Eflornithine

Eflornithine, sold under the brand name Vaniqa among others, is a medication used to treat African trypanosomiasis (sleeping sickness) and excessive hair growth on the face in women. Specifically it is used for the second stage of sleeping sickness caused by T. b. gambiense and may be used with nifurtimox. It is taken intravenously (injection into a vein) or topically. It is an ornithine decarboxylase inhibitor.

Eflornithine
Clinical data
Trade namesVaniqa, Iwilfin, others
Other namesα-difluoromethylornithine or DFMO
AHFS/Drugs.comMonograph
License data
Routes of
administration
intravenous, topical
ATC code
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability100% (Intravenous)
Negligible (topical)
MetabolismNot metabolized
Elimination half-life8 hours
ExcretionKidney
Identifiers
  • (RS)-2,5-Diamino-2-(difluoromethyl)pentanoic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC6H12F2N2O2
Molar mass182.171 g·mol−1
3D model (JSmol)
SMILES
  • FC(F)C(N)(C(=O)O)CCCN
  • InChI=1S/C6H12F2N2O2/c7-4(8)6(10,5(11)12)2-1-3-9/h4H,1-3,9-10H2,(H,11,12) Y
  • Key:VLCYCQAOQCDTCN-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

Common side effects when applied as a cream include rash, redness, and burning. Side effects of the injectable form include bone marrow suppression, vomiting, and seizures. It is unclear if it is safe to use during pregnancy or breastfeeding. It is recommended typically for children over the age of 12.

Eflornithine was developed in the 1970s and came into medical use in 1990. It is on the World Health Organization's List of Essential Medicines. In the United States the injectable form can be obtained from the US Centers for Disease Control and Prevention. In regions of the world where the disease is common eflornithine is provided for free by the World Health Organization.

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