Histrelin

Gonadotropin Releasing Hormone Receptor Agonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Histrelin is a drug in the Gonadotropin Releasing Hormone Receptor Agonist class catalogued in DrugCentral. It was first approved by the FDA in 1991. Its mechanism of action is classified as Gonadotropin Releasing Hormone Receptor Agonists. DrugCentral lists 1 molecular target, including GNRHR. Recorded indications include Advanced Prostatic Carcinoma and Precocious puberty.

• Drug class: Gonadotropin Releasing Hormone Receptor Agonist.
• Mechanism of action: Gonadotropin Releasing Hormone Receptor Agonists.
• Molecular targets: GNRHR (1 listed in DrugCentral).
• Indications: Advanced Prostatic Carcinoma and Precocious puberty.
• ATC code: L02AE05 (Gonadotropin releasing hormone analogues).
• Molecular formula: C66H86N18O12; molecular weight 1323.53 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Advanced Prostatic Carcinoma
• Precocious puberty

Contraindications (10)

• Breastfeeding (mother)
• Cardiovascular event risk
• Diabetes mellitus
• Hypercholesterolemia
• Hyperglycemia
• Hypertensive disorder
• Obesity
• Pregnancy, function
• Smokes tobacco daily
• Vertebral Metastases

Mechanism & targets

• Mechanism of action (MoA): Gonadotropin Releasing Hormone Receptor Agonists
• Established pharmacologic class: Gonadotropin Releasing Hormone Receptor Agonist

Molecular targets (1)

Target	Gene	Action	Activity
Gonadotropin-releasing hormone receptor	GNRHR	agonist	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1991-12-24	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
L02AE05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONES AND RELATED AGENTS › Gonadotropin releasing hormone analogues

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Device breakage	438.7
Incorrect product administration duration	434.8
Procedural complication	343.7
Implant site rash	210.9
Delayed puberty	114.9
Implant site pain	91.6
Device expulsion	79.7
Drug ineffective	76.3
Implant site erythema	73.0
Implant site infection	72.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Histrelin is on its molecule page.

• Molecular formula: C₆₆H₈₆N₁₈O₁₂
• Molecular weight: 1323.53 g/mol
• CAS number: 76712-82-8
• InChIKey: HHXHVIJIIXKSOE-QILQGKCVSA-N
• PubChem CID: 25077993

CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1=CN(CC2=CC=CC=C2)C=N1)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CC1=CNC2=C1C=CC=C2)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H]1CCC(=O)N1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Histrelin used for?

DrugCentral lists the following indications for Histrelin: Advanced Prostatic Carcinoma and Precocious puberty.

How does Histrelin work?

Histrelin is classified as Gonadotropin Releasing Hormone Receptor Agonists; its molecular targets in DrugCentral include GNRHR (agonist).

When was Histrelin first approved?

Histrelin was first approved by the FDA in 1991.

What drug class does Histrelin belong to?

Histrelin is in the Gonadotropin Releasing Hormone Receptor Agonist class.

What is the chemical formula of Histrelin?

Histrelin has the molecular formula C66H86N18O12 and a molecular weight of 1323.53 g/mol.

Sources

• DrugCentral drug card 2975 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200509 — compound record and bioactivity
• PubChem CID 25077993 — chemical identifiers
• DrugBank DB06788 — drug record
• FDA UNII H50H3S3W74 — substance identity
• DailyMed: FDA labels for Histrelin — current prescribing information (label search)
• UniProt P30968 (GNRHR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.