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Identification
NameGoserelin
Accession NumberDB00014  (BTD00113, BIOD00113)
TypeSmall Molecule
GroupsApproved
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.
Structure
Thumb
Synonyms
Goserelin
Goserelin acetate
ICI-118630
Zoladex
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ZoladexImplant3.6 mg/1SubcutaneousAstra Zeneca Pharmaceuticals Lp2003-05-05Not applicableUs
ZoladexImplant3.6 mg/1SubcutaneousA S Medication Solutions2003-05-05Not applicableUs
ZoladexImplant10.8 mg/1SubcutaneousAstra Zeneca Pharmaceuticals Lp2003-05-05Not applicableUs
Zoladex Inj Depot 3.6mgImplant3.6 mgSubcutaneousAstrazeneca Canada Inc1994-12-31Not applicableCanada
Zoladex LA Inj Depot 10.8mgImplant10.8 mgSubcutaneousAstrazeneca Canada Inc1996-08-28Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Goserelin acetate
Thumb
  • InChI Key: IKDXDQDKCZPQSZ-JHYYTBFNSA-N
  • Monoisotopic Mass: 1328.662568858
  • Average Mass: 1329.4624
DBSALT000093
Categories
UNII0F65R8P09N
CAS number65807-02-5
WeightAverage: 1269.4105
Monoisotopic: 1268.641439486
Chemical FormulaC59H84N18O14
InChI KeyBLCLNMBMMGCOAS-URPVMXJPSA-N
InChI
InChI=1S/C59H84N18O14/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90)/t38-,39-,40-,41-,42-,43-,44-,45+,46-/m0/s1
IUPAC Name
(2S)-1-[(2S)-2-[(2S)-2-[(2R)-3-(tert-butoxy)-2-[(2S)-2-[(2S)-3-hydroxy-2-[(2S)-2-[(2S)-3-(1H-imidazol-5-yl)-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1H-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]propanamido]-4-methylpentanamido]-5-[(diaminomethylidene)amino]pentanoyl]-N-(carbamoylamino)pyrrolidine-2-carboxamide
SMILES
CC(C)C[[email protected]](NC(=O)[C@@H](COC(C)(C)C)NC(=O)[[email protected]](CC1=CC=C(O)C=C1)NC(=O)[[email protected]](CO)NC(=O)[[email protected]](CC1=CNC2=CC=CC=C12)NC(=O)[[email protected]](CC1=CN=CN1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[[email protected]]1C(=O)NNC(N)=O
Pharmacology
IndicationUsed 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.
Structured Indications
PharmacodynamicsThe pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.
Mechanism of actionGoserelin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Lutropin-choriogonadotropic hormone receptorProteinyes
agonist
HumanP22888 details
Gonadotropin-releasing hormone receptorProteinyes
agonist
HumanP30968 details
Related Articles
AbsorptionInactive orally, rapidly absorbed following subcutaneous administration.
Volume of distribution
  • 44.1 ± 13.6 L [subcutaneous administration of 250 mcg]
Protein binding27.3%
Metabolism

Hepatic

Route of eliminationClearance 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.
Half life4-5 hours
Clearance
  • 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot]
ToxicityNo experience of overdosage from clinical trials.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.Approved, Investigational
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Goserelin.Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Goserelin.Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Goserelin.Experimental
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Goserelin.Approved
AmantadineAmantadine may increase the QTc-prolonging activities of Goserelin.Approved
AmiodaroneGoserelin may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Goserelin.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Goserelin.Approved
AnagrelideGoserelin may increase the QTc-prolonging activities of Anagrelide.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Goserelin.Investigational
ApomorphineApomorphine may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
Arsenic trioxideGoserelin may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherGoserelin may increase the QTc-prolonging activities of Artemether.Approved
AsenapineGoserelin may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirAtazanavir may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Goserelin.Approved
AzithromycinGoserelin may increase the QTc-prolonging activities of Azithromycin.Approved
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Goserelin.Investigational
BedaquilineGoserelin may increase the QTc-prolonging activities of Bedaquiline.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Goserelin.Approved, Investigational
BortezomibBortezomib may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Goserelin.Withdrawn
BuserelinBuserelin may increase the QTc-prolonging activities of Goserelin.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Goserelin.Approved
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Goserelin.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Goserelin.Experimental
CeritinibGoserelin may increase the QTc-prolonging activities of Ceritinib.Approved
ChloroquineGoserelin may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineGoserelin may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Goserelin.Approved
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Goserelin.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Goserelin.Experimental
CiprofloxacinGoserelin may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideGoserelin may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramGoserelin may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinGoserelin may increase the QTc-prolonging activities of Clarithromycin.Approved
ClomipramineClomipramine may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
ClozapineGoserelin may increase the QTc-prolonging activities of Clozapine.Approved
Corifollitropin AlfaThe therapeutic efficacy of Corifollitropin Alfa can be increased when used in combination with Goserelin.Approved
CrizotinibGoserelin may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Goserelin.Approved, Investigational
DabrafenibDabrafenib may increase the QTc-prolonging activities of Goserelin.Approved
DasatinibDasatinib may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Goserelin.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Goserelin.Investigational
DesfluraneDesflurane may increase the QTc-prolonging activities of Goserelin.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Goserelin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Goserelin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Goserelin.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Goserelin.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Goserelin.Approved
DisopyramideGoserelin may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Goserelin.Approved, Investigational
DofetilideGoserelin may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronGoserelin may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneGoserelin may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Goserelin.Approved
DronedaroneGoserelin may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolGoserelin may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Goserelin.Approved
EliglustatGoserelin may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Goserelin.Approved
EribulinEribulin may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
ErythromycinGoserelin may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramGoserelin may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Goserelin.Approved, Investigational
EzogabineEzogabine may increase the QTc-prolonging activities of Goserelin.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Goserelin.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Goserelin.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
FlecainideGoserelin may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Goserelin.Approved
FluoxetineGoserelin may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolGoserelin may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FormoterolFormoterol may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
FoscarnetFoscarnet may increase the QTc-prolonging activities of Goserelin.Approved
Gadobenic acidGoserelin may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Goserelin.Approved
GemifloxacinGoserelin may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Goserelin.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Goserelin.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Goserelin.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Goserelin.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Goserelin.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Goserelin.Approved
