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Eflornithine | CAS No: 70052-12-9 | GMP-certified suppliers
A medication that reduces relapse risk in high-risk neuroblastoma patients following multiagent therapy, supporting maintenance treatment in adult and pediatric oncology settings.
Therapeutic categories
Primary indications
- Eflornithine is indicated to reduce the risk of relapse in adult and pediatric patients with high-risk neuroblastoma (HRNB) who have demonstrated at least a partial response to prior multiagent, multimodality therapy including anti-GD2 immunotherapy
- It was also previously indicated for the treatment of female hirsutism and African trypanosomiasis but has since been discontinued
Product Snapshot
- Eflornithine is available primarily as a topical cream and oral tablet formulation
- It is mainly used to reduce relapse risk in high-risk neuroblastoma patients who have responded to prior multiagent therapy
- The product has regulatory approvals in the US, Canada, and the EU, with certain indications, such as treatment for hirsutism and African trypanosomiasis, withdrawn
Clinical Overview
Clinically, eflornithine is currently approved as an oral maintenance therapy to reduce the risk of relapse in adult and pediatric patients with high-risk neuroblastoma (HRNB) who show at least a partial response to prior multiagent, multimodality therapy including anti-GD2 immunotherapy. This indication was granted based on evidence demonstrating significant reductions in relapse and mortality risks in this population. Historically, eflornithine was also used in the treatment of African trypanosomiasis and female facial hirsutism but those indications have since been discontinued.
Pharmacodynamically, eflornithine’s inhibition of ODC reduces polyamine synthesis, which downregulates components of the LIN28/Let-7 metabolic pathway implicated in cancer stem cell regulation and glycolytic metabolism. In MYCN-amplified neuroblastoma models, eflornithine decreases oncogenic driver expression (MYCN and LIN28B), induces cellular senescence, suppresses tumor-initiating neurosphere formation, and delays tumor development in vivo, consistent with a cytostatic mechanism.
Key ADME characteristics of eflornithine include oral bioavailability aligning with its approved oral maintenance dosing. Its clearance and distribution parameters support its use in pediatric and adult populations, although detailed pharmacokinetic data are limited in the public domain.
Safety and toxicity considerations center on its enzyme-inhibitory activity and potential off-target effects due to polyamine suppression. While generally well tolerated in approved contexts, monitoring for adverse events related to cytostatic effects and potential impacts on rapidly dividing normal cells is prudent.
Notable brands include the historic ORNIDYL and VANIQUA, which are no longer marketed, and the recently approved IWILFIN for neuroblastoma relapse prevention.
From an API sourcing perspective, due diligence is required to ensure GMP-compliant manufacture, with particular attention to the compound’s irreversible enzyme inhibition properties that may pose handling risks. Quality control should emphasize high purity, consistent potency, and absence of related impurities or degradation products that could affect clinical safety and efficacy profiles.
Identification & chemistry
| Generic name | Eflornithine |
|---|---|
| Molecule type | Small molecule |
| CAS | 70052-12-9 |
| UNII | ZQN1G5V6SR |
| DrugBank ID | DB06243 |
Pharmacology
| Summary | Eflornithine irreversibly inhibits ornithine decarboxylase (ODC), the rate-limiting enzyme in polyamine biosynthesis, reducing polyamine-mediated cell proliferation and differentiation. This inhibition modulates oncogenic pathways including MYCN and LIN28B, leading to cytostatic effects and suppression of tumor formation in MYCN-amplified neuroblastoma models. Additionally, eflornithine’s impact on polyamine synthesis affects keratinocyte proliferation, influencing hair folicle activity. |
|---|---|
| Mechanism of action | 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 the differentiation and proliferation of mammalian cells and are important for neoplastic transformation. |
| Pharmacodynamics | Inhibition of polyamine synthesis by eflornithine restored the balance of the LIN28/Let-7 metabolic pathway, which is involved in the 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. Additionally, polyamines are also involved in keratin synthesis, and inhibition of polyamines can decrease the proliferation of hair matrix cells and thus inhibit the anagen phase of hair production. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Ornithine decarboxylase | Humans | inhibitor |
ADME / PK
| Absorption | Following oral administrations of eflornithine, peak plasma concentrations of eflornithine (C<sub>max</sub>) were achieved (T<sub>max</sub>) 3.5 hours post-dosing. The C<sub>max</sub> 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 (C<sub>max</sub> and AUC<sub>6h</sub>). 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 C<sub>max</sub>, C<sub>trough</sub> and AUC<sub>12hr</sub> 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 (C<sub>max</sub>) 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. |
|---|---|
| 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. |
| Protein binding | Eflornithine does not specifically bind to human plasma proteins. |
| Metabolism | This compound is not known to be metabolized and is primarily excreted unchanged in the urine. |
| Route of elimination | This compound is not known to be metabolized and is primarily excreted unchanged in the urine. |
| Volume of distribution | Eflornithine volume of distribution (Vz/F) is 24.3 L. |
| Clearance | The clearance (CL/F) of eflornithine is 5.3 L/h. |
Formulation & handling
- Eflornithine is a small molecule alpha amino acid available for topical and oral administration.
