Abstract
Improvements have been made to the safety and efficacy of bumped kinase inhibitors, and they are advancing toward human and animal use for treatment of cryptosporidiosis. As the understanding of bumped kinase inhibitor pharmacodynamics for cryptosporidiosis therapy has increased, it has become clear that better compounds for efficacy do not necessarily require substantial systemic exposure. We now have a bumped kinase inhibitor with reduced systemic exposure, acceptable safety parameters, and efficacy in both the mouse and newborn calf models of cryptosporidiosis. Potential cardiotoxicity is the limiting safety parameter to monitor for this bumped kinase inhibitor. This compound is a promising pre-clinical lead for cryptosporidiosis therapy in animals and humans.
Original language | English (US) |
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Pages (from-to) | 753-763 |
Number of pages | 11 |
Journal | International Journal for Parasitology |
Volume | 47 |
Issue number | 12 |
DOIs | |
State | Published - Oct 2017 |
Keywords
- BKI 1369
- Calcium-dependent protein kinase 1
- Cryptosporidiosis
- Drug target
- Gatekeeper residue
ASJC Scopus subject areas
- Parasitology
- Infectious Diseases