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Losartan

CHEMBL191 Phase 4 Đã phê duyệt Small molecule
Half-Life
2 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
422.9 g/mol
LogP
4.3
Phase
4

Losartan lowers blood pressure by selectively blocking the AT1 receptor, the site through which angiotensin II constricts blood vessels. Preventing that hormone from binding allows vessels to relax, and as an angiotensin II receptor blocker it achieves this without the bradykinin-related cough associated with ACE inhibitors. It is used for high blood pressure, the kidney disease of diabetes, and heart failure. A small molecule (C22H23ClN6O) with a parent half-life of about 2 hours, its effect is carried further by an active metabolite that sustains receptor blockade through the day. By acting at the receptor rather than on the enzyme that makes angiotensin II, it blocks the hormone's effect at the final step of the pathway. Losartan is an approved cardiovascular medicine widely used for blood-pressure and kidney protection.

An angiotensin II receptor blocker (ARB) used to treat high blood pressure, diabetic kidney disease, and heart failure, and studied for potential benefits in Alzheimer's disease and atrial fibrillation. It selectively blocks the AT1 receptor to relax blood vessels.

Khối lượng phân tử

422,9200 g/mol

LogP

4,30

TPSA

92,50 Ų

Lipinski RO5

Đạt

Lĩnh vực điều trị

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Cardiovascular Disease Non-Small Cell Lung Cancer Rheumatoid Arthritis Chronic Obstructive Pulmonary Disease Alzheimer's Disease Schizophrenia Bipolar Disorder Melanoma Systemic Lupus Erythematosus Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Stroke Hyperlipidemia Obesity Lymphoma Type 2 Diabetes Hypertension Major Depressive Disorder Breast Cancer HIV/AIDS Hepatitis C Heart Failure Atrial Fibrillation Prostate Cancer Colorectal Cancer Leukemia

Phân loại thuốc

C — C - Cardiovascular System

Cơ chế tác dụng

Angiotensin II receptor type 1 antagonist.

Pharmacokinetics (PK)

Half-Life 2 hours

Pharmacodynamics (PD)

Cơ chế

Angiotensin II receptor type 1 antagonist.

Cấu trúc 2D

SVG PNG

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SMILES

                    
CCCCc1nc(Cl)c(CO)n1Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C22H23ClN6O/c1-2-3-8-20-24-21(23)19(14-30)29(20)13-15-9-11-16(12-10-15)17-6-4-5-7-18(17)22-25-27-28-26-22/h4-7,9-12,30H,2-3,8,13-14H2,1H3,(H,25,26,27,28)

                

                

                

                    
                    

                        
Molecular Formula

                        
C22H23ClN6O

                    

                    
                    

                        
HBD / HBA

                        
2 / 5

                    

                    
                    

                        
Liên kết có thể quay

                        
8

                    

                    
                    
                    

                        
Nguyên tử nặng

                        
30

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            AGTR1 (Angiotensin II Type 1 Receptor)
                            Antagonist
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            CYP3A4 (Cytochrome P450 3A4)
                            Substrate
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Moderate


                            
                                Losartan + Spironolactone
                            
                        

                        
                        
ARBs combined with spironolactone substantially increase hyperkalemia risk through additive suppression of renal potassium excretion.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Losartan + Trimethoprim
                            
                        

                        
                        
Trimethoprim blocks renal tubular secretion of potassium, acting like a potassium-sparing diuretic; combined with losartan's reduction of aldosterone-mediated potassium excretion, the risk of hyperkalaemia is substantially increased.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Losartan + Lisinopril
                            
                        

                        
                        
Dual RAAS blockade with ACE inhibitors and ARBs provides no additional cardiovascular benefit over either agent alone and significantly increases the risk of hypotension, hyperkalemia, and acute kidney injury.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Losartan + Hydrochlorothiazide
                            
                        

                        
                        
Losartan + hydrochlorothiazide is a guideline-recommended combination for hypertension; the primary interactions are additive hypotension and variable electrolyte effects.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Losartan + Empagliflozin
                            
                        

                        
                        
Empagliflozin and losartan can both reduce blood pressure and lower serum potassium/sodium; combined use may increase the risk of dehydration, hypotension, and electrolyte imbalance.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Losartan + Ibuprofen
                            
                        

                        
                        
Ibuprofen attenuates the antihypertensive effect of ARBs and increases the risk of renal impairment and hyperkalemia.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Câu hỏi thường gặp

                

                    
                    

                        
                        

                            
An angiotensin II receptor blocker (ARB) used to treat high blood pressure, diabetic kidney disease, and heart failure, and studied for potential benefits in Alzheimer's disease and atrial fibrillation. It selectively blocks the AT1 receptor to relax blood vessels.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Angiotensin II receptor type 1 antagonist.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Losartan: Half-life: 2 hours.

                        

                    

                    

                    

                        
                        

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

                        

                    

                

            

            

            
            
            

                
                
                    ADME Journey →
                
                
                
            

            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Atorvastatin
                            Small molecule
                        
                        
                        
                            Amlodipine
                            Small molecule
                        
                        
                        
                            Lisinopril
                            Small molecule
                        
                        
                        
                            Metoprolol
                            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

    
    
        
        
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                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL191.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 3961.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
Tuyên bố miễn trách y tế

    

        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.