U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Description
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/cdi/gonadorelin.html

Gonadorelin 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 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. Gonadorelin is used 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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.0 nM [IC50]
Target ID: Q96P88
Gene ID: NA
Gene Symbol: GNRHR2
Target Organism: Homo sapiens (Human)
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Diagnostic
FACTREL

Approved Use

Hypogonadism (diagnosis)—Gonadorelin as a single dose (gonadorelin test) is indicated for evaluation of the functional capacity and response of gonadotropes in the anterior pituitary in postpubertal patients who are suspected of having gonadotropin deficiency, whether due to hypothalamic function impairment alone or in combination with anterior pituitary function failure.

Launch Date

1982
Primary
FACTREL

Approved Use

Amenorrhea treatment

Launch Date

1982
PubMed

PubMed

TitleDatePubMed
[A case of fulminant hepatitis caused by antiandrogen, flutamide in a patient with prostate cancer].
1997 Jul
Cross talk in hormonally regulated gene transcription through induction of estrogen receptor ubiquitylation.
2005 Aug
Kisspeptin immunoreactive cells of the ovine preoptic area and arcuate nucleus co-express estrogen receptor alpha.
2006 Jul 3
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment: subcutaneous route is possible
Usual Adult Dose for Gonadotropin Deficiency 0.1 mg injected once subcutaneously or intravenously as a single dose. Usual Adult Dose for Amenorrhea 5 mcg every 90 minutes (range of 1 to 20 mcg) delivered intravenously by a pump over 1 minute, every ninety minutes for 21 days.
Route of Administration: Intravenous
In Vitro Use Guide
47 ng/ml Gonadorelin induced luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 5 ng, sc measured at 30 mins post dose by RIA (Rvb = 5.3 +/- 1.5 ng/ml)
Substance Class Mixture
Created
by admin
on Sat Dec 16 04:54:24 GMT 2023
Edited
by admin
on Sat Dec 16 04:54:24 GMT 2023
Record UNII
2RG1XQ1NYJ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GONADORELIN ACETATE
EP   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
GONADORELIN ACETATE [EP MONOGRAPH]
Common Name English
GONADORELIN ACETATE [USAN]
Common Name English
GONADORELIN ACETATE [JAN]
Common Name English
GONADORELIN ACETATE [USP MONOGRAPH]
Common Name English
GONADORELIN ACETATE [USP-RS]
Common Name English
GONADORELIN ACETATE [GREEN BOOK]
Common Name English
5-OXO-L-PROLYL-L-HISTIDYL-L-TRYPTOPHYL-L-SERYL-L-TYROSYLGLYCYL-L-LEUCYL-L-ARGINYL-L-PROLYLGLYCINAMIDE ACETATE (SALT) HYDRATE
Common Name English
GONADORELIN ACETATE [VANDF]
Common Name English
LUTEINIZING
Brand Name English
GONADORELIN ACETATE [ORANGE BOOK]
Common Name English
GONADORELIN ACETATE MIXTURE [MI]
Common Name English
GONADORELIN ACETATE (MIXTURE OF MONOACETATE AND DIACETATE HYDRATES)
Common Name English
ABBOTT-41070
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 17086
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
NCI_THESAURUS C1910
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
CFR 21 CFR 522.1073
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
Code System Code Type Description
RS_ITEM_NUM
1296756
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
CAS
78308-49-3
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
ALTERNATIVE
DAILYMED
2RG1XQ1NYJ
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
EVMPD
SUB14015MIG
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
MERCK INDEX
m5831
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY Merck Index
SMS_ID
100000089787
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
NCI_THESAURUS
C65814
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
ChEMBL
CHEMBL1007
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
RXCUI
204193
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY RxNorm
CAS
52699-48-6
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
FDA UNII
2RG1XQ1NYJ
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
DRUG BANK
DBSALT001155
Created by admin on Sat Dec 16 04:54:24 GMT 2023 , Edited by admin on Sat Dec 16 04:54:24 GMT 2023
PRIMARY
Related Record Type Details
IMPURITY -> PARENT
sum of impurities C and D: maximum 1.0 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
sum of impurities F and G: maximum 1.5 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
sum of impurities F and G: maximum 1.5 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
sum of impurities C and D: maximum 1.0 per cent
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Related Record Type Details
ACTIVE MOIETY
Definition References