Uranovia (eflornithine HCl)
Hair Growth Inhibitors, Topical Topical Cream (Gram)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Eflornithine hydrochloride, an ornithine decarboxylase inhibitor, is an antineoplastic agent.
Eflornithine is an irreversible inhibitor of the enzyme ornithine decarboxylase (ODC), the first and rate-limiting enzyme in the biosynthesis of polyamines and a transcriptional target of MYCN. Polyamines are involved in differentiation and proliferation of mammalian cells and are important for neoplastic transformation. Inhibition of polyamine synthesis by eflornithine restored the balance of the LIN28/Let-7 metabolic pathway, which is involved in regulation of cancer stem cells and glycolytic metabolism, by decreasing expression of the oncogenic drivers MYCN and LIN28B in MYCN-amplified neuroblastoma.
In vitro, eflornithine induced senescence and suppressed neurosphere formation in MYCN-amplified and MYCN non-amplified neuroblastoma cells, indicating a cytostatic effect. Treatment with eflornithine prevented or delayed tumor formation in mice injected with limiting dilutions of MYCN-amplified neuroblastoma cells.
Following oral administration of eflornithine, peak plasma concentrations (Cmax) were achieved 3.5 hours post dosing. The Cmax and AUC are not affected by food (high fat and high calories). Administration of crushed tablets in a standard pudding admixture did not alter eflornithine exposure.
Eflornithine does not specifically bind to human plasma proteins. The terminal plasma elimination half-life of eflornithine is 3.5 hours. Eflornithine is not highly metabolized; 80% is excreted unchanged in the urine.
Pharmacokinetic analyses suggests that age (range: 1 to 19 years), sex, or body surface area (range: 0.4 to 2 m2) and mild hepatic impairment (bilirubin <= the upper limit of normal (ULN) and AST > ULN or bilirubin <1 times ULN and any AST) had no clinically meaningful effects on eflornithine exposure. Exposure of eflornithine was 2- or 4-fold higher in adults with moderate or severe renal impairment, respectively, when compared to adults with normal renal function following administration of a single 576 mg dose.
USES: This medication is used to slow down the growth of unwanted hair on the face and under the chin in women. It should not be used for hair on other parts of the body. It blocks a certain natural substance (an enzyme) that is needed for hair growth in the skin.
This effect slows hair growth and may also make the hair finer and lighter. It does not remove hair or cause the hair to fall out. This drug is not for use in children younger than 12 years.
Generic name: eflornithine HCl
Pronunciation: (eh-FLOOR-nith-een)
Drug class: Hair Growth Inhibitors, Topical
Therapeutic class: Dermatological
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Uranovia
Indications
The following indications are listed for Uranovia:
- Female Facial Hirsutism
Dosing
Available as eflornithine hydrochloride; dosage is expressed in terms of eflornithine.
The recommended eflornithine dosage modifications for adverse reactions are provided below in Tables 2 and 3. If subsequent adverse reactions occur, continue dosage reduction until reaching the minimum dosage of 192 mg orally once per day. Permanently discontinue eflornithine if the patient is unable to tolerate the minimum dosage of 192 mg once per day.
Table 2. Recommended Actions for Eflornithine Adverse Reactions
Adverse Reaction Severity Dosage Modification Neutrophil count <500/mm3 Withhold eflornithine decreased until recovery to >=500/mm3. If recovered within 7 days, resume eflornithine at the same dosage. If recovered after 7 days, resume eflornithine at the next reduced dosage level (Table 3). Platelet count decreased <25,000/mm3 Withhold eflornithine until recovery to >=25,000/mm3. If recovered within 7 days, resume eflornithine at the same dosage. If recovered between 7 and 14 days, resume eflornithine at the next reduced dosage level (Table 3). If not recovered within 14 days, p ermanently discontinue eflornithine. Anemia <8 g/dL Withhold eflornithine until hemoglobin recovery to >=8 g/dL, then resume eflornithine at the same dosage. If anemia recurs (hemoglobin <8 g/dL), withhold eflornithine until recovery to >=8 g/dL and resume eflornithine at the next reduced dosage level (Table 3). Hepatotoxicity (AST or AST or ALT >=10 times Withhold eflornithine ALT increased) the upper limit of until recovery to <10 normal (ULN) times ULN. If recovered within 7 days, resume eflornithine at the same dosage. If recovered after 7 days, resume eflornithine at the next reduced dosage level (Table 3). Hearing loss Clinically concerning Continue dosing with new or worsening hearing eflornithine and repeat loss compared to audiogram in 3 weeks. If baseline audiogram improved, continue eflornithine at the same dosage. If clinically concerning changes persist, hold eflornithine for up to 30 days and repeat audiogram. If stable or improved, resume efl ornithine at the next reduced dosage level (Table 3). Nausea, vomiting, or Grade 3 If symptoms respond to diarrhea supportive treatment (e.g., anti-emetic, anti-diarrheal therapy), continue eflornithine at the same dosage. If symptoms do not respond to treatment, withhold eflornithine until recovery to <=Grade 2. Resume eflornithine at the next r educed dosage level (Table 3). Other adverse reactions Grade 3 or 4 Withhold eflornithine until recovery to <=Grade 2. Resume eflornithine at the next reduced dosage level (Table 3). Other adverse reactions Recurrent Grade 4 Permanently discontinue eflornithine.
