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.

Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for the treatment of gout and asymptomatic hyperuricemia. Verinurad specifically inhibits URAT1 with a potency of 25 nM. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike other available uricosuric agents, the requirement for Cys-32 is unique to verinurad. Verinurad doses as low as 2.5 mg produce significant sUA lowering in humans, and this greater reduction in sUA may lead to improved outcomes and medical benefits for patients with gout. Verinurad in monotherapy studies has been associated with increased urinary uric acid concentrations and low rates of serum creatinine (sCr) elevation. Verinurad combined with febuxostat decreased sUA dose-dependently while maintaining uric acid excretion similar to baseline. All dose combinations of verinurad and febuxostat were generally well tolerated.

Gadocoletic acid (also Gadoletic acid trisodium salt, or B22956/1) is a magnetic resonance contrast agent. Based on results from animal imaging experiments and pharmacokinetic data it was suggested that gadocoletic acid trisodium salt has strong potential for clinical use in Magnetic Resonance Coronary Angiography and Myocardial Perfusion Imaging. The small molecules of gadocoletic acid are bound after injection to large human serum albumin molecules in coronary vessels with the result of high vessel/muscle contrast. The ability of B229563− (anion) to bind to more than one site on the albumin molecule allows a positive correlation between dose and blood relaxation rate enhancement at doses higher than 0.05 mmol/kg, the dose that produces roughly a total plasma concentration equimolar to the albumin concentration at equilibrium distribution. Gadocoletic acid is thought to be highly efficacious in inversion recovery-prepared 3D gradient-recalled echo, navigator echo-gated coronary angiography in humans already at doses below 0.1 mmol/kg.

Piridronic acid is pyridinyl bisphosphonate. It is the bone calcium metabolism regulator. Piridronic acid was used for the treatment of osteoporosis. It is the human farnesyl pyrophosphate synthase inhibitor. When expressed on an actual or anticipated clinical dose basis for osteoporosis piridronic acid may have a greater potential for inducing gastric damage than do pyridinyl bisphosphonates. Piridronic acid induced significantly more antral damage than risedronate and a greater number of lesions compared to pamidronate and risedronate.

Tungstic acid is a fairly strong acid, it catalyzes the oxidation by hydrogen peroxide of alkenes to the corresponding epoxides. Tungstic acid is widely used in the production of tungsten metal, alloys, and is used as a mordant for textiles and plastics. Tungstic acid has been reported to rapidly precipitate the quaternary ammonium cations in cholinergic nerve terminals, such as ACh or choline. Also, tungsten dietary supplementation has successfully been used to reduce xanthine oxide (XO) activity, resulting in decreased gastrointestinal (GI) mucosal damage because of lowered XO activity. Tungstic acid has been shown to effectively antagonize stress-induced gastric ulcers, possibly by decreasing motility and mass cell degranulation. Tungstic acid gel has been used as an epileptogenic agent since 1960. Epilepsy produced by this agent is characterized by good localization, short latency and limited duration. It is effective in cerebral cortex, brain stem and spinal cord.

Gluceptate sodium also known as sodium glucoheptonate (H-Quest A300) is a non-toxic, a non-hazardous chelating agent, which forms stable complexes with di- and trivalent metal ions such as Ca2+, Fe2+, Fe3+, Al3+, etc. This substance is highly compatible with strong alkaline mediums and can prevent the bacterial degradation of the solution. Gluceptate sodium has various applications in water treatment, agricultural, cosmetics, textile processing and in some others fields.

Squaric acid is a dibasic organic acid and useful intermediate in a variety of synthetic reactions involving the synthesis of photosensitive squarylium dyes and inhibitors of protein tyrosine phosphatases. Medically, squaric acid dibutyl ester or dibutyl squarate derives from a squaric acid is used for the treatment of warts.

D-aspartic acid is an essential amino acid and a key ingredient in various testosterone boosting anti-estrogen supplements. D-aspartic acid is not used to build proteins; instead, it plays a role in making and releasing hormones in the body. It is an endogenous NMDA receptor agonist with similar activity to the L-isomer. D-aspartic acid also enhances the release of luteinizing hormone (LH) and testosterone. This action is mediated in the pituitary by cGMP and in the testis by cAMP, which acts as the second messengers in the signal transduction in the pituitary and testes respectively. The pituitary and testis possess a D-Aspartate racemase, which provides the necessary production of this isomer.