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Histrelin

CHEMBL1201255 Phase 4 Approved Protein
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
1323.5 g/mol
LogP
0.7
Phase
4

A synthetic gonadotropin-releasing hormone agonist that, with continuous administration, suppresses production of sex hormones by desensitizing pituitary GnRH receptors, used to treat prostate cancer, precocious puberty, and hormone-sensitive cancers. It is delivered via an implant placed under the skin that releases medication continuously for one year. By reducing testosterone or estrogen levels, it slows the growth of hormone-dependent tumors.

Molecular Weight

1323.5000 g/mol

LogP

0.70

TPSA

449.00 Ų

Lipinski RO5

Fail

Therapeutic Areas

Prostate Cancer

Mechanism of Action

Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanism

Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.

2D Structure

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cn(Cc2ccccc2)cn1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1

                

                

                
                

                    
InChI

                    
InChI=1S/C66H86N18O12/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71)/t47-,48-,49-,50-,51-,52-,53+,54-,55-/m0/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C66H86N18O12

                    

                    
                    

                        
HBD / HBA

                        
15 / 15

                    

                    
                    

                        
Rotatable Bonds

                        
34

                    

                    
                    
                    

                        
Heavy Atoms

                        
96

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Frequently Asked Questions

                

                    
                    

                        
                        

                            
A synthetic gonadotropin-releasing hormone agonist that, with continuous administration, suppresses production of sex hormones by desensitizing pituitary GnRH receptors, used to treat prostate cancer, precocious puberty, and hormone-sensitive cancers. It is delivered via an implant placed under the skin that releases medication continuously for one year. By reducing testosterone or estrogen levels, it slows the growth of hormone-dependent tumors.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Modulates gonadotropin-releasing hormone (GnRH) signaling, ultimately suppressing luteinizing hormone and follicle-stimulating hormone secretion and reducing gonadal steroid hormone production.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Histrelin is an approved drug. It has reached clinical phase 4. It is classified as a Protein.

                        

                    

                

            

            

            
            

            
            

            
            
{# 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).
                CHEMBL1201255.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 25077993.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
Medical Disclaimer

    

        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.