Cloquinate is an amoebicidal drug, discovered in the 1950s. It is a salt of 7-iodo-8-oxyquinoline-5-sulfonic acid (Yatren) with resochin. Cloquinate was marketed by Bayer under tradename Resotren. In clinical trials, it was demonstrated to treat abdominal and hepatic symptoms of amoebiasis.

Sipoglitazar (TAK 654) was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARγ, PPARα, and PPARδ. Sipoglitazar was developed to improve peripheral insulin sensitivity, normalize circulating lipid profiles, and reduce body weight in patients with metabolic syndrome and type 2 diabetes mellitus (T2DM). Sipoglitazar was being developed by Takeda for the treatment of diabetes mellitus, however in September 2006, development was discontinued.

Irosustat is a first-generation, orally active, irreversible steroid sulfatase inhibitor. It did not stimulate the growth of estrogen-sensitive MCF-7 breast cells in vitro. Irosustat was in phase II clinical trials for the treatment of breast cancer and endometrial cancer and phase I clinical trial for the treatment of prostate cancer. However, this research has been discontinued.

Roxolonium, a derivative of glycyrrhetic acid, was studied as an antiulcer agent. Information about the further development of this compound is not available.

Ciclafrine is azaspiroalkane derivative patented by pharmaceutical company Goedecke A.-G. for the low blood pressure treatment

Deferitazole is an iron chelator, developed by the FerroKin BioSciences (later acquired by Shire, and then by Takeda). Deferitazole is a member of the desazadesferrithiocin class of siderophore-related tridentate chelators. It binds Fe(III) with very high affinity and selectivity over Fe(II) and other biologically important metals. Deferitazole was investigated in phase 2 clinical trials in patients with iron overload due to repeated red blood cell transfusion and beta-thalassemia, however, the development of the drug was discontinued. In preclinical models, deferitazole demonstrated efficacy for the treatment and prevention of malaria.

Lorglumide (CR1409) is the first nonpeptidic, selective and potent inhibitor of the cholecystokinin-A and cholecystokinin-B receptors. Lorglumide prevented dose-dependently the emptying of the gallbladder in both experimental models; proglumide exhibited a comparable activity at much higher doses. Lorglumide was associated with significantly inhibited cell growth of human pancreatic cancer cell line Mia PaCa-2 in vitro. Lorglumide also induced G0/G1 cell cycle arrest and apoptosis. The change of invasion ability appeared to be mediated by MMP-2 expression, which was upregulated by CCK-8S and downregulated by lorglumide. Lorglumide had been in preclinical phase for the treatment of biliary dyskinesia, pancreatitis and cancer. However, this development was discontinued.

Lopobutan is an antiseptic agent.

FLOVAGATRAN is a potent, reversible, low-molecular-weight, highly selective synthetic direct thrombin inhibitor that has demonstrated promising pharmacokinetic properties and biological activity in preclinical studies. However, its development for thrombosis was discontinued in Phase II.

Cu-64 is a radioisotope of copper with T1/2 12.7 hours. It decays by emission of beta+ particles with energies 0.653 (17.8%) MeV, which makes it suitable for positron emission tomography. The most widely used Cu chelators are DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid). Cu-64 acetate is used as a model compound to study metabolism and distribution of Cu-64.