Identification

Name
Goserelin
Accession Number
DB00014  (BTD00113, BIOD00113)
Type
Small Molecule
Groups
Approved
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
Thumb
Synonyms
Not Available
External IDs
ICI 118,630 / ICI-118630
Product Ingredients
IngredientUNIICASInChI Key
Goserelin acetate6YUU2PV0U8145781-92-6IKDXDQDKCZPQSZ-JHYYTBFNSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ZoladexImplant10.8 mg/1SubcutaneousAstra Zeneca Lp2003-05-05Not applicableUs
ZoladexImplant3.6 mgSubcutaneousTersera Therapeutics Llc1994-12-31Not applicableCanada
ZoladexImplant3.6 mg/1SubcutaneousA-S Medication Solutions2003-05-05Not applicableUs
ZoladexImplant3.6 mg/1SubcutaneousAstra Zeneca Lp2003-05-05Not applicableUs
ZoladexImplant3.6 mg/1SubcutaneousTersera Therapeutics Llc2018-03-31Not applicableUs
ZoladexImplant10.8 mg/1SubcutaneousTersera Therapeutics Llc2018-01-26Not applicableUs
Zoladex LAImplant10.8 mgSubcutaneousTersera Therapeutics Llc1996-08-28Not applicableCanada
International/Other Brands
Zoladex
Categories
UNII
0F65R8P09N
CAS number
65807-02-5
Weight
Average: 1269.4105
Monoisotopic: 1268.641439486
Chemical Formula
C59H84N18O14
InChI Key
BLCLNMBMMGCOAS-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[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

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.

Associated Conditions
Associated Therapies
Pharmacodynamics

The 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 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.

TargetActionsOrganism
ALutropin-choriogonadotropic hormone receptor
agonist
Human
AGonadotropin-releasing hormone receptor
agonist
Human
Absorption

Inactive orally, rapidly absorbed following subcutaneous administration.

Volume of distribution
  • 44.1 ± 13.6 L [subcutaneous administration of 250 mcg]
Protein binding

27.3%

Metabolism

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.

