U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C6H12F2N2O2
Molecular Weight 182.1685
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EFLORNITHINE

SMILES

NCCCC(N)(C(F)F)C(O)=O

InChI

InChIKey=VLCYCQAOQCDTCN-UHFFFAOYSA-N
InChI=1S/C6H12F2N2O2/c7-4(8)6(10,5(11)12)2-1-3-9/h4H,1-3,9-10H2,(H,11,12)

HIDE SMILES / InChI
Molecular Formula C6H12F2N2O2
Molecular Weight 182.1685
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf

Eflornithine is a prescription drug indicated in the treatment of facial hirsutism (excessive hair growth). Eflornithine hydrochloride cream for topical application is intended for use in women suffering from facial hirsutism and is sold by Allergan, Inc. under the brand name Vaniqa. Besides being a non-mechanical and non-cosmetic treatment, eflornithine is the only non-hormonal and non-systemic prescription option available for women who suffer from facial hirsutism. Eflornithine for injection against sleeping sickness was manufactured by Sanofi Aventis and sold under the brand name Ornidyl in the USA. It is now discontinued. Eflornithine is on the World Health Organization's List of Essential Medicines. Eflornithine prevents hair growth by inhibiting the anagen phase of hair production. This occurs by eflornithine irreversibly binding (also called suicide inhibition) to ornithine decarboxylase (ODC) and physically preventing the natural substrate ornithine from accessing the active site.

CNS Activity

Originator

Bacchi, C.
3
Curator's Comment: Eflornithine was discovered in 1980 by Dr Cyrus Bacchi

Approval Year

1990
111
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Inhibitor
8504
 8.3 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
VANIQA

Approved Use

Reduction of unwanted facial hair in women.

Launch Date

2000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
484 μM
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/15141331
100 mg/kg 4 times / day steady-state, oral
dose: 100 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFLORNITHINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4430 μM × h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/15141331
100 mg/kg 4 times / day steady-state, oral
dose: 100 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFLORNITHINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10.6 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/15141331
100 mg/kg 4 times / day steady-state, oral
dose: 100 mg/kg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
EFLORNITHINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Other AEs: Diarrhea, Dizziness...
Other AEs:
Diarrhea (grade 1, 2 patients)
Dizziness (grade 1-2, 1 patient)
Malaise (grade 1-2, 1 patient)
Mood change (grade 1, 1 patient)
Myalgia (grade 1, 1 patient)
Nausea (grade 1, 3 patients)
Nosebleed (grade 1, 2 patients)
Pruritus (grade 1, 1 patient)
Skin rash (grade 1-2, 1 patient)
Stomatitis (grade 1, 3 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Other AEs: Acne, Pseudofolliculitis barbae...
Other AEs:
Acne (10.8%)
Pseudofolliculitis barbae (4.9%)
Stinging skin (4.1%)
Headache (4%)
Burning skin (3.5%)
Dry skin (3.3%)
Pruritus (3.1%)
Erythema (2.5%)
Tingling skin (2.2%)
Dyspepsia (1.9%)
Skin irritation (1.8%)
Rash (1.5%)
Alopecia (1.3%)
Dizziness (1.3%)
Folliculitis (1%)
Ingrown hair (0.9%)
Edema face (0.7%)
Anorexia (0.7%)
Nausea (0.7%)
Asthenia (0.3%)
Vertigo (0.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Mood change grade 1, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Myalgia grade 1, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Pruritus grade 1, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Diarrhea grade 1, 2 patients
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Nosebleed grade 1, 2 patients
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Nausea grade 1, 3 patients
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Stomatitis grade 1, 3 patients
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Dizziness grade 1-2, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Malaise grade 1-2, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Skin rash grade 1-2, 1 patient
1 g/m2 1 times / day multiple, oral
Highest studied dose
Dose: 1 g/m2, 1 times / day
Route: oral
Route: multiple
Dose: 1 g/m2, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
unhealthy, 23-41
Health Status: unhealthy
Age Group: 23-41
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9516915/
Vertigo 0.1%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Asthenia 0.3%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Anorexia 0.7%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Edema face 0.7%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Nausea 0.7%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Ingrown hair 0.9%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Folliculitis 1%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Alopecia 1.3%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Dizziness 1.3%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Rash 1.5%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Skin irritation 1.8%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Dyspepsia 1.9%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Acne 10.8%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Tingling skin 2.2%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Erythema 2.5%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Pruritus 3.1%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Dry skin 3.3%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Burning skin 3.5%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Headache 4%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Stinging skin 4.1%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Pseudofolliculitis barbae 4.9%
13.9 % 2 times / day multiple, topical
Recommended
Dose: 13.9 %, 2 times / day
Route: topical
Route: multiple
Dose: 13.9 %, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:41948
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:41948
eMolecules
32452415
https://www.emolecules.com/cgi-bin/more?vid=32452415
MolPort
MolPort-006-169-327
https://www.molport.com/shop/molecule-link/MolPort-006-169-327
PubMed

