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Table 2—

Characteristics of DPP-IV inhibitors and GLP-1R agonists

DPP-IV inhibitorsGLP-1R agonists
Orally available Injectable 
Multiple targets Single known GPCR target 
GLP-1 PK favorable Higher levels of GLP-1 achievable, but narrow PK profile 
Short- versus long-acting Longer acting—days to weeks 
Less potent agents More potent glucose lowering 
Drug overdose nontoxic Drug overdose problematic 
No central nervous system side effects Nausea and vomiting 
Less defined side effect profile Well-described and tolerable side effect profile 
DPP-IV inhibitorsGLP-1R agonists
Orally available Injectable 
Multiple targets Single known GPCR target 
GLP-1 PK favorable Higher levels of GLP-1 achievable, but narrow PK profile 
Short- versus long-acting Longer acting—days to weeks 
Less potent agents More potent glucose lowering 
Drug overdose nontoxic Drug overdose problematic 
No central nervous system side effects Nausea and vomiting 
Less defined side effect profile Well-described and tolerable side effect profile 

GPCR, G protein–coupled receptor; PK, pharmacokinetic.

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