FENIROFIBRATE, (-)- is a metabolite of fenofibrate, an antilipemic agent which reduces both cholesterol and triglycerides in the blood.

Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.

BMS-191011, an opener of the cloned large-conductance, Ca2+-activated potassium (maxi-K) channel, demonstrated efficacy in in vivo stroke models, which led to its nomination as a candidate for clinical evaluation. Its maxi-K channel opening properties were consistent with its structural topology, being derived by combining elements from other known maxi-K openers. BMS-191011 demonstrated efficacy as an opener of the cloned large-conductance Ca2+-activated potassium (maxi-K) channel in in vivo stroke models

Propafenone, (S)- is an enantiomer Propafenone with anti-arrhythmic and beta-adrenoceptor antagonist activities. In humans (S)-Propafenone administration resulted in a significant reduction of systolic blood pressure and the rate pressure product without any significant effects on heart rate, diastolic blood pressure, PR interval, QRS duration, and QT and QTc values. The difference between the effects of (R)- and (S)-propafenone on systolic blood pressure and rate pressure product was significant. The results from the radioligand binding studies indicate that (S)-propafenone exerts beta-blocking activity in the administered dose. This is further supported by a biochemical assay showing (S)-propafenone to be 54 times more potent than the (R)-enantiomer in displacing (S)-(1251)iodocyanopindolol from 3-receptors of sarcolemma-enriched membranes from the guinea pig heart. (R)- and (S)-propafenone exert different beta-blocking actions but equal effects on the sodium channel-dependent antiarrhythmic class 1 activity. Antiarrhythmic class 1 therapy with reduction of beta-blocking side effects may be attained with optically pure (R)-propafenone hydrochloride instead of the currently used racemic mixture.

Qilu Pharmaceutical has developed selatinib, an orally available dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor 2 receptor (HER-2) for the treatment of cancer. Selatinib participates in phase I of the ongoing clinical trial to evaluate its safety and tolerability, and explore the maximum tolerated dose (MTD) and dose-limiting toxicity in patients with advanced breast cancer.

NSI-189 is a novel oral drug which was developed by Neuralstem for the treatment of cognitive disorders. Now the drug is being tested in phase II of clinical trials in patients suffering from major depressive disorder. The mechanism of NSI-189 action is explained by its ability to stimulate the generation of new neurons in the hippocampus, however the exact target molecule is still unknown.