CG-200745 is a novel inhibitor of histone deacetylases (HDACs), initially developed by CrystalGenomics, Inc for treatment of various hematological and solid cancers. Combinations of CG-200745 with SN38 (the active form of irinotecan), or oxaliplatin were more effective than the agents alone when used to inhibit the growth of HCT116 cells. The protein expressions of acetyl-H3, p21, caspase-3, -8, and -9, PARP, and XIAP were affected in a time- and dose-dependent manner in HCT116 cells treated with the CG-200745 alone or combined CG-200745 and SN-38. In HCT116 xenografts, the HDACI CG-200745 in combination with irinotecan dramatically inhibited tumor growth without showing additive toxicity.

Cenerimod is an orally available sphingosine-1-phosphate receptor 1 (S1P1) modulator that is being developed by Idorsia Pharmaceuticals for the treatment of systemic lupus erythematosus. Sphingosine-1-phosphate (S1P), a lipid mediator, regulates lymphocyte migration between lymphoid tissue and blood. Cenerimod is a potent, selective, safe and orally administrable S1P1 receptor modulator, which reportedly reduced blood lymphocytes and attenuated murine experimental autoimmune encephalomyelitis (EAE) in a murine model. Cenerimod has potential as novel therapy with an improved safety profile for autoimmune diseases with a high unmet medical need.

Pranolium (UM-272) is propranolol derivative. It can reduce the extent of myocardial injury sustained during severe ischemia. UM-272 lacks significant beta-adrenergic blocking activity but retains the negative chronotropic, negative inotropic and antiarrhythmic effects common to both d- and l-propranolol. The protective effects of UM-272 during myocardial ischemia cannot be due to metabolic effects of the beta-adrenergic blockade but may be due to effects on oxygen consumption or to effects on myocardial membrane properties that are related to its antiarrhythmic and myocardial depressant activity. The ability of UM-272 to enhance blood flow to subendocardial myocardium may also play a role in its beneficial effects during ischemia. UM-272 may protect the ischemic heart through direct effects on myocardial Ca++ regulating mechanisms. UM-272 has kinetically similar use-dependent inhibitory action of the fast sodium channels of cardiac muscles as other Class Ia antiarrhythmic drugs like quinidine or procainamide. Pranolium was investigated as an antiarrhythmic agent.

Mitoglitazone (previously known as MSDC-0160 or CAY-10415) is a mTOT (mitochondrial target of thiazolidinediones) modulator that targets the mitochondrial pyruvate carrier (MPC), which is a key controller of cellular metabolism. MSDC-0160 is modulated MPC and act as insulin sensitizers without activating PPAR gamma. (Mitoglitazone exhibits very low binding affinity and activity at PPARγ). Mitoglitazone has been used in trials phase II studying the treatment of Type 2 Diabetes and Alzheimer's disease; the treatment for diabetes was discontinued. In addition, MSDC-0160 has demonstrated significant neuroprotective effects in the En1+/- mouse model of Parkinson’s disease via modulation of the mTOR-autophagy signaling cascade.