Identification

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Name
Gonadorelin
Accession Number
DB00644  (APRD01001)
Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Description

Gonadorelin is another name for gonadotropin-releasing hormone (GnRH). It is a synthetic decapeptide prepared using solid phase peptide synthesis. GnRH is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pituitary.

Structure
Thumb
Synonyms
  • GnRH
  • Gonadorelin
  • Gonadorelina
  • Gonadoréline
  • Gonadorelinum
  • Gonadotropin-releasing hormone
External IDs
Abbott 41070 / AY 24031 / Hoe 471 / RU 19847
Product Ingredients
IngredientUNIICASInChI Key
Gonadorelin acetate2RG1XQ1NYJ52699-48-6OOBWZCWPKJOGPF-UHFFFAOYSA-N
Gonadorelin diacetate tetrahydrateL8CRY8PWF2Not AvailableQZBIKDNLZRFYMZ-KYOBJPNESA-N
Gonadorelin hydrochloride3PFC574ITA51952-41-1CXLJLMYFZCNNQA-HBBGHHHDSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Factrel Inj 0.5mg/vialPowder, for solutionIntravenous; SubcutaneousAyerst Laboratories1976-12-311996-09-10Canada
Factrel Pws 100mcg/vialPowder, for solutionIntravenous; SubcutaneousWyeth Ayerst Canada Inc.1994-12-311999-10-26Canada
Factrel Pws 500mcg/vialPowder, for solutionIntravenous; SubcutaneousWyeth Ayerst Canada Inc.1995-12-311999-10-26Canada
LutrepulsePowder, for solutionIntravenous; SubcutaneousFerring Pharmaceuticals1994-12-31Not applicableCanada
Lutrepulse Pws 0.8mg/vialPowder, for solutionIntravenous; SubcutaneousFerring Pharmaceuticals1994-12-31Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Relisorm 100 for Inj.-pws Liq-kit Sc IVGonadorelin (100 mcg) + Sodium chloride (0.9 %)Liquid; Powder, for solutionIntravenous; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-31Not applicableCanada
Relisorm 500 for Inj.-pws Liq-kit IV ScGonadorelin (500 mcg) + Sodium chloride (.9 %)Liquid; Powder, for solutionIntravenous; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-31Not applicableCanada
International/Other Brands
Fertagyl / Gonadorelin (Intrapharm) / HRF (Intrapharm) / Hypocrine (Tanabe Mitsubishi Pharma) / Kryptocur (Sanofi-Aventis) / Lutrelef (Ferring) / Relefact (Sanofi-Aventis)
Categories
UNII
9O7312W37G
CAS number
33515-09-2
Weight
Average: 1182.2901
Monoisotopic: 1181.573025571
Chemical Formula
C55H75N17O13
InChI Key
XLXSAKCOAKORKW-UHFFFAOYSA-N
InChI
InChI=1S/C55H75N17O13/c1-29(2)19-38(49(80)67-37(9-5-17-60-55(57)58)54(85)72-18-6-10-43(72)53(84)62-25-44(56)75)66-46(77)26-63-47(78)39(20-30-11-13-33(74)14-12-30)68-52(83)42(27-73)71-50(81)40(21-31-23-61-35-8-4-3-7-34(31)35)69-51(82)41(22-32-24-59-28-64-32)70-48(79)36-15-16-45(76)65-36/h3-4,7-8,11-14,23-24,28-29,36-43,61,73-74H,5-6,9-10,15-22,25-27H2,1-2H3,(H2,56,75)(H,59,64)(H,62,84)(H,63,78)(H,65,76)(H,66,77)(H,67,80)(H,68,83)(H,69,82)(H,70,79)(H,71,81)(H4,57,58,60)
IUPAC Name
N-(1-{2-[(carbamoylmethyl)carbamoyl]pyrrolidin-1-yl}-5-[(diaminomethylidene)amino]-1-oxopentan-2-yl)-2-{2-[2-(3-hydroxy-2-{2-[3-(1H-imidazol-5-yl)-2-[(5-oxopyrrolidin-2-yl)formamido]propanamido]-3-(1H-indol-3-yl)propanamido}propanamido)-3-(4-hydroxyphenyl)propanamido]acetamido}-4-methylpentanamide
SMILES
CC(C)CC(NC(=O)CNC(=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)NCC(N)=O

Pharmacology

Indication

For evaluating the functional capacity and response of the gonadotropes of the anterior pituitary also for evaluating residual gonadotropic function of the pituitary following removal of a pituitary tumor by surgery and/or irradiation.

