Identification | |
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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 |
|
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 |
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Interactions | |
Drug Interactions | Not Available |
Food Interactions | Not Available |
Lutropin-choriogonadotropic hormone receptor | |
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Name | Lutropin-choriogonadotropic hormone receptor |
Gene Name | LHCGR |
Pharmacological action | yes |
Actions | agonist |
References |
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DTHybrid score | 1.3643 |
Gonadotropin-releasing hormone receptor | |
Name | Gonadotropin-releasing hormone receptor |
Gene Name | GNRHR |
Pharmacological action | yes |
Actions | agonist |
References |
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DTHybrid score | 1.661 |
Id | Partner name | Gene Name | Score |
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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 |