Half life

4-5 hours

Clearance
  • 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot]
Toxicity

No experience of overdosage from clinical trials.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Goserelin.
AbacavirGoserelin may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbexinostatThe risk or severity of QTc prolongation can be increased when Goserelin is combined with Abexinostat.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Goserelin.
AcebutololThe risk or severity of QTc prolongation can be increased when Goserelin is combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Goserelin which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Goserelin which could result in a higher serum level.
AceprometazineThe risk or severity of QTc prolongation can be increased when Goserelin is combined with Aceprometazine.
AcetaminophenGoserelin may decrease the excretion rate of Acetaminophen which could result in a higher serum level.
Food Interactions
Not 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 References
Not Available
External Links
Human Metabolome Database
HMDB0014259
KEGG Drug
D00573
PubChem Compound
5311128
PubChem Substance
46507336
ChemSpider
4470656
ChEBI
5523
ChEMBL
CHEMBL1201247
Therapeutic Targets Database
DAP000023
PharmGKB
PA164747674
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Goserelin
ATC Codes
L02AE03 — Goserelin
AHFS Codes
  • 68:18.00 — Gonadotropins
  • 92:00.00 — Miscellaneous Therapeutic Agents
FDA label
Download (992 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingOtherProstate Cancer1
1Active Not RecruitingTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
1Active Not RecruitingTreatmentBreast Cancer - Female / Breast Cancer - Male / Cancer, Breast1
1Active Not RecruitingTreatmentHormone Receptor Positive, HER2-negative, Advanced Breast Cancer1
1Active Not RecruitingTreatmentProstate Cancer1
1CompletedTreatmentBioequivalence1
1CompletedTreatmentProstate Cancer4
1RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentCancer, Breast / Carcinoma, Breast / Malignant Neoplasm of Breast1
1TerminatedTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer1
1TerminatedTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Male Breast Carcinoma / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1WithdrawnTreatmentMetastatic Breast Cancer (MBC)1
1, 2Active Not RecruitingTreatmentProstate Cancer1
1, 2CompletedTreatmentProstate Cancer3
1, 2RecruitingTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
1, 2TerminatedTreatmentAdenocarcinoma, Prostate / Stage IIA Prostate Cancer / Stage IIA Prostate Cancer AJCC v7 / Stage IIB Prostate Cancer / Stage IIB Prostate Cancer AJCC v71
2Active Not RecruitingBasic ScienceCancer, Breast1
2Active Not RecruitingTreatmentAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / Prostate Cancer / PSA Level Greater Than or Equal to 0.2 / PSA Progression / Recurrent Prostate Carcinoma1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentProstate Cancer3
2CompletedPreventionCancer, Breast1
2CompletedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer1
2CompletedTreatmentAdenocarcinoma of the Prostate / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2CompletedTreatmentAdenocarcinoma, Prostate / Recurrent Prostate Carcinoma / Stage IV Prostate Cancer1
2CompletedTreatmentAdenocarcinoma, Prostate / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
2CompletedTreatmentAdvanced Breast Cancer1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer1
2CompletedTreatmentCancer, Breast3
2CompletedTreatmentCancers / Hormonal Cycling / Prostate1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentMetastatic Cancers / Prostate Cancer1
2CompletedTreatmentProstate Cancer14
2CompletedTreatmentRecurrent Prostate Cancer2
2CompletedTreatmentRecurrent Prostate Carcinoma / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
2Not Yet RecruitingPreventionOvarian Failure1
2Not Yet RecruitingTreatmentBreast Cancer Triple Negative1
2Not Yet RecruitingTreatmentCancer, Breast1
2Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2Not Yet RecruitingTreatmentProstate Cancer1
2RecruitingDiagnosticProstate Cancer1
2RecruitingSupportive CareAdenocarcinoma of the Prostate / Recurrent Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2RecruitingTreatmentAdenocarcinoma, Prostate1
2RecruitingTreatmentCancer of the Breast / Cancer, Breast / Carcinoma, Breast1
2RecruitingTreatmentCancer of the Breast / Cancer, Breast / Carcinoma, Breast / Malignant Tumor of Breast1
2RecruitingTreatmentCancer of the Breast / Cancer, Breast / Neoplasms, Breast1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentEarly-Stage Breast Carcinoma / Estrogen Receptor Positive Tumor1
2RecruitingTreatmentEarly-Stage Breast Carcinoma / Hormone Receptor Positive Tumor1
2RecruitingTreatmentNeoplasms, Breast2
2RecruitingTreatmentProstate Cancer2
2SuspendedSupportive CareAdenocarcinoma, Prostate / Cancers / Prostate Cancer1
2TerminatedTreatmentAdenocarcinoma, Prostate / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentEstrogen Receptor Positive / HER2/Neu Negative / Recurrent Breast Carcinoma / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2TerminatedTreatmentEstrogen Receptor-Positive Breast Cancer / HER2-Negative Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2TerminatedTreatmentHormone-sensitive Metastatic Breast Cancer1
2TerminatedTreatmentProstate Cancer1
2Unknown StatusTreatmentBreast Cancer Nos Premenopausal / Estrogen Receptor Positive Tumor / Metastatic Breast Cancer (MBC)1
2Unknown StatusTreatmentCancer, Breast1
2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)1
2Unknown StatusTreatmentProstate Cancer1
2WithdrawnNot AvailableProstate Cancer1
2WithdrawnTreatmentCancer, Breast2
2WithdrawnTreatmentMetabolic Syndromes1
2WithdrawnTreatmentMetastatic Breast Cancer (MBC)1
2WithdrawnTreatmentProstate Cancer1
2, 3Not Yet RecruitingTreatmentCancer treatment / Cancer, Breast / Endocrine Breast Diseases1
2, 3RecruitingTreatmentCastration-resistant Prostate Cancer Patients With Oligometastases1
2, 3RecruitingTreatmentStage I Prostate Adenocarcinoma / Stage II Prostate Adenocarcinoma / Stage III Prostate Adenocarcinoma1
3Active Not RecruitingTreatmentAdvanced Metastatic Breast Cancer / Advanced, Metastatic Breast Cancer1
3Active Not RecruitingTreatmentEstrogen Receptor Positive / HER2/Neu Positive / Progesterone Receptor Positive / Stage IB Breast Cancer / Stage IB Breast Cancer AJCC v7 / Stage II Breast Cancer / Stage IIA Breast Cancer / Stage IIA Breast Cancer AJCC v6 and v7 / Stage IIB Breast Cancer / Stage IIB Breast Cancer AJCC v6 and v7 / Stage IIIA Breast Cancer / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v71
3Active Not RecruitingTreatmentGastrointestinal Complications / Prostate Cancer / Sexual Dysfunctions / Urinary Complications1
3Active Not RecruitingTreatmentProstate Cancer7
3CompletedPreventionCancer, Breast1
3CompletedSupportive CareCancer, Breast / Infertilities / Menopausal Symptoms2
3CompletedTreatmentAdenocarcinoma of the Prostate / Prostate Cancer1
3CompletedTreatmentCancer, Breast7
3CompletedTreatmentEarly-Stage Breast Cancer1
3CompletedTreatmentEndometriosis1
3CompletedTreatmentMale Breast Cancer1
3CompletedTreatmentProstate Cancer18
3Not Yet RecruitingTreatmentCancer, Breast1
3Not Yet RecruitingTreatmentCancer, Breast / Chemotherapy Induced Amenorrhea / Ovarian Function Suppression1
3RecruitingBasic ScienceMuscle Hypotrophy / Muscle Wasting / Sarcopenia1
3RecruitingPreventionCancer, Breast1
3RecruitingTreatmentAdvanced Metastatic Breast Cancer1
3RecruitingTreatmentAnemias / Bone destruction / Cardiovascular Complications / Menopausal Hot Flushes / Prostate Cancer1
3RecruitingTreatmentBreast Adenocarcinoma / Estrogen Receptor Positive / HER2/Neu Negative / Male Breast Carcinoma / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer / Stage IIIC Breast Cancer AJCC v7 / Stage IV Breast Cancer / Stage IV Breast Cancer AJCC v6 and v71
3RecruitingTreatmentBreast Neoplasm Female1
3RecruitingTreatmentCancer, Breast6
3RecruitingTreatmentCastration Levels of Testosterone / Metastatic Prostatic Adenocarcinoma / Stage IV Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v8 / Stage IVB Prostate Cancer AJCC v81
3RecruitingTreatmentNeoplasms, Breast1
3TerminatedTreatmentCancer, Breast2
3TerminatedTreatmentProstate Cancer5
3Unknown StatusTreatmentCancer, Breast2
3Unknown StatusTreatmentInfertilities1
3Unknown StatusTreatmentProstate Cancer2
3WithdrawnPreventionCancer, Breast / Ovarian Function1
4CompletedNot AvailableLeiomyomas1
4CompletedTreatmentEndometriosis / Infertilities1
4CompletedTreatmentKennedy's Disease / Spinobulbar Muscular Atrophy1
4Not Yet RecruitingTreatmentMetastatic Breast Cancer (MBC)1
4TerminatedTreatmentProstate Cancer1
4Unknown StatusSupportive CareEndometriosis1
4Unknown StatusTreatmentPatients With T1-4 Advanced Prostate Cancer1
4Unknown StatusTreatmentUterine Leiomyomas1
4WithdrawnTreatmentMetastatic Hormone Refractory Prostate Cancer1
Not AvailableCompletedBasic ScienceMajor Depressive Disorder (MDD) / Menopause / Neurodegeneration / Postpartum Depression / Postpartum Psychosis / Schizophrenic Disorders1
Not AvailableCompletedDiagnosticHealthy Volunteers1
Not AvailableCompletedPreventionCancer, Breast1
Not AvailableCompletedPreventionBone destruction1
Not AvailableCompletedTreatmentCancer, Breast1
Not AvailableCompletedTreatmentEndometrium / Estrogens / Lipemia / Mammography / Ultrasonography1
Not AvailableNot Yet RecruitingNot AvailableProstate Cancer1
Not AvailableNot Yet RecruitingBasic ScienceAndrogen Deprivation Therapy / Prostate Cancer / Resistance Exercise1
Not AvailableNot Yet RecruitingTreatmentInfertility Associated With Endometriosis1
Not AvailableRecruitingNot AvailableProstate Cancer1
Not AvailableRecruitingTreatmentAdenocarcinoma of the Prostate1
Not AvailableRecruitingTreatmentProstate Cancer1
Not AvailableSuspendedTreatmentMetabolic Syndromes1
Not AvailableUnknown StatusHealth Services ResearchCancer, Breast1
Not AvailableUnknown StatusTreatmentMetabolic Syndromes1

