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 disorderThyroid peroxidaseP07202T51120Not Available
Thyroid disorderProtein bric-a-brac 2Q9W0K4Not AvailableNot Available
Thyroid disorderAnti-thyroglobulin heavy chain variable regionQ8IZD7Not 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)
Sleep disorder19.02.04.001--Not Available
Somnolence19.02.05.003; 17.02.04.006--
Spinal fracture15.08.05.001; 12.04.04.002--
Spinal osteoarthritis15.01.04.003--Not Available
Suicidal ideation19.12.01.003--
Swelling08.01.03.015--Not Available
Swelling face23.04.01.018; 10.01.05.018--Not Available
Syncope24.06.02.012; 17.02.04.008; 02.01.02.008--
Tachycardia02.03.02.007--Not Available
Tearfulness19.15.02.005--Not Available
Tenderness08.01.08.005--Not Available
Tenosynovitis15.07.01.004--Not Available
Tension19.06.02.005--Not Available
Testicular atrophy21.13.01.001; 05.05.02.004--Not Available
Testicular pain21.13.01.005--
Thrombosis24.01.01.006--Not Available
Thyroid neoplasm16.24.01.002; 05.02.05.002--Not Available
Tinnitus04.04.01.002; 17.04.07.004--
Transient ischaemic attack24.04.06.005; 17.08.04.001--
Tremor17.01.06.002--
Ulcer08.03.06.001--Not Available
Urinary incontinence20.02.02.010; 17.05.01.008--
Urinary retention20.02.02.011--
Urinary tract disorder20.08.01.001--Not Available
Urinary tract infection20.08.02.001; 11.01.14.004--
Urticaria23.04.02.001; 10.01.06.001--
Vaginal discharge21.08.02.002--
Vaginal haemorrhage24.07.03.005; 21.08.01.001--
Vaginal infection21.14.02.002; 11.01.10.002--
Vaginal inflammation21.14.02.001--
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