Severity as defined by National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 4.03.
Table 3. Recommended Eflornithine Oral Dosage Reduction for Toxicity Management
Current Dosage Reduced Dosage 768 mg (4 tablets) twice daily 576 mg (3 tablets) twice daily 576 mg (3 tablets) twice daily 384 mg (2 tablets) twice daily 384 mg (2 tablets) twice daily 192 mg (1 tablet) twice daily 192 mg (1 tablet) twice daily 192 mg (1 tablet) once daily
Eflornithine is administered orally as tablets, with or without food.
Eflornithine tablets can be swallowed whole, chewed, or crushed.
For patients who have difficulty swallowing tablets, eflornithine can be chewed or crushed and mixed with 2 tablespoons of soft food or liquid. Visually confirm that the entire contents are consumed. If any crushed tablet particles remain in the container, mix with an additional small volume (no more than 1 ounce or 30 mL) of soft food or liquid. The crushed tablet preparation should be discarded after 1 hour.
A missed dose of eflornithine should be administered as soon as possible. If the next dose is due within 7 hours, the missed dose should be skipped.
If vomiting occurs after taking eflornithine, an additional dose should not be administered; continue with the next scheduled dose.
Store eflornithine tablets at 20 to 25degreesC, with excursions permitted between 15 to 30degreesC.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Uranovia 13.9% Cream Pump | Maintenance | Apply a thin layer to the affected area(s) by topical route 2 times per day. |
No dosing information is available for this tab.
Drug interactions
Eflornithine has no clinically relevant drug interactions.
Eflornithine does not induce or inhibit any cytochrome P-450 (CYP) enzymes or act as a substrate or inhibitor of major drug transporters.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
The most common adverse effects of eflornithine (>=5% of patients) reported in clinical studies include hearing loss, otitis media, pyrexia, pneumonia, and diarrhea. The most common Grade 3 or 4 laboratory abnormalities (>=2% of patients) reported in clinical studies include increased ALT, increased AST, decreased neutrophil count, and decreased hemoglobin.
There are no severe adverse reactions for this drug.
More Frequent
- Acne vulgaris
- Stinging of skin
Rare or Very Rare
- Acne rosacea
- Cheilitis
- Contact dermatitis
- Erythema
- Folliculitis
- Head sensation disturbance
- Herpes simplex infection
- Lip hypertrophy
- Skin rash
Precautions
No enhanced messaging available.
The safety and effectiveness of eflornithine have been established in pediatric patients with high-risk neuroblastoma who have demonstrated at least a partial response to prior multiagent, multimodality therapy including anti-GD2 immunotherapy. Use of eflornithine for this indication is supported by evidence from adequate and well-controlled studies in pediatric patients with a median age of 4 years (range: 1 to 17).
The safety and effectiveness of eflornithine have not been established in pediatric patients for other indications.
Based on findings from animal studies and its mechanism of action, eflornithine can cause fetal harm when administered to a pregnant woman. In animal reproduction studies, oral administration of eflornithine to pregnant rats and rabbits during the period of organogenesis resulted in embryolethality at doses equivalent to the recommended human dose. There are no available data on the use of eflornithine in pregnant women. Advise pregnant women and females of reproductive potential of the potential risk to a fetus.
There are no data on the presence of eflornithine in human milk, the effects on the breast-fed child, or the effects on milk production. Because of the potential for serious adverse reactions in breast-fed children, advise women not to breastfeed during treatment with eflornithine and for 1 week after the last dose.
The manufacturer makes no specific dosage recommendations for geriatric patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Female facial hirsutism | ||
| L68.0 | ICD10CM | Hirsutism |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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