Structural Approach to Assessing the Innovativeness of New Drugs Finds Accelerating Rate of Innovation

Measuring innovation
in the pharmaceutical industry is challenging.
Counts of new molecular entities (NMEs) approved by the Food and Drug
Administration (FDA) are commonly used, but this measure only gauges
quantity not innovativeness. A new indicator of innovation for small
molecule and peptide drugs based on structural novelty is proposed
and used to analyze recent trends in pharmaceutical innovation. We
show pharmaceutical innovation has significantly increased over the
last several decades despite recent concerns over an innovation crisis
and find Pioneers (a NME whose shape and scaffold were not used in
any previously FDA-approved drugs) are significantly more likely to
be the source of promising new therapies. Analysis of the underlying
source of structural innovation indicates that scaffolds first reported
in the CAS REGISTRY five or less years prior to their Investigational
New Drug application (IND) or on scaffolds populated with 50 or less
other compounds at the time of IND tend to be the main source of Pioneers.
Our analysis also shows a widening structural innovation gap between
large pharmaceutical companies (Big Pharma) and the rest of the ecosystem
even though the number of Big Pharma originated Pioneers has increased.