Early Biotherapeutic Lead Optimization for More Efficient Drug Discovery and Development
Abstract:
Lead optimization for discovery of small molecule drug candidates is well established, but less so for biological drug candidates. While biologics are much easier to modify than non-natural small molecules via introduction of changes in their amino acid sequence through genetic engineering technologies, this approach is frequently met with trepidation. Generally, the risk-benefit balance of small improvements resulting from a few mutations tilts towards potential safety concerns. However, large improvements in biologics function can drive significant benefits in efficacy and safety and are thus highly relevant to patients and should be extremely attractive to the pharmaceutical industry. Up until now, such improvements have been difficult to generate.