leuprorelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
pituitary hormone-release stimulating peptides	1559	53714-56-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: leuprorelin leuprolide acetate eligard leupline leuprolide leuprorelin acetate leuprorelin mesilate	A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. Molecular weight: 1209.42 Formula: C59H84N16O12 CLOGP: -3.18 LIPINSKI: 3 HAC: 28 HDO: 16 TPSA: 429.04 ALOGS: -4.55 ROTB: 32 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

leuprorelin
leuprolide acetate
eligard
leupline
leuprolide
leuprorelin acetate
leuprorelin mesilate

A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.

Molecular weight: 1209.42
Formula: C59H84N16O12
CLOGP: -3.18
LIPINSKI: 3
HAC: 28
HDO: 16
TPSA: 429.04
ALOGS: -4.55
ROTB: 32

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
60	mcg	implant
1	mg	P
0.13	mg	P

ADMET properties:

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Property	Value	Reference
S (Water solubility)	66.66 mg/mL	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	2.90 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.54 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.38 L/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.01 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
April 9, 1985	FDA
May 24, 2022	EMA	ACCORD HEALTHCARE S.L.U.

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intercepted product preparation error	965.68	17.58	162	13924	535	63474401
Syringe issue	753.61	17.58	165	13921	2704	63472232
Hot flush	753.19	17.58	317	13769	50842	63424094
Device leakage	504.07	17.58	143	13943	6953	63467983
Occupational exposure to product	401.31	17.58	93	13993	1985	63472951
Pelvic pain	382.55	17.58	135	13951	13384	63461552
Ovarian hyperstimulation syndrome	368.62	17.58	99	13987	3915	63471021
Off label use	309.47	17.58	541	13545	673921	62801015
Vaginal haemorrhage	283.62	17.58	133	13953	27354	63447582
Heavy menstrual bleeding	205.16	17.58	93	13993	17680	63457256

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intercepted product preparation error	19156.83	13.92	3629	56648	449	34896205
Syringe issue	16475.73	13.92	3378	56899	2286	34894368
Device leakage	12708.38	13.92	2801	57476	3774	34892880
Wrong technique in product usage process	5891.54	13.92	2239	58038	33747	34862907
Prostatic specific antigen increased	2739.25	13.92	1008	59269	13672	34882982
Hot flush	2567.27	13.92	1017	59260	17049	34879605
Product physical consistency issue	2197.63	13.92	437	59840	177	34896477
Blood testosterone abnormal	989.87	13.92	213	60064	225	34896429
Death	928.92	13.92	2080	58197	395969	34500685
Intercepted medication error	822.52	13.92	188	60089	320	34896334

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intercepted product preparation error	16225.99	13.03	2694	52482	866	79688346
Syringe issue	13403.57	13.03	2494	52682	3804	79685408
Device leakage	9993.47	13.03	2138	53038	8718	79680494
Wrong technique in product usage process	4038.61	13.03	1616	53560	72259	79616953
Prostatic specific antigen increased	2743.48	13.03	749	54427	9637	79679575
Product physical consistency issue	1733.52	13.03	329	54847	576	79688636
Hot flush	1724.50	13.03	814	54362	54063	79635149
Blood testosterone abnormal	672.87	13.03	121	55055	127	79689085
Intercepted medication error	630.71	13.03	143	55033	786	79688426
Blood testosterone increased	623.60	13.03	145	55031	907	79688305

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L02AE02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONES AND RELATED AGENTS Gonadotropin releasing hormone analogues
ATC	L02AE51	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONES AND RELATED AGENTS Gonadotropin releasing hormone analogues
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:50751	anti-estrogenic drug
CHEBI has role	CHEBI:63533	gonadotropin releasing hormone agonists
FDA EPC	N0000175655	Gonadotropin Releasing Hormone Receptor Agonist
FDA MoA	N0000175654	Gonadotropin Releasing Hormone Receptor Agonists
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018931	Antineoplastic Agents, Hormonal
MeSH PA	D005300	Fertility Agents, Female

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Endometriosis	indication	129103003
Precocious puberty	indication	400179000
Anemia due to Bleeding Uterine Leiomyoma	indication
Advanced Prostatic Carcinoma	indication
Malignant tumor of ovary	off-label use	363443007	DOID:2394
Urinary tract obstruction	contraindication	7163005	DOID:5200
Hypercholesterolemia	contraindication	13644009
Myocardial infarction	contraindication	22298006	DOID:5844
Hypertensive disorder	contraindication	38341003	DOID:10763
Diabetes mellitus	contraindication	73211009	DOID:9351

