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avanafil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| inhibitors of phosphodiesterase PDE5 with vasodilator action | 4305 | 330784-47-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a selective inhibitor of cGMP-specific PDE5 has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of NO by inhibiting PDE5, which is responsible for degradation of cGMP in the corpus cavernosum
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,ITK,MAP3K21,MAPK7,MARK4,MET,NTRK2,PDK2,PDK4,PIK3CB,PRKDC,SIK2,SIK3,TEK,TTK | 28 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 21, 2013 | EMA | ||
| April 27, 2012 | FDA | VIVUS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G04BE10 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction |
| FDA MoA | N0000020026 | Phosphodiesterase 5 Inhibitors |
| FDA EPC | N0000175599 | Phosphodiesterase 5 Inhibitor |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:50218 | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
G04BE Drugs used in erectile dysfunction 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Impotence | indication | 397803000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.01 | acidic |
| pKa2 | 4.93 | Basic |
| pKa3 | 3.61 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| cGMP-specific 3',5'-cyclic phosphodiesterase | Enzyme | INHIBITOR | IC50 | 8.28 | WOMBAT-PK | CHEMBL | |||
| Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' | Enzyme | IC50 | 6.20 | WOMBAT-PK | |||||
| cGMP-specific 3',5'-cyclic phosphodiesterase | Enzyme | IC50 | 8.28 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D03217 | KEGG_DRUG |
| 4032978 | VANDF |
| CHEBI:66876 | CHEBI |
| E6L | PDB_CHEM_ID |
| CHEMBL1963681 | ChEMBL_ID |
| C553414 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7448 | IUPHAR_LIGAND_ID |
| DB06237 | DRUGBANK_ID |
| DR5S136IVO | UNII |
| 1291301 | RXNORM |
| 189434 | MMSL |
| 28514 | MMSL |
| 390498 | MMSL |
| d07863 | MMSL |
| 015259 | NDDF |
| 703956007 | SNOMEDCT_US |
| 703957003 | SNOMEDCT_US |
| C2698280 | UMLSCUI |
| 8572 | INN_ID |
| 9869929 | PUBCHEM_CID |
| DR5S136IVO | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Avanafil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-440 | TABLET | 50 mg | ORAL | ANDA | 28 sections |
| Avanafil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-441 | TABLET | 100 mg | ORAL | ANDA | 28 sections |
| Avanafil | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-442 | TABLET | 200 mg | ORAL | ANDA | 28 sections |
| Stendra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72384-751 | TABLET | 50 mg | ORAL | NDA | 28 sections |
| Stendra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72384-752 | TABLET | 100 mg | ORAL | NDA | 28 sections |
| Stendra | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72384-753 | TABLET | 200 mg | ORAL | NDA | 28 sections |