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.

Fipamezole is a fluorine substituted imidazole compound with high antagonist specificity for the presynaptic alpha2-adrenoceptor. There were no significant differences between the affinity of Fipamezole for the different subtypes, thus characterizing Fipamezole as a non-subtype–selective alpha2 antagonist. Fipamezole had been in phase III clinical trials for the treatment of dyskinesia associated with Parkinson’s disease. Detected side effects are hypertension, nausea, vomiting, dysgeusia, facial flushing.

LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM. Eli Lilly is developing LY 2608204 as an orally administered, once-daily therapy for type 2 diabetes. LY-2608204 is in phase I clinical trials for the treatment of type 2 diabetes.

Premafloxacin is an 8-methoxy fluoroquinolone derivative patented by American pharmaceutical company Warner-Lambert Co. as an antibacterial agent. In preclinical studied. Premafloxacin was equivalent to ciprofloxacin, enrofloxacin, and danofloxacin in activity against the gram-negative bacilli but was much more active than the comparison antimicrobial agents (against the staphylococci, streptococci, and anaerobes. Premafloxacin acts as a topoisomerase IV inhibitor with enhanced activity against Staphylococcus aureus.

Axelopran (previously known as TD-1211), a peripherally selective, multivalent µ-opioid receptor antagonist that is under development by Theravance Biopharma. This drug participated in phase II clinical trials in subjects with opioid-induced constipation. The most common adverse events were abdominal pain, nausea, and diarrhea. There were no indications of opioid withdrawal effects or reductions in opioid analgesia in patients treated with axelopran.

Luminespib (NVP-AUY922) is a highly potent isoxazole-based, nongeldanamycin HSP90 inhibitor that inhibits the adenosine triphosphatase activity of HSP90. Luminespib is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib potently inhibited in vitro growth in all 41 NSCLC cell lines evaluated with IC50 less than 100 nM. IC100 value less than 40 nM was seen in 36 of 41 lines. Luminespib (NVP-AUY922) has greater potency, reduced hepatotoxicity, and lower dependence on DT-diaphorase than the first-generation HSP90 inhibitors. Luminespib was discovered in a multiparameter lead optimization program based on a high-throughput screening hit methodology developed jointly by The Institute of Cancer Research, UK and the pharmaceutical company Vernalis. It has been licensed to Novartis. Luminespib activity is independent of NQO1/DT-diaphorase, maintained in drug-resistant cells and under hypoxic conditions. The molecular signature of HSP90 inhibition, comprising induced HSP72 and depleted client proteins, was readily demonstrable. Pre-clinical studies proved that Luminespib acts via several processes (cytostasis, apoptosis, invasion, and angiogenesis) to inhibit tumor growth and metastasis. These results helped Luminespib to enter clinical trials for various cancers including breast cancers. From 2011 to 2014 it was in Phase II clinical trials.

AstraZeneca and BIND Therapeutics (formerly BIND Biosciences) are collaborating to develop AZD-1152HQPA (AZD2811) for the treatment of cancer. AZD2811, a novel, selective inhibitor of Aurora B kinase that has been shown to be active in both solid and hematological tumors in preclinical models, is the second Accurin candidate to enter clinical development. AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay. AZD1152-HQPA inhibited the proliferation of AML lines (HL-60, NB4, MOLM13), ALL line (PALL-2), biphenotypic leukemia (MV4-11), acute eosinophilic leukemia (EOL-1), and the blast crisis of chronic myeloid leukemia K562 cells with an IC50 ranging from 3 nM to 40 nM. The phase 1 trial is enrolling patients with advanced solid tumors, including patients with small cell lung cancer, and is being conducted by AstraZeneca under the companies’ 2013 collaboration agreement with BIND managing all chemistry, manufacturing and control activities.

Aftobetin, also known as ANCA11 and NCE-11, is a novel amyloid–binding compound applied topically in the form of an ophthalmic ointment. Aftobetin offers a promising way for a noninvasive eye-scan to diagnose Alzheimer’s disease early.

Stilbazium is a pyridinium derivative with considerable anthelminthic activity against some animal nematodes, including Syphacia obvelata, Ancylostoma caninum, Uncinaria stenocephala and Toxocara cati.