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Sitagliptin

CHEMBL1422 Phase 4 Aprovado Small molecule
Half-Life
12.4 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
407.3 g/mol
LogP
0.7
Phase
4

This once-daily pill helps control blood sugar in type 2 diabetes by preventing the breakdown of incretin hormones that naturally stimulate insulin release after eating. It works gently without causing significant low blood sugar on its own and is often combined with metformin or other diabetes medications.

Peso Molecular

407,3140 g/mol

LogP

0,70

TPSA

77,00 Ų

Regra dos 5 de Lipinski

Aprovado

Áreas Terapêuticas

Benign Prostatic Hyperplasia Cardiovascular Disease Rheumatoid Arthritis Osteoporosis Psoriasis Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Stroke Hyperlipidemia Obesity Lymphoma Type 2 Diabetes Hypertension Hepatitis C Heart Failure Colorectal Cancer Leukemia

Classes de Medicamentos

A — A - Alimentary Tract and Metabolism

Mecanismo de Ação

DPP-4 inhibitor increasing incretin levels.

Pharmacokinetics (PK)

Half-Life 12.4 hours

Pharmacodynamics (PD)

Mecanismo

DPP-4 inhibitor increasing incretin levels.

Estrutura 2D

SVG PNG

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SMILES

                    
N[C@@H](CC(=O)N1CCn2c(nnc2C(F)(F)F)C1)Cc1cc(F)c(F)cc1F

                

                

                
                

                    
InChI

                    
InChI=1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C16H15F6N5O

                    

                    
                    

                        
HBD / HBA

                        
1 / 10

                    

                    
                    

                        
Ligações Rotacionáveis

                        
4

                    

                    
                    
                    

                        
Átomos Pesados

                        
28

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            PPARG (Peroxisome Proliferator-Activated Receptor Gamma)
                            Inhibitor
                        

                        
                        Primary Target
                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Moderate


                            
                                Sitagliptin + Tirzepatide
                            
                        

                        
                        
Combining tirzepatide (dual GIP/GLP-1 agonist) with sitagliptin (DPP-4 inhibitor) produces overlapping incretin-based mechanisms with additive hypoglycaemia risk and no meaningful additional benefit over either agent alone.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Sitagliptin + Digoxin
                            
                        

                        
                        
Sitagliptin modestly increases digoxin exposure through inhibition of P-glycoprotein-mediated renal tubular secretion, though the effect is unlikely to be clinically significant at therapeutic digoxin doses.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Perguntas frequentes

                

                    
                    

                        
                        

                            
This once-daily pill helps control blood sugar in type 2 diabetes by preventing the breakdown of incretin hormones that naturally stimulate insulin release after eating. It works gently without causing significant low blood sugar on its own and is often combined with metformin or other diabetes medications.

                        

                    

                    

                    

                    
                    

                        
                        

                            
DPP-4 inhibitor increasing incretin levels.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Sitagliptin: Half-life: 12.4 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Sitagliptin is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Metformin
                            Small molecule
                        
                        
                        
                            Omeprazole
                            Small molecule
                        
                        
                        
                            Pantoprazole
                            Small molecule
                        
                        
                        
                            Lansoprazole
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL1422.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 4369359.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
Aviso Médico

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.