Table 1.
Flavonoid-based marketed drugs (1–19) and candidates for clinical trials (or submitted to clinical trials) (20–55) undergoing or already excluded in different phases of pharmacological evaluation.
| NO. | Compound namea | CAS No. | Anatomical Therapeutic Chemical (ATC) | Therapeutic Class (Indication) | Originator or Developer b | More advanced phase of research |
|---|---|---|---|---|---|---|
| 1 | Eupatilin [36] | 22368–21-4 | Alimentary tract and metabolism | Gastric ulcer; Gastritis | Dong-A ST Co. Ltd.; Korea | Marketed |
| 2 | Diosmin [37] | 520–27-4 | Cardiovascular system | Venous lymphatic insufficiency | Servier Pharmaceutical Co., Ltd.; France | Marketed |
| 3 | Efloxate [38] | 119–41-5 | Cardiovascular system | Coronary heart disease treatment, relieve angina pectoris | Recordati S.P.A., Italy | Marketed |
| 4 | Baicalin [39], [40] | 21967–41-9 | Musculo-skeletal system | Osteoarthritis | Primus Pharmaceuticals, Inc.; United States | Marketed |
| Antiinfectives for systemic use | Chronic hepatitis B | Jiangxi Puzhong Pharmaceutical Co., Ltd.; China | Marketed | |||
| 5 | Dosmalfate [41] | 122312–55-4 | Alimentary tract and metabolism | Duodenal ulcer; esophageal dysfunction | Faes Farma Co., Ltd.; Spain | Marketed |
| 6 | Scutellarin [42] | 27740–01-8 | Cardiovascular system | Angina pectoris; stroke; coronary heart disease | Yunnan Pharmaceutical Research Institute; China | Marketed |
| 7 | Disodium flavodate [43] | 13358–62-8 | Antineoplastic and immunomodulating agents | Reduce capillary fragility and permeability | Farmaceutici Formenti S.P.A., Italy | Marketed |
| 8 | Troxerutin [44] | 7085–55-4 | Cardiovascular system | Chronic venous insufficiency | Inpharma S.A.; France | Marketed |
| 9 | Icaritin [45] | 118525–40-9 | Antineoplastic and immunomodulating agents | Liver cancer | Shenogen Pharma Group Ltd.; China | Marketed |
| 10 | Dimefline Hydrochloride [46] | 2740–04-7 | Respiratory system | Respiratory dysfunction | Recordati S.P.A., Italy | Marketed |
| 11 | Flavoxate [47] | 15301–69-6 | Genito-urinary system and sex hormones | Neuropathy; urinary incontinence; dysuria | Recordati S.P.A., Italy | Marketed |
| 12 | Hesperidin [48] | 520–26-3 | Cardiovascular system | Chronic venous insufficiency | Technological Unit of Nutrition and Health; Spain | Marketed |
| 13 | Silibinin [49], [50] | 22888–70-6 | Alimentary tract and metabolism | Liver disorders; Poisoning | Rottapharm Madaus Co., Ltd; Italy | Marketed |
| 14 | umbralisib (TGR-1202) [51] | 1532533–67-7 | Antineoplastic and immunomodulating agents | Chronic lymphocytic leukaemia | Rhizen Pharmaceuticals S.A.; Switzerland | Marketed |
| 15 | Puerarin [52] | 3681–99-0 | Cardiovascular system | Myocardial infarction | Weifang Medical University, Shandong Provincial Academy of Medical Science, etc.; China | Marketed |
| 16 | Ipriflavone [53], [54] | 35212–22-7 | Musculo-skeletal system | Osteoporosis | Takeda Pharmaceuticals Co., Ltd.; Japan | Marketed |
| 17 | Daidzein [55] | 486–66-8 | Cardiovascular system | Hypertension, coronary heart disease, cerebral thrombosis, vertigo | Liaoning Yihe Pharmaceutical Co. Ltd, China | Marketed |
