Degarelix information

Degarelix
Clinical data
Trade names	Firmagon, others
Other names	FE-200486
AHFS/Drugs.com	Monograph
MedlinePlus	a609022
License data	EU EMA: by INN; US DailyMed: Degarelix; US FDA: Degarelix;
Pregnancy; category	AU: D; Contraindicated;
Routes of; administration	Subcutaneous injection
Drug class	GnRH analogue; GnRH antagonist; Antigonadotropin
ATC code	L02BX02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); UK: POM (Prescription only); US: ℞-only; EU: Rx-only; In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	30–40%
Protein binding	~90%
Metabolism	Subject to common peptidic degradation during passage through the hepato-biliary system; not a substrate for the human CYP450 system
Elimination half-life	23–61 days
Excretion	Feces: 70–80%; Urine: 20–30%
Identifiers
CAS Number	214766-78-6 ;
PubChem CID	16136245;
IUPHAR/BPS	5585;
DrugBank	DB06699 ;
ChemSpider	17292756 ;
UNII	SX0XJI3A11;
KEGG	D08901 ; D09400 ;
ChEMBL	ChEMBL264089 ;
ECHA InfoCard	100.234.843
Chemical and physical data
Formula	C82H103ClN18O16
Molar mass	1632.29 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc(cc2)NC(=O)N)NC(=O)[C@H](Cc3ccc(cc3)NC(=O)[C@@H]4CC(=O)NC(=O)N4)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc5cccnc5)NC(=O)[C@@H](Cc6ccc(cc6)Cl)NC(=O)[C@@H](Cc7ccc8ccccc8c7)NC(=O)C;
	InChI InChI=1S/C82H103ClN18O16/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+/m1/s1 ; Key:MEUCPCLKGZSHTA-XYAYPHGZSA-N ;
	(what is this?) (verify)

Degarelix, sold under the brand name Firmagon among others, is a hormonal therapy used in the treatment of prostate cancer.^[3]^[5]

Testosterone is a male hormone that promotes growth of many prostate tumours and therefore reducing circulating testosterone to very low (castration) levels is often the treatment goal in the management of advanced prostate cancer. Degarelix has an immediate onset of action, binding to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocking their interaction with GnRH. This induces a fast and profound reduction in luteinizing hormone (LH), follicle-stimulating hormone (FSH) and in turn, testosterone suppression.^[6]

^ ^a ^b "Degarelix (Firmagon) Use During Pregnancy". Drugs.com. 3 February 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
^ "Firmagon 120mg Injection - Summary of Product Characteristics (SmPC)". (emc). 15 January 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
^ ^a ^b "Firmagon- degarelix kit". DailyMed. 18 September 2019. Archived from the original on 12 August 2020. Retrieved 26 February 2020.
^ Cite error: The named reference Firmagon EPAR was invoked but never defined (see the help page).
^ "Degarelix Acetate Monograph for Professionals". Drugs.com. 7 October 2019. Archived from the original on 26 February 2020. Retrieved 25 February 2020.
^ Princivalle M, Broqua P, White R, Meyer J, Mayer G, Elliott L, et al. (March 2007). "Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist". The Journal of Pharmacology and Experimental Therapeutics. 320 (3): 1113–8. doi:10.1124/jpet.106.112326. PMID 17179469. S2CID 2892725.

[Drugs.com_pregnancy-1] "Degarelix (Firmagon) Use During Pregnancy". Drugs.com. 3 February 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.

[2] "Firmagon 120mg Injection - Summary of Product Characteristics (SmPC)". (emc). 15 January 2020. Archived from the original on 26 February 2020. Retrieved 25 February 2020.

[Firmagon_FDA_label-3] "Firmagon- degarelix kit". DailyMed. 18 September 2019. Archived from the original on 12 August 2020. Retrieved 26 February 2020.

[Firmagon_EPAR-4] Cite error: The named reference Firmagon EPAR was invoked but never defined (see the help page).

[5] "Degarelix Acetate Monograph for Professionals". Drugs.com. 7 October 2019. Archived from the original on 26 February 2020. Retrieved 25 February 2020.

[PrincivalleBroqua2007-6] Princivalle M, Broqua P, White R, Meyer J, Mayer G, Elliott L, et al. (March 2007). "Rapid suppression of plasma testosterone levels and tumor growth in the dunning rat model treated with degarelix, a new gonadotropin-releasing hormone antagonist". The Journal of Pharmacology and Experimental Therapeutics. 320 (3): 1113–8. doi:10.1124/jpet.106.112326. PMID 17179469. S2CID 2892725.

Degarelix information

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