Skip to main content

Table 1 In vitro selectivity of LCI699 in human, rat and monkey enzymes

From: Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects

Assay Aldosterone synthase (CYP11B2) IC50, nmol/L 11β-hydroxylase (CYP11B1) IC50, nmol/L Selectivity ratioa(CYP11B2:CYP11B1)
Recombinant human enzyme 0.7 ± 0.01 (6) 2.5 ± 0.1 (4) 3.6
Recombinant rat enzyme 160 ± 9 (3) 410 ± 5 (3) 2.6
Rat adrenal homogenate 802 (2) 3045 (2) 3.8
Monkey adrenal homogenate 12 ± 1 (6) 62 ± 5 (6) 5.2
  1. Table shows selectivity ratios for LCI699 for inhibition of aldosterone synthase (CYP11B2) over 11β-hydroxylase (CYP11B1). All values are mean ± SEM (n) except for rat adrenal homogenate where only mean values from two experiments are presented.
  2. aSelectivity ratio is defined as the ratio of IC50 values obtained in the CYP11B2 and CYP11B1 assays.
  3. CYP, cytochrome P450; IC50, half maximal inhibitory concentration.