Azaspirium was studied as a spasmolytic and antihypertensive agent.

Otenabant (CP-945,598) is Pfizer developed as a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, which exhibits 10,000-fold greater selectivity against human CB2 receptor, for treatment of obesity. In clinical trial III Pfizer decided to discontinue the development program based on changing regulatory perspectives on the risk/benefit profile of the CB1 class and likely new regulatory requirements for approval.

1,​2-​Dioleoyl-​sn-​glycero-​3-​phospho-​L-​serine Sodium Salt is a lipid being studied in the assembly and long-term stability of solid supported lipid bilayers from artificial and natural lipid mixtures.

Elacytarabine (CP-4055 or araC-5'elaidic acid ester) is a lipid-conjugated derivative of the nucleoside analog cytarabine. Elacytarabine blocks cell division and may kill cancer cells. It is a type of antimetabolite. It was studied in clinical trials for the treatment of solid tumors. In preclinical and clinical studies, elacytarabine has demonstrated both safety and efficacy in acute myeloid leukemia (AML), with noteworthy activity among the cytarabine-refractory AML population. Elacytarabine was granted orphan drug designation status from the European Commission in 2007 and from the US FDA in 2008, with a fast-track approval designation from the FDA in 2010. Elacytarabine development has been discontinued.

Omtriptolide (previously known as PG490-88 or F60008), an immunosuppressant that has been shown to be the safe and potent antitumor agent and it has been approved entry into Phase I clinical trial for the treatment of prostate cancer in the USA. In addition, the drug is participating in phase I clinical trial for the treatment of myeloid leukemia. Experiments on animals have shown omtriptolide was highly effective in the prevention of murine graft-versus-host disease (GVHD). The immunosuppressive effect of the drug was mediated by inhibition of alloreactive T cell expansion through interleukin-2 production. However, this study was discontinued. Recently published article has shown omtriptolide possesses the potential as a prophylactic agent to prevent ischemia/reperfusion (I/R)-induced lung injury.

FIDUXOSIN is a selective alpha1-adrenoceptor antagonist with higher affinity for alpha1A-adrenoceptors and for alpha1D-adrenoceptors than for alpha1B-adrenoceptors. It was in clinical trials for the treatment of benign prostatic hyperplasia.

BIIB021 binds in the ATP-binding pocket of Hsp90, interferes with Hsp90 chaperone function, and results in client protein degradation and tumor growth inhibition. Hsp90 is overexpressed in many types of cancer and acts to stabilize malignancy producing oncoproteins. Therefore, inhibition of Hsp90 with BIIB021 leads to the degradation of oncoproteins that drive malignancy.

Sprodiamide is a nonionic paramagnetic dysprosium chelate agent patented by Salutar, Inc.as diagnostic imaging contrast media. Compare with gadolinium-based agents Sprodiamide shows a stronger T2 effect and negligible T1 effect. This property makes Sprodiamide useful for blood volume imaging. In a preclinical model of reperfused ischemia of the rat intestine administration of Sprodiamide improved the contrast between the normal and ischemic intestine on T2-weighted images, and administration of both gadodiamide and Sprodiamide improved the contrast on T1- and T2-weighted images.

Tiviciclovir (A188) is a nucleoside analog used in the synthesis of antiviral drugs. This acyclic guanosine analog has a potential for the treatment of hepatitis B virus. However, as with penciclovir and the related compounds acyclovir and ganciclovir, the intestinal absorption of Tiviciclovir is limited. One approach to overcome this is through synthesis of the 6-deoxy prodrug version of AM188, i.e. AM365, which has improved intestinal absorption. Following absorption, the 6-deoxyguanosine analog AM365 is converted to the corresponding anti-virally active guanosine analog, AM188, probably by the liver molybdenum hydroxylases, aldehyde oxidase and xanthine oxidase. Renal tubular secretion of AM188 involves organic anion and cation transport systems.

SN38 (7-ethyl-10-hydroxy camptothecin) is a prominent and efficacious anticancer agent. It is poorly soluble in both water and pharmaceutically approved solvents; therefore, the direct formulation of SN38 in solution form is limited. SN38 is formed via hydrolysis of irinotecan by carboxylesterases and metabolized via glucuronidation by UGT1A1. Currently, the water soluble prodrug of SN38, irinotecan (CPT-11), is formulated as a low pH solution and is approved for chemotherapy. SN38 causes the strongest inhibition of DNA topoisomerase I, followed by CPT and then CPT-11. CPT-11 dose dependently shifts the position of relaxed DNA in the direction of nicked DNA, but SN38 and CPT shows no effect on the position of relaxed DNA. SN38 dose-dependently and time-dependently inhibit DNA synthesis. Respective IC50 values of SN38, in DNA synthesis is 0.077 uM.