The advent of modern drug discovery techniques such as quantitative structure-activity relationships, combinatorial and high-throughput chemistry has contributed to this quest. The Lipinski Rule of 5 and variants thereof, acknowledge that potential drug molecules tend to be more lipophilic with logP values up to 5 and sometimes higher. Water solubility-enhancing formulation strategies have therefore become […]
Ion channels have been excellent drug discovery targets for decades with clinically meaningful drugs identified targeting sodium channels, including (e.g. lamotrigine), calcium channels (e.g. amlopdipine), GABA receptors (e.g. diazepam) and ATP-gated potassium channels (e.g. glipizide) and several others. However, new ion channel modulators have not been emerging at a rapid pace in the recent years, […]
As a medication becomes widely used, new insights emerge on modes of action, side effects and patient response. At the same time, advances in molecular biology, receptor pharmacology and better understanding of the clinical condition may create possibilities for new indications or for better treatment of the existing indication by altering dosage regimen or by […]