1. Academic Validation
  2. Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015-2018)

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

  • Expert Opin Ther Pat. 2019 Feb;29(2):137-149. doi: 10.1080/13543776.2019.1567713.
Xingrui He 1 2 3 Xiabin Chen 1 2 3 Hancheng Zhang 4 Tian Xie 1 2 3 Xiang-Yang Ye 1 2 3
Affiliations

Affiliations

  • 1 a Key Laboratory of Elemene Class Anti-Cancer Chinese Medicine of Zhejiang Province, Hangzhou Normal University , Hangzhou , Zhejiang Province , China.
  • 2 b Engineering Laboratory of Development and Application of Traditional Chinese Medicine from Zhejiang Province, Hangzhou Normal University , Hangzhou , Zhejiang Province , China.
  • 3 c Holistic Integrative Pharmacy Institutes (HIPI), School of Medicine , Hangzhou Normal University , Hangzhou, Zhejiang , China.
  • 4 d Drug Discovery , Hangzhou Innogate Pharma Co., Ltd , Hangzhou , Zhejiang Province , China.
Abstract

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 INFα, 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.

Keywords

IFNα; IL-12; IL-23; JAK-STAT; Small molecules; selective Tyk2 inhibitors.

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