| 18 | Catechin [56] | 154–23-4 | Musculo-skeletal system | Osteoarthritis | Primus Pharmaceuticals, Inc.; United States | Marketed |
| 19 | Sofalcone [57] | 64506–49-6 | Antiinfectives for systemic use | Stomach disease | Taisho Pharmaceutical Co., Ltd.; Japan | Marketed |
| 20 | Baicalein [58] | 491–67-8 | Antiinfectives for systemic use | Influenzas virus infections | CSPC Ouyi Pharmaceutical Co., Ltd.; China | Phase II |
| 21 | Wogonin [59] | 632–85-9 | Antineoplastic and immunomodulating agents | Liver cancer, breast cancer, leukemia | China Pharmaceutical University, China | Phase I |
| 22 | Alvocidib (Flavopiridol) [60], [61] | 146426–40-6 | Antineoplastic and immunomodulating agents | Acute myeloid leukaemia; Germ cell and embryonal neoplasms | Sanofi-Aventis U.S. LLC; United States | Phase II |
| 23 | TP-1287 [62] | 2044686–42-0 | Antineoplastic and immunomodulating agents | Sarcoma; Solid tumors | Tolero Pharmaceuticals Inc.; United States | Phase I |
| 24 | Voruciclib (P1446A) [63] |
1000023–04-0 | Antineoplastic and immunomodulating agents | Acute myeloid leukaemia; B-cell lymphoma | Piramal Life Sciences Co., Ltd.; India | Phase I |
| 25 | Recoflavone [64] | 203191–10-0 | Alimentary tract and metabolism | Gastritis | Dong-A St Co., Ltd.; Korea | Phase III |
| Sensory organs | Dry Eye | Dong-A St Co., Ltd.; Korea | Phase II | |||
| 26 | Oroxylin A (CPU-118) [65] | 480–11-5 | Antineoplastic and immunomodulating agents | Liver neoplasms, cellular lymphomas | China Pharmaceutical University; China | Phase I |
| 27 | Fisetin [66] | 528–48-3 | Musculo-skeletal system | Knee Osteoarthritis; Meniscus Repair | Austin V Stone; University of Kentucky; United States | Phase II |
| 28 | Quercetin [67] | 117–39-5 | Respiratory system | Chronic obstructive pulmonary disease | Internal Medicine, University of Michigan; United States | Phase II |
| 29 | Isoquercitrin [68] | 482–35-9 | Cardiovascular system | Venous thromboembolism | Quercis Pharma AG; Switzerland | Phase III |
| 30 | Pinocembrin [69] | 480–39-7 | Cardiovascular system | Ischemic stroke | CSPC ZhongQi Pharmaceutical Technology; China | Phase II |
| 31 | Naringenin [70], [71] | 93602–28-9 | Antiinfectives for systemic use | Hepatitis C Virus; HCV Infection; Chronic HCV Hepatitis C | Massachusetts General Hospital; Harvard University; United States | Phase I |
| 32 | Naringin [72] | 10236–47-2 | Respiratory system | Cough | Sun Yat-Sen University; China | Phase I |
| 33 | Tenalisib [73] | 1639417–53-0 | Antineoplastic and immunomodulating agents | Breast cancer; Chronic lymphocytic leukaemia; Non-Hodgkin's lymphoma | Rhizen Pharmaceuticals S.A.; Switzerland | Phase II |
| 34 | Genistein [74] | 446–72-0 | Respiratory system | Pulmonary fibrosis | National Institutes of Health; United States | Phase III |
| 35 | Epicatechin [75] | 490–46-0 | Musculo-skeletal system | Friedreich's ataxia | Cardero Therapeutics, Inc.; United States. | Phase II |
| 36 | Epigallocatechin [76] | 989–51-5 | Antiinfectives for systemic use | Hepatitis C virus infection | Egyptian Liver Research Institute and Hospital (ELRIAH), Egypt | Phase III |
| 37 | ABBV-2222 (GLPG2222) [77], [78] | 1918143–53-9 | Respiratory system | Cystic fibrosis | AbbVie, Inc.; United States | Phase II |