GranisetronGoserelin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Goserelin.Investigational
HaloperidolGoserelin may increase the QTc-prolonging activities of Haloperidol.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Goserelin.Approved
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Goserelin.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
IbutilideGoserelin may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidoneGoserelin may increase the QTc-prolonging activities of Iloperidone.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Goserelin.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Goserelin.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Goserelin.Approved
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Goserelin.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Goserelin.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Goserelin.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Goserelin.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Goserelin.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Goserelin.Approved
IsofluraneIsoflurane may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Goserelin.Approved
ItraconazoleItraconazole may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Goserelin.Approved
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
LenvatinibGoserelin may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
LevofloxacinGoserelin may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Goserelin.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Goserelin.Approved
LithiumLithium may increase the QTc-prolonging activities of Goserelin.Approved
LopinavirGoserelin may increase the QTc-prolonging activities of Lopinavir.Approved
LumefantrineGoserelin may increase the QTc-prolonging activities of Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Goserelin.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Goserelin.Approved
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Goserelin.Approved
MethadoneGoserelin may increase the QTc-prolonging activities of Methadone.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Goserelin.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Goserelin.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Goserelin.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Goserelin.Approved
MirabegronMirabegron may increase the QTc-prolonging activities of Goserelin.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Goserelin.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Goserelin.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Goserelin.Approved
MoxifloxacinGoserelin may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Goserelin.Approved, Investigational
NelfinavirNelfinavir may increase the QTc-prolonging activities of Goserelin.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Goserelin.Approved
NilotinibGoserelin may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Goserelin.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Goserelin.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
OfloxacinGoserelin may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
OlodaterolOlodaterol may increase the QTc-prolonging activities of Goserelin.Approved
OndansetronGoserelin may increase the QTc-prolonging activities of Ondansetron.Approved
OuabainOuabain may decrease the cardiotoxic activities of Goserelin.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Goserelin.Approved, Vet Approved
PaliperidoneGoserelin may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatGoserelin may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
ParoxetineParoxetine may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Goserelin.Approved
PazopanibGoserelin may increase the QTc-prolonging activities of Pazopanib.Approved
PentamidineGoserelin may increase the QTc-prolonging activities of Pentamidine.Approved
PerflutrenGoserelin may increase the QTc-prolonging activities of Perflutren.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Goserelin.Approved, Withdrawn
PimozideGoserelin may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Goserelin.Approved, Investigational
PosaconazolePosaconazole may increase the QTc-prolonging activities of Goserelin.Approved, Investigational, Vet Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Goserelin.Approved, Investigational
PrimaquineGoserelin may increase the QTc-prolonging activities of Primaquine.Approved
ProcainamideGoserelin may increase the QTc-prolonging activities of Procainamide.Approved
PromazineGoserelin may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Goserelin.Approved
PropafenoneGoserelin may increase the QTc-prolonging activities of Propafenone.Approved
PropofolPropofol may increase the QTc-prolonging activities of Goserelin.Approved, Investigational, Vet Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Goserelin.Approved
QuetiapineGoserelin may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineGoserelin may increase the QTc-prolonging activities of Quinidine.Approved
QuinineGoserelin may increase the QTc-prolonging activities of Quinine.Approved
RanolazineRanolazine may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Goserelin.Approved, Investigational
RilpivirineRilpivirine may increase the QTc-prolonging activities of Goserelin.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
RitonavirRitonavir may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Goserelin.Approved, Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Goserelin.Approved
SaquinavirGoserelin may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Goserelin.Approved
SertralineSertraline may increase the QTc-prolonging activities of Goserelin.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Goserelin.Approved, Investigational
SolifenacinSolifenacin may increase the QTc-prolonging activities of Goserelin.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
SotalolGoserelin may increase the QTc-prolonging activities of Sotalol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Goserelin.Approved
SulfisoxazoleGoserelin may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Goserelin.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Goserelin.Approved
TelavancinGoserelin may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinGoserelin may increase the QTc-prolonging activities of Telithromycin.Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Goserelin.Approved
TetrabenazineGoserelin may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Goserelin.Investigational
ThioridazineGoserelin may increase the QTc-prolonging activities of Thioridazine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Goserelin.Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Goserelin.Approved
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Goserelin.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Goserelin.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
ToremifeneGoserelin may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Goserelin.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Goserelin.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Goserelin.Approved, Vet Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Goserelin.Withdrawn
VandetanibGoserelin may increase the QTc-prolonging activities of Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Goserelin.Approved
VemurafenibGoserelin may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Goserelin.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Goserelin.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Goserelin.Approved, Investigational
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Goserelin.Approved, Investigational
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Goserelin.Approved, Investigational
ZiprasidoneGoserelin may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolGoserelin may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Kripa S. Srivastava, Matthew R. Davis, “Solid Phase Peptide for the Production of Goserelin.” U.S. Patent US20100311946, issued December 09, 2010.

