TIC10 (TIC10 isomer or ONC201 isomer) is a potent, orally active, and stable small molecule and is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). The isomeric structure of TIC10/ONC201 is critical to its activity: anti-cancer activity is associated with the angular structure and not the linear TIC10 isomer. TIC10 transcriptionally induces a sustained up-regulation TRAIL in tumors and normal cells in a p53-independent manner. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 crosses the blood-brain barrier. TIC10 treatment caused tumor regression in the HCT116 p53−/− xenograft, RKO human colon cancer xenograft–bearing mice and human triple-negative breast cancer xenografts and significantly prolonged the survival of Eμ-myc transgenic mice, which spontaneously develop metastatic lymphoma from weeks 9 to 12 of age by 4 weeks.

Dexecadotril is powerful and selective inhibitor of neprilysin. It is anti-hypotensive agent. Dexecadotril was found to possess chemoprotective activity. It might be biologically active against multiple myeloma. It was under clinical evaluation as an intestinal antisecretatory agent.

Ampion (LMWF-5A) is a low molecular weight fraction of human serum albumin (HSA) currently being developed for the treatment of pain due to osteoarthritis of the knee. The primary constituent ingredient of Ampion is aspartyl-alanyl diketopiperazine, or DA-DKP, an endogenous immunomodulatory molecule derived from the N-terminus of HSA. Based on published pre-clinical and clinical research, DA-DKP plays a significant role in the regulation of inflammation. DA-DKP is believed to reduce inflammation by suppressing pro-inflammatory cytokine production in T-cells. Ampion also contains other known small molecules that confer anti-inflammatory effects to complement the activity of DA-DKP and derive demonstrated in-vitro and in-vivo effects. Ampio is currently developing Ampion as an intra-articular injection to treat osteoarthritis of the knee, and the final US pivotal trial is underway. Additional pre-clinical and clinical studies have been completed or are underway for Ampion and other chronic inflammatory conditions.