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amtolmetin guacil
- Development stage
- Unknown
- Lead developer
- Alfasigma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Amtolmetin guacil is a non-acidic prodrug of tolmetin, classified as a nonsteroidal anti-inflammatory drug (NSAID). It exhibits anti-inflammatory, analgesic, and antipyretic properties similar to tolmetin but with additional gastroprotective effects. The drug is absorbed orally and hydrolyzed to active metabolites including tolmetin. Its mechanism of action involves inhibition of cyclooxygenase (COX), leading to reduced prostaglandin synthesis, stimulation of capsaicin receptor (TRPV1) in the gastrointestinal wall due to its vanillic moiety, and release of nitric oxide (NO), which contributes to its gastroprotective profile. Amtolmetin guacil has been shown in studies to have improved gastric tolerability compared with traditional NSAIDs[1][3][4][6][8].
- Brand names
- EufansArtromed
- Other names
- amtolmetin guacyltolmetin glycine amideN-((1-methyl-5-p-toluoylpyrrol-2-yl)acetyl)glycine o-methoxyphenyl ester(2-methoxyphenyl) 2-(2-(1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2 yl)acetamido)acetate
02
Targets
TRPV1 (Transient receptor potential cation channel subfamily V member 1)COX
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