Peringatan Keamanan

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 embryo lethality 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.L49298

In a 2-year carcinogenicity study, once daily oral administration of eflornithine to female rats did not result in drug-related neoplasms at doses up to 600 mg/kg/day (10.5 times the human Cmax at the recommended clinical dose of 1152 ± 384 mg/m2).L49298

Eflornithine was not mutagenic in the in vitro bacterial reverse mutation (Ames) assay.L49298

Dedicated fertility studies were not conducted with eflornithine.L49298

Eflornithine

DB06243

small molecule approved withdrawn

Deskripsi

Eflornithine is an irreversible ornithine decarboxylase inhibitor originally developed as a treatment for human African trypanosomiasis.A262829 Further research has also implicated ornithine decarboxylase in other conditions like facial hirsutism and cancer, especially when ornithine decarboxylase is highly upregulated in tumor cells.A4112, A262834 Additionally, ornithine decarboxylase is activated by c-myc or interacts with ras, both very well-known oncogenes, thus increasing the interest in targeting ornithine carboxylase as a potential cancer treatment.A262839

In 1960 and 2000, the FDA approved eflornithine under the brand names ORNIDYL and VANIQUA for the treatment of African trypanosomiasis and hirsutism, respectively, but has since been discontinued.A262823,L49318 Subsequently, on December 14, 2023, the FDA approved eflornithine again but under the brand name IWILFIN as an oral maintenance therapy to reduce the risk of relapse in adult and pediatric patients with high-risk neuroblastoma who have demonstrated at least a partial response to prior multiagent, multimodality therapy, including anti-GD2 immunotherapy. This approval is based on positive results obtained from a multi-site, single-arm, externally controlled study of children with high-risk neuroblastoma, where a 52% reduction in the risk of relapse and a 68% reduction in the risk of death were observed.L49313

Struktur Molekul 2D

Berat 182.171
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal plasma elimination half-life of eflornithine was 3.5 hours, and the apparent steady-state plasma half-life of eflornithine was approximately 8 hours.[L49298,L49298]
Volume Distribusi Eflornithine volume of distribution (Vz/F) is 24.3 L.[L49288]
Klirens (Clearance) The clearance (CL/F) of eflornithine is 5.3 L/h.[L49298]

Absorpsi

Following oral administrations of eflornithine, peak plasma concentrations of eflornithine (Cmax) were achieved (Tmax) 3.5 hours post-dosing. The Cmax and AUC (area under the concentration-time curve) of eflornithine were not affected by food (high fat and high calories). Administration of crushed tablets in a standard pudding admixture had no effect on eflornithine exposure (Cmax and AUC6h).L49288 The mean percutaneous absorption of eflornithine in women with unwanted facial hair, from a 13.9% w/w cream formulation, is < 1% of the radioactive dose, following either single or multiple doses under conditions of clinical use, that included shaving within 2 hours before radiolabeled dose application in addition to other forms of cutting or plucking and tweezing to remove facial hair. Steady state was reached within four days of twice-daily application. Following twice-daily application of 0.5 g of the cream (total dose 1.0 g/day; 139 mg as anhydrous eflornithine hydrochloride), under conditions of clinical use in women with unwanted facial hair (n=10), the steady-state Cmax, Ctrough and AUC12hr were approximately 10 ng/mL, 5 ng/mL, and 92 ng hr/mL, respectively, expressed in terms of the anhydrous free base of eflornithine hydrochloride. At steady state, the dose-normalized peak concentrations (Cmax) and the extent of daily systemic exposure (AUC) of eflornithine following twice-daily application of 0.5 g of the cream (total dose 1.0 g/day) is estimated to be approximately 100- and 60-fold lower, respectively, when compared to 370 mg/day once-daily oral doses.L49298

Metabolisme

This compound is not known to be metabolized and is primarily excreted unchanged in the urine.L49298

Rute Eliminasi

This compound is not known to be metabolized and is primarily excreted unchanged in the urine.L49298

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

38 Data
Etrasimod The risk or severity of immunosuppression can be increased when Eflornithine is combined with Etrasimod.
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Eflornithine.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Eflornithine.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Eflornithine.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Eflornithine.
Lidocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Tetrodotoxin.
Ambroxol The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Ambroxol.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Eflornithine is combined with Quinisocaine.

