cordycepin (OVI-123) / OncoVista - LARVOL DELTA

Pleiotropic Bioactivity of Caterpillar Fungus, Orange Cordyceps, and Cordycepin: Insight from Integrated Network Pharmacology and Food and Drug Regulatory Framework. (PubMed, Pharmaceuticals (Basel)) - "The systems-level network analysis and reductionistic molecular ligand preceptor pharmacology provide complementary approaches for understanding the multi-target bioactivity of these fungi. This review clarifies conceptual and regulatory barriers to recognizing resilience-supporting interventions and informs future regulatory innovation."

Journal • Review • Pulmonary Disease • Respiratory Diseases • AMPK

Cordycepin inhibits Intrahepatic cholangiocarcinoma progression by targeting NAT10-mediated ac4C RNA modification of VCAN (AACR 2026) - "This study demonstrates that cordycepin directly targets NAT10, attenuating its expression and global ac4C modification, thereby suppressing the downstream oncogenic effector VCAN and restraining ICC progression. These findings underscore the central role of the NAT10-ac4C axis in cordycepin's antitumor activity and identify this pathway as a promising therapeutic target in ICC."

Biliary Cancer • Cholangiocarcinoma • Oncology • Solid Tumor • NAT10

Mechanistic insights into cordycepin-enhanced CTLA-4 blockade efficacy via Eubacterium rectale-mediated immunomodulation in colon cancer (IMMUNOLOGY 2026) - "Non-targeted metabolomics analysis using LC-MS identified specific activation of the histidine metabolism pathway, with elevated levels of the key metabolite Cetirizine N-Oxide potentially contributing to enhanced immune activity. These results demonstrate a promising "microbiome-immune" dual-targeting strategy for colon cancer with clinical translational potential."

Clinical • Immunomodulating • Late-breaking abstract • Colon Cancer • Colorectal Cancer • Immunology • Oncology • Solid Tumor • BCL6 • CD8 • PTPRC

Nature's marvel: unravelling the multiphase composition of Cordyceps militaris mushroom and its implications as a dietary supplement. (PubMed, J Food Sci Technol) - "The multiphase composition of C. militaris encompasses bioactive compounds such as polysaccharides, cordycepin, adenosine, nucleosides, proteins, amino acids, sterols, and trace elements...Overall, C. militaris mushroom holds significant promise as a multiphase dietary supplement, but careful evaluation and consultation with healthcare professionals are advised for optimal use. The online version contains supplementary material available at 10.1007/s13197-025-06531-5."

Journal • Review

Mushrooms as potent autophagy modulators in cancer therapy: Current evidence and therapeutic prospects. (PubMed, Cancer Pathog Ther) - "The review lists over 18 mushroom species (e.g., Ganoderma lucidum, Cordyceps, Phellinus) and 28 bioactive compounds (such as Ganoderic acid DM, Cordycepin, Hispidin) that affect autophagy, demonstrating efficacy against 15 cancer types, including colorectal, lung, breast, and liver cancers...The context-dependent effects of autophagy, along with the limited clinical evidence, present considerable challenges. Future clinical trials must focus on developing standardized extracts and personalized approaches to effectively translate this potential into clinical practice."

Journal • Review • Breast Cancer • Colorectal Cancer • Immune Modulation • Immunology • Liver Cancer • Lung Cancer • Metabolic Disorders • Oncology • Solid Tumor • BECN1 • mTOR

Fe-Doped Carbon Dots Functionalized Nanoelectrode for In Situ Monitoring of Metabolism-Associated ROS Changes in Single Microglia. (PubMed, Anal Chem) - "Further investigations reveal that cordycepin may target hexokinase II, a key regulatory enzyme in glucose metabolism, thereby inducing metabolic reprogramming in microglia and mitigating the LPS + Aβ-induced elevation in intracellular ROS. This work provides an efficient strategy for in situ monitoring of ROS changes during metabolic reprogramming at the single-cell level, which is vital for advancing disease diagnosis and therapeutic development."