Associated Therapies
Pharmacodynamics

Gonadorelin is responsible for the release of follicle stimulating hormone and leutinizing hormone from the anterior pitutitary. In the pituitary GnRH stimulates synthesis and release of FSH and LH, a process that is controlled by the frequency and amplitude of GnRH pulses, as well as the feedback of androgens and estrogens. The pulsatility of GnRH secretion has been seen in all vertebrates, and it is necessary to ensure a correct reproductive function. Thus a single hormone, GnRH, controls a complex process of follicular growth, ovulation, and corpus luteum maintenance in the female, and spermatogenesis in the male. Its short half life requires infusion pumps for its clinical use

Mechanism of action

Systemic - Like naturally occurring gonadotropin-releasing hormone (GnRH), gonadorelin primarily stimulates the synthesis and release of luteinizing hormone (LH) from the anterior pituitary gland. Follicle-stimulating hormone (FSH) production and release is also increased by gonadorelin, but to a lesser degree. In prepubertal females and some gonadal function disorders, the FSH response may be greater than the LH response. For the treatment of amenorrhea, delayed puberty, and infertility the administration of gonadorelin is used to simulate the physiologic release of GnRH from the hypothalamus in treatment of delayed puberty, treatment of infertility caused by hypogonadotropic hypogonadism, and induction of ovulation in those women with hypothalamic amenorrhea. This results in increased levels of pituitary gonadotropins LH and FSH, which subsequently stimulate the gonads to produce reproductive steroids.

TargetActionsOrganism
AGonadotropin-releasing hormone receptor
agonist
Humans
APutative gonadotropin-releasing hormone II receptor
agonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

Rapidly absorbed when injected

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Rapidly hydrolyzed to inactive peptide components

Route of elimination
Not Available
Half life

Very short, initial, 2 to 10 minutes; terminal, 10 to 40 minutes

Clearance
Not Available
Toxicity

LD50>3000 mg/kg (rat, oral)

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

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
Capromab pendetideGonadorelin may decrease effectiveness of Capromab pendetide as a diagnostic agent.
Choline C 11Gonadorelin may decrease effectiveness of Choline C 11 as a diagnostic agent.
Conestat alfaThe risk or severity of thromboembolism can be increased when Gonadorelin is combined with Conestat alfa.
Corifollitropin alfaThe therapeutic efficacy of Corifollitropin alfa can be increased when used in combination with Gonadorelin.
Human C1-esterase inhibitorThe risk or severity of thromboembolism can be increased when Gonadorelin is combined with Human C1-esterase inhibitor.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
Not Available

References

Synthesis Reference

Rainer Uhmann, Kurt Radscheit, "Process for the low-racemization preparation of peptide intermediates of the synthesis of gonadorelin and gonadorelin analogs, and new intermediates for this process." U.S. Patent US4691008, issued December, 1984.

