DEGARELIX ACETATE ANHYDROUS

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C82H103ClN18O16.C2H4O2
Molecular Weight	1692.311
Optical Activity	UNSPECIFIED
Defined Stereocenters	11 / 11
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of DEGARELIX ACETATE ANHYDROUS

Structure Search

SMILES

CC(O)=O.[H][C@]1(CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC2=CC=C(NC(N)=O)C=C2)NC(=O)[C@H](CC3=CC=C(NC(=O)[C@@H]4CC(=O)NC(=O)N4)C=C3)NC(=O)[C@H](CO)NC(=O)[C@@H](CC5=CN=CC=C5)NC(=O)[C@@H](CC6=CC=C(Cl)C=C6)NC(=O)[C@@H](CC7=CC=C8C=CC=CC8=C7)NC(C)=O)C(=O)N[C@H](C)C(N)=O

InChI

InChIKey=AUTFSFUMNFDPLH-KYMMNHPFSA-N

InChI=1S/C82H103ClN18O16.C2H4O2/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;1-2(3)4/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);1H3,(H,3,4)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C2H4O2
Molecular Weight	60.052
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C82H103ClN18O16
Molecular Weight	1632.259
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	11 / 11
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://firmagon.com | https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022201s011lbl.pdf

DEGARELIX (FIRMAGON®) is a synthetic linear decapeptide amide containing seven unnatural amino acids, five of which are D-amino acids. It is a GnRH receptor antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release of gonadotropins and consequently testosterone. DEGARELIX (FIRMAGON®) is effective in achieving and maintaining testosterone suppression below the castration level of 50 ng/dL and is indicated for the treatment of patients with advanced prostate cancer.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Gonadotropin-releasing hormone receptor 41 Target ID: CHEMBL1855 Sources: http://www.ncbi.nlm.nih.gov/pubmed/16759096	Antagonist 2778		0.58 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Advanced prostate cancer 9 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022201s011lbl.pdf	Primary		Approved 8429	FIRMAGON Approved Use FIRMAGON is a GnRH receptor antagonist indicated for treatment of patients with advanced prostate cancer. Launch Date 2008

C_max

Value	Dose	Co-administered	Analyte	Population
66 ng/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/26513436/	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
26.2 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022201s016lbl.pdf	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
635 ng × day/mL REVIEW https://pubmed.ncbi.nlm.nih.gov/26513436/	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1054 ng × day/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022201s016lbl.pdf	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
43 day REVIEW https://pubmed.ncbi.nlm.nih.gov/26513436/	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
53 day DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022201s016lbl.pdf	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
10% REVIEW https://pubmed.ncbi.nlm.nih.gov/26513436/	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022201s016lbl.pdf	240 mg single, subcutaneous dose: 240 mg route of administration: Subcutaneous experiment type: SINGLE co-administered:		DEGARELIX plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482	unhealthy, 74.2 n = 137 Health Status: unhealthy Condition: Advanced prostate cancer Age Group: 74.2 Sex: M Population Size: 137 Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482	Disc. AE: Injection site induration, Malaise... AEs leading to discontinuation/dose reduction: Injection site induration (2.19%) Malaise (1.46%) Hepatic function abnormal (1.46%) Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482
240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022201lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Advanced prostate cancer Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022201lbl.pdf Page: p.1	Disc. AE: QT interval prolonged... AEs leading to discontinuation/dose reduction: QT interval prolonged Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022201lbl.pdf Page: p.1
10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	Other AEs: Sick sinus syndrome, Ileus... Other AEs: Sick sinus syndrome (serious, 1 patient) Ileus (serious, 1 patient) Subileus (serious, 1 patient) Abscess intestinal (serious, 1 patient) Contusion (serious, 1 patient) Osteoarthritis (serious, 1 patient) Adenosquamous cell carcinoma (serious, 1 patient) Prostate cancer (serious, 1 patient) Carotid sinus syndrome (serious, 1 patient) Cerebrovascular accident (serious, 1 patient) Pulmonary embolism (serious, 1 patient) Respiratory failure (serious, 1 patient) Deep vein thrombosis (serious, 1 patient) Injection site erythema (below serious, 11 patient) Injection site pain (below serious, 2 patients) Injection site induration (below serious, 6 patients) Nasopharyngitis (below serious, 7 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	Other AEs: Clostridium difficile colitis, Intervertebral disc protrusion... Other AEs: Clostridium difficile colitis (serious, 1 patient) Intervertebral disc protrusion (serious, 1 patient) Injection site erythema (below serious, 14 patients) Injection site pain (below serious, 10 patients) Injection site induration (below serious, 7 patients) Hot flush (below serious, 4 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	Other AEs: Atrioventricular block complete, Intervertebral disc protrusion... Other AEs: Atrioventricular block complete (serious, 1 patient) Intervertebral disc protrusion (serious, 1 patient) Osteoarthritis (serious, 1 patient) Colon cancer metastatic (serious, 1 patient) Depression (serious, 1 patient) Chronic obstructive pulmonary disease (serious, 1 patient) Hypertension (serious, 1 patient) Injection site erythema (below serious, 18 patients) Injection site pain (below serious, 18 patients) Injection site induration (below serious, 11 patient) Hypertension (below serious, 9 patients) Hot flush (below serious, 8 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT00947882