US20100311946
General ReferencesNot Available
External Links
ATC CodesL02AE03
AHFS Codes
  • 68:18.00
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (992 KB)
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9771
Blood Brain Barrier-0.8816
Caco-2 permeable-0.7772
P-glycoprotein substrateSubstrate0.9016
P-glycoprotein inhibitor INon-inhibitor0.5834
P-glycoprotein inhibitor IINon-inhibitor0.8342
Renal organic cation transporterNon-inhibitor0.7673
CYP450 2C9 substrateNon-substrate0.7534
CYP450 2D6 substrateNon-substrate0.7806
CYP450 3A4 substrateSubstrate0.6353
CYP450 1A2 substrateNon-inhibitor0.8265
CYP450 2C9 inhibitorNon-inhibitor0.7506
CYP450 2D6 inhibitorNon-inhibitor0.8835
CYP450 2C19 inhibitorNon-inhibitor0.7254
CYP450 3A4 inhibitorNon-inhibitor0.6347
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9054
Ames testNon AMES toxic0.5851
CarcinogenicityNon-carcinogens0.6406
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6730 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8841
hERG inhibition (predictor II)Inhibitor0.5249
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astrazeneca uk ltd
Packagers
Dosage forms
FormRouteStrength
ImplantSubcutaneous10.8 mg/1
ImplantSubcutaneous3.6 mg/1
ImplantSubcutaneous3.6 mg
ImplantSubcutaneous10.8 mg
Prices
Unit descriptionCostUnit
Zoladex 10.8 mg implant syringe1380.65USD syringe
Zoladex 3.6 mg implant syringe451.19USD syringe
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7118552 No2002-04-132022-04-13Us
US7220247 No2002-04-092022-04-09Us
US7500964 No2001-02-262021-02-26Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0283 mg/mLALOGPS
logP0.3ALOGPS
logP-5.2ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)9.27ChemAxon
pKa (Strongest Basic)10.82ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count18ChemAxon
Hydrogen Donor Count17ChemAxon
Polar Surface Area495.89 Å2ChemAxon
Rotatable Bond Count33ChemAxon
Refractivity325.84 m3·mol-1ChemAxon
Polarizability131.22 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as peptides. These are compounds containing an amide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentPeptides
Alternative Parents
Substituents
  • Alpha peptide
  • N-acyl-alpha amino acid or derivatives
  • Triptan
  • Alpha-amino acid amide
  • Phenylpropylamine
  • Amphetamine or derivatives
  • N-substituted-alpha-amino acid
  • Indole or derivatives
  • Indole
  • Pyrrolidine-2-carboxamide
  • Pyrrolidine carboxylic acid or derivatives
  • N-acylpyrrolidine
  • Phenol
  • Fatty acyl
  • Benzenoid
  • Hydrazinecarboxamide
  • Substituted pyrrole
  • 2-pyrrolidone
  • Pyrrolidone
  • N-acyl-amine
  • Fatty amide
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Semicarbazide
  • Pyrrolidine
  • Pyrrole
  • Imidazole
  • Azole
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactam
  • Guanidine
  • Carboxylic acid hydrazide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidamide
  • Ether
  • Dialkyl ether
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Luteinizing hormone receptor activity
Specific Function:
Receptor for lutropin-choriogonadotropic hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
Gene Name:
LHCGR
Uniprot ID:
P22888
Molecular Weight:
78642.01 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. 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:17016423 ]
  3. Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. [PubMed:20053189 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Peptide binding
Specific Function:
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
Gene Name:
GNRHR
Uniprot ID:
P30968
Molecular Weight:
37730.355 Da
References
  1. Kirby RS, Fitzpatrick JM, Clarke N: Abarelix and other gonadotrophin-releasing hormone antagonists in prostate cancer. BJU Int. 2009 Dec;104(11):1580-4. doi: 10.1111/j.1464-410X.2009.08924.x. [PubMed:20053189 ]
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Drug created on June 13, 2005 07:24 / Updated on December 02, 2016 02:41