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)
Pituitary infarction05.03.04.006; 24.04.06.016; 18.02.02.004; 17.08.01.027--Not Available
Pleural rub22.02.08.009--Not Available
Pleuritic pain22.02.04.008--
Pneumonia22.07.01.003; 11.01.09.003--Not Available
Pollakiuria20.02.02.007--
Prostatic pain21.04.01.004--
Pruritus23.03.12.001--
Puberty26.03.01.003--Not Available
Pulmonary embolism24.01.06.001; 22.06.02.001--Not Available
Pulmonary fibrosis22.01.02.006--
Purpura24.07.06.005; 23.06.01.004; 01.01.04.003--
Pyuria11.01.08.043; 20.02.01.012--Not Available
Rales22.02.04.004--Not Available
Rash23.03.13.001--Not Available
Rectal polyp16.05.02.003; 07.20.01.005--Not Available
Red blood cell count decreased13.01.05.007--Not Available
Rhinitis22.07.03.006; 11.01.13.004--
Rhonchi22.02.04.005--Not Available
Seborrhoeic dermatitis23.03.04.018--Not Available
Seizure17.12.03.001--
Sensory loss17.02.07.007--Not Available
Shock24.06.02.002--Not Available
Sinus congestion22.04.06.001--Not Available
Sinusitis22.07.03.007; 11.01.13.005--
Skin cancer23.08.02.002; 16.03.02.002--Not Available
Skin disorder23.03.03.007--Not Available
Skin hypertrophy23.01.04.002--Not Available
Skin odour abnormal23.03.03.012--
Skin reaction23.03.03.013; 10.01.03.019--Not Available
Skin striae23.01.05.002--Not Available
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