NLRP3 inhibitors(NACHT, LRR and PYD domains-containing protein 3 inhibitors), SPTLC1 inhibitors(serine palmitoyltransferase long chain base subunit 1 inhibitors)

Therapeutic Areas

Digestive System Disorders

Active Indication-

Inactive Indication

Nonalcoholic Steatohepatitis

Originator Organization

Asan Medical Center

Active Organization-

Inactive Organization

Asan Medical Center

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

100 Clinical Results associated with KDDF-201406-03

100 Translational Medicine associated with KDDF-201406-03

100 Patents (Medical) associated with KDDF-201406-03

Literatures (Medical) associated with KDDF-201406-03

10 Jan 2018·Recent Patents on Anti-Cancer Drug DiscoveryQ4 · MEDICINE

NLRP3 Inflammasome Activation Inhibitors in Inflammation-Associated Cancer Immunotherapy: An Update on the Recent Patents

Q4 · MEDICINE

Review

Author: Koppula, Sushruta ; Lee, Kwang-Ho ; Kopalli, Spandana R. ; Kang, Tae-Bong

BACKGROUNDInflammasomes are recognized as key regulators in innate immunity from the pathogenic to endogenous danger signals. Although controlled activation of inflammasome is highly beneficial, dysregulation of inflammasome activation plays central role in various autoimmune, inflammatory disorders and aid in promoting various forms of cancers in humans such as breast cancer, fibrosarcoma, gastric carcinoma, and lung metastasis. NLRP3 inflammasome activation has been emerged as a topic of interest and is under profound investigation for its involvement in multiple forms of cancers.OBJECTIVEThis review emphasizes an overview of the recent patents on NLRP3 inflammasome activation inhibitors with their relevant biological/pharmacological properties for the prevention and treatment of inflammation-associated cancer disorders.METHODSData were obtained from online patent searchers such as World Intellectual Property Organization (WIPO®), Free Patent Online (FPO), Espacenet® and Google Patents.RESULTSSeveral NLRP3 inflammasome activation inhibitors were recently patented from naturally derived and synthetic agents mainly by academic researchers. Most of the claimed patents have been validated and confined to cell lines and animal models limiting their entry into clinical settings.CONCLUSIONThe vigorous effort to discover and develop agents to specifically inhibit NLRP3 inflammasome activation, may pave the way to therapeutic intervention targeting inflammasome-regulated pathways that are involved in the pathogenesis of various forms of cancer.

16 Dec 2016·Organic LettersQ1 · CHEMISTRY

Spirodalesol, an NLRP3 Inflammasome Activation Inhibitor

Q1 · CHEMISTRY

Article

Author: Jiang, Nan ; Liu, Wen ; Zhang, Ai Hua ; Tan, Ren Xiang ; Xu, Qiang

Autoimmune and inflammatory diseases are associated with inappropriate activation of the NOD-like receptor protein 3 (NLRP3) inflammasome, but suitable inhibitors against such improper activations remain scarce. Here, spirodalesol (1) from Daldinia eschscholzii was structurally characterized and is biosynthetically proposed as an NLRP3 inflammasome activation inhibitor with an unprecedented carbon skeleton.

Frontiers in Cell and Developmental BiologyQ3 · BIOLOGY

TI: NLRP3 Inflammasome-Dependent Pyroptosis in CNS Trauma: A Potential Therapeutic Target

Q3 · BIOLOGY

ReviewOA

Author: Fan, Yunpeng ; Wu, Junsong ; Zheng, Jinfeng ; Zhou, Conghui

Central nervous system (CNS) trauma, including traumatic brain injury (TBI) and traumatic spinal cord injury (SCI), is characterized by high morbidity, disability, and mortality. TBI and SCI have similar pathophysiological mechanisms and are often accompanied by serious inflammatory responses. Pyroptosis, an inflammation-dependent programmed cell death, is becoming a major problem in CNS post-traumatic injury. Notably, the pyrin domain containing 3 (NLRP3) inflammasome is a key protein in the pyroptosis signaling pathway. Therefore, underlying mechanism of the NLRP3 inflammasome in the development of CNS trauma has attracted much attention. In this review, we briefly summarize the molecular mechanisms of NLRP3 inflammasome in pyroptosis signaling pathway, including its prime and activation. Moreover, the dynamic expression pattern, and roles of the NLRP3 inflammasome in CNS post-traumatic injury are summarized. The therapeutic applications of NLRP3 inflammasome activation inhibitors are also discussed.

100 Deals associated with KDDF-201406-03

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Nonalcoholic Steatohepatitis	Preclinical	KR	Asan Medical Center	-

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