The 4th International symposium entitled ‘‘Current Trends in Drug Discovery Research’’ (CTDDR-2010) was organized in the sprit of the 1st, 2nd, and 3rd CTDDR (2001, 2004, and 2007) symposia from February 17 to 21st, 2010. The symposium had a focus on the innovative drug discovery approaches for infectious and tropical diseases (malaria, filaria, leishmania, HIV, and tuberculosis), aging, genetic, metabolic and endocrine disorders (neurodegenerative, diabetes, obesity, CNSand CVSrelated disorders), and reproductive disorders (osteoporosis). The deliberations contained the cocktail of computational endeavors, innovative drug discovery approaches and indepth analysis of structure-activity relationships (SAR), new drug targets and state of art techniques for the syntheses of organic molecules of biological interest. A preliminary classification of sub-areas for discussions included cellular and molecular signaling, virtual library design and screening, system biology, drugs from nature/bioimaging and bioprospecting, molecular approaches to disease therapy, validated therapeutic targets, drug design, synthesis, QSAR, CADD, and CAMM, novel approaches to drug discovery, pharmacokinetics/pharmaceutical sciences, translational research, informatics in drug discovery, and preclinical/clinical trials. The symposium was an outstanding success as it covered the above topics in 56 lectures delivered in 16 sessions, 280 posters presented in 4 poster sessions. It provided a platform to about 600 researchers including 45 from other countries including USA, Germany, France, UK, Switzerland, Greece, Hungary, Denmark, Canada, South Africa, Russia, Italy, Belgium, Netherlands, Hong Kong, Japan, Egypt, Turkey, Australia and other countries for lively interactions during the 5-day deliberations. In this special issue, a total 68 manuscripts were submitted for publication. The manuscripts were peerreviewed by at least two experts in the field and 43 manuscripts were successful in navigating the process and were included in this particular issue of Medicinal Chemistry Research. I, as guest editor gratefully acknowledge the reviewers of manuscripts, Mr. A.S. Kushwaha for secretarial assistance, Dr. Stephen J. Cutler, his team and Birkhauser Verlag for providing all out support for successfully bringing out this special issue.