Drug intelligence / Profile preview

licofelone

Development stage
Phase 4
Lead developer
Merckle
Modality
Small Molecules
Administration
Oral
01

Overview

Licofelone is a dual-acting anti-inflammatory and analgesic small molecule that simultaneously inhibits cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), the key enzymes involved in the synthesis of pro-inflammatory prostaglandins and leukotrienes. Developed by Merckle GmbH with partners Alfa Wassermann and Lacer, it represents the first member of a new class of COX/LO inhibitors. Licofelone was primarily developed for the management of osteoarthritis, aiming to provide effective pain relief while reducing gastrointestinal toxicity commonly associated with traditional NSAIDs by also blocking leukotriene production. In addition to its anti-inflammatory effects, licofelone has demonstrated neuroprotective properties in preclinical studies related to central nervous system inflammation. Although phase III trials for osteoarthritis were completed, regulatory approval was not pursued due to mixed results[1][3][4][7].

02

Targets

CNR1 (Cannabinoid receptor 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PTGES (Microsomal prostaglandin E synthase-1)ALOX12 (Arachidonate 12-lipoxygenase, 12S type)PGHS-1 (Prostaglandin G/H Synthase 1)

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