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vadadustat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| hypoxia inducible factor (HIF) prolyl hydroxylase inhibitors | 5420 | 1000025-07-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Vadadustat is an oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor induces endogenous erythropoietin synthesis and enhances iron mobilization.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.30 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.044 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 71.121 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 12.794 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.173 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.490 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.420 | % | High | 1 |
| herg | hERG pIC50 | 4.416 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.904 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.055 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.290 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,IKBKB,ITK,JAK1,KDR,KIT,MAP2K6,MAP3K21,MAPK7,MTOR,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1 | 42 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,EIF2AK3,GRK2,PRKDC,TGFBR1 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 8.913 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 6.039 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.730 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.624 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.800 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 6.166 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 69.170 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.420 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 897.429 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 29, 2020 | PMDA | Mitsubishi Tanabe Pharma | |
| April 24, 2023 | EMA | AKEBIA EUROPE LIMITED |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Marasmus | 79.97 | 60.30 | 9 | 46 | 814 | 90627578 |
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 |
|---|---|---|---|---|---|---|
| Marasmus | 95.72 | 60.63 | 13 | 192 | 1678 | 110587416 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B03XA08 | BLOOD AND BLOOD FORMING ORGANS ANTIANEMIC PREPARATIONS OTHER ANTIANEMIC PREPARATIONS Other antianemic preparations |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D064800 | Prolyl-Hydroxylase Inhibitors |
| FDA MoA | N0000190111 | Organic Anion Transporter 3 Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| FDA MoA | N0000194079 | Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors |
| FDA EPC | N0000194080 | Hypoxia-inducible Factor Prolyl Hydroxylase Inhibitor |
| CHEBI has role | CHEBI:75835 | anti-anaemic agent |
Related Drugs by ATC class:
B03XA Other antianemic preparations 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anemia of renal disease | indication | 234348004 | |
| Anemia in chronic kidney disease | indication | 707323002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8940773 | June 26, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8940773 | June 26, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8940773 | June 26, 2027 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8323671 | April 3, 2028 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8323671 | April 3, 2028 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 8323671 | April 3, 2028 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 12569474 | June 4, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 12569474 | June 4, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 12569474 | June 4, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11857543 | June 9, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11857543 | June 9, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11857543 | June 9, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11065237 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 9987262 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11065237 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 9987262 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11065237 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 9987262 | Nov. 14, 2034 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11844756 | March 31, 2036 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11844756 | March 31, 2036 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | 11844756 | March 31, 2036 | TREATMENT OF ANEMIA DUE TO CHRONIC KIDNEY DISEASE IN ADULTS WHO HAVE BEEN RECEIVING DIALYSIS FOR AT LEAST THREE MONTHS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 150MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | March 27, 2029 | NEW CHEMICAL ENTITY |
| 300MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | March 27, 2029 | NEW CHEMICAL ENTITY |
| 450MG | VAFSEO | AKEBIA | N215192 | March 27, 2024 | RX | TABLET | ORAL | March 27, 2029 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Egl nine homolog 1 | Enzyme | INHIBITOR | IC50 | 7.81 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 2 | Enzyme | INHIBITOR | IC50 | 7.93 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Egl nine homolog 3 | Enzyme | INHIBITOR | IC50 | 8.12 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Vascular endothelial growth factor A | Secreted | EC50 | 5.12 | CHEMBL | |||||
| Hypoxia-inducible factor 1-alpha inhibitor | Enzyme | IC50 | 4.54 | CHEMBL | |||||
| Aspartyl/asparaginyl beta-hydroxylase | Enzyme | IC50 | 5.36 | CHEMBL | |||||
| Methylcytosine dioxygenase TET2 | Enzyme | IC50 | 5.30 | CHEMBL | |||||
| Prolyl 3-hydroxylase OGFOD1 | Enzyme | IC50 | 5.85 | CHEMBL | |||||
| Vascular endothelial growth factor receptor 1 | Kinase | EC50 | 5.12 | CHEMBL | |||||
| Gamma-butyrobetaine dioxygenase | Enzyme | IC50 | 6.55 | CHEMBL | |||||
| Prolyl 4-hydroxylase | Enzyme | Ki | 6.55 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D11078 | KEGG_DRUG |
| I60W9520VV | UNII |
| C4519730 | UMLSCUI |
| CHEBI:755674 | CHEBI |
| A1Z | PDB_CHEM_ID |
| CHEMBL3646221 | ChEMBL_ID |
| 23634441 | PUBCHEM_CID |
| DB12255 | DRUGBANK_ID |
| 10289 | INN_ID |
| C000624313 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11831 | IUPHAR_LIGAND_ID |
| 1701801000168108 | SNOMEDCT_US |
| 4043278 | VANDF |
| 374936 | MMSL |
| 42224 | MMSL |
| d10143 | MMSL |
| 019623 | NDDF |
| 2679296 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VAFSEO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59922-641 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 32 sections |
| VAFSEO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59922-642 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 32 sections |
| VAFSEO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59922-643 | TABLET, FILM COATED | 450 mg | ORAL | NDA | 32 sections |