4.5 Review

Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015-2018)

Journal

EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 29, Issue 2, Pages 137-149

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/13543776.2019.1567713

Keywords

Small molecules; selective Tyk2 inhibitors; IFN alpha; IL-12; IL-23; JAK-STAT

Funding

  1. National Science Foundation of China [81803417, 81730108]
  2. Key Project of Zhejiang Province Ministry of Science and Technology [2015C03055]
  3. Key Project of Hangzhou Ministry of Science and Technology [20162013A07, 20142013A63]

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Introduction: Tyrosine kinase 2 (Tyk2) is a non-receptor tyrosine-protein kinase, an enzyme that in humans is encoded by the TYK2 gene. Tyk2, together with three other family subtypes, namely, Jak1, Jak2, and Jak3, belong to the JAK family. Before 2014, far more publications and patents appeared in public domain attributing to the development of selective Jak2 and Jak3 inhibitors than those for selective Tyk2 and Jak1 inhibitors. Areas covered: This review sought to give an overview of patents related to small molecule selective Tyk2 inhibitors published from 2015 to 2018. The article also covers clinical activities of small molecule selective Tyk2 inhibitors in recent years. Expert opinion: As a key component of the JAK-STAT signaling pathway, Tyk2 regulates INF alpha, IL12, and IL23. Selective inhibition of Tyk2 can provide pharmacological benefits in the treatment of many diseases such as psoriasis, systemic lupus erythematosus (SLE), inflammatory bowel disease (IBD), rheumatoid arthritis (RA), cancer, and diabetes. The selectivity against other Jak family subtypes (such as Jak2) is crucial in order to minimize the potential side effects and to maximize the desired pharmacological effects. In this context, this review of recent selective Tyk2 inhibitor patents may prove valid, interesting, and promising within the therapeutic paradigm.

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