Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis.

DOI
Publisher DOI
PubMed ID
28899690
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.
Date Issued
2017-10
Publication Type
Article
Subject(s)
Subjects
BKI 1369 Calcium-dependent protein kinase 1 Cryptosporidiosis Drug target Gatekeeper residue
Language(s)
en
Author(s)
Hulverson, Matthew A
Choi, Ryan
Arnold, Samuel L M
Schaefer, Deborah A
McCloskey, Molly C
Betzer, Dana P
Vidadala, Rama S R
Whitman, Grant R
Rivas, Kasey L
Barrett, Lynn K
Hackman, Robert C
Love, Melissa S
McNamara, Case W
Shaughnessy, Thomas K
Kondratiuk, Alison
Kurnick, Matthew
Banfor, Patricia N
Lynch, James J
Freiberg, Gail M
Kempf, Dale J
Maly, Dustin J
Riggs, Michael W
Ojo, Kayode K
Van Voorhis, Wesley C
Additional Credits
Journal
International journal for parasitology
Publisher
Elsevier
ISSN
0020-7519
Access(Rights)
restricted
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