| 38 | Erteberel (LY500307) [79] | 533884–09-2 | Nervous system | Perimenopause-Related Depression | National Institute of Mental Health (NIMH); United States | Phase II |
| 39 | Elafibranor (GFT505) [80], [81] | 923978–27-2 | Alimentary tract and metabolism | Primary biliary cirrhosis | GENFIT S.A.; France | Phase III |
| 40 | Mitoflaxone (FAA) [82] | 87626–55-9 | Antineoplastic and immunomodulating agents | Cancer | Lipha Pharmaceuticals; France | Not in progress c |
| 41 | Riviciclib (P276-00) [83], [84] | 920113–02-6 | Antineoplastic and immunomodulating agents | Mantle-cell lymphoma; Solid tumors | Piramal Enterprises Limited, India | Not in progress |
| 42 | PD 98,059 [85] | 167869–21-8 | Antineoplastic and immunomodulating agents | Cancer | Pfizer Inc.; United States | Not in progress |
| 43 | Aminoflovone (AFP-464) [86], [87] | 165179–35-1 | Antineoplastic and immunomodulating agents | Breast cancer; Solid tumors | National Cancer Institute; United States | Not in progress |
| 44 | Flavodilol [88], [89] | 79619–31-1 | Cardiovascular system | Hypertension | Pennwalt Corporation; United States | Not in progress |
| 45 | Vitexin [90] | 3681–93-4 | Antineoplastic and immunomodulating agents | Radioprotective effects | Vietnam Institute of Traditional Medicine, Vietnam | Not in progress |
| 46 | Upidosin (Rec 15/2739) [91] | 152735–23-4 | Genito-urinary system and sex hormones | Benign prostatic hyperplasia | Recordati S.P.A.; Italy | Not in progress |
| 47 | Terflavoxate [92] | 86433–40-1 86433–39-8 |
Genito-urinary system and sex hormones | Urination disorders | Recordati S.P.A.; Italy | Not in progress |
| 48 | NPC-16377 [93] | 139652–86-1 | Nervous system | Neurological disorders; Psychotic disorders | Nova Pharmaceutical Corporation; United States | Not in progress |
| 49 | (±)-3′-Hydroxyfarrerol (IdB-1031) [94] | 95272–99-4 | Respiratory system | Respiratory tract disorders | Indena S.p.A.; Italy | Not in progress |
| 50 | Liquiritigenin [95] | 578–86-9 | Antineoplastic and immunomodulating agents | Menopausal hot flashes | Bionovo Inc.; United States | Not in progress |
| 51 | WS-7528 [96] | 132147–69-4 | Antineoplastic and immunomodulating agents | Cancer | Fujisawa Pharmaceutical Co. Ltd.; Japan | Not in progress |
| 52 | Silipid (IdB 1016) [97] | 134499–06-2 | Antineoplastic and immunomodulating agents | Ovarian cancer | Indena S.p.A.; Italy | Not in progress |
| 53 | Tectorigenin sodium sulfonate [98] | 807636–25-5 | Respiratory system | Acute respiratory infection and viral pneumonia | Sichuan Academy of Chinese Medicine Sciences; China | Not in progress |
| 54 | YM-26734 [99] | 144337–18-8 | Musculo-skeletal system | Rheumatoid arthritis | Yamanouchi Pharmaceutical Co. Ltd.; Japan | Not in progress |
| 55 | SU-740 [100] | 134336–72-4 | Alimentary tract and metabolism | Peptic ulcer | Taisho Pharmaceutical Co Ltd.; Japan | Not in progress |
Note: a) The compounds can be referred to by their common name, trade name, or code name; b) The research team responsible for the initial discovery or development of the pharmaceutical compounds; c) Not in progress means there are no clinical trial updates after 01/01/2015.