Pharmacoeconomics

Manufacturers
  • Astrazeneca uk ltd
Packagers
  • AstraZeneca Inc.
Dosage forms
FormRouteStrength
ImplantSubcutaneous10.8 mg/1
ImplantSubcutaneous3.6 mg
ImplantSubcutaneous3.6 mg/1
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)
US7118552No2002-04-132022-04-13Us
US7220247No2002-04-092022-04-09Us
US7500964No2001-02-262021-02-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilitySolubleNot Available
logP-2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0283 mg/mLALOGPS
logP0.3ALOGPS
logP-5.2ChemAxon
logS-4.6ALOGPS
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 FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as oligopeptides. These are organic compounds containing a sequence of between three and ten alpha-amino acids joined by peptide bonds.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Oligopeptides
Alternative Parents
Tyrosine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Leucine and derivatives / Proline and derivatives / N-acyl-alpha amino acids and derivatives / Tryptamines and derivatives / Serine and derivatives / Alpha amino acid amides / 3-alkylindoles
show 26 more
Substituents
Alpha-oligopeptide / Tyrosine or derivatives / Phenylalanine or derivatives / Histidine or derivatives / Leucine or derivatives / Proline or derivatives / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / Triptan / Serine or derivatives
show 51 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not 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
Uniprot Name
Lutropin-choriogonadotropic hormone receptor
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...
Gene Name
GNRHR
Uniprot ID
P30968
Uniprot Name
Gonadotropin-releasing hormone receptor
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]

Drug created on June 13, 2005 07:24 / Updated on October 21, 2018 20:19