The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Thapsigargin is a potent inhibitor of Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) and is widely used to study Ca2+-signaling. Thapsigargin is a non-cell-type specific toxin with documented ability to kill a broad spectrum of cancer cell lines as well as normal endothelial cells, fibroblasts and osteoblasts. It induces a rapid and pronounced increase in the concentration of cytosolic calcium, due to blockade of the Sarcoplasmic/Endoplasmic Reticulum Calcium ATPase (SERCA) pump to which it binds with high affinity. The increase in cytosolic calcium leads to induction of apoptosis and ensuing cell death. A prodrug, G-202 (mipsagargin) has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. G-202 consists of a cytotoxic analog of thapsigargin coupled to a masking peptide which inhibits its biologic activity until proteolytic cleavage at the tumor site. The first clinical trials of this drug were initiated in 2008 for the treatment Advanced Solid Tumors.

DCFBC F-18 is a radioconjugate containing a low molecular weight tracer, DCFBC, specific for prostate-specific membrane antigen (PSMA) and labeled with the positron-emitting isotope fluorine F 18 with potential prostate tumor imaging upon positron emission tomography (PET). Upon administration, the DCFBC moiety of fluorine F 18 DCFBC specifically targets and binds to the tumor-associated antigen PSMA, thereby allowing the visualization of tumor cells expressing PSMA upon PET. F 18 DCFBC is investigated in phase 2 clinical trials in patients with prostate cancer.

Phenovalin is the laxative agent.

D-Methyldopa is an inactive isomer of methyldopa. It is known, that only L-isomer has the ability to inhibit dopa decarboxylase and possesses the antihypertensive activity in man. Moreover, about twice the dose of the racemate (DL-form of methyldopa) is required for the equal antihypertensive effect.

TRC-150094 is a synthetic compound that displays the capacity to stimulate energy expenditure. TRC-150094 increases whole body energy expenditure, increases mitochondrial fatty acid oxidation (FAO), and reduces abdominal adiposity in rats fed a high-fat diet. TRC-150094 attenuates the progression of hypertension, insulin resistance, dysglycemia, and atherogenic dyslipidemia, factors reported to signify significant cardiovascular (CV) risk amongst viscerally obese dysglycemic subjects. Moreover, at organ level, TRC150094 reduced steatohepatitis, reduced progression of nephropathy, and preserved cardiac contractile function. Pharmacological profile of TRC-150094 may constitute a promising new class of molecules that may have a potential beneficial therapeutic approach for the treatment of nontraditional CV risk factors and may reduce residual risk in viscerally obese dysglycemic patients. Moreover, the observed metabolic and functional effects on skeletal muscle suggest that TRC-150094 as a therapy may help to facilitate adherence to prescribed exercise, which would remain the mainstay along with diet control in such patients. Simultaneous systemic administration of TRC-150094 to rats receiving an high-fat diet results in a reduction in fat accumulation within the liver and a marked reduction in adipose tissue mass. TRC-150094 is in phase-III clinical trials for the treatment of diabetes mellitus, hypertension and dyslipidaemias (adjunctive treatment) in India.

There is no information about biological o medical application of ferrous orotate. But is known, that this substance may be used for nutritional purposes to food supplements.

p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials. Based on X-ray cocrystal structures a model of AMG 232 bound to MDM2 was developed. The model shows that the m-chlorophenyl, the p-chlorophenyl, and C-linked isopropyl fragments of AMG 232 bind to the Leu 26(p53), Trp 23(p53), and Phe 19(p53) pockets of MDM2, respectively. The carboxylic acid forms a salt bridge with His 96 and the isopropyl sulfone forms a novel interaction with the glycine shelf region of MDM2. AMG 232 in phase II in combination with trametinib and dabrafenib in subjects with metastatic melanoma; in phase I for the treatment of solid tumors, multiple myeloma and Acute Myeloid Leukemia.