Methods for Evaluating the in vitro-in vivo Activity Relationship of Antibacterial Compounds

Drug discovery cycle illustration

Available for Licensing

IP Status

US Patent: US 10287617


​Susan E Knudson
Richard A Slayden

Reference No: 14-026
Licensing Manager

Steve Foster

At a Glance

Researchers at Colorado State University have developed patented methods for evaluating the in vitro-in vivo activity relationship of antibacterial compounds to better prioritize and advance drugs through the drug discovery pipeline for treatment of M. tuberculosis.


The drug discovery strategy developed here is incorporated into all of the team’s drug discovery programs, NIH funded drug assessment contracts, and industrial drug discovery partnerships, amounting to at least 5 different programs and thousands of tests. The approach describes prioritized progression of compounds into efficacy studies using animal models of infection.



It is estimated that a third of the world’s population is infected with Mycobacteria tuberculosis, the causative agent of tuberculosis (TB), and between 5-10% of those infected individuals will develop the active disease over their lifetime. As a result, TB is the second leading cause of death from an infectious disease and the leading cause of death from a bacterial infection worldwide. In addition to the global burden, the increasing rates of multi-drug resistant strains (MDR) that require extensive treatment regimens with second line drugs impacts disease management. Therefore, there is a need to develop new therapeutics with unique modes of action that can be used to treat TB or that can be co-administered with existing antitubercular drugs.

Cell division is an attractive under-exploited target for the development of new chemotherapeutics against pathogenic bacteria, which are often medically important, difficult to treat, and drug resistant. Developing small molecule inhibitors with specificity for these targets through rational drug design has demonstrated potency with low or negligible cytotoxicity. However, the determination of in vivo efficacy cannot be determined by analysis of minimal inhibitory concentrations (MIC) alone, and adequate in vitro methods for determining in vivo efficacy are urgently needed.

  • Modern drug discovery protocols do not adequately find new compositions because they rely primarily on the MIC – these methods are far more advanced
  • Discovery of new lead compounds from chemical libraries can be determined to have high efficacy in vivo, even though they may demonstrate poor MIC