degarelix 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 |
|---|---|
|
Synonyms:
|
FE-200486 is the acetate salt
|
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 |
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)
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 |
Drug Use (View source of the data)
| 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 | |
| Congenital long QT syndrome | contraindication | 442917000 |
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 | 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 | 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 |
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 | 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 |
| CHEBI:135961 | CHEBI |
| 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 |
| 441758000 | SNOMEDCT_US |
| 441864003 | SNOMEDCT_US |
Pharmaceutical products:
None