_Small molecule drugs_ are **chemically synthesized** which means made by a series of chemical reactions in the lab. They are typically taken as a **pill or capsule**. The pill or capsule **dissolves in the gastrointestinal tract** and the active ingredient is easily absorbed into the bloodstream via the intestinal wall.  The molecules that make up these drugs are so tiny they are able to penetrate cell membranes and get inside of cells. Small molecules make up **90% of pharmaceutical drugs** (such as insulin, ibuprofen, aspirin, and antihistamines) (2021, DOI: [10.1016/j.medidd.2020.100075](http://dx.doi.org/10.1016/j.medidd.2020.100075 "Read the article here: DOI: 10.1016/j.medidd.2020.100075")). In 2021, **62% of new drug approvals** were for small molecules, including new treatments for HIV, cancer, infections, heart and kidney disease, and neurological disorders. Although market share may shift as [[Biologics]] discovery grows, small molecules—both alone and as part of mixed entities—will undoubtedly remain reliable and cost-effective treatment options for a wide range of common conditions. ![[Pasted image 20240721153256.png]] There is, in fact, target and drug space beyond what has traditionally been possible; however, stagnated approaches to small molecule drug discovery just won’t get us there. Innovation is key. Just as novel methodologies and technologies have propelled biologics from theoretical concepts into the realm of available treatments, so too will they help deliver a second coming of small molecules. There is much potential to be realised in small molecule drug discovery as we see advances in screening technologies, target exploration, and computational methods, including artificial intelligence. https://www.sciencedirect.com/science/article/pii/S1359644622000733 ---