US4691008
General References
  1. Dungan HM, Clifton DK, Steiner RA: Minireview: kisspeptin neurons as central processors in the regulation of gonadotropin-releasing hormone secretion. Endocrinology. 2006 Mar;147(3):1154-8. Epub 2005 Dec 22. [PubMed:16373418]
  2. Franceschini I, Lomet D, Cateau M, Delsol G, Tillet Y, Caraty A: Kisspeptin immunoreactive cells of the ovine preoptic area and arcuate nucleus co-express estrogen receptor alpha. Neurosci Lett. 2006 Jul 3;401(3):225-30. Epub 2006 Apr 18. [PubMed:16621281]
External Links
Human Metabolome Database
HMDB0014782
KEGG Compound
C07607
PubChem Compound
36523
PubChem Substance
46506144
ChemSpider
33562
ChEMBL
CHEMBL1981292
Therapeutic Targets Database
DAP001052
PharmGKB
PA449801
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Gonadorelin
ATC Codes
V04CM01 — GonadorelinH01CA01 — Gonadorelin
AHFS Codes
  • 68:18.00 — Gonadotropins and Antigonadotropins
  • 36:66.00 — Pituitary Function
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedScreeningInfertilities1
0RecruitingBasic ScienceSleep Restriction1
0RecruitingTreatmentAdenocarcinoma of the Prostate / Advanced Prostate Cancer / Prostate Cancer / Stage IV Prostate Cancer1
1Active Not RecruitingTreatmentProstate Cancer1
1CompletedNot AvailableHypogonadism1
1RecruitingBasic ScienceSleep Restriction1
1RecruitingOtherAgonadism / Healthy Postmenopausal Women / Hypergonadotropic Hypogonadism in Men / Idiopathic Hypogonadotropic Hypogonadism / Klinefelter's Syndrome / Primary Gonadal Insufficiency in Men1
1RecruitingOtherGonadotrophin releasing hormone deficiency / Idiopathic hyperprolactinemic disorder / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia / Polycystic Ovarian Syndrome1
1RecruitingOtherGonadotrophin releasing hormone deficiency / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia / Puberty, Delayed1
1RecruitingPreventionIdiopathic Hypogonadotropic Hypogonadism1
1, 2CompletedTreatmentHealthy Males1
1, 2CompletedTreatmentHormone-Resistant Prostate Cancer / Prostate Cancer / Recurrent Prostate Cancer / Stage IV Prostate Cancer1
1, 2CompletedTreatmentOvarian Stimulation1
2Active Not RecruitingTreatmentAdenocarcinoma, Prostate / Diseases of Male Genital Organs / Prostate Cancer / PSA Level Greater Than Ten / Stage IIB Prostate Cancer AJCC v8 / Stage IIC Prostate Cancer AJCC v8 / Stage IIIA Prostate Cancer AJCC v8 / Stage IIIC Prostate Cancer AJCC v8 / Testosterone Greater Than 150 ng/dL1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentControlled Ovarian Stimulation / Ovarian Stimulation1
2CompletedTreatmentEndometriosis1
2CompletedTreatmentHighly Endocrine Responsive Operable Breast Cancer1
2CompletedTreatmentHormonal Cycling / Malignancies / Prostate1
2CompletedTreatmentInfertilities2
2CompletedTreatmentProstate Cancer1
2Not Yet RecruitingTreatmentProstate Cancer1
2RecruitingTreatmentAdenocarcinoma, Prostate / Stage IIC Prostate Cancer AJCC v8 / Stage III Prostate Cancer AJCC v8 / Stage IIIA Prostate Cancer AJCC v8 / Stage IIIB Prostate Cancer AJCC v8 / Stage IIIC Prostate Cancer AJCC v8 / Stage IVA Prostate Cancer AJCC v81
2RecruitingTreatmentAmenorrhea / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
2RecruitingTreatmentHIV-1-infection1
2RecruitingTreatmentHypogonadism / Idiopathic hyperprolactinemic disorder1
2RecruitingTreatmentInfertility, Female1
2RecruitingTreatmentOHSS1
2RecruitingTreatmentProstate Cancer3
2RecruitingTreatmentStage II Prostate Adenocarcinoma / Stage III Prostate Adenocarcinoma1
2TerminatedTreatmentHypogonadism / Olfacto genital dysplasia1
2TerminatedTreatmentInfertilities / Ovulation induction therapy1
2, 3Active Not RecruitingNot AvailableHealthy Volunteers / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
2, 3Active Not RecruitingOtherHealthy Volunteers1
2, 3Active Not RecruitingTreatmentEwing's Sarcoma (ES) / Malignancies / Malignant Lymphomas / Sarcoma, Osteogenic / Sarcomas / Toxicity Due to Chemotherapy1
2, 3Active Not RecruitingTreatmentInflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Mucinous Breast Cancer / Tubular Breast Carcinoma1
2, 3CompletedTreatmentInfertilities1
2, 3Not Yet RecruitingTreatmentInfertility, Female1
2, 3RecruitingTreatmentAtypical Endometrial Hyperplasia / Endometrial Cancers1
3Active Not RecruitingBasic ScienceMuscle Hypotrophy / Muscle Wasting / Sarcopenia1
3Active Not RecruitingTreatmentBreast Cancer1
