Global Fragment Based Drug Discovery Market Trends

Market Driver - Higher hit rates and enhanced chemical diversity in drug discovery

When developing new drugs, pharmaceutical companies aim to maximize success rates while minimizing risks and costs during development. Fragment based drug discovery provides a potent approach to achieve this by facilitating identification of novel hits with improved chemical qualities. Compared to traditional high throughput screening which relies on whole molecules, fragment-based screening employs small molecule fragments with lower molecular weight between 100-300 Daltons. These fragments have increased potential to bind promiscuously to different regions of target proteins. During screening, any fragments demonstrating binding are then grown step-wise to develop drug-like molecules optimized for interactions with the target.

This incremental process of growing fragments translates to higher hit rates. Fragments make more productive use of chemical space during initial screening since their simple structure allows efficient exploring of potential binding locations on target proteins. Even weak binding fragments can be optimized into strong leads through growing techniques. Pharmaceutical firms have observed success rates up to 10-15% for fragment screens, significantly higher than 1% typically seen with high throughput screening of whole drug-like molecules. Additional chemicalization of screening hits also furthers diversity in generated lead matter. Starting from different fragments binding to diverse sites on a target protein yields structurally unique lead scaffolds over traditional search from one or few starting points.

Expanded chemical libraries from screening further reduce chances of duplicating work of competitors. This enhanced hit rate and diversity addresses a major challenge of drug discovery - identifying new therapeutically relevant molecular structures. It optimizes use of time and resources spent on earlier stages of research by advancing higher quality hits into later development phases. For pharmaceutical companies, fragment-based approaches provide a productive solution to mitigate compound attrition rates downstream and higher probability of clinical success.

Expanding applications in therapeutic areas like oncology

Having established its ability to efficiently explore chemical space and generate quality leads, fragment based drug discovery is increasingly applied across various disease classes. One key therapeutic area witnessing rising adoption is oncology due to growing need for novel cancer treatments. Tumors are genetically complex with multiple dysregulated pathways contributing to uncontrolled growth and metastasis. This has accelerated search for targeted therapies tackling specific cancer vulnerabilities or multipronged treatment regimens. Fragment based methods are well-suited for oncology research aiming to disrupt malignant signaling at its source.

Early binding information from fragment screening provides insight into feasibility of modulating oncology-related protein targets. Even weak binding fragments that may not directly translate to drug candidates can reveal functional pocket points of interest on target proteins like kinases. Efforts are ongoing to develop potent kinase inhibitors for blocking growth and survival signals driving numerous cancer subtypes. Fragment growing may yield selective compounds targeting treatment-resistant cancer mutations or selectively hitting multiple kinases involved in interconnected signaling webs sustaining tumor progression. This maximizes chances of achieving more durable clinical responses.

Besides kinases, applications continue expanding to other underexplored oncology targets such as protein-protein interactions modulating cell cycle, apoptosis, epigenetics. Fragment screening allows methodical interrogating these "undruggable" yet crucial nodes in cancer pathways. It generates starting points for developing substrate-competitive or allosteric inhibitors not readily found through conventional approaches. This widens options for rationally designed combination regimens adding synergistic modes of killing tumor cells. Overall, fragment based methods strategically strengthen oncology pipelines with targeted preclinical candidates worth validating in clinical biomarker-driven trials.

Market Challenge - High costs associated with fragment-based drug discovery

One of the major challenges for the global fragment based drug discovery market is the high costs associated with the process. Fragment based drug discovery involves screening large libraries of low molecular weight fragments to identify initial hits that can be optimised into potential drug candidates. However, developing and screening these fragment libraries is an expensive endeavor. It requires sophisticated biophysical techniques such as x-ray crystallography, nuclear magnetic resonance (NMR) spectroscopy and surface plasmon resonance (SPR) to detect interactions between fragments and target proteins. Additionally, hit validation and hit-to-lead stage where fragments are elaborated also incurs substantial costs. The development of one new drug using fragment based approach is estimated to cost over USD 2 billion, making it inaccessible for many small pharmaceutical and biotechnology companies. Further, maintaining state-of-the-art infrastructure and skilled personnel for fragment screening also contributes to increased operational expenses. While the approach has potential to improve hit rates and optimize drug-like properties in early stages, the high costs pose a significant challenge for widespread adoption of this technique, especially in therapeutics areas with lower commercial potential.

Market Opportunity- Growth Of Biophysical Techniques in Drug Discovery

One of the major opportunities for the global fragment-based drug discovery market is the growth of biophysical techniques. As mentioned earlier, biophysical methods such as X-ray crystallography, NMR spectroscopy and SPR play a crucial role in detection of fragment hits by enabling characterization of molecular interactions. In recent years, there have been significant technological advancements in these techniques, allowing for improved data acquisition rates and sensitivity. For instance, new generations of NMR spectrometers and crystallography equipment have enhanced automated fragment screening capabilities. Additionally, analytical methods like isothermal titration calorimetry (ITC) and thermal shift assays (ThermoFluor) are also being increasingly used as complementary techniques. The growth of these techniques has made fragment screening for a wider range of targets and libraries feasible and more cost-effective. It has also facilitated elaboration of hits by enabling structure-based design. The continued evolution of biophysical tools is expected to further optimize the fragment-based workflow and make it an increasingly attractive drug discovery approach. This growing technical capability presents considerable opportunity for growth of the overall fragment-based drug discovery market.