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Fomepizole | CAS No: 7554-65-6 | GMP-certified suppliers
A medication that supports treatment of confirmed or suspected methanol and ethylene glycol poisoning, helping reduce severe toxicologic complications in emergency care settings.
Therapeutic categories
Primary indications
- Antizol is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning, or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis
Product Snapshot
- Fomepizole is supplied as an intravenous injectable formulation for parenteral administration
- It is used as an antidotal agent for ethylene glycol and methanol toxicity in industrial and emergency settings
- It is approved in the US and Canada, including veterinary approval where applicable
Clinical Overview
The pharmacological action of fomepizole is based on competitive inhibition of alcohol dehydrogenase. By occupying the enzyme’s active site, it blocks conversion of ethylene glycol to glycoaldehyde and subsequently to glycolate, glyoxylate, and oxalate, metabolites implicated in acidosis and crystal-mediated renal damage. In methanol poisoning, the same enzyme blockade prevents formation of formaldehyde and formic acid, the latter being the principal driver of metabolic acidosis and optic nerve toxicity. Hemodialysis may be co-administered to enhance clearance of parent alcohols and correct severe acidosis.
Fomepizole is administered intravenously. It distributes primarily in total body water and undergoes hepatic metabolism, with 4-carboxypyrazole identified as the major metabolite. Elimination is mainly renal, involving both unchanged drug and metabolites. The compound induces CYP2E1, which can increase its own metabolic clearance during repeated dosing. Fomepizole is also listed as a substrate and inhibitor of several cytochrome P450 pathways, though these interactions are generally less clinically significant in the acute toxicology setting.
Safety considerations include monitoring for infusion-site reactions, headache, nausea, and potential increases in liver enzymes. Toxicity is mainly associated with overdose or prolonged exposure but is uncommon at therapeutic doses. Dose adjustments may be required during hemodialysis due to extracorporeal clearance.
For API procurement, sourcing should focus on verified identity, control of pyrazole-related impurities, and adherence to pharmacopeial or regional quality standards. Reliable documentation of impurity profiles and stability data is essential for formulation and regulatory use.
Identification & chemistry
| Generic name | Fomepizole |
|---|---|
| Molecule type | Small molecule |
| CAS | 7554-65-6 |
| UNII | 83LCM6L2BY |
| DrugBank ID | DB01213 |
Pharmacology
| Summary | Fomepizole is a competitive inhibitor of alcohol dehydrogenase, blocking the enzyme’s conversion of ethylene glycol and methanol into their toxic downstream metabolites. By preventing formation of glycolate, oxalate, and formic acid, it reduces the metabolic pathways responsible for acidosis, renal injury, and visual toxicity. Its activity primarily involves alcohol dehydrogenase isoforms ADH1A, ADH1B, ADH1C, and, to a lesser degree, catalase. |
|---|---|
| Mechanism of action | Antizol (fomepizole) is a competitive inhibitor of alcohol dehydrogenase. Alcohol dehydrogenase catalyzes the oxidation of ethanol to acetaldehyde. Alcohol dehydrogenase also catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. |
| Pharmacodynamics | Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Ethylene glycol is first metabolized to glycoaldehyde which then undergoes further oxidation to glycolate, glyoxylate, and oxalate. Glycolate and oxalate are primarily responsible for metabolic acidosis and renal damage seen in ethylene glycol toxicity. {01}{03} Methanol is first metabolized to formaldehyde and then undergoes subsequent oxidation via formaldehyde dehydrogenase to become formic acid. It is formic acid that is primarily responsible for the metabolic acidosis and visual disturbances that are associated with methanol poisoning. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alcohol dehydrogenase 1A | Humans | inhibitor |
| Alcohol dehydrogenase 1B | Humans | inhibitor |
| Alcohol dehydrogenase 1C | Humans | inhibitor |
ADME / PK
| Absorption | Rapid and complete |
|---|---|
| Half-life | The plasma half-life of Antizol varies with dose, even in patients with normal renal function, and has not been calculated. |
| Metabolism | Primarily hepatic. the primary metabolite is 4-carboxypyrazole (approximately 80 to 85% of an administered dose). Minor metabolites include 4-hydroxymethylpyrazole and the N -glucuronide conjugates of 4-carboxypyrazole and 4-hydroxymethylpyrazole. |
| Route of elimination | In healthy volunteers, only 1-3.5% of the administered dose of Antizol® (7-20 mg/kg oral and IV) was excreted unchanged in the urine, indicating that metabolism is the major route of elimination. In humans, the primary metabolite of Antizol® is 4-carboxypyrazole (approximately 80-85% of administered dose), which is excreted in the urine. The metabolites of Antizol® are excreted renally. |
| Volume of distribution | * 0.6 to 1.02 L/kg |
Formulation & handling
- High aqueous solubility and liquid state support straightforward preparation of IV solutions, typically requiring minimal solubilization aids.