3Active Not RecruitingTreatmentBreast Cancer / Estrogen Receptor Positive Breast Cancer / Progesterone Receptor Positive Tumor / Recurrent Breast Carcinoma / Stage IA Breast Cancer / Stage IB Breast Cancer / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer1
3Active Not RecruitingTreatmentProstatic Neoplasms1
3CompletedNot AvailableBreast Cancer / Sleep disorders and disturbances / Tiredness1
3CompletedPreventionBreast Cancer1
3CompletedPreventionInfertilities1
3CompletedTreatmentAssisted Reproductive Technology therapy1
3CompletedTreatmentEffects of Gonadotropin / Oocyte Maturation / Ovarian Hyperstimulation Syndrome1
3CompletedTreatmentEmbryo Transfer / Luteal Hormone Supplementation in In-vitro Fertilization1
3CompletedTreatmentInfertilities5
3CompletedTreatmentInfertilities / OHSS / Polycystic Ovarian Syndrome1
3CompletedTreatmentInfertilities / Polycystic Ovaries Syndrome1
3CompletedTreatmentMale Breast Cancer1
3CompletedTreatmentMalignant Neoplasm of Female Breast1
3CompletedTreatmentMetastatic Cancers / Prostate Cancer1
3CompletedTreatmentPrimary Amenorrhea With Hypogonadotropic Hypogonadism1
3CompletedTreatmentProstate Cancer1
3CompletedTreatmentUterine Leiomyomas1
3Not Yet RecruitingTreatmentEndometriosis of Uterus1
3Not Yet RecruitingTreatmentIn-Vitro Fertilization1
3RecruitingTreatmentInfertility, Female1
3RecruitingTreatmentProstate Cancer2
3TerminatedNot AvailableInfertilities1
3TerminatedTreatmentBreast Cancer1
3Unknown StatusPreventionEndometriosis1
3Unknown StatusScreeningEmbryo's Genetic and Chromosomal Quality1
3Unknown StatusTreatmentEndometriosis / Menstrual Cramps / Painful Intercourse1
3Unknown StatusTreatmentInfertilities2
4CompletedNot AvailableInfertilities / Premature Ovarian Failure (POF)1
4CompletedNot AvailableLeiomyomas1
4CompletedBasic ScienceDepression / Hot Flushes / Menopause1
4CompletedTreatmentAssisted Reproduction1
4CompletedTreatmentControlled ovarian hyperstimulation therapy / Infertilities1
4CompletedTreatmentEndometriosis1
4CompletedTreatmentFertility / Optimal Stimulation Protocol / Reproductive Endocrinology1
4CompletedTreatmentInfertilities6
4CompletedTreatmentInfertility Indicated for ICSI1
4CompletedTreatmentInfertility, Female Infertility, Male Infertility1
4CompletedTreatmentOvarian Stimulation1
4Not Yet RecruitingTreatmentAmenorrhea / Endometriosis / Quality of Life1
4Not Yet RecruitingTreatmentEndometriosis of Uterus1
4Not Yet RecruitingTreatmentInfertilities / Ovulatory Dysfunction / Polycystic Ovaries Syndrome1
4Not Yet RecruitingTreatmentInvitro Fertilization1
4RecruitingBasic ScienceAging / Menopause / Obesity, Abdominal / Weight Gain1
4RecruitingPreventionAspirin / GnRH Antagonist / Ovarian Hyperstimulation Syndrome / Pigment Epithelium Derived Factor / Vascular Endothelial Growth Factor1
4RecruitingSupportive CareCastration-Resistant Prostatic Cancer / Hormone-Refractory Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Recurrent Prostate Carcinoma / Stage IV Prostate Cancer1
4RecruitingTreatmentAbortions spontaneous / Egg Retrieval / IVF Cycle / Ovarian Hyperstimulation / Ovarian Stimulation / Pregnancy1
4RecruitingTreatmentEmbryo Transfer / Luteal Support1
4RecruitingTreatmentInfertilities1
4RecruitingTreatmentInfertilities / Polycystic Ovarian Syndrome1
4RecruitingTreatmentUterine Hemorrhage / Uterine Leiomyomas1
4TerminatedDiagnosticEndometrial Receptivity / Ovarian Hyperstimulation Syndrome1
4TerminatedTreatmentAssisted Reproductive Technology therapy1
4TerminatedTreatmentInfertilities1
4Unknown StatusDiagnosticCentral Precocious Puberty (CPP) / Sexual Precocity1
4Unknown StatusPreventionCentral Precocious Puberty (CPP)1
4Unknown StatusTreatmentIdiopathic Hypogonadotropic Hypogonadism1
4Unknown StatusTreatmentInfertilities1
4Unknown StatusTreatmentInfertility, Female / Poor Responder1
4Unknown StatusTreatmentPoor Responders Undergoing IVF1
4WithdrawnPreventionOvarian Function / Preservation of Ovarian Function1
Not AvailableActive Not RecruitingTreatmentEndometriosis / Infertilities1
Not AvailableActive Not RecruitingTreatmentGonadotrophin releasing hormone deficiency / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
Not AvailableCompletedNot AvailableAdvanced Prostate Cancer / Lower Urinary Tract Symptoms (LUTS)1
Not AvailableCompletedNot AvailableAssisted Reproductive Technology therapy1
Not AvailableCompletedNot AvailableBMI >30 kg/m21
Not AvailableCompletedNot AvailableEndometriosis / Endometriosis of Uterus1
Not AvailableCompletedNot AvailableEndometriosis / Pelvic Pain1