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781	inducer 389 inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP3A4/5 278 CYP2C19 1478 CYP2E1 882 P-gp 1461 OATP1B3 706 BCRP 699 MRP2 383 BSEP 402 OATP1B1 788 OATP2B1 123	CYP450 65 P-gp 1537 BCRP 561 MRP2 205 BSEP 52 OATP1B1 406 OATP2B1 104	CYP1A2 701 CYP2C8 168 CYP2C19 293 BCRP 75 MRP2 111 BSEP 6 OATP1B1 26 OATP2B1 6

Drug as perpetrator

Target	Modality	Activity
BCRP 773	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
BSEP 403	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2C8 965	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	no
MRP2 475	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
MRP2 475	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP1B1 803	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP2B1 126	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP2B1 126	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	unlikely
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	yes [IC50 10 uM]

Drug as victim

Target	Modality	Activity
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
BSEP 52	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
MRP2 205	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP2B1 104	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=34 Page: 34.0	no
CYP450 65	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_ClinPharmR.pdf#page=33 Page: 33.0	poor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022201s000_PharmR_P1.pdf#page=38 Page: 38.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA00BF3V	https://www.aablocks.com/goods/Goods/detail?id=AA00BF3V
Achemtek	0102-014289	http://www.achemtek.com/214766-78-6
Adooq BioScience	A12840	https://www.adooq.com/degarelix-acetate.html
Alsachim	2920	http://www.alsachim.com/product-C3990-glo.bal-view.html
Aurum Pharmatech LLC	Z-3147	http://www.Aurumpharmatech.com/Product/ProductDetails/Z_3147
BOC Sciences	214766-78-6	https://www.bocsci.com/degarelix-acetate-cas-214766-78-6-item-465293.html
CSNpharm	CSN18109	https://www.csnpharm.com/products/degarelix.html
Chem Scene	CS-5350	http://www.chemscene.com/214766-78-6.html
ChemMol	49400009	http://www.chemmol.com/chemmol/49400009.html
Chemenu	CM100964	http://www.chemenu.com/products/CM100964
Chemspace	CSSB00161189522	https://chem-space.com/CSSB00161189522
Glentham Life Sciences	GP2084	http://www.glentham.com/products/product/GP2084/
Lab Network	LN01345459	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01345459
MedChem Express	HY-16168A	https://www.medchemexpress.com/Degarelix.html
MolPort	MolPort-046-417-128	https://www.molport.com/shop/molecule-link/MolPort-046-417-128
MuseChem	I002648	https://www.musechem.com/product/I002648.html
OChem	25795	http://www.ocheminc.com/index.php?act=psearch&pid=766D786
Renno Tech	RL02641	http://www.rennotech.com/product_show.asp?id=2890
eNovation Chemicals	D320201	https://www.enovationchem.com/ProductDetails.asp?ProductID=D320201
iChemical	EBD29766	http://www.ichemical.com/chemicals/cas-214766-78-6

PubMed

Title	Date	PubMed
Evaluation of degarelix in the management of prostate cancer.	2010 Jan 25	21188095

Patents

Sample Use Guides

In Vivo Use Guide

FIRMAGON® is for subcutaneous administration only: Treatment is started with a dose of 240 mg given as two injections of 120 mg each. The starting dose is followed by maintenance doses of 80 mg administered as a single injection every 28 days.

