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

Details

Stereochemistry RACEMIC
Molecular Formula C6H12F2N2O2.ClH.H2O
Molecular Weight 236.645
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EFLORNITHINE HYDROCHLORIDE

SMILES

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

InChI

InChIKey=FJPAMFNRCFEGSD-UHFFFAOYSA-N
InChI=1S/C6H12F2N2O2.ClH.H2O/c7-4(8)6(10,5(11)12)2-1-3-9;;/h4H,1-3,9-10H2,(H,11,12);1H;1H2

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
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 ( + / - )
Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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 Mon Mar 31 17:57:02 GMT 2025
Edited
by admin
on Mon Mar 31 17:57:02 GMT 2025
Record UNII
4NH22NDW9H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EFLORNITHINE HYDROCHLORIDE
MART.   ORANGE BOOK   USAN   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
EFLORNITHINE HYDROCHLORIDE MONOHYDRATE
MI  
Preferred Name English
EFLORNITHINE HYDROCHLORIDE [ORANGE BOOK]
Common Name English
DL-ORNITHINE, 2-(DIFLUOROMETHYL)-, MONOHYDROCHLORIDE, MONOHYDRATE
Common Name English
MDL 71,782 A
Code English
Eflornithine hydrochloride [WHO-DD]
Common Name English
2,5-DIAMINO-2-(DIFLUOROMETHYL)PENTANOIC ACID, MONOHYDROCHLORIDE, MONOHYDRATE
Common Name English
ORNIDYL
Brand Name English
RMI-71782-A
Code English
EFLORNITHINE HYDROCHLORIDE [MART.]
Common Name English
EFLORNITHINE HYDROCHLORIDE MONOHYDRATE [MI]
Common Name English
MDL-71782-A
Code English
IWILFIN
Brand Name English
VANIQA
Brand Name English
EFLORNITHINE HYDROCHLORIDE [USP-RS]
Common Name English
EFLORNITHINE HCL
Common Name English
2-(DIFLUOROMETHYL)-DL-ORNITHINE MONOHYDROCHLORIDE, MONOHYDRATE
Systematic Name English
EFLORNITHINE HYDROCHLORIDE [USAN]
Common Name English
EFLORNITHINE HYDROCHLORIDE [VANDF]
Common Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/02/087
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
FDA ORPHAN DRUG 13686
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
FDA ORPHAN DRUG 13586
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
EMA ASSESSMENT REPORTS VANIQUA (AUTHORIZED: HIRSUTISM)
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
NCI_THESAURUS C2088
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
FDA ORPHAN DRUG 472715
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
Code System Code Type Description
ChEMBL
CHEMBL830
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
EPA CompTox
DTXSID4045765
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
RS_ITEM_NUM
1234249
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
CAS
96020-91-6
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
NCI_THESAURUS
C1579
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
USAN
X-80
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
RXCUI
81945
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY RxNorm
PUBCHEM
441361
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
EVMPD
SUB01861MIG
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
SMS_ID
100000087997
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
CHEBI
4762
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
DRUG BANK
DBSALT001150
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
EVMPD
SUB23283
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
FDA UNII
4NH22NDW9H
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
DAILYMED
4NH22NDW9H
Created by admin on Mon Mar 31 17:57:02 GMT 2025 , Edited by admin on Mon Mar 31 17:57:02 GMT 2025
PRIMARY
Related Record Type Details
Structure of EFLORNITHINE HYDROCHLORIDE ANHYDROUS
ANHYDROUS->SOLVATE
Structure of EFLORNITHINE HYDROCHLORIDE, (S)-
ENANTIOMER -> RACEMATE
Structure of EFLORNITHINE
PARENT -> SALT/SOLVATE
Structure of EFLORNITHINE HYDROCHLORIDE, (R)-
ENANTIOMER -> RACEMATE
Related Record Type Details
Structure of EFLORNITHINE
ACTIVE MOIETY
NIH
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