CYP11B2-IN-1

CYP11B2-IN-1 (Compound 32) also inhibits CYP19 with an IC₅₀ of 1021 nM ^{[1] .}

In a rhesus pharmacodynamic model, CYP11B2-IN-1 (Compound 32) produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels^[1].
CYP11B2-IN-1also displays a good rhesus pharmacokinetics profile, with low plasma clearance and acceptable oral exposure.When dosed i.v. at 0.01 and 0.3 mg/kg, CYP11B2-IN-1 produces reductions in aldosterone AUC of 62% and 95%, respectively, compared to baseline^[1].

References:
[1]. Hoyt SB, et al. Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.ACS Med Chem Lett. 2015 Apr 7;6(5):573-8.