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,we investigated the efficacy and safety of Icaritin administered in conjunction with AG in patients newly diagnosed with advanced pancreatic ductal adenocarcinoma, compare with AG only.

Start Date01 Mar 2025

Sponsor / Collaborator

Sir Run Run Shaw Hospital

ChiCTR2400094250

/ SuspendedPhase 4IIT

Study on the Efficacy and Safety of Icaritin in the Treatment of Unresectable Hepatocellular Carcinoma (HCC) with Child-Pugh B and C Liver Function

Start Date23 Dec 2024

Sponsor / Collaborator

West China Hospital

NCT06644937

/ Not yet recruitingPhase 2/3IIT

Single-arm Clinical Trial of TACE in Combination With Acoradine as Adjuvant Therapy After Surgery in Patients With Hepatocellular Carcinoma at High Risk of Recurrence

To assess 1-year recurrence-free survival (RFS) in patients with hepatocellular carcinoma (HCC) who are at high risk of Inguinal orchiectomy recurrence usingTACE combined with Acoradine

Start Date09 Oct 2024

Sponsor / Collaborator

Zhujiang Hospital of Southern Medical University

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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339

Literatures (Medical) associated with Icaritin

01 Apr 2025·Biomaterials

Pulmonary delivery of dual-targeted nanoparticles improves tumor accumulation and cancer cell targeting by restricting macrophage interception in orthotopic lung tumors

Article

Author: Wei, Jiaxing ; Li, Yunfei ; Ma, Si-Qi ; Wang, Chen-Ao ; Wang, Chenao ; Sun, Tingting ; Liao, Yonghong ; Li, Yun-Fei ; Ma, Siqi ; Ge, Di ; Chen, Xiaoyuan ; Liao, Yong-Hong ; Sun, Ting-Ting ; Wei, Jia-Xing

Despite the recognized potential of inhaled nanomedicines to enhance and sustain local drug concentrations for lung cancer treatment, the influence of macrophage uptake on targeted nanoparticle delivery to and within tumors remains unclear. Here, we developed three ligand-coated nanoparticles for pulmonary delivery in lung cancer therapy: phenylboronic acid-modified nanoparticles (PBA-NPs), PBA combined with folic acid (FA-PBA-NPs), and PBA with mannose (MAN-PBA-NPs). In vitro, MAN-PBA-NPs were preferentially internalized by macrophages, whereas FA-PBA-NPs exhibited superior uptake by cancer cells compared to macrophages. Following intratracheal instillation into mice with orthotopic Lewis lung carcinoma tumors, all three nanoparticles showed similar lung retention. However, MAN-PBA-NPs were more prone to interception by lung macrophages, which limited their accumulation in tumor tissues. In contrast, both PBA-NPs and FA-PBA-NPs achieved comparable high tumor accumulation (∼11.3% of the dose). Furthermore, FA-PBA-NPs were internalized by ∼30% of cancer cells, significantly more than the 10-18% seen with PBA-NPs or MAN-PBA-NPs. Additionally, FA-PBA-NPs loaded with icaritin effectively inhibited the Wnt/β-catenin pathway, resulting in superior anti-tumor efficacy through targeted cancer cell delivery. Overall, FA-PBA-NPs demonstrated advantageous competitive uptake kinetics by cancer cells compared to macrophages, enhancing tumor targeting and therapeutic outcomes.

01 Mar 2025·Brain Research Bulletin

Discovery and validation of CREB1 as a transcription target of icaritin: Implications for the treatment of depressive-like behavior

Article

Author: Ling, Yuyan ; Ma, Ruiting ; Xu, Huiying ; Gu, Ling ; Li, Lei ; Chen, Meijuan

