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.

Levovirin is a guanosine nucleoside analog and the L-enantiomer of ribavirin. It is an investigational drug for the treatment of hepatitis C virus-mediated diseases. Levovirin has a similar immunomodulatory potency to ribavirin in vitro without accumulating in red blood cells or causing hemolytic anemia, a known side effect of ribavirin. Levovirin has been shown to stimulate host immune responses (enhanced Th1 and reduced Th2 cytokine expression). Significantly improved oral absorption of levovirin was achieved following administration of a valine ester prodrug of levovirin R1518. Levovirin was found more potent to inhibit Tick-borne encephalitis virus (TBEV) on the basis of robust binding affinity between protein-drug interactions. This finding may help to understand the nature of helicase and development of specific anti-TBEV therapies.

Agnuside (AGN), an iridoid glycoside, is the principle active phytoconstituent and a chemotaxonomic marker of the genus Vitex. It is isolated from V. agnus castus, V. negundo, and V. cymosa and composed of aucubin and p-hydroxy benzoic acid (PHBA). Agnuside has exhibited estrogen-like activity which might be the reason for its use in premenstrual syndrome problems in women of fertile age as well as in menopause. It has also been reported to possess anti-arthritic activity in the polyarthritis rats which was associated with significant suppression of the inflammatory mediators and T-cell mediated cytokinines. Recently, Agnuside has shown higher hepatoprotective potential in rats in comparison to silymarin, a commercially available herbal hepatoprotective agent. In addition, Agnuside has shown an inhibitory effect on P-glycoprotein (P-gp) ATPase activity. The diversified therapeutic indications of AGN with a profoundly high medicinal value have created great curiosity among researchers for its further investigation as a medicinal agent.

Roquinimex (Linomide, LS 2616) is a quinoline-3-carboxamide with pleiotropic immune modulating capacity and it has therapeutic effects in several experimental animal models of autoimmune diseases. Linomide has been evaluated in clinical trials for multiple sclerosis, and was indeed shown to have disease inhibitory effects. However, due to unexpected side effects recorded in patients treated with Linomide, premature termination of clinical trials was required. The basic mechanism(s) of action of Linomide in inducing beneficial effects in autoimmune diseases is still elusive. Some experimental evidence indicates that Linomide influences the regulation of the cytokine profile, resulting in the inhibition of autoimmune and inflammation pathologies. Roquinimex possesses potential antineoplastic activity. Roquinimex inhibits endothelial cell proliferation, migration, and basement membrane invasion; reduces the secretion of the angiogenic factor tumor necrosis factor alpha by tumor-associated macrophages (TAMs); and inhibits angiogenesis. Roquinimex was in phase III clinical trials with Pharmacia Corporation in Europe and the US for the treatment of multiple sclerosis.

Levovirin is a guanosine nucleoside analog and the L-enantiomer of ribavirin. It is an investigational drug for the treatment of hepatitis C virus-mediated diseases. Levovirin has a similar immunomodulatory potency to ribavirin in vitro without accumulating in red blood cells or causing hemolytic anemia, a known side effect of ribavirin. Levovirin has been shown to stimulate host immune responses (enhanced Th1 and reduced Th2 cytokine expression). Significantly improved oral absorption of levovirin was achieved following administration of a valine ester prodrug of levovirin R1518. Levovirin was found more potent to inhibit Tick-borne encephalitis virus (TBEV) on the basis of robust binding affinity between protein-drug interactions. This finding may help to understand the nature of helicase and development of specific anti-TBEV therapies.