halofantrine
Trade name: halfan
Approved
Jul 24, 1992
Halofantrine is a blood schizonticidal antimalarial agent with no apparent action on the sporozoite, gametocyte or hepatic stages of the infection. It is used only to treat but not to prevent malaria. Has been marketed by GlaxoSmithKline as HALFAN (halofantrine hydrochloride) in 250 mg tablets indicated for the treatment of adults who can tolerate oral medication and who have mild to moderate malaria (equal to or less than 100,000 parasites/mm3) caused by Plasmodium falciparum or Plasmodium vivax. Among side effects is cardiac arrhythmia. It belongs to the phenanthrene class of compounds that includes quinine and lumefantrine. It was reported that halofantrine binds to hematin in vitro (crystal structure of the complex) and to to plasmpesin, a haemoglobin degrading enzyme unique to the malarial parasites. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 1 marketing orgs
Timeline
1990s
- Nov 4, 1991
Orphan Drug Designation
- Jul 24, 1992
GlaxoSmithKline — Earliest FDA Approval
- Jul 24, 1992
GlaxoSmithKline — NDA Organization
- Jul 24, 1992
GlaxoSmithKline — NDA Secondary Org
Indications
Mechanism of action
- Ferriprotoporphyrin IXINHIBITOR
Ferriprotoporphyrin IX inhibitor
Approval history
- approvedPriority reviewJul 24, 1992
Chemistry & pharmacology
SMILES
CCCCN(CCCC)CCC(O)c1cc2c(Cl)cc(Cl)cc2c2cc(C(F)(F)F)ccc12- Mol. weight
- 500.43 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1107 ↗
- WikipediaHalofantrine ↗
- NCATSQ2OS4303HZ ↗
- ChEMBLCHEMBL1200901 ↗
Also known as
- 1-(1,3-dichloro-6-trifluoromethyl-9-phenanthryl)-3-di(n-butyl)aminopropanol hcl
- halfan
- halfan
- halfan
- halfan
- halfan
- halofantrina
- halofantrina
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine
- halofantrine hcl
- halofantrine hcl
- halofantrine hcl
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrine hydrochloride
- halofantrinum
- halofantrinum
- wr 171669
- wr-171669
- wr-171669
- wr-171,669
- wr 171,699
- wr-171699
Organizations
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| GlaxoSmithKline | For profit | NDA | Jul 24, 1992 |
| GlaxoSmithKline | For profit | NDA2 | Jul 24, 1992 |