Not AvailableCompletedNot AvailableHypogonadism1
Not AvailableCompletedNot AvailableImplantation, Embryo / Pregnancy1
Not AvailableCompletedNot AvailableInfertilities1
Not AvailableCompletedNot AvailableInfertility, Subfertility1
Not AvailableCompletedNot AvailableNeonates / Pregnancy3
Not AvailableCompletedNot AvailablePolycystic Ovaries Syndrome1
Not AvailableCompletedNot AvailableProstate Cancer2
Not AvailableCompletedNot AvailablePuberty, Central Precocious / Puberty, Precocious1
Not AvailableCompletedNot AvailableReproductive Techniques, Assisted1
Not AvailableCompletedBasic ScienceBMI >30 kg/m21
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Fertility1
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Infertilities1
Not AvailableCompletedBasic ScienceHealthy Volunteers / Volunteers1
Not AvailableCompletedBasic SciencePuberty, Precocious1
Not AvailableCompletedDiagnosticEndometriosis / Endometriosis of Uterus / Pelvic Pain / Uterine Leiomyomas1
Not AvailableCompletedHealth Services ResearchGonadal Disorders / Hypogonadism / Olfacto genital dysplasia1
Not AvailableCompletedOtherInfertilities1
Not AvailableCompletedTreatmentEndometriotic Cysts1
Not AvailableCompletedTreatmentFertility Preservation / Infertilities / Oocyte Donation / Ovulation induction therapy / Vitrification1
Not AvailableCompletedTreatmentInfertilities4
Not AvailableCompletedTreatmentSGA and Growth1
Not AvailableCompletedTreatmentUterine Leiomyomas1
Not AvailableEnrolling by InvitationScreeningInfertility, Female / Single Nucleotide Polymorphism,GnRH Receptor, IVF1
Not AvailableNot Yet RecruitingNot AvailableBreast Cancer1
Not AvailableNot Yet RecruitingDiagnosticInvitro Fertilization1
Not AvailableNot Yet RecruitingTreatmentOvarian Hyperstimulation Syndrome1
Not AvailableRecruitingNot AvailableAndrogen Deprivation Therapy / Metastatic Hormone Refractory Prostate Cancer1
Not AvailableRecruitingNot AvailableProstate Cancer1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Hyperinsulinemia / Hypogonadotropic Hypogonadotropism / Infertilities1
Not AvailableRecruitingDiagnosticBMI >30 kg/m2 / Fertility1
Not AvailableRecruitingDiagnosticGonadotrophin releasing hormone deficiency / Idiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
Not AvailableRecruitingDiagnosticIVF Treatment1
Not AvailableRecruitingDiagnosticProstate Cancer1
Not AvailableRecruitingHealth Services ResearchCongenital Uterine Anomalies / Endometriosis / Extrauterine Pregnancy / Female Infertility - Cervical/Vaginal / Female Infertility Due to Ovulatory Disorder / Female Infertility Due to Tubal Block / Female Infertility Due to Tubal Occlusion / Female Infertility Endocrine / Female Infertility of Other Origin / Female Infertility of Tubal Origin / Hydrosalpinx / Infections Uterine / Infertility, Female / Leiomyomas / Polycystic Ovaries Syndrome / Premature Ovarian Failure (POF) / Salpingitis1
Not AvailableRecruitingOtherEmbryonic Quality Using MitoScore (DuoStim x Conventional Stimulation Protocol) / Infertility, Female / Potential Usefulness of the DuoStim Protocol / Rate of Euploid Embryos Per Cycle (DuoStim x Conventional Stimulation Protocol)1
Not AvailableRecruitingTreatmentClinical Pregnancy Rate1
Not AvailableRecruitingTreatmentClinical Pregnancy Rate / Ovulation induction therapy1
Not AvailableRecruitingTreatmentEndometriosis1
Not AvailableRecruitingTreatmentInfertilities / IVF / Preimplantation Diagnosis1
Not AvailableRecruitingTreatmentIdiopathic Hypogonadotropic Hypogonadism1
Not AvailableRecruitingTreatmentInfertilities1
Not AvailableRecruitingTreatmentProstate Cancer1
Not AvailableTerminatedNot AvailableGender Dysphoria1
Not AvailableTerminatedTreatmentAssisted Reproductive Technology therapy / Diminished Ovarian Reserve (DOR) / Infertilities1
Not AvailableUnknown StatusNot AvailableInvitro Fertilization / Ovarian Hyperstimulation Syndrome / Polycystic Ovarian Syndrome1
Not AvailableUnknown StatusBasic ScienceIn Vitro Fertilization Protocols / Infertilities1
Not AvailableUnknown StatusDiagnosticPuberty, Precocious1
Not AvailableUnknown StatusPreventionInfertile High-risk Patients With Polycystic Ovaries1
Not AvailableUnknown StatusTreatmentBMI >30 kg/m2 / Insulin Resistance1
Not AvailableUnknown StatusTreatmentComplications Associated With Artificial Fertilization / Female Infertility Due to Nonimplantation of Ovum1
Not AvailableUnknown StatusTreatmentImplantation, Embryo1

