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.

Valnivudine, also known as FV-100, a prodrug that has been indicated as a potential antiviral for the treatment of shingles (herpes zoster) that could both reduce the pain burden of the acute episode and reduce the incidence of post‐herpetic neuralgia compared to available treatments. Phase I clinical trial with FV100 showed safety and tolerability in healthy volunteers. Valnivudine also participated in phase III, where its efficacy was compared with valacyclovir; however, the study was terminated.

Heidelberg Pharma Research developed fosalvudine tidoxil, a prodrug derived from the nucleoside reverse transcriptase inhibitor alovudine, for the treatment of HIV infections. This drug had reached phase II clinical trials before its development was discontinued.

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.

Flumatinib (HHGV678) is an orally bioavailable antineoplastic tyrosine kinase inhibitor. Flumatinib inhibits the wild-type forms of Bcr-Abl, platelet-derived growth factor receptor (PDGFR) and mast/stem cell growth factor receptor (SCFR; c-Kit) and forms of these proteins with certain point mutations. Flumatinib was extensively metabolized after oral administration, and the major metabolic pathways observed were amide hydrolysis, demethylation, oxidation, and glucuronide conjugation. It is in phase III clinical trials for the treatment of Chronic myeloid leukemia (in China).

Atopaxar, also known as E 5555 is a novel reversible protease-activated receptor-1 (PAR-1) thrombin receptor antagonist. The inhibition of thrombin-mediated platelet activation by means of protease-activated receptor-1 inhibitors represents an attractive therapeutic option for patients with atherothrombotic disease processes. In preclinical studies, atopaxar demonstrated inhibition of thrombin receptor-activating peptides (TRAP)- and thrombin-induced platelet aggregation. Atopaxar was being developed by Eisai for acute coronary syndromes (ACS) and coronary disorders, including atherothrombosis, unstable angina pectoris and myocardial infarction. Atopaxar was in phase II clinical development in the US, EU and Japan. However, development was discontinued in May 2012.

Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.

Bombesin (BN), a neuropeptide that originally was purified from the skin of the European frog (Bombina bombina). It has many biological effects including hormone release, stimulation of pancreatic enzyme secretion, gallbladder contraction and bronchoconstriction. Bombesin is a highly specific marker of neuroendocrine differentiation and thus a valuable tumor marker. It activates three different G-protein-coupled receptors known as BBR1, -2, and -3.