Route of Administration: Other

Substance Class	Chemical Created by `admin` on `Fri Dec 15 21:00:01 GMT 2023` Edited by `admin` on `Fri Dec 15 21:00:01 GMT 2023`
Record UNII	EXT215F4ZU
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DEGARELIX ACETATE ANHYDROUS

Common Name

English

DEGARELIX MONOACETATE ANHYDROUS

Common Name

English

Code System Code Type Description

EPA CompTox

DTXSID201027699

Created by admin on Fri Dec 15 21:00:01 GMT 2023 , Edited by admin on Fri Dec 15 21:00:01 GMT 2023

PRIMARY

CAS

934016-19-0

Created by admin on Fri Dec 15 21:00:01 GMT 2023 , Edited by admin on Fri Dec 15 21:00:01 GMT 2023

PRIMARY

PUBCHEM

16144848

Created by admin on Fri Dec 15 21:00:01 GMT 2023 , Edited by admin on Fri Dec 15 21:00:01 GMT 2023

PRIMARY

FDA UNII

EXT215F4ZU

Created by admin on Fri Dec 15 21:00:01 GMT 2023 , Edited by admin on Fri Dec 15 21:00:01 GMT 2023

PRIMARY

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					SX0XJI3A11

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PARENT -> SALT/SOLVATE

Amount:


					I18S89P20R

DEGARELIX ACETATE

SOLVATE->ANHYDROUS

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					SX0XJI3A11

DEGARELIX

ACTIVE MOIETY

Amount:

AE	Significance	Dose	Population
Hepatic function abnormal	1.46% Disc. AE	240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482	unhealthy, 74.2 n = 137 Health Status: unhealthy Condition: Advanced prostate cancer Age Group: 74.2 Sex: M Population Size: 137 Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482
Malaise	1.46% Disc. AE	240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482	unhealthy, 74.2 n = 137 Health Status: unhealthy Condition: Advanced prostate cancer Age Group: 74.2 Sex: M Population Size: 137 Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482
Injection site induration	2.19% Disc. AE	240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482	unhealthy, 74.2 n = 137 Health Status: unhealthy Condition: Advanced prostate cancer Age Group: 74.2 Sex: M Population Size: 137 Sources: https://pubmed.ncbi.nlm.nih.gov/22457321 Page: p.482
QT interval prolonged	Disc. AE	240 mg 1 times / 4 weeks multiple, subcutaneous Recommended Dose: 240 mg, 1 times / 4 weeks Route: subcutaneous Route: multiple Dose: 240 mg, 1 times / 4 weeks Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022201lbl.pdf Page: p.1	unhealthy Health Status: unhealthy Condition: Advanced prostate cancer Sex: M Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022201lbl.pdf Page: p.1
Injection site erythema	below serious, 11 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site pain	below serious, 2 patients	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site induration	below serious, 6 patients	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Nasopharyngitis	below serious, 7 patients	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Abscess intestinal	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Adenosquamous cell carcinoma	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Carotid sinus syndrome	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Cerebrovascular accident	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Contusion	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Deep vein thrombosis	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Ileus	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Osteoarthritis	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Prostate cancer	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Pulmonary embolism	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Respiratory failure	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Sick sinus syndrome	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Subileus	serious, 1 patient	10 mg single, subcutaneous Dose: 10 mg Route: subcutaneous Route: single Dose: 10 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 101 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 101 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site pain	below serious, 10 patients	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site erythema	below serious, 14 patients	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Hot flush	below serious, 4 patients	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site induration	below serious, 7 patients	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Clostridium difficile colitis	serious, 1 patient	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Intervertebral disc protrusion	serious, 1 patient	20 mg single, subcutaneous Dose: 20 mg Route: subcutaneous Route: single Dose: 20 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 100 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 100 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site induration	below serious, 11 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site erythema	below serious, 18 patients	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Injection site pain	below serious, 18 patients	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Hot flush	below serious, 8 patients	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Hypertension	below serious, 9 patients	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Atrioventricular block complete	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Chronic obstructive pulmonary disease	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Colon cancer metastatic	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Depression	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Hypertension	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Intervertebral disc protrusion	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882
Osteoarthritis	serious, 1 patient	30 mg single, subcutaneous Dose: 30 mg Route: subcutaneous Route: single Dose: 30 mg Sources: https://clinicaltrials.gov/ct2/show/NCT00947882	unhealthy n = 105 Health Status: unhealthy Condition: Lower Urinary Tract Symptoms Population Size: 105 Sources: https://clinicaltrials.gov/ct2/show/NCT00947882

Details

SMILES

InChI

DescriptionSources: https://firmagon.com | https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022201s011lbl.pdf

Originator

Approval Year

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Overview

OverviewOther

Drug as perpetrator​

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PubMed

Patents

Sample Use Guides

Description
Sources: https://firmagon.com | https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022201s011lbl.pdf

C_max

T_1/2

F_unbound

Drug as perpetrator