Target Protein

Ornithine decarboxylase ODC1

Referensi & Sumber

Synthesis reference: https://www.google.com/patents/US4330559
Artikel (PubMed)
  • PMID: 18388383
    Namazi MR: Hypothesis: the potential utility of topical eflornithine against cutaneous leishmaniasis. Indian J Dermatol Venereol Leprol. 2008 Mar-Apr;74(2):158-9.
  • PMID: 18321960
    Priotto G, Pinoges L, Fursa IB, Burke B, Nicolay N, Grillet G, Hewison C, Balasegaram M: Safety and effectiveness of first line eflornithine for Trypanosoma brucei gambiense sleeping sickness in Sudan: cohort study. BMJ. 2008 Mar 29;336(7646):705-8. doi: 10.1136/bmj.39485.592674.BE. Epub 2008 Mar 5.
  • PMID: 18086592
    Hoffmann R: A 4-month, open-label study evaluating the efficacy of eflornithine 11.5% cream in the treatment of unwanted facial hair in women using TrichoScan. Eur J Dermatol. 2008 Jan-Feb;18(1):65-70. Epub 2007 Dec 18.
  • PMID: 17921631
    Jobanputra KS, Rajpal AV, Nagpur NG: Eflornithine. Indian J Dermatol Venereol Leprol. 2007 Sep-Oct;73(5):365-6.
  • PMID: 25182303
    Kumar A, Naguib YW, Shi YC, Cui Z: A method to improve the efficacy of topical eflornithine hydrochloride cream. Drug Deliv. 2016 Jun;23(5):1495-501. doi: 10.3109/10717544.2014.951746. Epub 2014 Sep 3.
  • PMID: 12811548
    Burri C, Brun R: Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res. 2003 Jun;90 Supp 1:S49-52. doi: 10.1007/s00436-002-0766-5. Epub 2002 Dec 10.
  • PMID: 32912061
    Alhosin M, Razvi SSI, Sheikh RA, Khan JA, Zamzami MA, Choudhry H: Thymoquinone and Difluoromethylornithine (DFMO) Synergistically Induce Apoptosis of Human Acute T Lymphoblastic Leukemia Jurkat Cells Through the Modulation of Epigenetic Pathways. Technol Cancer Res Treat. 2020 Jan-Dec;19:1533033820947489. doi: 10.1177/1533033820947489.
  • PMID: 25248858
    Mohammed A, Janakiram NB, Madka V, Ritchie RL, Brewer M, Biddick L, Patlolla JM, Sadeghi M, Lightfoot S, Steele VE, Rao CV: Eflornithine (DFMO) prevents progression of pancreatic cancer by modulating ornithine decarboxylase signaling. Cancer Prev Res (Phila). 2014 Dec;7(12):1198-209. doi: 10.1158/1940-6207.CAPR-14-0176. Epub 2014 Sep 23.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Florexa
    Cream • 4170 mg/30g • Topical • US
  • Iwilfin
    Tablet • 250 mg/1 • Oral • US • Approved
  • Vaniqa
    Cream • 139 mg/1g • Topical • US • Approved
  • Vaniqa
    Cream • 139 mg/1g • Topical • US • Approved
  • Vaniqa
    Cream • 139 mg/1g • Topical • US • Approved
  • Vaniqa
    Cream • 13.9 % w/w • Topical • Canada • Approved
  • Vaniqa
    Cream • 11.5 % • Cutaneous • EU • Approved
  • Vaniqa
    Cream • 11.5 % • Cutaneous • EU • Approved
Menampilkan 8 dari 9 produk.

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