Ore Pharmaceuticals developed ORE1001 previously known as MLN-4760 as an orally administered, small molecule compound, for the treatment of inflammatory bowel diseases. ORE1001 is a specific angiotensin-converting enzyme 2 inhibitor. It was shown that ORE1001 markedly decreased tissue myeloperoxidase activity, a well-known marker of inflammation. As a result, ORE1001 was studied as a treatment of gastrointestinal inflammatory conditions. ORE1001 was involved in phase I clinical trial to investigate its safety and activity in subjects with ulcerative colitis. In addition, the drug was studied for NSAID-induced ulcer and obesity. However, all these studies were discontinued.

AZD-7687 is a potent inhibitor of Diacylglycerol O-acyltransferase 1 (DGAT1) which was developed by AstraZeneca for the treatment obesity and type 2 diabetes mellitus. AZD-7687 reached phase I of clinical trials, but was discontinued by unknown reasons.

Saroglitazar, a dual peroxisome proliferator-activated receptor PPAR-α/γ agonist, was an emerging therapeutic option on glycemic and lipid parameters. The Zydus Group has launched LipaglynTM ((Saroglitazar) in India for diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In addition, saroglitazar participated in phase II clinical trials that completed enrolment in patients with primary biliary cholangitis and in patients with non-alcoholic steatohepatitis.

RO-638695 (also known as Miridesap, CPHPC and GSK-2315698) is an antineoplastic and a serum amyloid P component inhibitor. RO-638695 almost completely depletes circulating serum amyloid P component (SAP), but a small amount of SAP is left for recognition by subsequently administered therapeutic IgG anti-SAP antibodies. SAP is a blood protein that is the target of a novel immunotherapy approach. RO-638695 has therefore been evaluated in phase I and II clinical trials for its safety and potential in treatment of diseases like Alzheimer’s disease, HIV infection and other diseases with systemic amyloid deposition.

Arena Pharmaceuticals was developing APD-597 (JNJ-38431055), a small molecule, an orally active agonist of the G-protein coupled receptor 119 (GPR119), for the treatment of Type 2 diabetes mellitus. JNJ-38431055 was selected for preclinical development based on a good balance between agonist potency, intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. In addition, extensive in vivo studies showed a more favorable metabolic profile that may avoid the generation of long-lasting metabolites with the potential to accumulate in clinical studies. In humans, single-dose oral JNJ-38431055 increased postmeal plasma glucagon-like peptide 1 (GLP-1), glucose-dependent insulinotropic peptide (GIP), and peptide YY (PYY) concentrations but did not significantly decrease glucose excursion or increase insulin secretion. However, in a graded glucose infusion study, JNJ-38431055 was shown to induce a higher insulin secretion rate (ISR) relative to placebo at elevated plasma glucose levels. These studies provide evidence for the potential efficacy of JNJ-38431055 as an antidiabetes agent in humans.

Iodopyracet (Diodone) is a radiocontrast agent used in urography before 1950. Renal clearance of iodopyracet is characterized by supply-limited elimination at low plasma concentrations and capacity-limited elimination at high plasma levels. Iodopyracet to be an effective agent for the estimation of renal plasma flow and tubular function has been used extensively in physiological studies. In 1945 was found, that p-aminohippuric acid was in some ways superior to diodone for these estimations in man because the urine and plasma blanks are small and because diodone penetrates human red blood cells whereas p-aminohippuric acid does not.

Iodopyracet I-125 is radiolabeled Iodopyracet