Eflornithine

Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.

Signaling Pathways >> Others >> Others

Research Areas >> Others

Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases[1]. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism[2]. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles[3]. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension[4].

Mice: The skin area where the hair is removed is then treated with the eflornithine hydrochloride 13.9% cream (∼50 mg per mouse per treatment) using a spatula 2 times a day in an interval of at least 8 h for a maximum period of 36 days[3].

[1]. Burri C, et al. Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52.

[2]. Balfour JA, et al. Topical eflornithine. Am J Clin Dermatol. 2001;2(3):197-201; discussion 202.

[3]. Kumar A, et al. A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501.

[4]. Lipke DW, et al. Eflornithine alters changes in vascular responsiveness associated with coarctation hypertension. Clin Exp Hypertens. 1997 Apr;19(3):297-312.

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MOLECULAR FORMULA :

C6-H12-F2-N2-O2

MOLECULAR WEIGHT :

182.20

WISWESSER LINE NOTATION :

Z3XZVQYFF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

800 mg/kg/4D-I

TOXIC EFFECTS :

Gastrointestinal - nausea or vomiting Blood - thrombocytopenia

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

67 mg/kg/40M-C

TOXIC EFFECTS :

Cardiac - cardiomyopathy including infarction Cardiac - pulse rate Vascular - BP lowering not characterized in autonomic section

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

9084 mg/kg/2W-I

TOXIC EFFECTS :

Gastrointestinal - nausea or vomiting Blood - thrombocytopenia

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intraperitoneal

DOSE :

1600 mg/kg

SEX/DURATION :

female 4-7 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

1 gm/kg

SEX/DURATION :

female 16-20 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

2500 mg/kg

SEX/DURATION :

female 15-17 day(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - urogenital system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - biochemical and metabolic

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

500 mg/kg

SEX/DURATION :

female 11-13 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Embryo or Fetus - other effects to embryo

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

2500 mg/kg

SEX/DURATION :

female 13-17 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Embryo or Fetus - other effects to embryo Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - physical

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intrauterine

DOSE :

50 ug/kg

SEX/DURATION :

female 4 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - other measures of fertility

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

800 mg/kg

SEX/DURATION :

female 8 day(s) after conception

TOXIC EFFECTS :

Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

MUTATION DATA

TEST SYSTEM :

Rodent - rat

DOSE/DURATION :

2800 mg/kg

REFERENCE :

BBACAQ Biochimica et Biophysica Acta. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1947- Volume(issue)/page/year: 696,179,1982