Eflornithine
- (RS ) -2,5- diamino- 2 - ( difluoromethyl) pentanoic acid (IUPAC)
- Difluoromethyl -ornithine
- DFMO
- 70052-12-9
- 96020-91-6 ( monohydrochloride monohydrate )
D11AX16 P01CX03
Antiprotozoals
Template: Infobox chemical / molecular formula search available
Eflornithine is a drug against sleeping sickness, Trypanosoma brucei gambiense is the causative agent. Its chemical name is difluoromethyl - ornithine, DFMO short.
As Vaniqa ® eflornithine is marketed for the treatment of unwanted hair growth ( hirsutism ) on the face in women.
History
In view of the toxicity of the drug and the onset of resistance problems of the already few and old trypanosome agent eflornithine, which originates from the oncology was considered in the 1980s, almost as a panacea. The production was, however, set in the 1990s for financial reasons, despite some protests; similar fate overtook endangered or other means to diseases of the African continent. Only when eflornithine came on the market in an anti - beard - for women and was heavily advertised, the absurdity of the situation is also brought to light in the public and politicians.
An agent that could save many lives in Africa, was not sold there, but used in the industrialized countries as a cosmetic. The company Sanofi -Aventis, through mergers meanwhile rights holders and the WHO finally agreed on a program that funds will be reinstated to Africa.
Effect
Eflornithine is an irreversible inhibitor of the enzyme ornithine decarboxylase ( ODC), which catalyzes the conversion of ornithine to putrescine and other polyamines which in turn are involved in the regulation of cell growth and differentiation, and in the hair follicle. Characterized the formation of the hair is slowed down. Vaniqa is approved for women with unwanted hair growth ( hirsutism ) on the face. According to the studies Vaniqa should slow the growth of facial hair clearly within eight weeks - provided it is applied daily twice at an interval of eight hours on clean, dry skin, massaged in and left there for at least four hours. For lasting success long-term treatment is necessary, as set in their original condition about eight weeks after completion of therapy.
Despite its specific inhibition of ODC eflornithine is only effective against the causative agent of West African sleeping sickness, Trypanosoma brucei rhodesiense, but not against. The reason for this is that in these cells, the ODC is renewed much faster gambiense ( after a few hours) than in T.brucei and therefore eflornithine only shorter time can be effective.
Studies on hirsutism
The efficacy and safety has been tested according to product information in two studies involving nearly 600 women with excessive hair growth on the face for 24 weeks.
Result
- 6 % pure, almost pure
- 29 % significant improvement
- 35 % improvement
- 30 % no improvement / deterioration
In comparison, also one third improved in hair growth on the basis of the cream base.
As a very common side effect (> 10 %) was generally mild acne has been found frequently (1% to 10 %) occurred Pseudofolliculitis barbae, alopecia, tingling, itching, burning, stinging, dry skin, redness, irritation, rash and folliculitis on.
Since Vaniqa is not a depilatory cream, a conventional hair removal is still necessary. However, the distances between the hair removal will be greater by the slowdown in growth.