Rabeximod is an indolo[2,3-b]quinoxaline derivative patented by OxyPharma AB as anti-inflammatory agent useful for the treatment of autoimmune disease. Rabeximod impaired monocyte differentiation into monocyte-derived dendritic cells and pro-inflammatory allostimulated macrophages. Monocyte-derived dendritic cells that were treated with Rabeximod resulted in a significant decrease in their ability to pinocytose antigens, while no effect was exerted by the drug on the ability of allostimulated macrophages and anti-inflammatory macrophages to phagocytose. Rabeximod reduces the severity of arthritis in rodent models of rheumatoid arthritis and multiple sclerosis. Rabeximod efficiently prevented arthritis during the time window when TLR2 or TLR4 ligands activate inflammatory macrophages.

Eucatropine is known as an anticholinergic agent, which acts as antagonist of muscarinic cholinergic receptors.

Moxilubant is an orally active leukotriene B4 antagonist patented by Ciba-Geigy A.-G. and studied for psoriasis, rheumatoid arthritis, and chronic obstructive pulmonary disease treatment. Moxilubant inhibits LTB4 signaling with a potency of 2–4 nM. In a phase 1 study in 10 healthy volunteers, Moxilubant was administered orally once or twice daily for 7 days at doses ranging from 100 to 500 mg. At dose levels of 150 mg and above, LTB4 pathway inhibition reached at least 75%. At doses of 300 mg and above, pathway inhibition reached 100%. A Phase 2 study was conducted in 24 patients with COPD treated with 240 mg/day Moxilubant for 4 weeks. In this study, there were no changes in sputum cell counts or biomarkers or in spirometry measures, even though plasma levels of Moxilubant were sufficient to significantly reduce pathway signaling.

Pentapiperide is an anticholinergic drug with antisecretory and antimotility activity on the upper gastrointestinal tract, which was used as adjunctive therapy for relieving the symptoms of peptic ulcer. pentapiperide methylsulfate) has approximately the same in vitro antispasmodic activity as atropine. In vivo, however, the quaternary ammonium compounds such as pentapiperide methylsulfate are less readily absorbed from the gastrointestinal tract than are the tertiary amines such as atropine. Pentapiperide methylsulfate is contraindicated in patients with glaucoma or a predisposition to glaucoma, in patients with pyloric obstruction or stenosis, gastric retention, known or suspected obstructive disease of the gastrointestinal tract, and urinary bladder neck obstruction. It is also contraindicated in prostatic hypertrophy, stenosing peptic ulcer, megaesophagus, organic cardiospasm, and in patients with a hypersensitivity to the drug. Xerostomia was the most frequently encountered complaint. In decreasing order of frequency, visual blurring, difficult micturition, constipation, and nausea were reported.

Vinfosiltine (also known as S 12363) was developed as a vinca alkaloid derivative. It is known that vinca alkaloids are widely used in the medical treatment of breast cancer. Vinfosiltine participated in the phase II clinical trial to treat the patients with advanced breast cancer. The results have shown that the drug didn’t have significant single-agent activity. As a result, the development of vinfosiltine was discontinued.

Leukotriene B4 is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Leukotriene B4 induces recruitment and activation of neutrophils, monocytes and eosinophils. It also stimulates the production of a number of proinflammatory cytokines and mediators indicating an ability to augment and prolong tissue inflammation. Elevated levels of leukotriene B4 have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Leukotriene B4 has a central role in metabolic dysfunctions. By increasing MyD88 expression, leukotriene B4 enhances macrophage response to TLR/IL1 receptor agonists potentiating the sterile inflammation, a central event in metabolic disease progression. Thus, leukotriene B4 is a potential therapeutic target for the treatment of metabolic disorders. Leukotriene B4 could serve as a biomarker for evaluating bestatin efficacy in colorectal cancer.