Stem definition | Drug id | CAS RN |
---|---|---|
gonadotropin-releasing-hormone (GnRH) inhibitors, peptides | 4379 | 214766-78-6 |
Dose | Unit | Route |
---|---|---|
2.70 | mg | P |
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Dec. 24, 2008 | FDA | FERRING | |
June 26, 2012 | PMDA | Astellas Pharma Inc. |
None
None
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 |
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 |
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 |
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 |
None
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 |
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 |
None