Efonidipine (NZ-105)

Efonidipine is an inhibitor of L- and T-type voltage-gated calcium channels (Ca_vs).¹ It inhibits Ca_v1.2a (IC₅₀ = 1.8 nM for the hamster channel), an L-type Ca_v, and Ca_v3.2 (IC₅₀ = 350 nM for the human channel), a T-type Ca_v. It also inhibits L- and T-type calcium channels and fetal bovine serum-induced hypertrophy in isolated mouse cardiomyocytes.² Efonidipine (200 mg/kg) increases survival in a mouse model of acute myocardial infarction induced by ligation of the left coronary artery.³ Efonidipine is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro; IC₅₀ = 38.5 nM).⁴

1.Lee, T.-S., Kaku, T., Takebayashi, S., et al.Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca2+ channels with distinct inhibitory mechanismsPharmacology78(1)11-20(2006) 2.Horiba, M., Muto, T., Ueda, N., et al.T-type Ca2+ channel blockers prevent cardiac cell hypertrophy through an inhibition of calcineurin-NFAT3 activation as well as L-type Ca2+ channel blockersLife Sci.82(11-12)554-560(2008) 3.Kinoshita, H., Kuwahara, K., Takano, M., et al.T-type Ca2+ channel blockade prevents sudden death in mice with heart failureCirculation120(9)743-752(2009) 4.Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al.Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2ACS Med. Chem. Lett.11(12)2526-2533(2020)