Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor. It selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. The major organ of icotinib metabolism is the liver, with the primarily enzymes being CYP2C19 and CYP3A4 from the cytochrome P450 monooxygenase system. Icotinib Hydrochloride was approved for the treatment of patients with advanced stage Nonsmall cell lung cancer by the State Food and Drug Administration (SFDA) of China. The major drug related adverse reactions of the traditional cytotoxic agents include rash, diarrhea, severe bone marrow suppression, neuropathy, hair loss, and gastrointestinal reactions. Icotinib is under investigation as an active agent against other EGFR mutation-positive cancers, like lung adenocarcinoma, oesophageal cancer, nasopharyngeal cancer and others.

Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor used for the treatment of type 2 diabetes mellitus. Trelagliptin (as the salt Trelagliptin succinate) was approved for use in Japan in March 2015. Takeda, the company that developed Trelagliptin, chose to not get approval for the drug in the USA and EU.

Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is the major lipophilic flavonoid from Artemísia umbellifórmis, mountain wormwood used for the production of the celebrated alpine liqueur genepy. Eupatilin is the active ingredient of Stillen, a herbal drug from the Asian wormwood Artemisia asiatica, developed in South Korea for the treatment of gastritis and peptic ulcer. Eupatilin has been shown to exert cytoprotective and antiapoptotic effects on gastric and esophageal epithelial primary cells and is endowed with antispasmodic and antimutagenic properties, while apoptotic and anti-proliferative activities have been demonstrated on cancer cells. Eupatilin has also been evaluated, with promising results, in several assays of relevance for inflammation and allergy. Thus, this flavonoid inhibits in vitro mast cell degranulation and histamine release, shows in vivo anti-allergic properties is an antioxidant, inhibits 5-lipoxygenase and the leukotrienes synthesis, decreases prostaglandin E2 production, and inhibits the activation of nuclear transcription factor NF-κB and the expression of cyclooxygenase-2 and different pro-inflammatory cytokines, such as interleukins (IL-4, IL-6, and IL-8) and tumor necrosis factor-R (TNF-R)

Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.

Vitexin, identified as apigenin-8-C-β-D-glucopyranoside, is a flavonoid compound found in Anthurium versicolor, Ficaria verna Huds. (Ranunculaceae), Cucumis sativus L. (Cucurbitaceae), and Acer palmatum (Aceraceae). Vitexin is an active component of many traditional Chinese medicines. Vitexin has recently received increased attention due to its wide range of pharmacological effects, including but not limited to anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.

Indirubin is derived from the Indigo Plant (Isatis Root, Isatis Leaf). It is used as part of a traditional Chinese herbal prescription called Dang Gui Long Hui Wan, to treat chronic myelogenous leukemia (CML). Indirubin inhibits DNA synthesis in several cell lines, in a cell-free assay and in vivo in rats with Walker-256 sarcoma. A weak binding of indirubin to DNA in vitro has been described. Indirubin inhibited all cyclin-dependent kinases (1,2,4,5) almost equally. Indirubin has been approved for clinical trials against chronic myelocytic and chronic granulocytic leukaemia. A few studies show that Indirubin is effective against psoriasis. Mild to severe nausea, vomiting, abdominal pain, diarrhea, headache, and edema are reported adverse events of Indirubin. Long-term oral ingestion has also occasionally been associated with hepatitis, pulmonary arterial hypertension and cardiac insufficiency.

Gentiopicrin is a naturally occurring iridoid glycoside. It is a bioactive component of gentian species of medical plants. It has proved to be the strongest inhibitor of myeloperoxidase. It could be absorbed rapidly in mice, but with a low bioavailability, and could distribute to tissues extensively. Gentiopicrin has been reported to be effective against inflammatory conditions such as rheumatoid arthritis, liver illness, fever, digestive and intestinal disorders. Gentiopicrin treatment can exert anti-inflammatory effects on experimental acute colitis through attenuating the expression levels of TNF-α, IL-1β, IL-6, iNOS and COX-2, and it may present the therapeutic potential in the treatment of colitis. The drug inhibits reserpine-induced pain/depression dyad by downregulating GluN2B receptors in the amygdala. Gentiopicrin injection was approved by SFDA for the treatment of acute jaundice and chronic active hepatitis.

Luseogliflozin (TS-071), a derivative of a novel scaffold, C-phenyl 1-thio-D-glucitol, exhibited potent sodium-dependent glucose cotransporter (SGLT) 2 inhibition activity. Luseogliflozin exhibits a blood glucose lowering effect, excellent urinary glucose excretion properties, and promising pharmacokinetics profiles in animals. It showed good metabolic stability toward cryo-preserved human hepatic clearance, have acceptable human pharmacokinetics properties. Luseogliflozin [Lusefi(®) (Japan)] was developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus. The drug has received its first global approval for this indication in Japan, either as monotherapy or in combination with other antihyperglycaemic agents.

Nitrovin (hydrochloride salt) is a discontinued food additive that was used in veterinarian practice to promote growth. Nitrovin was shown to inhibit Salmonella growth both in vitro and in vivo (in chickens).

Hydroxynaphthoic acid is a salt part of discontinued drug Bephenium hydroxynaphthoate. It was also shown to have anti-diabetic effect in mice, acting as a chemical chaperone and reducing ER stress.