licofelone (Pending for approval)

Action and Spectrum

Actions and spectrum: 

It works by inhibiting COX and 5-LOX enzymes, thereby preventing inflammation. The enzyme        5-lipoxygenase is associated with the synthesis of gastronomic and pro-inflammatory leukotrienes 

Drug Interaction

Adverse Reaction

Frequency not defined 

Gastrointestinal bleed 

Cardiovascular complications 

bronchospasm 

Black Box Warning

Black Box Warning  

Not available 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hypersensitivity 

Renal impairment 

Pregnancy / Lactation

Pregnancy consideration:  

USFDA pregnancy category: Safety and efficacy data is not available 

Lactation:  

Data about the excretion of licofelone into breast milk is not known. 

Pregnancy category:  

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There was a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category  

Pharmacology

Pharmacology: 

Licofelone is a dual COX/5-LOX inhibitor 

Pharmacodynamics: 

It is a selective, non-steroidal anti-inflammatory drug used in the treatment of osteoarthritis by reducing the levels of leukotrienes and prostaglandins. 

Licofelone was found to have potential disease-modifying effects in osteoarthritis (OA) by reducing the expression of matrix metalloproteinases, cathepsin K, and IL-1beta in preclinical studies and preventing chondrocyte death. 

Pharmacokinetics: 

Metabolism 

Human metabolites of licofelone include licofelone M2, licofelone M4 and (2S,3S,4S,5R)-6-[2-[2-(4-chlorophenyl)-6,6-dimethyl-1-phenyl-5,7-dihydropyrrolizin-3-yl]acetyl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid 

Adminstartion

Administration: 

The drug is pending for approval 

Patient Information Leaflet

Patient information leaflet 

Generic Name: licofelone  

Why do we use licofelone? 

Licofelone is used in the management of pain and inflammation in patients suffering from osteoarthritis. Currently, the drug has completed phase III clinical trials and is under approval from the regulatory authority.