Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Leuprolide acetate
Drug ID BADD_D01260
Description Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours.[A203222] As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.[A203126, A203132] Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename Lupron™ by Abbvie Endocrine Inc.[L13850] Since this initial approval, various long-acting intramuscular and subcutaneous products have been developed such that patients can be dosed once every six months.[L13781, L13790] Leuprolide remains frontline therapy in all conditions for which it is indicated for use.
Indications and Usage For treatment of prostate cancer, endometriosis, uterine fibroids and premature puberty
Marketing Status Prescription; Discontinued
ATC Code L02AE02
DrugBank ID DB00007
KEGG ID D00989
MeSH ID D016729
PubChem ID 657180
TTD Drug ID D04ASH
NDC Product Code 62935-453; 41701-013; 62935-303; 62756-346; 0074-3641; 11532-3680; 0074-3779; 0074-2108; 11532-1455; 0074-2440; 62935-753; 0074-3683; 60870-0425; 11532-1450; 72664-611; 11532-1453; 0074-3663; 0074-3346; 11532-1451; 11532-3338; 11532-1452; 0074-3473; 47335-936; 11532-1457; 0074-2282; 11532-1454; 11532-1456; 71052-620; 11532-3662; 38779-2629; 59651-089; 52416-122; 0074-9694; 62935-223; 62935-153; 63629-8821; 73569-006; 51927-0126; 0074-3642; 0781-4003; 54127-9002; 51927-0066
Synonyms Leuprolide | Leuprorelin | Enantone | Leuprolide Acetate | Acetate, Leuprolide | Leuprolide Monoacetate | Monoacetate, Leuprolide | Leuprolide, (L-Leu)-Isomer | Lupron | TAP-144 | TAP 144 | TAP144 | A-43818 | A 43818 | A43818 | Leuprolide, (DL-Leu)-Isomer
Chemical Information
Molecular Formula C61H88N16O14
CAS Registry Number 74381-53-6
SMILES CCNC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC2=CC=C( C=C2)O)NC(=O)C(CO)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C(CC5=CN=CN5)NC(=O)C6CCC(=O)N 6.CC(=O)O
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Thyroid disorderAnti-thyroglobulin heavy chain variable regionQ8IZD7Not AvailableNot Available
Thyroid disorderThyroid peroxidaseP07202T51120Not Available
Thyroid disorderProtein bric-a-brac 2Q9W0K4Not AvailableNot Available
Thyroid hyperfunction disordersThyroxine-binding globulinP05543Not AvailableNot Available
Thyroid hypofunction disordersThyroxine-binding globulinP05543Not AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Injection site pain12.07.03.011; 08.02.03.010--Not Available
Injection site reaction12.07.03.015; 08.02.03.014--
Injection site warmth08.02.03.036; 12.07.03.036--Not Available
Injury12.01.08.004--Not Available
Insomnia19.02.01.002; 17.15.03.002--
Irritability19.04.02.013; 08.01.03.011--
Joint effusion15.01.02.005--
Lethargy19.04.04.004; 17.02.04.003; 08.01.01.008--
Leukoderma23.05.02.001--Not Available
Libido decreased19.08.03.001; 21.03.02.005--
Loss of consciousness17.02.04.004--Not Available
Loss of libido19.08.03.003--Not Available
Lung infiltration22.01.02.004--Not Available
Malaise08.01.01.003--
Memory impairment19.20.01.003; 17.03.02.003--
Menopausal symptoms21.02.02.002--Not Available
Menstrual disorder21.01.01.004--Not Available
Metastases to spine16.22.02.007; 15.09.03.007--Not Available
Micturition urgency20.02.02.006--
Migraine24.03.05.003; 17.14.02.001--Not Available
Mood swings19.04.03.001--Not Available
Mucous membrane disorder08.01.06.004--Not Available
Multiple fractures15.08.02.005; 12.04.02.009--Not Available
Muscle atrophy17.05.03.004; 15.05.03.003--Not Available
Muscle spasms15.05.03.004--
Musculoskeletal pain15.03.04.007--
Myalgia15.05.02.001--
Myocardial infarction24.04.04.009; 02.02.02.007--
Myopathy15.05.05.001--Not Available
Nail disorder23.02.05.002--
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