Table 2.
Concentration of drugs against metabolic diseases in clinical and experimental setting.
| Clinical dose | Clinical Cmax (approximate) |
In vivo
experiment |
Model |
In vitro
experiment |
Cell type | Disease | Ref. | |
|---|---|---|---|---|---|---|---|---|
| Metformin | 850-2550 mg/day | 6.2-12.1 µM | 1% enriched chow | Mouse, smoking | 0.25 nM-1M | Bronchial epithelial cell | COPD | (112) |
| 50-250 mg/kg, oral | Mouse, elastase | COPD | (114) | |||||
| 2.5-5 mg/ml, in water | βENaC-Tg mouse | 5 mM | Bronchial epithelial cell | COPD | (115) | |||
| 1-2 mM | Bronchial epithelial cell | COPD | (116) | |||||
| 300 mg/kg, i.p. | Mouse, bleomycin | 1-10 mM | Fibroblast | IPF | (131) | |||
| 65 mg/kg, i.p. | Mouse, bleomycin | 0.5 mM | Fibroblast | IPF | (132) | |||
| 1.5 mg/ml, in water | Mouse, bleomycin | 1-10 mM | Fibroblast | IPF | (133) | |||
| Statin | ||||||||
| Simvastatin | 5-20 mg/day | 5.0-9.6 nM | 5 mg/kg, oral | Rat, smoking | 0.1-10 mM | Vascular endothelial cell | COPD | (134) |
| Atorvastatin | 10-40 mg/day | 6.1-48.4 nM | 20 mg/kg, i.p. | Mouse, bleomycin | 10 µM | Fibroblast | IPF | (135) |
| 20-40 mg/kg oral | Rat, paraquat | 3.6 µM-1.1mM | Alveolar epithelial cell | Lung injury | (136) | |||
| Pravastatin | 20-40 mg/day | 38.9-76.1 nM | 3-30 mg/kg, i.p. | Mouse, LPS | Lung injury | (137) | ||
| Fibrate | ||||||||
| Ciprofibrate | 100 mg/day | 72.6-124.5 µM | 150-600 µM | Fibroblast | IPF | (138) | ||
| 10 mg/kg, oral | Rat, smoking | 2.5-80 µM | Airway smooth muscle cell | COPD | (139) | |||
| Fenofibrate | 106.6-160 mg/day | 24.9-32.7 µM | 1-25 µM | Fibroblast | COPD | (140) | ||
| Gemfibrozil | 1200 mg/day | 59.9-99.9 µM | 40 mg/kg, i.p. | Mouse, smoking | 10 µM | Bronchial epithelial cell | COPD | (141) |
| Pemafibrate | 0.2-0.4 mg/day | 3.2-7.3 nM | 0.5-2 mg/kg, i.p. | Mouse, bleomycin | 10 µM | Fibroblast | IPF | (142) |
| Thiazolidinedione | ||||||||
| Rosiglitazone | 4-8 mg/day | 0.4-1.7 µM | 6 mg/kg, oral; 10-300 µg/kg, i.n. | Mouse, smoking | 0.1-3µM | Macrophage | COPD | (143) |
| Ciglitazone | N/A | N/A | 3.5 µg/body twice a week, i.n. | Mouse, smoking | 10 µM | Dendritic cell | COPD | (144) |
| 200-400 mg/kg, oral | Mouse, bleomycin | 1-20 µM | Fibroblast | IPF | (145) | |||
| Troglitazone | N/A | N/A | 200-400 mg/kg, oral | Mouse, bleomycin | 1-20 µM | Fibroblast | IPF | (145) |
Clinical dose and clinical Cmax were mainly based on the information from the National Library of Medicine in the USA, the electronic medicines compendium (emc) in the UK, and the Kyoto Encyclopedia of Genes and Genomes (KEGG) MEDICUS in Japan. COPD, chronic obstructive pulmonary disease; IPF, idiopathic pulmonary fibrosis; i.p., intraperitoneal injection; i.n., intranasal administration; LPS, lipopolysaccharide; N/A, not applicable.