giripladib

Giripladib is a small molecule inhibitor of cytosolic phospholipase A2 alpha (cPLA2α). It was initially developed by Pfizer and has been investigated primarily for the treatment of osteoarthritis and rheumatoid arthritis. The drug acts by inhibiting cPLA2α, an enzyme involved in the release of arachidonic acid from membrane phospholipids—a key step in the production of pro-inflammatory eicosanoids. In preclinical models, inhibition of cPLA2α by giripladib has been shown to reduce tumor progression and radioresistance as well as attenuate radiation-induced increases in phosphorylated ERK and Akt signaling pathways. Clinical development included phase I studies for gastrointestinal safety and pharmacokinetics; however, a phase II study was terminated and further development appears to have been discontinued[1][2][4].

Other names

giripladib