- Used exclusively as an intravenous small‑molecule antidote, with formulation emphasis on maintaining purity and controlling oxidative degradation in solution.
- Handling of concentrated solutions may require dilution and pH control to ensure chemical stability during storage and administration.
Regulatory status
| Lifecycle | The API is marketed in the US and Canada and remains under U.S. patent protection until mid‑2027. With expiry approaching, the product is nearing a transition toward a more mature, potentially competitive market phase. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Fomepizole is supplied by multiple packagers, with a single established originator brand (Antizol) that has been distributed primarily in the US and Canada. Branded products appear limited to North American markets, while the presence of several packagers indicates a mature distribution base. The US patent expiring in 2027 suggests room for future generic expansion, though broad generic competition may not fully emerge until after expiry. |
|---|
Safety
| Toxicity | Headache, nausea, dizziness |
|---|
- Exposure to the compound has been associated with CNS effects such as headache and dizziness
- Appropriate controls to limit inhalation or dermal contact are recommended
- Nausea has been observed in toxicity profiles, indicating the need for adequate ventilation and mitigation of fugitive emissions during handling
Good Manufacturing Practices
Active pharmaceutical ingredients are made in GMP-certified manufacturing facilities. GMP stands for Good Manufacturing Practices and is the main standard in the pharmaceutical industry. cGMP or Current GMP means that the company complies with the most recent requirements/version of GMP. The WHO has its own guideline for GMP, the World Health Organization or WHO GMP. The authority that has audited the company can also be from a country like China (Chinese GMP) or from the EU (EU GMP), every authority has different GMP requirements.
Fomepizole is a type of Antidotes
Antidotes are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in counteracting the toxic effects of certain substances or drugs. These specialized substances are developed to treat and reverse the harmful effects caused by accidental or intentional poisonings, drug overdoses, or adverse reactions.
Antidotes work through various mechanisms to neutralize or counteract the toxic effects of specific substances. They may function by binding to the toxin directly, preventing it from interacting with its target receptors or enzymes. Alternatively, they may stimulate enzymatic pathways that metabolize and eliminate the toxic substance from the body more rapidly.
The development of antidotes involves rigorous research and testing to ensure their safety and efficacy. Clinical trials are conducted to evaluate their effectiveness in treating poisoning cases and to establish appropriate dosing regimens. Furthermore, antidotes are subject to stringent regulatory guidelines to ensure their quality, purity, and consistency.
Medical professionals, particularly toxicologists and emergency healthcare providers, rely on antidotes to manage and treat poisoning emergencies effectively. Antidotes are essential tools in the emergency department and poison control centers, where timely administration can be life-saving.
In summary, antidotes are specialized pharmaceutical APIs designed to counteract the toxic effects of specific substances. Their development, testing, and regulatory compliance are crucial to ensure their efficacy and safety. These critical medications are indispensable in the field of emergency medicine and play a pivotal role in saving lives affected by poisoning incidents.
Fomepizole (Antidotes), classified under Antidotes, Deterrents, and Toxicologic Agents
Antidotes, Deterrents, and Toxicologic Agents are an important category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that play a critical role in healthcare and toxicology. These substances are designed to counteract the effects of poisons, toxins, and overdoses, thereby saving lives and preventing severe health consequences.
Antidotes are substances that neutralize the toxic effects of certain drugs, chemicals, or poisons. They work by either directly binding to the toxic substance or by blocking its harmful actions on the body. Antidotes are administered in emergency situations to quickly reverse the effects of poisoning and restore normal physiological functions.
Deterrents, on the other hand, are pharmaceutical agents used to discourage or prevent harmful behaviors, such as substance abuse. They are designed to make the ingestion or misuse of certain substances unpleasant or less desirable. Deterrents can be formulated to cause unpleasant side effects, such as nausea or vomiting, when a particular substance is consumed in excessive amounts.
Toxicologic agents encompass a broad range of pharmaceutical APIs used in toxicology studies and research. These substances are employed to investigate the toxicity, metabolism, and mechanisms of action of various chemicals and compounds. Toxicologic agents are vital for understanding the potential hazards and risks associated with certain substances, ensuring the safety of drugs, and developing effective treatments for poisoning cases.
In conclusion, Antidotes, Deterrents, and Toxicologic Agents are essential categories of pharmaceutical APIs that address poisoning emergencies, deter harmful behaviors, and enable toxicological research. Their development and availability are crucial for safeguarding public health, enhancing patient care, and advancing our understanding of toxicology.
Fomepizole API manufacturers & distributors
Compare qualified Fomepizole API suppliers worldwide. We currently have 3 companies offering Fomepizole 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 |
|---|---|---|---|---|---|
| NAVINTA | Producer | United States | Unknown | CoA, USDMF | 15 products |
| Orgapharm | Producer | France | France | CoA, GMP | 9 products |
| Seratec | Producer | France | France | CoA, GMP, USDMF | 5 products |
When sending a request, specify which Fomepizole API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Fomepizole API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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