Delving into the Latest Updates on Icaritin with Synapse

Icaritin is a drug that has been approved by the National Medical Products Administration (NMPA) based on a multicenter, randomized, double-blind, parallel-controlled Phase III clinical trial - SNG1705 ICR-1. It is used for patients with unresectable hepatocellular carcinoma who are not suitable for or refuse standard treatment and have not previously received systemic therapy. According to numerous studies, in tumor cells, Icaritin can downregulate the expression of TNF-α, IL-6, PD-L1 and exert anti-tumor effects. At the same time, it regulates the tumor immune microenvironment by reducing the secretion of TNFa and IL-6 as well as inhibiting PD-L1 expression through decreasing MDSC cell proportion. Importantly, Icaritin has excellent safety profile and greatly ensure patients' quality of life clinically. Rare grade 3-4 TRAEs were observed in clinical trials which is uncommon among existing standard drugs. Good safety is a prerequisite for combination therapy; therefore, further exploration of optimal drug combinations is worth considering. Thus, TACE+Icaritin may potentially optimize treatment strategies for patients with poor liver function reserve.

Start Date01 Mar 2024

Sponsor / Collaborator

Henan Cancer Hospital

NCT06269445 / RecruitingPhase 4IIT

The Efficacy and Safety of Lcaritin Combined With Bevacizumab and FOLFIRI in Treatment of Liver Metastases From Colorectal Cancer: A Prospective, Single-arm Study

To evaluate the efficacy and safety of the combination regimen of Icaritin with bevacizumab + FOLFIRI in patients with liver metastases from advanced colorectal cancer.

Start Date01 Jan 2024

Sponsor / Collaborator

Sir Run Run Shaw Hospital

100 Clinical Results associated with Icaritin

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100 Translational Medicine associated with Icaritin

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100 Patents (Medical) associated with Icaritin

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341

Literatures (Medical) associated with Icaritin

01 Dec 2024·Journal of Controlled Release

Alendronate-functionalized polymeric micelles target icaritin to bone for mitigating osteoporosis in a rat model

Article

Author: Liu, Zhen ; Lin, Yan ; Tima, Singkome ; Chen, Xin ; Fan, Chao ; Zhou, Xiangyu ; Du, Xingjie ; Zhong, Zhirong ; Jiang, Jun ; Zhong, Xingyue ; Luo, Zaiyi ; Zhang, Zhirong ; Sun, Xiaoduan ; Wu, Jili

Formulating drugs into nanoparticles that target sites of disease can lead to strong therapeutic effects with lower doses of drugs and lower rates of off-target adverse effects. Few ways to target drugs to bone have been described, hampering the treatment of osteoporosis. Here we exploit the ability of alendronate to bind tightly to hydroxyapatite in bone as a tactic to target polymeric micelles loaded with the plant flavonoid icaritin to osteoporotic lesions. The traditional Chinese medicine icaritin, from Herba Epimedii, has previously been shown to inhibit adipogenesis and enhance osteogenesis by bone mesenchymal stem cells, but the compound on its own persists only briefly in the bloodstream. Our delivery system led to stronger inhibition of adipogenesis and activation of osteogenesis in a rat model of osteoporosis than when the icaritin-loaded micelles lacked alendronate. These results establish the feasibility of using alendronate to target osteogenic phytomolecules to sites of bone injury, which may guide the development of effective therapies against osteoporosis and, by extension, other bone disorders.

01 Dec 2024·International Immunopharmacology

Synergistic effect and mechanism of monoacylglycerol lipase inhibitor and Icaritin in the treatment of ulcerative colitis

Article

Author: Liu, Yifan ; Zhang, Guimin ; Yao, Jingchun ; Tang, Hongguang ; Cui, Deyu ; Li, Meng ; Lu, Xiaoyan ; Wang, Kun ; Liu, Mingfei ; Li, Shirong ; Shen, Mengmeng