Pharmacoeconomics

Manufacturers
  • Ferring pharmaceuticals inc
  • Baxter healthcare corp anesthesia critical care
Packagers
  • Hospira Inc.
  • Intervet International
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous; Subcutaneous
PowderNot applicable1 g/1g
Liquid; powder, for solutionIntravenous; Subcutaneous
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
water solubility1 mg/mLNot Available
logP-3.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0588 mg/mLALOGPS
logP-0.09ALOGPS
logP-6.3ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)9.47ChemAxon
pKa (Strongest Basic)11.16ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count17ChemAxon
Hydrogen Donor Count16ChemAxon
Polar Surface Area474.63 Å2ChemAxon
Rotatable Bond Count31ChemAxon
Refractivity302.51 m3·mol-1ChemAxon
Polarizability121.19 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9695
Blood Brain Barrier-0.9781
Caco-2 permeable-0.8941
P-glycoprotein substrateSubstrate0.8607
P-glycoprotein inhibitor INon-inhibitor0.8452
P-glycoprotein inhibitor IINon-inhibitor0.7859
Renal organic cation transporterNon-inhibitor0.6797
CYP450 2C9 substrateNon-substrate0.769
CYP450 2D6 substrateNon-substrate0.7647
CYP450 3A4 substrateSubstrate0.5996
CYP450 1A2 substrateNon-inhibitor0.842
CYP450 2C9 inhibitorNon-inhibitor0.8493
CYP450 2D6 inhibitorNon-inhibitor0.9054
CYP450 2C19 inhibitorNon-inhibitor0.8136
CYP450 3A4 inhibitorNon-inhibitor0.7529
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9411
Ames testNon AMES toxic0.6992
CarcinogenicityNon-carcinogens0.7961
BiodegradationNot ready biodegradable0.9933
Rat acute toxicity2.6799 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9038
hERG inhibition (predictor II)Non-inhibitor0.5274
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 polypeptides. These are peptides containing ten or more amino acid residues.
Kingdom
Organic compounds
Super Class
Organic Polymers
Class
Polypeptides
Sub Class
Not Available
Direct Parent
Polypeptides
Alternative Parents
Peptides / Tyrosine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Leucine and derivatives / N-acyl-alpha amino acids and derivatives / Proline and derivatives / Tryptamines and derivatives / Serine and derivatives / Alpha amino acid amides
show 23 more
Substituents
Polypeptide / Alpha peptide / Tyrosine or derivatives / Phenylalanine or derivatives / Histidine or derivatives / Leucine or derivatives / N-acyl-alpha amino acid or derivatives / Proline or derivatives / Triptan / Alpha-amino acid amide
show 48 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Gonadotropin-releasing hormone [KO:K05252] (C07607)

