Pentoxifylline (BL-191)

Pentoxifylline is a methylxanthine derivative. It has been shown to have anti-inflammatory activity, inhibiting LPS-induced TNF-α production in isolated peripheral blood mononuclear cells (IC₅₀ = 85 ?M) and suppressing LPS-induced leukopenia in mice.¹ Pentoxifylline weakly inhibits the generation of phosphatidic acid (IC₅₀ = 500 ?M) from LPS-activated lysophosphatidic acyl transferase (LPAAT), and weakly antagonizes A₁ and A₂ adenosine receptors.^2,3 It also inhibits human acidic mammalian chitinase, human chitotriosidase, and chitinase B1 from Aspergillus fumigatus (IC₅₀s = 49, 98, and 126 ?M, respectively).⁴

1.Cottam, H.B., Shih, H., Tehrani, L.R., et al.Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor αJ. Med. Chem.392-9(1996) 2.Rice, G.C., Brown, P.A., Nelson, R.J., et al.Protection from endotoxic shock in mice by pharmacologic inhibition of phosphatidic acidProc. Natl. Acad. Sci. USA91(9)3857-3861(1994) 3.Schwabe, U., Ukena, D., and Lohse, M.J.Xanthine derivatives as antagonists at A1 and A2 adenosine receptorsNaunyn Schmiedebergs Arch. Pharmacol.330(3)212-221(1985) 4.Rao, F.V., Andersen, O.A., Vora, K.A., et al.Methylxanthine drugs are chitinase inhibitors: Investigation of inhibition and binding modesChem. Biol.12(9)973-980(2005)