Lasofoxifene is in late-stage development for the prevention and treatment of osteoporosis. Digoxin is commonly prescribed for arrhythmias and congestive heart failure, has a narrow therapeutic index, and may be coadministered with lasofoxifene. This study was conducted to determine the effect of lasofoxifene (4-mg loading dose on day 11 followed by 0.5 mg/d on days 12-20) on the steady-state pharmacokinetics of digoxin (0.25 mg/d on days 1-20) in 12 healthy postmenopausal women. On days 10 and 20, blood and urine samples were collected for 24 hours to determine digoxin concentrations. The 90% confidence interval (CI) of least squares mean ratio for maximum concentration (C(max)) and area under the plasma concentration-time curve (AUC) was calculated. Lasofoxifene had no effect on digoxin plasma pharmacokinetics with a ratio (90% CI) of 95.4% (84.6%-107%) and 103% (97.7%-108%) for C(max) and AUC(0-24), respectively. The ratio of the percentage of dose eliminated unchanged in urine in 24 hours was 127% (116% to 142%). Coadministration of lasofoxifene had no effect on the steady state pharmacokinetics of digoxin.