1 | 1 | 6 | — | — | 8 |
| Malaria | D008288 | EFO_0001068 | B54 | — | — | 3 | — | — | 3 |
| Liver diseases | D008107 | EFO_0001421 | K70-K77 | — | 2 | 1 | — | — | 2 |
| Herpes simplex | D006561 | — | B00 | — | — | 2 | — | — | 2 |
| Papillomavirus infections | D030361 | — | — | 1 | — | 1 | — | — | 2 |
| Falciparum malaria | D016778 | EFO_0007444 | B50 | — | — | 2 | — | — | 2 |
| Gastrointestinal neoplasms | D005770 | — | C26.9 | — | 1 | 1 | — | — | 1 |
| Digestive system neoplasms | D004067 | — | — | — | 1 | 1 | — | — | 1 |
| Adenocarcinoma | D000230 | — | — | — | 1 | 1 | — | — | 1 |
Show 10 more
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Leishmaniasis | D007896 | EFO_0005044 | B55 | 1 | 2 | — | — | — | 2 |
| Postoperative nausea and vomiting | D020250 | EFO_0004888 | — | — | 1 | — | — | 1 | 2 |
| Virus diseases | D014777 | — | B34 | — | 2 | — | — | — | 2 |
| Herpes zoster | D006562 | EFO_0006510 | B02 | 1 | 2 | — | — | — | 2 |
| Stomach neoplasms | D013274 | EFO_0003897 | C16 | — | 1 | — | — | — | 1 |
| Head and neck neoplasms | D006258 | — | — | — | 1 | — | — | — | 1 |
| Squamous cell carcinoma | D002294 | — | — | — | 1 | — | — | — | 1 |
| Squamous cell neoplasms | D018307 | — | — | — | 1 | — | — | — | 1 |
| Liver failure | D017093 | — | K72.9 | — | 1 | — | — | — | 1 |
| Acute liver failure | D017114 | — | — | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 3 | — | — | — | 2 | 5 |
| Depressive disorder | D003866 | EFO_1002014 | F32.A | 2 | — | — | — | — | 2 |
| Vomiting | D014839 | — | R11.1 | 2 | — | — | — | — | 2 |
| Nausea | D009325 | — | R11.0 | 2 | — | — | — | — | 2 |
| Infections | D007239 | EFO_0000544 | — | 1 | — | — | — | 1 | 2 |
| Anxiety disorders | D001008 | EFO_0006788 | F41.1 | 1 | — | — | — | — | 1 |
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Disease | D004194 | EFO_0000408 | R69 | — | — | — | — | 2 | 2 |
| Cardiovascular diseases | D002318 | EFO_0000319 | I98 | — | — | — | — | 1 | 1 |
| Smoking cessation | D016540 | EFO_0004319 | — | — | — | — | — | 1 | 1 |
| Pain management | D059408 | — | — | — | — | — | — | 1 | 1 |
| Premature birth | D047928 | EFO_0003917 | O60 | — | — | — | — | 1 | 1 |
| Agnosia | D000377 | EFO_0007136 | F88 | — | — | — | — | 1 | 1 |
| Retinopathy of prematurity | D012178 | EFO_1001158 | H35.1 | — | — | — | — | 1 | 1 |
| Schizophrenia | D012559 | EFO_0000692 | F20 | — | — | — | — | 1 | 1 |
| Psychotic disorders | D011618 | — | F20.81 | — | — | — | — | 1 | 1 |
| Strabismus | D013285 | — | H50.2 | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Halofantrine |
| INN | halofantrine |
| Description | Halofantrine is a drug used to treat malaria. Halofantrine's structure contains a substituted phenanthrene, and is related to the antimalarial drugs quinine and lumefantrine. Marketed as Halfan, halofantrine is never used to prevent malaria and its mode of action is unknown, although a crystallographic study showed that it binds to hematin in vitro, suggesting a possible mechanism of action. Halofantrine has also been shown to bind to plasmepsin, a haemoglobin degrading enzyme unique to the malarial parasites.
|
| Classification | Small molecule |
| Drug class | — |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CCCCN(CCCC)CCC(O)c1cc2c(Cl)cc(Cl)cc2c2cc(C(F)(F)F)ccc12 |
Identifiers
| PDB | — |
| CAS-ID | 69756-53-2 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1107 |
| ChEBI ID | — |
| PubChem CID | 37393 |
| DrugBank | DB01218 |
| UNII ID | Q2OS4303HZ (ChemIDplus, GSRS) |
Target
Agency Approved
No data
Alternate
KCNH2
KCNH2
Organism
Homo sapiens
Gene name
KCNH2
Gene synonyms
ERG, ERG1, HERG
NCBI Gene ID
Protein name
potassium voltage-gated channel subfamily H member 2
Protein synonyms
Eag homolog, Eag-related protein 1, ERG-1, Ether-a-go-go-related gene potassium channel 1, ether-a-go-go-related potassium channel protein, Ether-a-go-go-related protein 1, H-ERG, hERG-1, hERG1, human ether-a-go-go-related, long QT syndrome type 2, potassium channel, voltage gated eag related subfamily H, member 2, potassium voltage-gated channel, subfamily H (eag-related), member 2, Voltage-gated potassium channel subunit Kv11.1
Uniprot ID
Mouse ortholog
Kcnh2 (16511)
potassium voltage-gated channel subfamily H member 2 (O35989)
Variants
No data
Financial
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Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
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