Bromadiolone

Bromadiolone is a second generation anticoagulant rodenticide and 4-hydroxycoumarin derivative.1,2 It is an inhibitor of vitamin K epoxide reductase (VKOR) that inhibits blood clotting. It inhibits human VKOR complex subunit 1 (VKORC1) with an IC50 value of 1.6 nM in a cell-based assay.3 Bromadiolone is toxic to rodents, including mice (LD50 = 1.75 mg/kg) and rats (LD50s = 1.05 and 1.83 mg/kg for males and females, respectively).4,5 It does not significantly affect breeding performance in mice when administered at a dose of up to 70% of the LD50 value.6 Resistance to bromadiolone is conferred by mutations to the VKOR gene, Vkorc1.7 Formulations containing bromadiolone have been used in the control of rodent pest populations.

|1. Watt, B.E., Proudfoot, A.T., Bradberry, S.M., et al. Anticoagulant rodenticides. Toxicol. Rev. 24(4), 259-269 (2005).|2. Misenheimer, T.M., Lund, M., Baker, A.E.M., et al. Biochemical basis of warfarin and bromadiolone resistance in the house mouse, Mus musculus domesticus. Biochem. Pharmacol. 47(4), 673-678 (1994).|3. Czogalla, K.J., Liphardt, K., H•ning, K., et al. VKORC1 and VKORC1L1 have distinctly different oral anticoagulant dose-response characteristics and binding sites. Blood Adv. 2(6), 691-702 (2018).|4. Vandenbroucke, V., Bousquet-Melou, A., De Backer, P., et al. Pharmacokinetics of eight anticoagulant rodenticides in mice after single oral administration. J. Vet. Pharmacol. Ther. 31(5), 437-445 (2008).|5. Garg, N., and Singla, N. Toxicity of second generation anticoagulant bromadiolone against Rattus Rattus: individual and sex specific variations. Cibtech J. Zoo. 3(2), 43-48 (2014).|6. Twigg, L.E., and Kay, B.J. The effect of sub-lethal doses of bromadiolone on the breeding performance of house mice (Mus domesticus). Comp. Biochem. Physiol. 110(1), 77-82 (1995).|7. Pelz, H.-J., Rost, S., HÜnerberg, M., et al. The genetic basis of resistance to anticoagulants in rodents. Genetics 170(4), 1839-1847 (2005).