| Drug | Drug class | Mode of action | Mode of administration and current dosage | Function | Toxicity | Study phase | Comment |
| AZD5847 | Oxazolidinone | Inhibition of microbial protein synthesis (blocks 50S ribosomal subunit) | Oral, 500–1200 mg per day | Bactericidal | Well tolerated, non-severe gastrointestinal symptoms, white blood cells count changes | IIa | Ongoing EBA, including dose-finding study |
| Bedaquiline (TMC207) | Diarylquinoline | Inhibition mycobacterial ATP synthase | Oral, 400 mg per day for 2 weeks, 200 mg three times per week for 22 weeks | Sterilising and bactericidal | QT-prolongation, unexplained excess mortality | III | FDA approved, EMA approved |
| Delamanid (OPC-67683) | Nitro-dihydro- imidazooxazole | Mycolic acid cell wall inhibition | Oral, 100 mg per day for 2 months, then 200 mg per day for 4 months | Bactericidal | Well tolerated, QT-prolongation | III | EMA approved |
| Gatifloxacin | Fluoroquinolone | DNA gyrase inhibition | Oral or intravenous | Sterilising? and bactericidal | QT-prolongation, dysglycaemia, hallucination, liver toxicity | II | Market withdrawal in 2006 due to risk of dysglycaemia |
| Linezolid | Oxazolidinone | Inhibition of microbial protein synthesis (blocks 50S ribosome subunit) | Oral or intravenous, 300–600 mg per day | Bactericidal | Myelosuppression, peripheral neuropathy, rhabdomyolysis | II | Used for MDR/XDR-TB since 2005 with good efficacy but substantial toxicity in long-term treatment |
| PA-824 | Nitroimidazole | Reactive nitrogen compound, cell wall synthesis inhibition | Oral, 100-200 mg per day | Sterilising and bactericidal | Well tolerated | IIb | Less expensive and easier to co-administer with antiviral drugs, with potential for shortening therapy using PA-824, moxifloxacin and pyrazinamide |
| SQ109 | 1,2-ethylenediamine | Cell wall synthesis inhibition | Oral, 300 mg per day | Bactericidal | No serious adverse events, gastro-intestinal predominantly | IIa | Currently under evaluation in MDR-TB patients in the Russian Federation |
| Sutezolid (PNU-100480) | Oxazolidinone | Inhibition of microbial protein synthesis (blocks 50S ribosomal subunit) | Oral, 600–1200 mg per day | Bactericidal | Well tolerated | II | Besides concerns about neurotoxicity after prolonged use, hepatotoxicity is a potentially important side-effect |
EBA: early bactericidal activity; FDA: US Food and Drug Administration; EMA: European Medicines Agency; XDR: extensively drug-resistant.