Last reviewed · How we verify
Antizol (FOMEPIZOLE)
Antizol works by competitively inhibiting the enzyme alcohol dehydrogenase, which is responsible for converting toxic alcohols into their more toxic metabolites.
At a glance
| Generic name | FOMEPIZOLE |
|---|---|
| Sponsor | Par Pharm Inc |
| Drug class | Antidote [EPC] |
| Target | Alcohol dehydrogenase |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 1997 |
Mechanism of action
Mechanism of Action. Fomepizole is 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.Ethylene glycol, the main component of most antifreezes and coolants, is metabolized to glycoaldehyde, which undergoes subsequent sequential oxidations to yield glycolate, glyoxylate, and oxalate. Glycolate and oxalate are the metabolic byproducts primarily responsible for the metabolic acidosis and renal damage seen in ethylene glycol toxicosis. The lethal dose of ethylene glycol in humans is approximately 1.4 mL/kg.Methanol, the main component of windshield wiper fluid, is slowly metabolized via alcohol dehydrogenase to formaldehyde with subsequent oxidation via formaldehyde dehydrogenase to yield formic acid. Formic acid is primarily responsible for the metabolic acidosis and visual disturbances (e.
Approved indications
- Accidental poisoning by methyl alcohol
- Ethylene Glycol Toxicity
Common side effects
- Headache
- Nausea
- Dizziness
- Increased drowsiness
- Bad taste metallic taste
- Abdominal pain
- Fever
- Multiorgan system failure
- Pain during fomepizole injection
- Inflammation at injection site
- Lumbalgia/backache
- Hangover
Key clinical trials
- The Use of Isocapnic Hyperventilation (iHV) for Treatment of Methanol Poisoned Patients (PHASE1)
- Evaluation of the Efficacy of Fomepizole in the Treatment of Acetaminophen Overdose (PHASE2)
- Fomepizole Dosing During Continuous Renal Replacement Therapy (CRRT)
- Phase IIa Study of Fomepizole for Acetaldehyde Toxicity After Ethanol Exposure in Subjects With Altered Ethanol Metabolism (PHASE2)
- Specified Drug-use Survey of Fomepizole Intravenous Infusion (All-case Surveillance)
- Phase 1 Pilot Study of 4-MP to Treat Stargardt Macular Dystrophy (PHASE1)
- 4-methylpyrazole and Acetaminophen Metabolism (EARLY_PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Antizol CI brief — competitive landscape report
- Antizol updates RSS · CI watch RSS
- Par Pharm Inc portfolio CI