- The API is highly water-soluble with a hydrophilic profile (logP -2.9), facilitating formulation in aqueous-based creams and oral tablets.
- No specific food interaction precautions are required; it can be administered with or without food.
Regulatory status
| Lifecycle | The API's patents expired between 1997 and 2014 in the United States and Canada, indicating established market presence primarily in these regions. The product is marketed in the US, Canada, and the EU, reflecting a mature lifecycle stage. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Eflornithine is marketed under multiple branded products across the US, Canada, and EU, indicating a presence of several originator companies managing its distribution in key markets. Patent expirations in the US and Canada, with the most recent dating back to 2014 and 2013 respectively, suggest that generic competition is likely established or forthcoming in these regions. The global supply landscape therefore includes both branded and generic manufacturers catering to diverse geographic markets. |
|---|
Safety
| Toxicity | 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. 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 C<sub>max</sub> at the recommended clinical dose of 1152 ± 384 mg/m2). Eflornithine was not mutagenic in the in vitro bacterial reverse mutation (Ames) assay. Dedicated fertility studies were not conducted with eflornithine. |
|---|
- Eflornithine demonstrated embryo lethality in animal reproduction studies at doses comparable to human therapeutic levels, indicating potential fetal toxicity
- Long-term carcinogenicity studies in rats showed no drug-related neoplasms at exposures exceeding clinical doses
- Eflornithine tested negative in in vitro mutagenicity assays
Eflornithine is a type of Antiprotozoics
Antiprotozoics are a vital subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) used to combat protozoan infections. Protozoa are single-celled microorganisms that can cause severe diseases in humans, such as malaria, leishmaniasis, and toxoplasmosis. Antiprotozoic APIs play a crucial role in the development of effective medications to treat these infections.
These APIs work by targeting specific metabolic pathways or enzymes within the protozoan organisms, effectively inhibiting their growth and reproduction. By interrupting essential processes, antiprotozoics can eliminate the protozoa from the body or suppress their activity, allowing the immune system to effectively combat the infection.
Pharmaceutical companies invest significant efforts in research and development to discover and synthesize new antiprotozoic APIs. The goal is to develop highly potent and selective compounds that can effectively eradicate protozoa while minimizing side effects on the human body. This involves rigorous testing and screening of various chemical compounds to identify potential drug candidates with optimal therapeutic properties.
Antiprotozoic APIs are then used as the active ingredients in the formulation of pharmaceutical drugs, such as tablets, capsules, or injectables. These drugs are prescribed by healthcare professionals to patients suffering from protozoan infections. The selection of the appropriate antiprotozoic API depends on the specific protozoan strain and the characteristics of the infection.
In summary, antiprotozoic APIs are essential pharmaceutical ingredients that play a vital role in treating protozoan infections. Their development involves rigorous research and testing to identify potent compounds that can effectively target and eliminate protozoa, leading to improved health outcomes for patients.
Eflornithine (Antiprotozoics), classified under Antiparasitics
Antiparasitics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are used to combat parasitic infections in humans and animals. These APIs play a crucial role in the field of medicine and veterinary care by targeting and eliminating various parasites, such as protozoa, helminths, and ectoparasites.
The use of antiparasitics is essential in preventing and treating parasitic diseases, which can cause significant health issues and even be life-threatening. These APIs work by interfering with the parasite's vital biological processes, such as reproduction, metabolism, and survival mechanisms.
Pharmaceutical companies develop and manufacture a wide range of antiparasitic APIs to cater to different parasitic infections. Some common examples of antiparasitics include anthelmintics (used against intestinal worms), antimalarials (used to treat malaria), and ectoparasiticides (used to control external parasites like ticks and fleas).
The development of antiparasitic APIs requires rigorous research, including the identification of suitable targets within the parasite's biology and the formulation of effective chemical compounds. Safety and efficacy are paramount in the manufacturing of antiparasitics, ensuring that they effectively combat the targeted parasites while minimizing adverse effects on the host.
Overall, antiparasitics are vital tools in the fight against parasitic infections, benefiting both human and animal health. Through ongoing research and development, the pharmaceutical industry continues to innovate and improve antiparasitic APIs, contributing to the advancement of healthcare and the well-being of individuals and their animal companions.
Eflornithine API manufacturers & distributors
Compare qualified Eflornithine API suppliers worldwide. We currently have 2 companies offering Eflornithine API, with manufacturing taking place in 2 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
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