TABLE 1

Drugs tested for in vitro binding to veverimer

Test Drug (Conc.; µg/mL)ClassBCS ClassMMpKaCharge at pH
1.24.56.8
Positively charged test drugs
 Amlodipine (5)Calcium channel blockerI408.99.21B+++
 Metformin (500)BiguanideIII129.22.94B, 13.7B+++
 Metoprolol (25)β blockerI267.49.61B+++
 Thiamine (1)Vitamin B1III265.44.8B+++
 Trimethoprim (100)AntibioticII290.37.14B+++
Neutral/zwitterionic test drugs
 Allopurinol (100)Xanthine oxidase inhibitorI136.19.31ANNN
 Lisinopril (5)ACE inhibitorIII405.51.63A, 3.13A, 7.13B, 10.75B+ZZ
 Riboflavin (1.2)Vitamin B2I376.49.69ANNN
 Spironolactone (25)Aldosterone antagonistsII416.6n/aNNN
Negatively charged test drugs
 Aspirin (81)Platelet aggregation inhibitorI180.23.50AN
 Ethacrynic acid (25)DiureticNA303.13.50AN
 Furosemide (20)DiureticIV330.73.62A, 10.16AN
 Gliclazide (40)SulfonylureaII323.45.80ANNN/–
 Rosuvastatin (5)HMG COA reductase inhibitorIII481.54.6ANN/–
 Valsartan (40)Angiotensin II antagonistIII435.53.9A 4.7AN
 Warfarin (1)AntithromboticII308.34.94ANN/–
  • –, negative; +, positive; ACE, angiotensin-converting enzyme inhibitor; BCS, Biopharmaceutics Classification System; HMG COA, hydroxymethylglutaryl-coenzyme A; N, neutral; NA, not applicable; Z, zwitterionic.