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troleandomycin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, produced by Streptomyces strains | 2769 | 2751-09-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A macrolide antibiotic that is similar to ERYTHROMYCIN.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.25 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.003 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.365 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 23.335 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 89.743 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 8.390 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 17.820 | % | High | 1 |
| herg | hERG pIC50 | 4.486 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 59.020 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 195.884 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 14.120 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK | 17 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.884 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 49.317 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.440 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 9.204 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 11.930 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 54.576 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 37.170 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 11.050 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 161.808 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 27, 1969 | FDA | PFIZER |
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 | J01FA08 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS Macrolides |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35703 | xenobiotic |
| CHEBI has role | CHEBI:86501 | EC 1.14.13.97 (taurochenodeoxycholate 6α-hydroxylase) inhibitor |
Related Drugs by ATC class:
J01FA Macrolides 13 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pneumococcal pneumonia | indication | 233607000 | |
| Upper Respiratory Streptococcal Infection | indication | ||
| Asthma | off-label use | 195967001 | DOID:2841 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.62 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 3A4 | Enzyme | INHIBITOR | Ki | 7.80 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4022401 | VUID |
| N0000146829 | NUI |
| D01322 | KEGG_DRUG |
| 4018507 | VANDF |
| 4022401 | VANDF |
| C0041165 | UMLSCUI |
| CHEBI:45735 | CHEBI |
| TAO | PDB_CHEM_ID |
| CHEMBL564085 | ChEMBL_ID |
| D014217 | MESH_DESCRIPTOR_UI |
| DB13179 | DRUGBANK_ID |
| 10209 | IUPHAR_LIGAND_ID |
| 805 | INN_ID |
| C4DZ64560D | UNII |
| 202225 | PUBCHEM_CID |
| 10864 | RXNORM |
| 5643 | MMSL |
| d01076 | MMSL |
| 002765 | NDDF |
| 371016002 | SNOMEDCT_US |
| 64130008 | SNOMEDCT_US |
Pharmaceutical products:
None