Itk inhibitors: a patent review.
Importance of field: IL-2 inducible T-cell kinase (Itk) is a non-receptor tyrosine kinase of the Tec family. It plays an important role in T cell signaling and the production of various pro-inflammatory cytokines such as IL-2, IL-4, IL-5, IL-10 and IL-13. Inhibition of Itk has been a target for the treatment of diseases related to inflammation disorders such as psoriasis and allergic asthma. Rich resources on the structural information for Itk made discovery of novel selective Itk inhibitors blossom in the past decade.


METHODS
In this report, distinct structural classes of specific Itk inhibitors are summarized and their in vitro/in vivo properties are discussed.


RESULTS
A summary of 21 patents including 16 different chemical structure classes of Itk inhibitors. The in vivo efficacies of some of the inhibitors in animal models are also discussed.


CONCLUSIONS
Although some of the inhibitors show efficacy in different animal models, which implies potential for therapeutic use in human, there is not yet a chemical entity reported in clinical trials. The prospects for Itk inhibitors will rely on the quality of the compound and the validity of the target in patients within the selected therapeutic area.
Lo
Ho Yin
HY
Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877, USA. ho-yin.lo@boehringer-ingelheim.com
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004195:Disease Models, Animal; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000201:enzymology; D007378:Interleukins / Q000378:metabolism; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D015398:Signal Transduction / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D007378:Interleukins; D047428:Protein Kinase Inhibitors; D011505:Protein-Tyrosine Kinases; C080813:emt protein-tyrosine kinase