TAK-875 (Fasiglifam) is the potent, selective and orally bioavailable GPR40 agonist. The drug was in Phase III clinical trials for the treatment of type 2 diabetes mellitus. Termination phase III development of TAK-875 for the potential treatment of type-2 diabetes mellitus was announced in 2013 due to concerns about liver safety.

Glutathione arsenoxide (GSAO) is a peptide trivalent arsenical that has potential anti-angiogenic capability, suggesting that it could be used for treatment in cancers where tumor metastasis relies on new blood vessel formation (angiogenesis). Endothelial cell proliferation drives new blood vessel formation. GSAO treatment causes a concentration-dependent increase in superoxide levels, ATP depletion, mitochondrial depolarization, and apoptosis in proliferating, but not endothelial cells. GSAO is able to block blood flow to solid tumors in mice, thereby inhibiting tumor growth in mice with no apparent toxicity at efficacious doses. Initial experiments have implicated GSAO in perturbing mitochondrial function. Other molecular effects of GSAO in human cells, for example on the phosphorylation of proteins, are still largely unknown. A phase I clinical trial has been terminated.

Iodohippuric acid I-125 (I-I25 Hippuran) is radioisotope that was used as a renogram probe in nefhrography in 1960s-1970s. It is an analog of I-131 labeled I(131) hippuran which has been recognized as the radiopharmaceutical standard for the measurement of effective renal plasma flow in subjects with renal failure but which use has been compromised by the suboptimal imaging characteristics of the 364-keV photon of 131I and the delivery of relatively high radiation doses to kidneys and thyroid in patients with impaired renal function. It was shown that radiation risk was rendered to a minimum with the use of the "cocktail" of 169U-EDTA and 125I-hippuran.

FLORILGLUTAMIC ACID F-18 is a radioactive L-glutamate derivative and a tumor-specific positron emission tomography (PET) tracer. Orphan designation (EU/3/16/1632) was granted by the European Commission to Piramal Imaging GmbH, Germany, for FLORILGLUTAMIC ACID F-18 for the diagnosis of hepatocellular carcinoma. Currently, it is in phase II trial as a PET tracer in early lung cancer in patients with lung nodules.

Golvatinib is a highly potent, small-molecule, ATP-competitive inhibitor of c-Met and multiple members of the Eph receptor family plus c-Kit and Ron. Eisai was developing an oral formulation of golvatinib, which acts as both a c-Met inhibitor and a vascular endothelial growth factor receptor 2 antagonist with potential antineoplastic activity. Golvatinib binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis. Clinical trials involving several forms of cancer are currently underway.

Oprozomib (PR-047) is an orally bioavailable derivative of carfilzomib, with similar biological activity, i.e. inhibition of the chymotrypsin-like activity of the proteasome. It inhibits the activity of the proteasome, thereby blocking the targeted proteolysis normally performed by the proteasome; this may result in an accumulation of unwanted or misfolded proteins. Disruption of various cell signaling pathways may follow, eventually leading to the induction of apoptosis and inhibition of tumor growth. Oprozomib (PR-047) is being investigated for the treatment of hematologic malignancies, specifically, multiple myeloma, with Phase I/II trial ongoing.

Carfluzepic Acid is benzodiazepine derivative with tranquilizing, anticonvulsant, and anxiolytic activity patented by pharmaceutical company C. M. Industries S. A.

Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.