Histrelin

DB06788ApprovedInvestigationalWithdrawnSmall moleculeGonadotropin Releasing Hormone Receptor Agonist

Histrelin is a GnRH agonist found in subcutaneous implants used for the treatment of pediatric patients with central precocious puberty and the palliative treatment of advanced prostate cancer. Histrelin is a gonadotropin-releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant delivering continuous therapeutic doses.

Mechanism: Histrelin is a gonadotropin-releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin. GnRH binds to the GnRH receptor located on the pituitary gonadotrophs, and this leads to the production of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as the regulation of sexual maturation and reproductive function.
When administered as an implant, histrelin is delivered in continuous therapeutic doses. As a GnRH agonist, this drug binds and, at first, activates the GnRH receptor. This increases the circulating levels of LH and FSH, leading to a transient increase in the concentration of gonadal steroids (testosterone and dihydrotestosterone in males and estrone and estradiol in premenopausal females). However, the continuous administration of histrelin induces the reversible down-regulation of the GnRH receptor and the desensitization of pituitary gonadotropes, which reduce LH and FSH levels.
Pediatric patients with central precocious puberty (CPP) have a lower height potential. When treated with histrelin, LH levels in CPP are lowered, reducing the concentration of sex steroids. In adult males with advanced prostate cancer, histrelin reduces testosterone production to castration levels, hindering the growth of prostate cancer cells.
Curator reviewed · 14 references
Primary indication: As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP).Curator reviewed · 2 structured indications
Formula / weight: C₇₀H₉₄N₁₈O₁₆ · 1443.632 g/mol (avg)
First approval: Canada, 2006 · United States, 2004
Code names: ORF-17070 · RWJ-17070
Brand names: Supprelin

Resolves to

Compound

UNIIH50H3S3W74CAS76712-82-8ChEMBLCHEMBL1201255ChEBI63530PubChem56927879KEGGD02369

Clinical / RWD

RxNorm50975ATCL02AE05

Structure

InChIKeyBKEMVGVBBDMHKL-VYFXDUNUSA-NSMILES

CC(O)=O.CC(O)=O.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

Targets

P30968GNRHR

What you can answer from here — as of September 12, 2026

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

485Drug interactionsStructured to mechanism, not free text

11Clinical trialsPhase, status and sponsor resolved per trial

2Structured indicationsCondition, population, route and combination as fields, not prose

2ContraindicationsEach with its own population and attribute set

5Marketed productsAcross 3 countries and 5 labellers

1ATC codeIncluding every combination product, plus 21 drug categories

11+ReferencesStructured and connected to the statements they support

Which drugs share a target with Histrelin, and which of those have an active Phase 3 trial?

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