Table 1

Summary of the most advanced SGLT2 inhibitor compounds (refs. 2831)

CompoundSGLT2 IC50 (nmol/L)SGLT1 IC50 (nmol/L)SGLT2/SGLT1 selectivityHighest approved dose (mg)aStatus
Canagliflozin4.2663160300Approved in U.S., EU, Japan, other countries
Dapagliflozin1.21,4001,20010Approved in U.S., EU, Japan, other countries
Empagliflozin3.18,3002,70025Approved in U.S., EU
Ipragliflozin5.33,00057050Approved in Japan
Luseogliflozin2.33,9901,7705Approved in Japan
Tofogliflozin6.412,0001,87520Approved in Japan
Ertugliflozin0.91,9602,20025Phase 3
LX-4211 (sotagliflozin)1.83620400Completed phase 2
  • aHighest approved dose or the highest dose still in development for compounds that have not yet been approved.