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Trilaciclib

CHEMBL3894860 Phase 4 Одобрено Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
446.5 g/mol
LogP
2.6
Phase
4

Trilaciclib is a first-in-class CDK4/6 inhibitor that transiently arrests hematopoietic stem and progenitor cells in G1 phase before chemotherapy administration, thereby protecting bone marrow from chemotherapy-induced damage. It is used to decrease the incidence of chemotherapy-induced myelosuppression in adults receiving certain chemotherapy regimens for small cell lung cancer. Its myeloprotective mechanism distinguishes it from CDK4/6 inhibitors used as antineoplastic agents.

Молекулярная масса

446,5000 g/mol

LogP

2,60

TPSA

91,20 Ų

Правило пяти Липинского

Соответствует

Терапевтические области

Pancreatic Cancer Bladder Cancer Non-Small Cell Lung Cancer Breast Cancer Colorectal Cancer

Механизм действия

Selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6), blocking the phosphorylation of retinoblastoma protein and arresting the cell cycle at the G1/S transition to prevent cancer cell proliferation.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Механизм

Selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6), blocking the phosphorylation of retinoblastoma protein and arresting the cell cycle at the G1/S transition to prevent cancer cell proliferation.

2D Структура

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
CN1CCN(c2ccc(Nc3ncc4cc5n(c4n3)C3(CCCCC3)CNC5=O)nc2)CC1

                

                

                
                

                    
InChI

                    
InChI=1S/C24H30N8O/c1-30-9-11-31(12-10-30)18-5-6-20(25-15-18)28-23-26-14-17-13-19-22(33)27-16-24(7-3-2-4-8-24)32(19)21(17)29-23/h5-6,13-15H,2-4,7-12,16H2,1H3,(H,27,33)(H,25,26,28,29)

                

                

                

                    
                    

                        
Molecular Formula

                        
C24H30N8O

                    

                    
                    

                        
HBD / HBA

                        
2 / 7

                    

                    
                    

                        
Вращаемые Связи

                        
3

                    

                    
                    
                    

                        
Тяжёлые Атомы

                        
33

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
No targets recorded

    
    
Target interaction data is not yet available for this drug.

    



                
            


            
            

                
                


    
    
        
    
    
    
No interactions recorded

    
    
Drug interaction data is not yet available for this compound.

    



                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Часто задаваемые вопросы

                

                    
                    

                        
                        

                            
Trilaciclib is a first-in-class CDK4/6 inhibitor that transiently arrests hematopoietic stem and progenitor cells in G1 phase before chemotherapy administration, thereby protecting bone marrow from chemotherapy-induced damage. It is used to decrease the incidence of chemotherapy-induced myelosuppression in adults receiving certain chemotherapy regimens for small cell lung cancer. Its myeloprotective mechanism distinguishes it from CDK4/6 inhibitors used as antineoplastic agents.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6), blocking the phosphorylation of retinoblastoma protein and arresting the cell cycle at the G1/S transition to prevent cancer cell proliferation.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Trilaciclib is an approved drug. It has reached clinical phase 4. It is classified as a 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).
                CHEMBL3894860.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 68029831.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
Медицинский отказ от ответственности

    

        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.