Ecalcidene (1-[(1alpha,3beta,5Z,7E,20S)-1,3-dihydroxy-24-oxo-9,10-secochola-5,7,10(19)-trien-24-yl]-piperidine) is a 1-hydroxyvitamin D analogue. Ecalcidene was being developed by Barrier Therapeutics as an oral therapy for psoriasis and acne. However, development has been discontinued.

Tisocalcitate is the vitamin D derivative. Tisocalcitate ointment is currently in phase 2 clinical development for mild to moderate psoriasis. Early studies have shown that, unlike other vitamin D3 analogues, tisocalcitate does not affect calcium metabolism. Tisocalcitate ointments were tolerated well and were safe to use on healthy skin. Tisocalcitate had been in phase II clinical trial for the treatment of psoriasis. However, this development was discontinued.

Transcrocetinate (TSC) is a novel compound that offers promise as a treatment for conditions caused by hypoxia or ischemia. Unlike crocetin, it worked well in the more severe hemorrhagic shock model. Although many of the earlier studies with TSC involved the treatment of the ischemic conditions of hemorrhagic shock in both rats and swine, a few other studies involved treating purely hypoxic situations. One study showed that TSC was capable of promoting survival in rats breathing 10% oxygen. TSC also was able to increase arterial PO2 values in a rat model of acute respiratory distress syndrome (ARDS) caused by injection of oleic acid. The drug acts via a mechanism that has not been previously exploited in a pharmaceutical. TSC increases the rate of oxygen diffusion between the erythrocytes and the tissues by altering the 'structure' of water in blood plasma. It does this by causing additional hydrogen bonds to form among the water molecules. Animal toxicology studies have demonstrated that high levels of TSC are well-tolerated, and a Phase I clinical study has shown that TSC is also safe in humans. Delayed TSC treatment improves outcomes in experimental models of both ischemic and hemorrhagic stroke. TSC may be a safe and beneficial therapeutic modality for early stroke intervention, irrespective of the type of stroke involved. Transcrocetinate is in phase III clinical trial for the treatment of glioblastoma.

Ortetamine, also known as 2-methylamphetamine, is a monoamine releaser that was studied as a stimulant drug. Information about the current use of this drug is not available.

Aldose reductase-IN-1 is an inhibitor of aldose reductase

OTS-167 is a maternal embryonic leucine zipper kinase (MELK) inhibitor which demonstrated antitumor properties in laboratory tests. It is being developed as an anti-cancer drug. The compound has been shown to suppress the growth of breast, lung, pancreatic and prostate cancer cells that express high levels of the MELK protein. OTS167 reached phase II clinical trials in patients with AML, ALL, advanced MDSs, advanced MPNs, or advanced CML and phase I in patients with breast cancer.

LY-3000328 is a Cathepsin S inhibitor with excellent in vitro potency and selectivity against other cysteine proteases. LY-3000328 is currently in clinical trials. Cathepsin S (Cat S) plays an important role in many pathological conditions, including abdominal aortic aneurysm (AAA). Inhibition of Cathepsin S may provide a new treatment for AAA.