Drug nameGoserelin
DescriptionGoserelin 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.
DrugBankPrimary Accession Number: DB00014
DIN02225905
TypeApproved, Biotech
IndicationBreast cancer; Prostate carcinoma; Endometriosis
Mechanism of ActionZOLADEX is a synthetic decapeptide analogue of LHRH. ZOLADEX 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.
AbsorptionInactive orally, rapidly absorbed following subcutaneous administration
ToxicityNo experience of overdosage from clinical trials
Protein Binding27.30%
Interactions
RXListhttp://www.rxlist.com/cgi/generic/goserel.htm
KEGGdrug: D00573 / compound: Not Available
PubChemcompound: 47725 / substance: 186963
PharmGKBNot available
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Target
NameGeneEntrezIDSwissprotSNP
Lutropin-choriogonadotropic hormone receptorLHCGR3973LSHR_HUMANrs2293275 rs11125179 rs58356637 rs10495960 rs34256682 rs13006488 rs12470652 rs4539842 rs1042551
FilesDB00014.mol | DB00014_1998-07-01.pdf | pdb_902504625473-0.pdb | sdf_597080514996-0.sdf |
Smilesisomeric:
CC(C)C[C@@H](NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@@H](CC1=CC=C(O)C=C1)NC(=
O)[C@@H](CO)NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CN=CN1)NC(=
O)[C@H]1CCC(=O)N1)C(=O)N[C@H](CCCN=C(/N)N)C(=O)N1CCC[C@H]1C(=O)NNC(N)=
O
canonical:
CC(C)CC(NC(=O)C(COC(C)(C)C)NC(=O)C(CC1=CC=C(O)C=C1)NC(=O)C(CO)NC(=O)C(
CC1=CNC2=CC=CC=C12)NC(=O)C(CC1=CN=CN1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCN=C
(N)N)C(=O)N1CCCC1C(=O)NNC(N)=O

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