Ulcerative colitis (UC) is a chronic, relapsing nonspecific intestinal inflammatory disease. It is difficult for a single drug to treat UC effectively and maintain long-term efficacy. There is an urgent need to find new drugs and treatment strategies. MAGL11 is a new kind of single acylglycerol lipase (MAGL) inhibitor. Icaritin (Y003) is the major metabolite of icariin in vivo. Several studies have confirmed the role of MAGL inhibitors and icariin in anti-inflammatory and regulation of intestinal stability. Therefore, this study adopted a new strategy of combining MAGL inhibitor with Icaritin to further explore the role and mechanism of drugs in the treatment of UC. Enzyme-linked immunosorbent assay (ELISA), hematoxylin-eosin staining (HE), immunohistochemical (IHC) and Western blot were used to detect the synergistic protective effects of MAGL11 and Y003 on intestinal pathological injury, intestinal mucosal permeability and inflammation in UC mice. 16S rDNA sequencing was used to detect the synergistic effect of MAGL11 and Y003 on gut microbiota. The effects of MAGL11 and Y003 combined therapy on serum and fecal metabolism of UC mice were analyzed by untargeted metabolomics. Proteomics method was applied to investigate the molecular mechanisms underlying MAGL11 and Y003 synergy in the treatment of UC. The results showed that MAGL11 and Y003 could synergistically improve the clinical symptoms, reduce intestinal inflammation and pathological damage, and improve intestinal mucosal permeability in UC mice. The mechanism study found that MAGL11 and Y003 could synergistically inhibit Toll-like receptors 4 (TLR4) / Myeloid differentiation primary response gene (Myd88)/Nuclear factor kappa-B (NF-κB) pathway and further regulate gut microbiota imbalance and metabolic disorders to treat UC.

01 Oct 2024·Food Chemistry: X

Accumulation patterns of flavonoids and phenolic acids in different colored sweet potato flesh revealed based on untargeted metabolomics

Article

Author: Xiao, Qiang ; Wu, Jiaqi ; Wang, Xiuzhi ; Wan, Xiaolin ; Cui, Lingjun

Sweet potatoes are rich in flavonoids and phenolic acids, showing incomparable nutritional and health value. In this investigation, we comprehensively analyzed the secondary metabolite profiles in the flesh of different-colored sweet potato flesh. We determined the metabolomic profiles of white sweet potato flesh (BS), orange sweet potato flesh (CS), and purple sweet potato flesh (ZS) using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The CS vs. BS, ZS vs. BS, and ZS vs. CS comparisons identified a total of 4447 secondary metabolites, including 1540, 1949, and 1931 differentially accumulated metabolites. Among them, there were significant differences in flavonoids and phenolic acids. There were 20 flavonoids and 13 phenolic acids that were common differential metabolites among the three comparison groups. The accumulation of paeoniflorin-like and delphinidin-like compounds may be responsible for the purple coloration of sweet potato flesh. These findings provide new rationale and insights for the development of functional foods for sweet potatoes.List of compoundsKaempferol (PubChem CID: 5280863); Peonidin 3-(6"-p-coumarylglucoside) (PubChem CID: 44256849); Swerchirin (PubChem CID: 5281660); Trilobatin (PubChem CID: 6451798); 3-Geranyl-4-hydroxybenzoate (PubChem CID: 54730540); Eupatorin (PubChem CID: 97214); Icaritin (PubChem CID: 5318980); Isorhamnetin (PubChem CID: 5281654); Glucoliquiritin apioside (PubChem CID: 74819335); Brazilin (PubChem CID: 73384).

100 Deals associated with Icaritin

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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hepatocellular Carcinoma	CN	Beijing Shenogen Pharmaceutical Co., Ltd	10 Jan 2022

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Unresectable Hepatocellular Carcinoma	Phase 3	CN	Beijing Shenogen Pharma Group Ltd.	12 Dec 2022
Liver Cancer	Phase 3	CN	Lee's Pharmaceutical Holdings Ltd.	30 Jan 2022
Advanced Hepatocellular Carcinoma	Phase 3	CN	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	08 Sep 2017
Hepatitis B Virus-Related Hepatocellular Carcinoma	Preclinical	CN	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	08 Sep 2017
Advanced cancer	Preclinical	CN	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	28 Nov 2011
Advanced Malignant Solid Neoplasm	Preclinical	CN	Beijing Shenogen Pharma Group Ltd.	01 Nov 2011
Advanced breast cancer	Preclinical	CN	Beijing Shenogen Pharma Group Ltd.	01 Nov 2010
Metastatic breast cancer	Preclinical	CN	Beijing Shenogen Pharma Group Ltd.	01 Nov 2010

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03236636 (ASCO2021) Manual	Phase 3	Hepatitis B Virus-Related Hepatocellular Carcinoma First line	283	icaritin	(doemugpkue) = zlqveqpxji luhedpxnnv (unrdszmvfv ) View more	Positive	20 May 2021
NCT03236636 (ASCO2021) Manual	Phase 3		283	huachashu	(doemugpkue) = gpawrtpuis luhedpxnnv (unrdszmvfv ) View more	Positive	20 May 2021
NCT02496949 (Pubmed \| BMC Cancer) Manual	Phase 1	Advanced Hepatocellular Carcinoma	20	Icaritin	(lbuvwrymdt) = pmcldnxucz padyifofyn (hrjoqebcmw ) View more	Positive	28 Mar 2019