rolitetracycline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, protein-synthesis inhibitors, tetracycline derivatives | 2399 | 751-97-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A pyrrolidinylmethyl TETRACYCLINE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.35 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1250 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 55 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 11.05 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.54 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.97 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.50 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 8.80 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
None
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 | J01AA09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE TETRACYCLINES Tetracyclines |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| CHEBI has role | CHEBI:35820 | antiprotozoal drugs |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
| CHEBI has role | CHEBI:48001 | protein synthesis inhibitors |
| CHEBI has role | CHEBI:50266 | Prodrugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.72 | acidic |
| pKa2 | 7.59 | acidic |
| pKa3 | 9.76 | acidic |
| pKa4 | 11.9 | acidic |
| pKa5 | 13.05 | acidic |
| pKa6 | 13.72 | acidic |
| pKa7 | 9.07 | Basic |
| pKa8 | 8.21 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Insulin-degrading enzyme | Enzyme | IC50 | 4 | CHEMBL | |||||
| DNA repair protein RAD52 homolog | Nuclear other | IC50 | 4.54 | CHEMBL | |||||
| Integrase | Enzyme | IC50 | 4.55 | CHEMBL | |||||
| Integrase | Enzyme | IC50 | 4.55 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167345 | NUI |
| D02282 | KEGG_DRUG |
| C0035823 | UMLSCUI |
| CHEBI:63334 | CHEBI |
| CHEMBL1237046 | ChEMBL_ID |
| D012382 | MESH_DESCRIPTOR_UI |
| DB01301 | DRUGBANK_ID |
| 12760 | IUPHAR_LIGAND_ID |
| 1041 | INN_ID |
| GH9IW85221 | UNII |
| 54682938 | PUBCHEM_CID |
| 9462 | RXNORM |
| 002746 | NDDF |
| 96076003 | SNOMEDCT_US |
Pharmaceutical products:
None