forodesine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5229 | 209799-67-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Forodesine is a transition state analogue that binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| CL (Clearance) | 1.56 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11.60 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 30, 2017 | PMDA | Mundi Pharma |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 80.43 | 68.86 | 20 | 68 | 135970 | 79608330 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
None
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Peripheral T-cell lymphoma | indication | 109977009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.32 | acidic |
| pKa2 | 12.91 | acidic |
| pKa3 | 13.39 | acidic |
| pKa4 | 13.93 | acidic |
| pKa5 | 8.65 | Basic |
| pKa6 | 5.46 | Basic |
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Purine nucleoside phosphorylase | Enzyme | INHIBITOR | Ki | 10.14 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Purine nucleoside phosphorylase | Enzyme | Ki | 9.07 | CHEMBL | |||||
| Purine nucleoside phosphorylase | Enzyme | Ki | 10.64 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 426X066ELK | UNII |
| 284490-13-7 | SECONDARY_CAS_RN |
| C0676720 | UMLSCUI |
| CHEBI:43362 | CHEBI |
| IMH | PDB_CHEM_ID |
| CHEMBL218291 | ChEMBL_ID |
| 135409409 | PUBCHEM_CID |
| DB06185 | DRUGBANK_ID |
| D04245 | KEGG_DRUG |
| CHEMBL550755 | ChEMBL_ID |
| CHEMBL549687 | ChEMBL_ID |
| 8558 | INN_ID |
| 8272 | IUPHAR_LIGAND_ID |
| 428525005 | SNOMEDCT_US |
| 428526006 | SNOMEDCT_US |
| 429322001 | SNOMEDCT_US |
| C113101 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None