Ponalrestat is the inhibitor of aldehyde reductase 2 from a number of sources. Ponalrestat blunted Prostaglandin F2 alpha synthesis by preadipocytes in basal and stimulated conditions. Ponalrestat suppresses IL-1 production both in vitro and in vivo, and inhibits the cachectic symptoms induced by colon26 adenocarcinoma in mice, suggesting that ponalrestat has a therapeutic potential for the treatment of cancer cachexia. In a 4-week study of 29 neuropathic diabetics treated with ponalrestat peripheral neuropathy did not improve during treatment. In a 6-week study of 21 diabetics without neuropathy, although vagal function improved in patients with autonomic neuropathy.

Poziotinib is an inhibitor of EGFR tyrosine kinase family. The drug is being tested in phase II of clinical trials for different cancers: breast cancer, lung adenocarcinoma, head and neck squamous cell carcinoma, HER-2 positive advanced gastric cancer (in combination with Paclitaxel and Trastuzumab).

Belizatinib, also known as TSR-011, is an orally available inhibitor of both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases (TRK) TRKA, TRKB, and TRKC, with potential antineoplastic activity. Upon administration, ALK/TRK inhibitor TSR-011 binds to and inhibits both ALK and TRK kinases. The inhibition leads to disruption of ALK- and TRK-mediated signaling and impedes tumor cell growth in ALK/TRK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors.

L-Arabinose is a monosaccharide extracted from plant gums, corn fiber and beet pulps. It is a poorly-absorbed, readily-available sweet-tasting pentose. L-Arabinose is known to suppress obesity by regulating the fasting blood glucose level and the insulin resistance index. L-arabinose is a non-caloric sugar. L-arabinose may inhibit intestinal sucrase activity and thereby delay sucrose digestion.

Semaxanib is a potent and selective vascular endothelial growth factor (VEGF) receptor protein tyrosine kinase 1/2 inhibitor that also inhibits other tyrosine kinases KIT, MET, FLT3, and RET. Semaxanib inhibited cell migration of human vascular endothelial cells expressing both Flt-1 and KDR in response to VEGF and also inhibited the cell migration in response to placenta growth factor (PIGF), a specific ligand for Flt-1. Chemotaxis of monocytes expressing only Flt-1 was also inhibited by SU5416 in a dose-dependent manner. Semaxanib targets the VEGF pathway, and both in vivo and in vitro studies have demonstrated antiangiogenic potential. On February 2002, Pharmacia, the then-parent of Sugen, prematurely ended Phase III clinical trials of Semaxinib in the treatment of advanced colorectal cancer due to discouraging results.

GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. In vivo efficacy studies in mouse xenograft or allograft models of human leukemia demonstrated that GZD824 successfully suppressed the growth of tumors driven by native Bcr-Abl, Bcr-Abl T315I, Bcr-Abl G250E, Bcr-Abl Q252H, Bcr-Abl E255K and Bcr-Abl F317L. GZD824 also provided a significant survival benefit leukemia model mice allografted with luciferase-expressing Ba/F3 cells driven by the mutant Bcr-Abl T315I kinase. The potential for compound GZD824 to overcome all of the Bcr-Abl mutations that result in clinically acquired resistance to imatinib indicates that this novel Bcr-Abl inhibitor is a promising lead candidate for further development. GZD824 has also being shown to suppresses pre-B ALL cells through inhibition of the SRC kinase and PI3K/AKT pathways and may be a potential therapeutic agent for the management of pre-B ALL.

Senexin B is a selective CDK8/CDK19 inhibitor developed by Senex Biotechnology Inc. Senexin B is an ATP pocket binder, with very high target selectivity as indicated by kinome profiling. CDK8/19 inhibition produces chemopotentiating, chemopreventive and anti-metastatic effects in different types of cancer.

(3,5-DIBROMO-4-HYDROXYPHENYL)(2,3-DIHYDRO-4H-PYRIDO[4,3-B][1,4]OXAZIN-4-YL)METHANONE (UR-1102/URC-1022) is currently under development for the management of hyperuricaemia in gout. It is a selective URAT1 inhibitor with Ki of 57 nM showing higher uricosuric effects than benzbromarone in monkeys with potentially lower mitochondrial toxicity which is supposed to be related to hepatotoxicity. There is also a probable inhibition of OAT1 and OAT3. UR-1102, which is derived from the chemical structure of benzbromarone, was designed to not only improve URAT1 selectivity and solubility but also to avoid the hepatic toxicity concern of benzbromarone, which is known to be associated with hepatic injury and to have the potential to cause fulminant hepatitis in humans. The results of two phase II trials presented at the 2017 ACR meeting suggested a high potency for reducing SU levels with a good safety profile on a short follow-up. No phase III trial has been registered so far.