DT-Web

DB00014 - Goserelin


Identification
Name Goserelin
Accession Number DB00014 (BIOD00113, BTD00113)
Type small molecule
Description Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 1269.4105
Groups approved
Monoisotopic Weight 1268.641439486
Pharmacology
Indication Used to treat hormone-sensitive cancers of the breast (in pre- and peri- menopausal women) and prostate, and some benign gynaecological disorders (endometriosis, uterine fibroids and endometrial thinning). In addition, goserelin is used in assisted reproduction and in the treatment of precocious puberty.
Mechanism of action Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels.
Absorption Inactive orally, rapidly absorbed following subcutaneous administration.
Protein binding 27.3%
Biotransformation Hepatic
Route of elimination Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine.
Toxicity No experience of overdosage from clinical trials.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Lutropin-choriogonadotropic hormone receptor
Name Lutropin-choriogonadotropic hormone receptor
Gene Name LHCGR
Pharmacological action yes
Actions agonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. - Pubmed
DTHybrid score 1.3643
Gonadotropin-releasing hormone receptor
Name Gonadotropin-releasing hormone receptor
Gene Name GNRHR
Pharmacological action yes
Actions agonist
References
  • Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. - Pubmed
DTHybrid score 1.661

Predictions


Id Partner name Gene Name Score
430 Follicle-stimulating hormone receptor FSHR 0.2925
3811 Cytochrome P450 19A1 CYP19A1 0.1048
1649 Small inducible cytokine A2 CCL2 0.0242
756 Sex hormone-binding globulin SHBG 0.017
614 Progesterone receptor PGR 0.0157
146 Androgen receptor AR 0.0135
136 Estrogen receptor ESR1 0.0125
4512 Cytochrome P450 3A4 CYP3A4 0.0079
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