PubMed

TitleDatePubMed
Effect of polyamine depletion on cone photoreceptors of the developing rabbit retina.
2002-09
Altered expression of c-myc, p16 and p27 in rat colon tumors and its reversal by short-term treatment with chemopreventive agents.
2002-09
Polyamines regulate beta-catenin tyrosine phosphorylation via Ca(2+) during intestinal epithelial cell migration.
2002-09
Stress-induced dynamic changes in mouse brain polyamines. Role in behavioral reactivity.
2002-07-05
Treatment of human African trypanosomiasis--present situation and needs for research and development.
2002-07
RhoA inactivation inhibits cell migration but does not mediate the effects of polyamine depletion.
2002-07
Polyamines modulate the interaction between nuclear receptors and vitamin D receptor-interacting protein 205.
2002-07
Polyamine uptake is necessary for a normal biochemical maturation of astrocytes in culture.
2002-06-12
Are polyamines involved in olfaction? An EAG and biochemical study in Periplaneta americana antennae.
2002-06
Involvement of polyamines in root development at low temperature in the subantarctic cruciferous species Pringlea antiscorbutica.
2002-06
Polyamine depletion prevents camptothecin-induced apoptosis by inhibiting the release of cytochrome c.
2002-06
Protein kinase Cdelta-mediated signal to ornithine decarboxylase induction is independent of skin tumor suppression.
2002-05-16
[Hypertrichosis and hirsutism].
2002-05
Selective exclusion by the polyamine transporter as a mechanism for differential radioprotection of amifostine derivatives.
2002-05
Effects of difluoromethylornithine on growth inhibition and apoptosis in human cervical epithelial and cancerous cell lines.
2002-05
The preovulatory rise of ovarian ornithine decarboxylase is required for progesterone secretion by the corpus luteum.
2002-04-26
Quantitation of polyamines in hypothalamus and pituitary of female and male developing rats.
2002-04-19
Plating densities, alpha-difluoromethylornithine effects and time dependence on the proliferation of IEC-6 cells.
2002-04
Polyamine-dependent migration of retinal pigment epithelial cells.
2002-04
Effects of polyamines on the release of gonadotropin-releasing hormone and gonadotropins in developing female rats.
2002-04
Activation of K(+) channels and increased migration of differentiated intestinal epithelial cells after wounding.
2002-04
Suppression of UV carcinogenesis by difluoromethylornithine in nucleotide excision repair-deficient Xpa knockout mice.
2002-03-01
Effects of ornithine 2-oxoglutarate on neutrophils in stressed rats: evidence for the involvement of nitric oxide and polyamines.
2002-03
Inhibition of placental ornithine decarboxylase by DL-alpha-difluoro-methyl ornithine causes fetal growth restriction in rat.
2002-02-08
Regulation of ornithine decarboxylase in B16 mouse melanoma cells: synergistic activation of melanogenesis by alphaMSH and ornithine decarboxylase inhibition.
2002-01-30
[Chemoprevention of colorectal cancer].
2002-01-26
The ornithine decarboxylase inhibitor, difluoromethylornithine, inhibits casein kinase II activity, c-Myc expression and normal human keratinocyte proliferation.
2002-01
Chemoprevention of colorectal cancer.
2002-01
Modulation of biologic endpoints by topical difluoromethylornithine (DFMO), in subjects at high-risk for nonmelanoma skin cancer.
2002-01
African trypanosomiasis in travelers returning to the United Kingdom.
2002-01
Activities of arginase I and II are limiting for endothelial cell proliferation.
2002-01
Winterbottom's sign and hypertrophic cardiomyopathy.
2002
Influence of polyamines on in vitro and in vivo features of aggressive and metastatic behavior by human breast cancer cells.
2002
Chemotherapy of human African trypanosomiasis.
2002
Eflornithine.
2001-12-01
Differential regulation of nitric oxide synthase-2 and arginase-1 by type 1/type 2 cytokines in vivo: granulomatous pathology is shaped by the pattern of L-arginine metabolism.
2001-12-01
The effect of polyamine biosynthesis inhibition on growth and differentiation of the phytopathogenic fungus Sclerotinia sclerotiorum.
2001-12
The future of colon cancer prevention.
2001-12
Beyond tamoxifen new endpoints for breast cancer chemoprevention, new drugs for breast cancer prevention.
2001-12
Chemopreventive agents inhibit aberrant proliferation of the aneuploid phenotype in a colon epithelial cell line established from Apc 1638N [+/-] mouse.
2001-12
No alterations in the performance of two interval timing operant tasks after alpha-difluoromethylornithine (DFMO)-induced cerebellar stunting.
2001-11-29
Spermidine is essential for normal proliferation of trypanosomatid protozoa.
2001-11-23
The effect of DFMO induced uptake of [3H] putrescine on human glioma cells.
2001-11
[Current treatment of hypertrichosis].
2001-11
Cell culture analysis of the regulatory frameshift event required for the expression of mammalian antizymes.
2001-11
Availability and affordability of treatment for Human African Trypanosomiasis.
2001-11
Cytoskeletal organization and cell motility correlates with metastatic potential and state of differentiation in prostate cancer.
2001-09
Glucocorticoids and polyamine inhibitors synergize to kill human leukemic CEM cells.
2001-07-24
Characterization of spermine uptake by Ehrlich tumour cells in culture.
2001
Topical eflornithine.
2001
Patents