Targets

Kind
Protein
Organism
Humans
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. Lu ZL, Gallagher R, Sellar R, Coetsee M, Millar RP: Mutations remote from the human gonadotropin-releasing hormone (GnRH) receptor-binding sites specifically increase binding affinity for GnRH II but not GnRH I: evidence for ligand-selective, receptor-active conformations. J Biol Chem. 2005 Aug 19;280(33):29796-803. Epub 2005 Jun 20. [PubMed:15967801]
  2. Moles G, Carrillo M, Mananos E, Mylonas CC, Zanuy S: Temporal profile of brain and pituitary GnRHs, GnRH-R and gonadotropin mRNA expression and content during early development in European sea bass (Dicentrarchus labrax L.). Gen Comp Endocrinol. 2007 Jan 1;150(1):75-86. Epub 2006 Sep 8. [PubMed:16962597]
  3. Mamputha S, Lu ZL, Roeske RW, Millar RP, Katz AA, Flanagan CA: Conserved amino acid residues that are important for ligand binding in the type I gonadotropin-releasing hormone (GnRH) receptor are required for high potency of GnRH II at the type II GnRH receptor. Mol Endocrinol. 2007 Jan;21(1):281-92. Epub 2006 Sep 14. [PubMed:16973761]
  4. Lee PA, Houk CP: Gonadotropin-releasing hormone analog therapy for central precocious puberty and other childhood disorders affecting growth and puberty. Treat Endocrinol. 2006;5(5):287-96. [PubMed:17002488]
  5. Bliss SP, Navratil AM, Breed M, Skinner DC, Clay CM, Roberson MS: Signaling complexes associated with the type I gonadotropin-releasing hormone (GnRH) receptor: colocalization of extracellularly regulated kinase 2 and GnRH receptor within membrane rafts. Mol Endocrinol. 2007 Feb;21(2):538-49. Epub 2006 Oct 26. [PubMed:17068198]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Gonadotropin-releasing hormone receptor activity
Specific Function
Putative receptor for gonadotropin releasing hormone II (GnRH II) which is most probably non-functional.
Gene Name
GNRHR2
Uniprot ID
Q96P88
Uniprot Name
Putative gonadotropin-releasing hormone II receptor
Molecular Weight
32536.935 Da
References
  1. Morgan K, Sellar R, Pawson AJ, Lu ZL, Millar RP: Bovine and ovine gonadotropin-releasing hormone (GnRH)-II ligand precursors and type II GnRH receptor genes are functionally inactivated. Endocrinology. 2006 Nov;147(11):5041-51. Epub 2006 Aug 17. [PubMed:16916952]
  2. Mamputha S, Lu ZL, Roeske RW, Millar RP, Katz AA, Flanagan CA: Conserved amino acid residues that are important for ligand binding in the type I gonadotropin-releasing hormone (GnRH) receptor are required for high potency of GnRH II at the type II GnRH receptor. Mol Endocrinol. 2007 Jan;21(1):281-92. Epub 2006 Sep 14. [PubMed:16973761]
  3. Montagnani Marelli M, Moretti RM, Januszkiewicz-Caulier J, Motta M, Limonta P: Gonadotropin-releasing hormone (GnRH) receptors in tumors: a new rationale for the therapeutical application of GnRH analogs in cancer patients? Curr Cancer Drug Targets. 2006 May;6(3):257-69. [PubMed:16712461]
  4. Li JH, Choe H, Wang AF, Maiti K, Wang C, Salam A, Chun SY, Lee WK, Kim K, Kwon HB, Seong JY: Extracellular loop 3 (EL3) and EL3-proximal transmembrane helix 7 of the mammalian type I and type II gonadotropin-releasing hormone (GnRH) receptors determine differential ligand selectivity to GnRH-I and GnRH-II. Mol Pharmacol. 2005 Apr;67(4):1099-110. Epub 2005 Jan 5. [PubMed:15635044]
  5. Silver MR, Sower SA: Functional characterization and kinetic studies of an ancestral lamprey GnRH-III selective type II GnRH receptor from the sea lamprey, Petromyzon marinus. J Mol Endocrinol. 2006 Jun;36(3):601-10. [PubMed:16720727]

Drug created on June 13, 2005 07:24 / Updated on November 13, 2019 18:22