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Prospects for anti-inflammatory therapy of osteoarthritis
Last reviewed: 04.07.2025
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A new direction in the symptomatic treatment of osteoarthritis and other diseases of the musculoskeletal system is the use of combined inhibitors of cyclooxygenase and lipoxygenase - COX and LOX. Experimental studies indicate that the alternative (lipoxygenase) pathway of arachidonic acid metabolism, which leads to the formation of leukotrienes (LT), causes a number of inflammatory effects in patients with joint diseases. Thus, LTB 4 is one of the most powerful factors of leukocyte chemotaxis, it also induces the production of cytokines by T-lymphocytes and immunoglobulins by B-lymphocytes. In addition, the so-called cysteinyl LTs (or peptide leukotrienes) - LTS 4, LT0 4 and LTE 4 cause a number of inflammatory effects, including edema, contraction of smooth muscles, which in the mucous membrane of the upper gastrointestinal tract can cause ischemia with subsequent formation of erosions and ulcers. Two other forms of LOX - 12-L OG and 15-LOG - catalyze the formation of lipoxins, which have an anti-inflammatory effect.
Inhibition of the cyclooxygenase pathway by non-selective or selective NSAIDs can cause a shift in the arachidonic acid cascade toward the lipoxygenase pathway with increased production of leukotrienes and lipoxins. Therefore, it would be advisable to block both pathways of arachidonate metabolism - cyclooxygenase and lipoxygenase - to achieve anti-inflammatory and analgesic effects. However, an important point is to maintain the production of anti-inflammatory lipoxins.
Licofelon is a new pharmacotherapeutic agent that blocks COX and 5-LOX. In vitro studies, licofelone inhibited COX (1C 50 ~0.16-0.21 uM) and 5-LOX (1C 50 ~0.18-0.23 uM).
The new technology, called "host-guest", imparts optimal pharmacokinetic properties to "classical" non-selective NSAIDs and improves their tolerability. PBC is a new pharmacotherapeutic agent in which the piroxicam molecule (the "guest" molecule) is embedded in β-cyclodextrin (the "host" molecule). This combination provides:
- high solubility,
- rapid absorption,
- minimal contact with the mucous membrane of the digestive tract,
- almost 100% bioavailability,
- rapid onset of action,
- pronounced analgesic effect when taken once a day.
In a pilot comparative controlled study of the use of RBC (20 mg/day) and etodolac (400 mg/day) in 30 patients with pain in the lower spine, the former had a more pronounced analgesic effect. Another small controlled study compared the effectiveness of RBC at a dose of 20 mg/day in 60 patients with diseases of the musculoskeletal system with intramuscular injections of diclofenac (75 mg) and ketoprofen (100 mg). All three drugs had a rapid and pronounced analgesic effect. Of course, it is impossible to judge the effectiveness and tolerability of RBC based on these studies; the results obtained require confirmation in large multicenter studies.
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