Patents

021145-001
3
US20070246057
3

Sample Use Guides

In Vivo Use Guide
Usual Adult Dose for Hirsutism Apply a thin layer of eflornithine topical cream to affected areas of the face and adjacent involved areas under the chin and rub in thoroughly. Do not wash treated area for at least 4 hours. Use twice a day, allowing at least 8 hours between applications or as directed by a physician. Continue to use hair removal techniques as needed in conjunction with eflornithine. Apply eflornithine at least 5 minutes after hair removal.
Route of Administration: Topical
In Vitro Use Guide
Eflornithine (0.01 - 1 mM) treatment suppressed proliferation of 4T1 murine mammary cancer cells in culture.
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:29:19 GMT 2025
Edited
by admin
on Wed Apr 02 09:29:19 GMT 2025
Record UNII
ZQN1G5V6SR
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EFLORNITHINE
EMA EPAR   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
eflornithine [INN]
Preferred Name English
DIFLUOROMETHYLORNITHINE
Systematic Name English
EFLORNITHINE [VANDF]
Common Name English
EFLORNITHINE [MI]
Common Name English
EFLORNITHINE [EMA EPAR]
Common Name English
.ALPHA.-DIFLUOROMETHYLORNITHINE
Systematic Name English
Eflornithine [WHO-DD]
Common Name English
DL-ORNITHINE, 2-(DIFLUOROMETHYL)-
Systematic Name English
2-(DIFLUOROMETHYL)-DL-ORNITHINE
Systematic Name English
DFMO
Common Name English
Classification Tree Code System Code
EMA ASSESSMENT REPORTS VANIQA (AUTHORIZED: HIRSUTISM)
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
WHO-ESSENTIAL MEDICINES LIST 6.5.5.1
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 321210
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
NDF-RT N0000175845
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
WHO-ATC D11AX16
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 229306
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 387012
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
EU-Orphan Drug EU/3/11/902
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
NCI_THESAURUS C2088
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 319610
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 547716
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
NDF-RT N0000175485
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
WHO-VATC QD11AX16
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 619917
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
NDF-RT N0000175844
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
WHO-ATC P01CX03
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
FDA ORPHAN DRUG 613217
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
Code System Code Type Description
PUBCHEM
3009
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
HSDB
7923
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
RXCUI
569
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY RxNorm
LACTMED
Eflornithine
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
DAILYMED
ZQN1G5V6SR
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
MESH
D000518
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
ChEMBL
CHEMBL830
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
SMS_ID
100000085407
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
FDA UNII
ZQN1G5V6SR
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
INN
5551
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
IUPHAR
5176
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
NCI_THESAURUS
C226
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
WIKIPEDIA
EFLORNITHINE
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
CAS
70052-12-9
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
EPA CompTox
DTXSID3020467
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
DRUG BANK
DB06243
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
EVMPD
SUB06468MIG
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
CHEBI
41948
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
DRUG CENTRAL
990
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY
MERCK INDEX
m4840
Created by admin on Wed Apr 02 09:29:19 GMT 2025 , Edited by admin on Wed Apr 02 09:29:19 GMT 2025
PRIMARY Merck Index
Related Record Type Details
Structure of EFLORNITHINE, (R)-
ENANTIOMER -> RACEMATE
Structure of EFLORNITHINE, (S)-
ENANTIOMER -> RACEMATE
Structure of EFLORNITHINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Structure of EFLORNITHINE HYDROCHLORIDE ANHYDROUS
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of EFLORNITHINE
ACTIVE MOIETY
NIH
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