Histrelin

DB06788

Approved Indication

As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer.

1 Targets

0 Resistance Mutations

3 References

3D Structure No structure available

No co-crystal structure available

Protein Targets

GNRHR P30968 ✓

Mechanism of Action

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes.

Details

DrugBank ID DB06788 ↗

Approval Date 2004-11-01

Molecular Weight 1443.632 g/mol

Drug Class Other

ATC Codes L02AE05

Synonyms histrelina, histreline, histrelinum

PubChem CID: 56927879 ↗

ChEMBL CHEMBL1201255 ↗

SMILES

CC(O)=O.CC(O)=O.[H][C@@](CO)(N=C(O)[C@]([H])(CC1=CNC2=CC=CC=C12)N=C(O)[C@]([H])(CC1=CN=CN1)N=C(O)[C@]1([H])CCC(O)=N1)C(O)=N[C@@]([H])(CC1=CC=C(O)C=C1)C(O)=N[C@]([H])(CC1=CN(CC2=CC=CC=C2)C=N1)C(O)=N[C@@]([H])(CC(C)C)C(O)=N[C@@]([H])(CCCNC(N)=N)C(=O)N1CCC[C@@]1([H])C(O)=NCC

ADMET Profile

Computing properties…

Drug References (DrugBank)

PMID:19920916 PMID:20735905 PMID:21851539