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.65	acidic
pKa2	11.9	acidic
pKa3	12.73	acidic
pKa4	13.09	acidic
pKa5	13.39	acidic
pKa6	13.69	acidic
pKa7	10.75	Basic
pKa8	6.69	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
22.5MG	ELIGARD KIT	TOLMAR	N021379	July 24, 2002	RX	POWDER	SUBCUTANEOUS	8470359	Oct. 15, 2023	METHOD OF TREATING CANCER
30MG	ELIGARD KIT	TOLMAR	N021488	Feb. 13, 2003	RX	POWDER	SUBCUTANEOUS	8470359	Oct. 15, 2023	METHOD OF TREATING CANCER
45MG	ELIGARD KIT	TOLMAR	N021731	Dec. 14, 2004	RX	POWDER	SUBCUTANEOUS	8470359	Oct. 15, 2023	METHOD OF TREATING CANCER
45MG	FENSOLVI KIT	TOLMAR	N213150	May 1, 2020	RX	POWDER	SUBCUTANEOUS	8470359	Oct. 15, 2023	METHOD OF TREATING PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH CENTRAL PRECOCIOUS PUBERTY
45MG	LUPRON DEPOT-PED KIT	ABBVIE ENDOCRINE INC	N020263	April 14, 2023	RX	POWDER	INTRAMUSCULAR	9617303	March 22, 2028	TREATMENT OF PEDIATRIC PATIENTS WITH CENTRAL PRECOCIOUS PUBERTY
45MG	LUPRON DEPOT	ABBVIE ENDOCRINE INC	N020517	June 17, 2011	RX	INJECTABLE	INJECTION	8921326	Feb. 5, 2031	PALLIATIVE TREATMENT OF PROSTATE CANCER

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
45MG	FENSOLVI KIT	TOLMAR	N213150	May 1, 2020	RX	POWDER	SUBCUTANEOUS	May 1, 2023	TREATMENT OF PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH CENTRAL PRECOCIOUS PUBERTY (CPP)
45MG	LUPRON DEPOT-PED KIT	ABBVIE ENDOCRINE INC	N020263	April 14, 2023	RX	POWDER	INTRAMUSCULAR	April 14, 2026	NEW STRENGTH

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Gonadotropin-releasing hormone receptor	GPCR	P30968	GNRHR_HUMAN	AGONIST	IC50	9.52		WOMBAT-PK	CHEMBL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_RAT		IC50	9.30		CHEMBL

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External reference:

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ID	Source
002675	NDDF
004751	NDDF
008314	NDDF
008315	NDDF
1175	IUPHAR_LIGAND_ID
11929	MMSL
203217	RXNORM
350364005	SNOMEDCT_US
37JNS02E7V	UNII
397198002	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Eligard	HUMAN PRESCRIPTION DRUG LABEL	1	62935-227	INJECTION, SUSPENSION, EXTENDED RELEASE	22.50 mg	SUBCUTANEOUS	NDA	26 sections
Eligard	HUMAN PRESCRIPTION DRUG LABEL	1	62935-306	INJECTION, SUSPENSION, EXTENDED RELEASE	30 mg	SUBCUTANEOUS	NDA	26 sections
Eligard	HUMAN PRESCRIPTION DRUG LABEL	1	62935-461	INJECTION, SUSPENSION, EXTENDED RELEASE	45 mg	SUBCUTANEOUS	NDA	26 sections
Eligard	HUMAN PRESCRIPTION DRUG LABEL	1	62935-756	INJECTION, SUSPENSION, EXTENDED RELEASE	7.50 mg	SUBCUTANEOUS	NDA	26 sections
Fensolvi	HUMAN PRESCRIPTION DRUG LABEL	1	62935-163	INJECTION, SUSPENSION, EXTENDED RELEASE	45 mg	SUBCUTANEOUS	NDA	25 sections
Leuprolide Acetate	HUMAN PRESCRIPTION DRUG LABEL	1	0185-7400	INJECTION, SOLUTION	1 mg	SUBCUTANEOUS	ANDA	25 sections

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