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telithromycin 🐶 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 | 2581 | 191114-48-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a ketolide; semisynthetic derivative of erythromycin with cycling of the C11-12 positions to form a carbamate ring to avoid acquired resistance to macrolides; binds 70S bacterial rRNA, specifically to the 23S part (23S RIBOSOMAL RNA), preventing protein synthesis
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.80 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 26 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 13 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 14.07 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 57 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 14 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.41 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 12 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.733 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 36.058 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.977 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 10.209 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 41.950 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 39.510 | % | High | 1 |
| herg | hERG pIC50 | 4.543 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.155 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 92.470 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 53.280 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK | 16 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 11.749 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 16.293 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 39.400 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 26.122 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 56.470 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 11.324 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 73.810 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 41.950 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 803.526 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 1, 2004 | FDA | SANOFI AVENTIS US |
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 |
|---|---|---|---|---|---|---|
| Drug hypersensitivity | 65.33 | 55.29 | 18 | 26 | 463591 | 90164812 |
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 | J01FA15 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE MACROLIDES, LINCOSAMIDES AND STREPTOGRAMINS Macrolides |
| FDA CS | M0462018 | Ketolides |
| FDA EPC | N0000175492 | Ketolide Antibacterial |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
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 |
|---|---|---|---|
| Pneumonia due to Mycoplasma pneumoniae | indication | 46970008 | |
| Haemophilus influenzae pneumonia | indication | 70036007 | |
| Pneumococcal pneumonia | indication | 233607000 | |
| Chlamydial pneumonia | indication | 233609002 | |
| Streptococcus pyogenes infection | indication | 302809008 | |
| Moraxella Catarrhalis Pneumonia | indication | ||
| Tonsillitis due to Streptococcus Pyogenes | indication | ||
| Torsades de pointes | contraindication | 31722008 | |
| Hypokalemia | contraindication | 43339004 | |
| Diarrhea | contraindication | 62315008 | |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Prolonged QT interval | contraindication | 111975006 | |
| Hypomagnesemia | contraindication | 190855004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Drug-induced hepatitis | contraindication | 235876009 | |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Congenital long QT syndrome | contraindication | 442917000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.0 | acidic |
| pKa2 | 12.69 | acidic |
| pKa3 | 8.65 | Basic |
| pKa4 | 6.18 | Basic |
| pKa5 | 4.29 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 4.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021470 | VUID |
| N0000148854 | NUI |
| D01078 | KEGG_DRUG |
| 4021470 | VANDF |
| C0907410 | UMLSCUI |
| CHEBI:29688 | CHEBI |
| TEL | PDB_CHEM_ID |
| CHEMBL1136 | ChEMBL_ID |
| DB00976 | DRUGBANK_ID |
| C106791 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10878 | IUPHAR_LIGAND_ID |
| 7803 | INN_ID |
| KI8H7H19WL | UNII |
| 3002190 | PUBCHEM_CID |
| 274786 | RXNORM |
| 17779 | MMSL |
| 50779 | MMSL |
| d04933 | MMSL |
| 009523 | NDDF |
| 395260006 | SNOMEDCT_US |
| 410908003 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Ketek | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5171 | TABLET, FILM COATED | 400 mg | ORAL | NDA | 28 sections |