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lusutrombopag 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| thrombopoietin agonists | 5059 | 1110766-97-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a thrombopoietin receptor agonist
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.545 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.105 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.832 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 18.197 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.160 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.140 | % | High | 1 |
| herg | hERG pIC50 | 4.803 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 16.293 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 21.528 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.470 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,EIF2AK3,GRK2,MAPK10,MAPK7,PDK1,PDK2,PDK4,PIK3CB,PRKDC | 11 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3,EPHB4,GRK2,MAPK7,PDK4,STK33,TEK | 9 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.819 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 8.091 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.180 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.733 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.160 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 10.715 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 0.320 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.180 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 4.355 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 31, 2018 | FDA | SHIONOGI INC | |
| Feb. 18, 2019 | EMA | SHIONOGI B.V. | |
| Sept. 28, 2015 | PMDA |
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 | B02BX07 | BLOOD AND BLOOD FORMING ORGANS ANTIHEMORRHAGICS VITAMIN K AND OTHER HEMOSTATICS Other systemic hemostatics |
Related Drugs by ATC class:
B02BX Other systemic hemostatics 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Thrombocytopenic disorder | indication | 302215000 | DOID:1588 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.45 | acidic |
| pKa2 | 7.41 | acidic |
| pKa3 | 0.94 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Thrombopoietin receptor | Membrane receptor | AGONIST | EC50 | 7.08 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 6LL5JFU42F | UNII |
| D10476 | KEGG_DRUG |
| 4037779 | VANDF |
| C4309207 | UMLSCUI |
| CHEBI:136051 | CHEBI |
| CHEMBL2107831 | ChEMBL_ID |
| 49843517 | PUBCHEM_CID |
| DB13125 | DRUGBANK_ID |
| 9410 | INN_ID |
| C000611387 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10032 | IUPHAR_LIGAND_ID |
| 2054984 | RXNORM |
| 286900 | MMSL |
| 34734 | MMSL |
| d08854 | MMSL |
| 017667 | NDDF |
| 773263005 | SNOMEDCT_US |
| 773265003 | SNOMEDCT_US |
| 6LL5JFU42F | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Mulpleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59630-551 | TABLET, FILM COATED | 3 mg | ORAL | NDA | 26 sections |
| Mulpleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 84230-551 | TABLET, FILM COATED | 3 mg | ORAL | NDA | 26 sections |
| Mulpleta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 85320-551 | TABLET, FILM COATED | 3 mg | ORAL | NDA | 26 sections |