tedizolid phosphate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| oxazolidinone antibacterials | 4873 | 856867-55-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid inhibits bacterial protein synthesis through a mechanism of action different from that of other non-oxazolidinone class antibacterial drugs; therefore, cross-resistance between tedizolid and other classes of antibacterial drugs is unlikely.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
| 0.20 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.10 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 23, 2018 | PMDA | Bayer Yakuhin Ltd. | |
| March 23, 2015 | EMA | Merck Sharp & Dohme Ltd | |
| June 20, 2014 | FDA | CUBIST PHARMS INC |
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 |
|---|---|---|---|---|---|---|
| Product use in unapproved indication | 100.92 | 58.30 | 44 | 518 | 250315 | 79493511 |
| Off label use | 71.95 | 58.30 | 55 | 507 | 907160 | 78836666 |
| Thrombocytopenia | 58.70 | 58.30 | 31 | 531 | 265228 | 79478598 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J01XX11 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER ANTIBACTERIALS Other antibacterials |
| FDA CS | M0361132 | Oxazolidinones |
| FDA EPC | N0000175495 | Oxazolidinone Antibacterial |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| CHEBI has role | CHEBI:33281 | antibiotics |
| CHEBI has role | CHEBI:48001 | protein synthesis inhibitors |
| CHEBI has role | CHEBI:49103 | drug metabolites |
| CHEBI has role | CHEBI:50266 | Prodrugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Bacterial infection of skin | indication | 128936008 | |
| Streptococcal infection of skin | indication | 402937004 | |
| Staphylococcal infection of skin | indication | 402938009 | |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 0.98 | acidic |
| pKa2 | 6.03 | acidic |
| pKa3 | 2.58 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | 8420676 | Feb. 23, 2028 | METHOD OF TREATING BACTERIAL INFECTIONS |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | 8420676 | Feb. 23, 2028 | METHOD OF TREATING BACTERIAL INFECTIONS |
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | 7816379 | June 20, 2028 | METHOD OF TREATING ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTIONS (ABSSSI) CAUSED BY DESIGNATED SUSCEPTIBLE BACTERIA |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | 7816379 | June 20, 2028 | METHOD OF TREATING ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTIONS (ABSSSI) CAUSED BY DESIGNATED SUSCEPTIBLE BACTERIA |
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | 9624250 | Feb. 3, 2030 | METHOD OF TREATING ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTIONS (ABSSSI) CAUSED BY DESIGNATED SUSCEPTIBLE BACTERIA |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | 9624250 | Feb. 3, 2030 | METHOD OF TREATING ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTIONS (ABSSSI) CAUSED BY DESIGNATED SUSCEPTIBLE BACTERIA |
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | 8426389 | Dec. 31, 2030 | METHOD OF TREATING BACTERIAL INFECTIONS |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | 8426389 | Dec. 31, 2030 | METHOD OF TREATING BACTERIAL INFECTIONS |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | June 20, 2019 | NEW CHEMICAL ENTITY |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | June 20, 2019 | NEW CHEMICAL ENTITY |
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | June 19, 2023 | NEW PATIENT POPULATION |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | June 19, 2023 | NEW PATIENT POPULATION |
| 200MG | SIVEXTRO | CUBIST PHARMS LLC | N205435 | June 20, 2014 | RX | TABLET | ORAL | June 20, 2024 | GENERATING ANTIBIOTIC INCENTIVES NOW |
| 200MG/VIAL | SIVEXTRO | CUBIST PHARMS LLC | N205436 | June 20, 2014 | RX | POWDER | INTRAVENOUS | June 20, 2024 | GENERATING ANTIBIOTIC INCENTIVES NOW |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Amine oxidase [flavin-containing] B | Enzyme | IC50 | 5.24 | CHEMBL | |||||
| Amine oxidase [flavin-containing] A | Enzyme | IC50 | 5.06 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D09685 | KEGG_DRUG |
| 4033460 | VUID |
| N0000190860 | NUI |
| 4033460 | VANDF |
| 4033461 | VANDF |
| CHEBI:83326 | CHEBI |
| CHEBI:82717 | CHEBI |
| U7V | PDB_CHEM_ID |
| CHEMBL2105669 | ChEMBL_ID |
| C515040 | MESH_SUPPLEMENTAL_RECORD_UI |
| C546016 | MESH_SUPPLEMENTAL_RECORD_UI |
| DB09042 | DRUGBANK_ID |
| DB14569 | DRUGBANK_ID |
| 1540824 | RXNORM |
| 221941 | MMSL |
| 30367 | MMSL |
| d08270 | MMSL |
| 015566 | NDDF |
| 015567 | NDDF |
| 703912007 | SNOMEDCT_US |
| 703913002 | SNOMEDCT_US |
| 703914008 | SNOMEDCT_US |
| C2930762 | UMLSCUI |
| C2744850 | UMLSCUI |
| CHEMBL1257051 | ChEMBL_ID |
| CHEMBL4297931 | ChEMBL_ID |
| 11476460 | PUBCHEM_CID |
| 9136 | INN_ID |
| 856866-72-3 | SECONDARY_CAS_RN |
| 11234049 | PUBCHEM_CID |
| 10865 | IUPHAR_LIGAND_ID |
| O7DRJ6R4DW | UNII |
| 97HLQ82NGL | UNII |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-040 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 200 mg | INTRAVENOUS | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-040 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 200 mg | INTRAVENOUS | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-040 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 200 mg | INTRAVENOUS | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-041 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-041 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67919-041 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-310 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-310 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-320 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 200 mg | INTRAVENOUS | NDA | 30 sections |
| SIVEXTRO | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72000-320 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 200 mg | INTRAVENOUS | NDA | 30 sections |