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

Stem definition	Drug id	CAS RN
gonadotropin-releasing-hormone (GnRH) inhibitors, peptides	4379	214766-78-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: degarelix firmagon degarelix acetate	FE-200486 is the acetate salt Molecular weight: 1632.29 Formula: C82H103ClN18O16 CLOGP: -0.74 LIPINSKI: 3 HAC: 34 HDO: 17 TPSA: 512.87 ALOGS: -5.60 ROTB: 41

Molecule

Description

Molfile Inchi Smiles

Synonyms:

degarelix
firmagon
degarelix acetate

FE-200486 is the acetate salt

Molecular weight: 1632.29
Formula: C82H103ClN18O16
CLOGP: -0.74
LIPINSKI: 3
HAC: 34
HDO: 17
TPSA: 512.87
ALOGS: -5.60
ROTB: 41

Drug dosage:

Dose	Unit	Route
2.70	mg	P

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	18.60 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.74 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.68 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.10 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 24, 2008	FDA	FERRING
June 26, 2012	PMDA	Astellas Pharma Inc.

FDA Adverse Event Reporting System (Female)

None

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
Injection site erythema	340.79	20.57	123	6316	15776	34934716
Injection site pain	314.59	20.57	150	6289	38855	34911637
Injection site swelling	216.57	20.57	81	6358	11446	34939046
Prostatic specific antigen increased	204.41	20.57	83	6356	14597	34935895
Injection site induration	169.28	20.57	48	6391	2812	34947680
Hot flush	162.37	20.57	75	6364	17991	34932501
Osteonecrosis of jaw	132.42	20.57	65	6374	17824	34932668
Injection site mass	100.92	20.57	40	6399	6586	34943906
Injection site nodule	85.11	20.57	25	6414	1658	34948834
Injection site reaction	77.87	20.57	41	6398	12992	34937500

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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
Prostatic specific antigen increased	236.40	21.75	66	5208	10320	79728794
Injection site erythema	184.53	21.75	94	5180	78103	79661011
Injection site pain	177.53	21.75	109	5165	129729	79609385
Osteonecrosis of jaw	135.05	21.75	63	5211	43163	79695951
Injection site swelling	126.84	21.75	62	5212	47070	79692044
Injection site induration	117.42	21.75	38	5236	9781	79729333
Hot flush	109.44	21.75	59	5215	54818	79684296
Injection site mass	74.28	21.75	33	5241	20151	79718963
Injection site nodule	63.57	21.75	19	5255	3761	79735353
Interstitial lung disease	58.66	21.75	53	5221	112547	79626567

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L02BX02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents
FDA EPC	N0000175839	Gonadotropin Releasing Hormone Receptor Antagonist
FDA MoA	N0000175084	Gonadotropin Releasing Hormone Receptor Antagonists
FDA PE	N0000008638	Decreased GnRH Secretion

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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
Advanced Prostatic Carcinoma	indication
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Chronic heart failure	contraindication	48447003
Prolonged QT interval	contraindication	111975006
Liver function tests abnormal	contraindication	166603001
Hypomagnesemia	contraindication	190855004
Disease of liver	contraindication	235856003	DOID:409
Pregnancy, function	contraindication	289908002
Osteopenia	contraindication	312894000

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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	10.99	acidic
pKa10	13.85	acidic
pKa11	9.64	Basic
pKa12	5.35	Basic
pKa2	11.49	acidic
pKa3	12.21	acidic
pKa4	12.25	acidic
pKa5	12.82	acidic
pKa6	13.11	acidic
pKa7	13.11	acidic

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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
EQ 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10729739	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10973870	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	9579359	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10695398	April 27, 2032	METHOD OF TREATING PROSTATE CANCER
EQ 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	9415085	April 27, 2032	METHOD OF TREATING PROSTATE CANCER
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10729739	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10973870	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	9579359	Feb. 10, 2029	TREATMENT OF ADVANCED PROSTATE CANCER WITH A REDUCED LIKELIHOOD OF CAUSING A GONADOTROPHIN RELEASING HORMONE AGONIST SIDE-EFFECT
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	10695398	April 27, 2032	METHOD OF TREATING PROSTATE CANCER
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	9415085	April 27, 2032	METHOD OF TREATING PROSTATE CANCER

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Orange Book exclusivity data (new drug applications)

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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	ANTAGONIST	Ki	8.77		IUPHAR	CHEMBL

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External reference:

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ID	Source
012979	NDDF
012980	NDDF
16136245	PUBCHEM_CID
164686	MMSL
168716	MMSL
26319	MMSL
4028567	VUID
4028567	VANDF
441758000	SNOMEDCT_US
441864003	SNOMEDCT_US

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Pharmaceutical products:

None