Topical non-steroidal anti-inflammatory drugs (
NSAIDs) patches are indispensable for the treatment of
musculoskeletal diseases, while they are considered less effective than oral
NSAIDs. LOQOA® tape is a tape-type patch containing esflurbiprofen (
SFP) as a major active ingredient with potent
cyclooxygenase inhibition and sufficient skin permeability.
SFP patch (SFPP) showed higher percutaneous absorption rate, rapid
pain relief, and potent anti-inflammatory efficacy comparing with existing
NSAIDs patches in rat. SFPP showed dramatically higher synovial fluid and tissue concentration on
SFP than that of
flurbiprofen (FP) patch after single application to
knee osteoarthritis (OA) patients. On the other hand, clinical dosage of SFPP was determined as not more than two patches a day from the estimation of systemic exposure to
SFP of SFPP and oral FP. SFPP showed statistically significant differences in
pain relief and all the other efficacy end points compared to inactive placebo or FP patch in knee OA patients. Efficacy on OA other than knee joint was also observed. In long-term study of SFPP, using up to two patches a day, a total of 201 patients was included and 161 patients achieved 52-week application. Among
drug-related side effects, skin reaction at the application sites was observed in 46.8% and discontinued in 4.3%. Although gastro-intestinal reaction and abnormal changes in laboratory tests related to kidney function were observed as systemic
drug-related side effects, most of them were mild in severity. SFPP, the new generation
NSAIDs patch, would be one of effective options for the treatment of symptomatic OA patients.