All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

degarelix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Drug dosage:

Dose	Unit	Route
2.70	mg	P

ADMET properties:

Property	Value	Reference
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
t_half (Half-life)	18.60 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

Date	Agency	Company	Orphan
Dec. 24, 2008	FDA	FERRING
June 26, 2012	PMDA	Astellas Pharma Inc.
Sept. 29, 2023	EMA	ACCORD HEALTHCARE S.L.U.

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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	317.39	19.64	125	7829	20070	42593311
Injection site pain	283.70	19.64	160	7794	57638	42555743
Prostatic specific antigen increased	235.47	19.64	96	7858	16829	42596552
Hot flush	216.09	19.64	98	7856	22253	42591128
Injection site swelling	208.17	19.64	88	7866	16885	42596496
Injection site induration	154.94	19.64	47	7907	3440	42609941
Osteonecrosis of jaw	142.45	19.64	70	7884	18979	42594402
Injection site mass	96.94	19.64	42	7912	8533	42604848
Injection site nodule	82.77	19.64	26	7928	2135	42611246
Injection site reaction	72.81	19.64	42	7912	15679	42597702
Injection site cellulitis	71.70	19.64	18	7936	648	42612733
Metastases to bone	69.74	19.64	40	7914	14769	42598612
Interstitial lung disease	62.39	19.64	75	7879	78387	42534994
Injection site warmth	61.75	19.64	22	7932	2661	42610720
Prostatic specific antigen abnormal	61.24	19.64	17	7937	907	42612474
Hypocalcaemia	50.14	19.64	43	7911	30130	42583251
Injection site inflammation	45.01	19.64	14	7940	1112	42612269
Prostate cancer metastatic	42.59	19.64	22	7932	6607	42606774
Necrotising retinitis	37.81	19.64	12	7942	1018	42612363
Injection site abscess	37.79	19.64	12	7942	1020	42612361
Blood testosterone abnormal	35.56	19.64	10	7944	559	42612822
Malignant neoplasm progression	34.81	19.64	68	7886	108332	42505049
Hormone-dependent prostate cancer	32.93	19.64	6	7948	43	42613338
Blood testosterone increased	32.87	19.64	12	7942	1555	42611826
Toxicity to various agents	31.89	19.64	3	7951	229133	42384248
Infusion site plaque	31.82	19.64	5	7949	12	42613369
Prescribed underdose	31.19	19.64	21	7933	10261	42603120
Hormone-refractory prostate cancer	29.97	19.64	10	7944	994	42612387
Drug ineffective	28.75	19.64	46	7908	630151	41983230
Injection site discomfort	28.18	19.64	12	7942	2334	42611047
Hepatic function abnormal	28.11	19.64	41	7913	51526	42561855
Product administered at inappropriate site	28.06	19.64	13	7941	3085	42610296
Prostate cancer	28.05	19.64	38	7916	44605	42568776
Decreased appetite	24.99	19.64	86	7868	193051	42420330
Fatigue	24.10	19.64	151	7803	435490	42177891
Urethral obstruction	23.82	19.64	6	7948	219	42613162
Urinary retention	23.64	19.64	34	7920	42180	42571201
Wrong technique in product usage process	23.38	19.64	34	7920	42601	42570780
Toxic cataract	23.18	19.64	4	7950	20	42613361
Bone pain	22.67	19.64	25	7929	23767	42589614
Metastases to liver	22.61	19.64	21	7933	16305	42597076
Syringe issue	22.48	19.64	16	7938	8540	42604841
Cerebral amyloid angiopathy	22.39	19.64	6	7948	280	42613101
Postrenal failure	22.26	19.64	7	7947	576	42612805
Metastases to spine	22.06	19.64	11	7943	3066	42610315
Spinal cord infarction	21.35	19.64	7	7947	659	42612722
Product lot number issue	20.86	19.64	4	7950	39	42613342
Metastases to lymph nodes	20.01	19.64	13	7941	5985	42607396
Mucocutaneous disorder	20.00	19.64	5	7949	177	42613204

FDA Adverse Event Reporting System (Geriatric)

