Bropirimine

Bropirimine is an immunomodulator with diverse biological activities.^1,2,3,4 It is a toll-like receptor 7 (TLR7) agonist that inhibits RANKL-induced osteoclast differentiation of murine bone marrow-derived macrophages (BMDMs) in a concentration-dependent manner, an effect that is reversed by an anti-IFN-β antibody.¹ Dietary administration of bropirimine (200 mg/kg twice per week) prevents development of transitional cell carcinomas (TCCs) in a mouse model of carcinogen-induced bladder carcinoma.² Bropirimine (100 mg/kg) reduces pulmonary collagen accumulation and bronchoalveolar lavage fluid (BALF) monocyte and eosinophil infiltration in a hamster model of bleomycin-induced lung fibrosis.³ It also delays disease onset and progression and increases plasma IFN levels in a mouse model of experimental autoimmune encephalomyelitis (EAE).⁴

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1. Suzuki, H., Mochizuki, A., Yoshimura, K., et al. Bropirimine inhibits osteoclast differentiation through production of interferon-β. Biochem. Biophys. Res. Commun. 467(1), 146-151 (2015).

2. Borden, E.C., Sidky, Y.A., Ertürk, E., et al. Protection from carcinogen-induced murine bladder carcinoma by interferons and an oral interferon-inducing pyrimidinone, bropirimine. Cancer Res. 50(4), 1071-1074 (1990).

3. Zia, S., Hyde, D.M., and Giri, S.N. Effects of an interferon inducer bropirimine on bleomycin-induced lung fibrosis in hamsters. Pharmacol. Toxicol. 71(1), 11-18 (1992).

4. Vroegop, S.M., Chapman, D.L., Galinet, L.A., et al. Pharmacology of the biological response modifier bropirimine (PNU-54461) on experimental autoimmune encephalomyelitis (EAE) in mice. Int. J. Immunopharmacol. 21(6), 391-409 (1999).