Aflapin®: A novel and selective 5-lipoxygenase inhibitor for arthritis management

Abstract

Osteoarthritis (OA) is the most common form of arthritis characterized by progressive destruction of joint cartilage tissue, pain and inflammation, stiffness, and impaired physical activity. It is the most prevalent and leading cause of pain and disability across the globe. During the pain and inflammatory process, 5-lipoxygenase (5-LOX) pathway is also involved, which generates leukotrienes (LTs), namely LTB4 and cysteinyl LTs. Osteoblasts also synthesize LTs, which stimulate and enhance the production of interleukin 1, tumor necrosis factor α, and various other cytokines that are potent inflammatory mediators. LT formation leads to cartilage degradation and compensates chondrocyte-mediated cartilage repair mechanism. Current therapies include nonsteroidal anti-inflammatory drugs, analgesics, and disease-modifying agents, but do not affect 5-LOX pathway. Boswellia serrata extract–derived boswellic acids are specific, non-redox inhibitors of 5-LOX, and 3-O-acetyl-11-keto-β-boswellic acid (AKBA) possesses the most potent 5-LOX inhibitory activity. B. serrata extracts have shown significant efficacy and safety in the treatment of various inflammatory disorders such as OA, rheumatoid arthritis, asthma, and inflammatory bowel diseases. Aflapin® is a novel synergistic composition containing B. serrata extract selectively enriched with 20% AKBA and B. serrata nonvolatile oil. Aflapin® is a patented, selective, and most potent 5-LOX inhibitor, which significantly reduces joint pain, inflammation, stiffness, and improves physical function compared to placebo and other B. serrata extract. Aflapin® also significantly reduces matrix metalloproteinase levels, enhances chondrocytes proliferation, and increases glycosaminoglycans levels, thereby providing cartilage protection in arthritis. Numerous in vitro studies, preclinical studies, and clinical studies suggest the potential of Aflapin® as a useful therapeutic intervention for the management of arthritis.