2.
Clinical parameters from clinical trials using HDi as single agents
| Drug | HDACs targeted | Phase | Method of delivery | Dosage range | Adverse reactions |
|---|---|---|---|---|---|
| Panobinostat (LBH589) | Class I, II | I | Oral | 20 mg/m2 | Grade 3 diarrhoea |
| MGCD0103 | Class I | I | Oral | 60 mg/m2 | Fatigue, nausea, vomiting and diarrhoea |
| Vorinostat | Class I, II | FDA approved | Oral | 200–600 mg/m2 | Fatigue, dehydration, nausea and vomiting |
| MS-275 | Class I | II | Oral | 2–6 mg/m2 | Hypophosphatemia, hyponatremia and hypoalbuminemia |
| VPA | Class I | II | Oral | 60 mg/kg/day | Grade 3, 4 neurocognitive impairment |
| Phenylbutyrate | Class I,II | I/II | Oral and intravenous (i.v.) infusion | 60–360 mg/kg/day | Reversible neurocortical toxicity characterized by somnolence and confusion, short-term memory loss, sedation, confusion, nausea and vomiting |
| Pivanex (AN-9) | II | i.v. infusion | 2.34 g/m2/day | Nausea, vomiting, hyperglycaemia, fatigue, diarrhoea and visual complaints | |
| CI-994 | Class I | I/II | Oral | 4–6 mg/m2/day | Thrombocytopenia, fatigue, nausea, vomiting, diarrhoea, constipation and mucositis |
| Belinostat (PXD101) | Class I, II | I/II | i.v. infusion | 1000 mg/m2/day | Nausea, vomiting, fatigue and flushing atrial fibrillation |
| Two cases of grade 4 renal failure | |||||
| Romidepsin | Class I | I/II | i.v. infusion | 10–26 mg/m2 | Reversible cardiac dysrhythmias and non-specific ECG abnormalities thromocytopenia |