Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Histrelin
Drug ID BADD_D01073
Description 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. 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.
Indications and Usage 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.
Marketing Status Discontinued
ATC Code L02AE05
DrugBank ID DB06788
KEGG ID D02369
MeSH ID C029256
PubChem ID 25077993
TTD Drug ID D0O7DG
NDC Product Code Not Available
Synonyms histrelin | 6-His(imBzl)-9-N-Et-ProNH2-10-des-GlyNH2-LHRH | GnRH, His(imBzl)(6)-N-Et-ProNH2(9)- | LHRH, His(imBzl)(6)-N-Et-ProNH2(9)- | LHRH, histidyl(imBzl)(6)-N-ethylprolinamide(9)-des-glycinamide(10)- | imbzl-His(6), Pro(9)-NET-GNRH | ((im bzl)-D-His(6), Pro(9)-NEt)LHRH | IBHPE-LHRH | Supprelin
Chemical Information
Molecular Formula C66H86N18O12
CAS Registry Number 76712-82-8
SMILES CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC2=CN(C=N2)CC3=CC=CC=C3 )NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CO)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CN=CN 7)NC(=O)C8CCC(=O)N8
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Not AvailableNot AvailableNot AvailableNot AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Discomfort08.01.08.003--Not Available
Dizziness24.06.02.007; 17.02.05.003; 02.01.02.004--
Dysmenorrhoea21.01.01.002--
Dyspnoea22.02.01.004; 02.01.03.002--
Dyspnoea exertional02.01.03.003; 22.02.01.005--Not Available
Dysuria20.02.02.002--
Emotional disorder19.04.02.0050.001471%Not Available
Enuresis20.02.02.003; 19.07.04.0010.001471%Not Available
Epistaxis24.07.01.005; 22.04.03.001--
Erythema23.03.06.0010.002942%Not Available
Fatigue08.01.01.0020.003677%
Feeling abnormal08.01.09.014--Not Available
Fluid retention20.01.02.003; 14.05.06.002--Not Available
Flushing24.03.01.002; 23.06.05.003; 08.01.03.025--
Gastrointestinal disorder07.11.01.001--Not Available
Growth accelerated15.03.01.001; 05.03.01.0010.002942%
Gynaecomastia21.05.04.003; 05.05.02.003--
Haematoma24.07.01.001--
Haematuria24.07.01.047; 20.02.01.006--
Hair growth abnormal23.02.06.0060.002942%Not Available
Headache17.14.01.0010.005148%
Heart rate increased13.14.04.0020.001471%Not Available
Hepatocellular injury09.01.07.008--Not Available
Hypercalcaemia14.04.01.003; 05.04.01.002--
Hypercholesterolaemia14.08.01.001--Not Available
Hyperhidrosis23.02.03.004; 08.01.03.0280.001471%
Hypersensitivity10.01.03.0030.003677%
Hypertension24.08.02.0010.002942%
Hypotrichosis23.02.02.003--Not Available
Implant site reaction12.07.02.009; 08.02.02.009--Not Available
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