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	275.85	19.92	76	6582	12435	110570206
Injection site erythema	184.74	19.92	97	6561	94079	110488562
Injection site pain	169.50	19.92	115	6543	177807	110404834
Hot flush	161.55	19.92	79	6579	65957	110516684
Osteonecrosis of jaw	140.52	19.92	65	6593	47952	110534689
Injection site swelling	127.82	19.92	66	6592	61724	110520917
Injection site induration	111.37	19.92	37	6621	11346	110571295
Interstitial lung disease	78.78	19.92	66	6592	139268	110443373
Injection site mass	74.09	19.92	34	6624	24579	110558062
Injection site cellulitis	62.21	19.92	16	6642	2004	110580637
Injection site nodule	61.46	19.92	19	6639	4627	110578014
Hypocalcaemia	59.13	19.92	41	6617	65325	110517316
Prostate cancer metastatic	56.16	19.92	18	6640	4925	110577716
Prostate cancer	55.06	19.92	32	6626	37609	110545032
Metastases to bone	54.91	19.92	30	6628	31342	110551299
Necrotising retinitis	46.04	19.92	12	6646	1584	110581057
Prostatic specific antigen abnormal	45.05	19.92	10	6648	669	110581972
Injection site abscess	43.32	19.92	12	6646	1994	110580647
Urinary retention	39.32	19.92	33	6625	69650	110512991
Hormone-refractory prostate cancer	36.98	19.92	9	6649	901	110581740
Infusion site plaque	36.66	19.92	5	6653	15	110582626
Malignant neoplasm progression	35.52	19.92	48	6610	174519	110408122
Hepatic function abnormal	34.15	19.92	34	6624	89261	110493380
Injection site warmth	31.44	19.92	17	6641	17388	110565253
Hormone-dependent prostate cancer	30.88	19.92	6	6652	208	110582433
Injection site inflammation	29.40	19.92	11	6647	4760	110577881
Decreased appetite	28.96	19.92	78	6580	475768	110106873
Urethral obstruction	28.74	19.92	6	6652	300	110582341
Prostatic specific antigen decreased	28.62	19.92	5	6653	95	110582546
Syringe issue	28.16	19.92	13	6645	9512	110573129
Toxic cataract	27.71	19.92	4	6654	20	110582621
Postrenal failure	27.27	19.92	7	6651	869	110581772
Rhabdomyolysis	25.85	19.92	34	6624	120367	110462274
Spinal cord infarction	25.71	19.92	7	6651	1091	110581550
Intercepted product preparation error	25.59	19.92	11	6647	6809	110575832
Cerebral amyloid angiopathy	25.18	19.92	6	6652	549	110582092
Metastases to spine	24.70	19.92	10	6648	5333	110577308
Mucocutaneous disorder	24.66	19.92	5	6653	216	110582425
Wrong technique in product usage process	24.12	19.92	28	6630	87320	110495321
Blood testosterone increased	24.01	19.92	7	6651	1395	110581246
Retinal detachment	23.33	19.92	12	6646	11088	110571553
Cerebral infarction	22.18	19.92	21	6637	51817	110530824
Drug ineffective	22.18	19.92	36	6622	1520504	109062137
Disseminated intravascular coagulation	22.15	19.92	19	6639	41267	110541374
Fall	20.42	19.92	81	6577	603401	109979240

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L02BX02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Other hormone antagonists and related agents
FDA PE	N0000008638	Decreased GnRH Secretion
FDA MoA	N0000175084	Gonadotropin Releasing Hormone Receptor Antagonists
FDA EPC	N0000175839	Gonadotropin Releasing Hormone Receptor Antagonist
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

L02BX Other hormone antagonists and related agents 3 drugs

abarelixabiraterone acetaterelugolix

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

Disease	Relation	SNOMED_ID	DOID
Advanced hormone-dependent prostate cancer	indication	722103009
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
Congenital long QT syndrome	contraindication	442917000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.99	acidic
pKa2	11.49	acidic
pKa3	12.21	acidic
pKa4	12.25	acidic
pKa5	12.82	acidic
pKa6	13.11	acidic
pKa7	13.11	acidic
pKa8	13.39	acidic
pKa9	13.47	acidic
pKa10	13.85	acidic
pKa11	9.64	Basic
pKa12	5.35	Basic

Orange Book patent data (new drug applications)

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 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 120MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	12514898	Feb. 20, 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	12533387	Feb. 20, 2029	TREATMENT OF ADVANCED PROSTATE CANCER
EQ 80MG BASE/VIAL	FIRMAGON	FERRING	N022201	Dec. 24, 2008	RX	POWDER	SUBCUTANEOUS	12514898	Feb. 20, 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	12533387	Feb. 20, 2029	TREATMENT OF ADVANCED PROSTATE CANCER
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	11766468	April 27, 2032	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	11826397	April 27, 2032	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	9415085	April 27, 2032	METHOD OF TREATING PROSTATE CANCER
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	11766468	April 27, 2032	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	11826397	April 27, 2032	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	9415085	April 27, 2032	METHOD OF TREATING PROSTATE CANCER

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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

External reference:

ID	Source
D08635	KEGG_DRUG
4028567	VUID
N0000178334	NUI
934246-14-7	SECONDARY_CAS_RN
4028567	VANDF
C1455035	UMLSCUI
CHEMBL415606	ChEMBL_ID
CHEMBL2028987	ChEMBL_ID
DB06699	DRUGBANK_ID
C431566	MESH_SUPPLEMENTAL_RECORD_UI
5585	IUPHAR_LIGAND_ID
8192	INN_ID
SX0XJI3A11	UNII
16136245	PUBCHEM_CID
475230	RXNORM
164686	MMSL
168716	MMSL
26319	MMSL
d07411	MMSL
012979	NDDF
012980	NDDF
16526211000001104	SNOMEDCT_US
441758000	SNOMEDCT_US
441864003	SNOMEDCT_US
CHEBI:135961	CHEBI
SX0XJI3A11	INXIGHT DRUGS

Pharmaceutical products:

None