Repositioning Candidate Details
| Candidate ID: | R0654 |
| Source ID: | DB04934 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Rifalazil |
| Synonyms: | 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl)benzoxazinorifamycin; Rifalazil |
| Molecular Formula: | C51H64N4O13 |
| SMILES: | CO[C@H]1\C=C\O[C@@]2(C)OC3=C(C)C(O)=C4C(=O)C(NC(=O)\C(C)=C/C=C/[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C)=C1OC5=CC(=CC(O)=C5N=C1C4=C3C2=O)N1CCN(CC(C)C)CC1 |
| Structure: |
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| DrugBank Description: | Rifalazil is a derivative of the antibiotic rifamycin. It is being investigated by ActivBiotics for the treatment of various bacterial infections. |
| CAS Number: | 129791-92-0 |
| Molecular Weight: | 941.088 |
| DrugBank Indication: | Investigated for use/treatment in atherosclerosis, bacterial infection, and peripheral vascular disease. |
| DrugBank Pharmacology: | Rifalazil represents a new generation of ansamycins that contain a unique four-ring structure. Originally rifalazil was developed as a therapeutic agent to replace rifampin as part of a multiple drug regimen in the treatment of tuberculosis. As a result of its superior antimicrobial activity and high intracellular levels, rifalazil has potential to treat indications caused by the intracellular pathogen, <i>Chlamydia trachomatis</i>, which causes non-gonococcal urethritis and cervicitis, often leading to pelvic inflammatory disease. Rifalazil also has potential to treat the related microorganism, <i>Chlamydia pneumoniae</i>, which may be involved in chronic inflammatory processes thought to be partly responsible for atherosclerosis. Due to its favourable antimicrobial spectrum and other positive attributes, rifalazil may also prove valuable in the treatment of gastric ulcer disease, caused by <i>Helicobacter pylori</i>, and antibiotic-associated colitis, the result of toxin production following the growth of <i>Clostridium difficile</i> in the colon. The potential value of rifalazil in the treatment of these indications will be assessed in human clinical trials. |
| DrugBank MoA: | The potent antimycobacterial activity of rifalazil is due to inhibition of bacterial RNA polymerase. |
| Targets: | DNA-directed RNA polymerase subunit beta |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I01 | 552 | Pneumonia | A lung disease that involves lung parenchyma or alveolar inflammation and abnormal alveolar filling with fluid (consolidation and exudation). It results from a variety of causes including infection with bacteria, viruses, fungi or parasites, and chemical or physical injury to the lungs. It is accompanied by fever, chills, cough, and difficulty in breathing. http://en.wikipedia.org/wiki/Pneumonia | disease of anatomical entity/respiratory system disease/ lower respiratory tract disease/lung disease | Details |
| I09 | 104 | Bacterial infectious disease | A disease by infectious agent that results_in infection, has_material_basis_in Bacteria. http://en.wikipedia.org/wiki/Pathogenic_bacteria | disease by infectious agent | Details |
| I07 | 1936 | Arteriosclerosis | Build-up of fatty material and calcium deposition in the arterial wall resulting in partial or complete occlusion of the arterial lumen.https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=ncit&code=C35768 | disease of anatomical entity/cardiovascular system disease/ vascular disease/ artery disease | Details |