Depression is a prevalent neuropsychiatric disorder characterized by persistent sadness and a lack of interest, significantly impacting the quality of life. Icaritin, a bioactive compound from Herba Epimedii, which has the antidepressant-like effects. However, the potential target of icaritin in the brain, especially concerning transcription factors, is not well understood. In this study, we demonstrated that icaritin significantly ameliorated depressive-like behaviors in a chronic corticosterone (CORT)-induced mouse model. This study aimed to investigate the role of icaritin in modulating the activity of cAMP-response element binding protein 1 (CREB1), a crucial transcription factor implicated in neuronal function and mood regulation. Through a combination of virtual screening and molecular docking, we identified CREB1 as a target by intersections of databases, leading to the selection of 43 candidate compounds, among which icaritin exhibited a favorable docking score and previously reported antidepressant effects. Biolayer interferometry (BLI) analysis confirmed the direct binding of icaritin to CREB1, with a dissociation constant (K_D) of 7.02E-06 M. Further mutational analysis revealed that residues Q65 and Q229 of CREB1 were essential for the binding of icaritin. Additionally, Quantitative Real-Time PCR (qRT-PCR) demonstrated that icaritin treatment upregulated the mRNA levels of CREB1 target genes in the hippocampus and cortex. Bioinformatics analysis indicated that CREB1 interacts with several neuroprotective pathways, reinforcing its potential significance in depression. In conclusion, our findings suggest that icaritin may represent a promising therapeutic candidate for depression by enhancing CREB1-mediated neuroprotection, warranting further investigation into its clinical applications and underlying mechanisms.

10 Feb 2025·Current Pharmaceutical Design

Therapeutic Effects and Mechanisms of Icaritin in Parkinson's Disease

Article

Author: Zheng, Chongbo ; Cai, Jiating ; Huang, Zhihua ; Tian, Keqiang ; Wu, Lizhen ; Luo, Liang

Parkinson's Disease (PD) is a neurodegenerative disorder of the central nervous system (CNS). Given the increasing age of the general population, PD has emerged as a significant public health and societal concern, impacting both individual well-being and socioeconomic progress. The present interventions have proven insufficient in impeding the progressive nature of PD. Consequently, it is imperative to promptly identify efficacious strategies for the prevention and treatment of PD. Icaritin (ICT) is a flavonoid extracted from Epimedium Brevicornu Maxim that is a phytoestrogen with antitumour, anti-inflammatory, antioxidant, antiaging, and neuroprotective properties. This paper reviews the protective effect of ICT on dopaminergic neurons through anti-oxidative stress, improving mitochondrial function, inhibiting neuroinflammatory responses, reducing Lewy body formation, and decreasing apoptosis. The primary objective of this article is to provide valuable insights and serve as a reference for the potential use of ICT in the prevention and treatment of PD.

100 Deals associated with Icaritin

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KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

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Indication	Country/Location	Organization	Date
Hepatocellular Carcinoma	China	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	China	Beijing Shenogen Pharma Group Ltd.	12 Dec 2022
Liver Cancer	Phase 3	China	Lee's Pharmaceutical Holdings Ltd.	30 Jan 2022
Advanced Hepatocellular Carcinoma	Phase 3	China	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	08 Sep 2017
Hepatitis B Virus-Related Hepatocellular Carcinoma	Phase 2	China	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	08 Sep 2017
Advanced cancer	Phase 2	China	Beijing Shen Aoji Medicine Science & Technology Co., Ltd.	28 Nov 2011
Advanced Malignant Solid Neoplasm	Phase 2	China	Beijing Shenogen Pharma Group Ltd.	01 Nov 2011
Advanced breast cancer	Phase 2	China	Beijing Shenogen Pharma Group Ltd.	01 Nov 2010
Metastatic breast cancer	Phase 2	China	Beijing Shenogen Pharma Group Ltd.	01 Nov 2010
Microsatellite instability-high colorectal cancer	IND Approval	China	Beijing Shenogen Pharma Group Ltd.	04 Mar 2025

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03236636 (ASCO 12021 \| ASCO 22021) Manual	Phase 3	Hepatitis B Virus-Related Hepatocellular Carcinoma First line	283	icaritin	(gvptbtnnxd) = fazouknkpg kkhkngjpor (jdbftuwauq ) View more	Positive	20 May 2021
NCT03236636 (ASCO 12021 \| ASCO 22021) Manual	Phase 3		283	huachashu	(gvptbtnnxd) = rcrshyexme kkhkngjpor (jdbftuwauq ) View more	Positive	20 May 2021
NCT02496949 (Pubmed \| BMC Cancer) Manual	Phase 1	Advanced Hepatocellular Carcinoma	20	Icaritin	(ixycrgnxub) = bcicnvvmsu tvpcxseeid (wtmlddkdbb ) View more	Positive	28 Mar 2019
WCO_IOF_ESCEO2015	Not Applicable	-	-	Icaritin	lykaazksgb(imwoqepapo) = elqnjgfeen qzhpomcegc (rlzuxfszxh ) View more	Positive	17 Apr 2015