Journal • Alzheimer's Disease • CNS Disorders

Current Evidence of Ergogenic and Post-Exercise Recovery Effects of Dietary Supplementation with Cordyceps militaris in Humans-A Narrative Review. (PubMed, Nutrients) - "The certainty of the evidence is limited by small sample sizes, heterogeneity of participants and exercise protocols, insufficient reporting of randomization, lack of trial registration in most studies, absence of standardized preparations with quantified bioactive constituents, and the use of multi-ingredient supplements. Well-designed randomized controlled trials using chemically characterized preparations and homogeneous athletic populations are required to clarify the efficacy and practical relevance of C. militaris in sports nutrition."

Journal • Review • Inflammation

Antithrombotic Effects of Cordycepin-Enriched WIB-801CE via Inhibition of Thromboxane A2-Induced αIIbβ3 Activation and Thrombin-Mediated Fibrin Clot Retraction. (PubMed, Int J Mol Sci) - "WIB-801CE disrupts TXA2-driven platelet activation and thrombus stabilization by selectively modulating phosphorylation of key signaling proteins at defined regulatory sites. These properties highlight its promise as a therapeutic candidate for thrombotic disorders with platelet hyperreactivity."

Journal • Thrombosis • MAPK8

Exploring the behavioural and biochemical effects of cordycepin in PTSD-like behaviour using an early life stress mouse model. (PubMed, Biochem Biophys Res Commun) - "Mice exhibiting PTSD-like behaviour were treated with fluoxetine (FLU, 10 mg/kg), an antidepressant drug, and COR (10 and 50 mg/kg). COR demonstrated a dose-dependent response with 50 mg/kg showing consistent improvement in both behavioural and biochemical parameters. Overall, COR exhibited promising activity in this model and may serve as a potential natural therapeutic strategy to investigate for the management of PTSD in clinics."

Journal • Preclinical • CNS Disorders • Inflammation • Mood Disorders • Oncology • Post-traumatic Stress Disorder • Psychiatry • IL1B • IL6 • NLRP3 • TNFA

Lactylation: a metabolic-epigenetic bridge in diabetic kidney disease and a therapeutic target for TCM. (PubMed, Chin Med) - "Specific agents such as Berberine, baicalin, ginsenoside compound K, and cordycepin have been demonstrated to mitigate renal injury by directly or indirectly reducing lactate production and modulating lactylation levels, thereby suppressing downstream inflammatory and fibrotic responses. This review systematically elucidates the pivotal role of the lactate-lactylation axis in the pathogenesis of DKD, highlighting traditional Chinese medicine's unique potential for precisely regulating this metabolic-epigenetic nexus. It offers innovative insights and strategies for the integrated management of DKD."

Journal • Review • Diabetic Nephropathy • Fibrosis • Immunology • Inflammation • Metabolic Disorders • Nephrology • Renal Disease

Ophiocordyceps indica from the Indian Himalayas Ameliorates the IgA Nephropathy in Mice. (PubMed, Appl Biochem Biotechnol) - "UPLC-based metabolomic profiling of O. indica confirmed the presence of key nucleosides, including adenosine and cordycepin, exhibiting a profile comparable to O. sinensis. The nephroprotective and anti-inflammatory effects of O. indica were comparable to those of O. sinensis and dexamethasone. Our findings highlight the potent anti-inflammatory and nephroprotective properties of O. indica, supporting its potential as a novel therapeutic agent for managing IgAN."

Journal • Preclinical • Chronic Kidney Disease • Fibrosis • Glomerulonephritis • IgA Nephropathy • Immunology • Lupus Nephritis • Nephrology • Renal Disease • IL18 • IL6 • TGFB1 • TNFA • WT1

Anti-Inflammatory Mechanisms and Translational Relevance of Cordyceps sinensis and Its Bioactive Constituents. (PubMed, J Inflamm Res) - "Its principal bioactive components, including cordycepin, cordycepic acid, polysaccharides, and sterols, exert significant protective effects in a wide range of inflammation-related diseases, primarily covering respiratory diseases, autoimmune disorders, neuroinflammatory conditions, and metabolic and gastrointestinal syndromes...This review summarizes recent progress in the identification of anti-inflammatory components of Cordyceps sinensis and their mechanisms of action, highlights current challenges in clinical translation, and outlines future research directions. Collectively, these findings emphasize the broad potential of Cordyceps sinensis as a multi-target natural product-based anti-inflammatory therapy."

Journal • Review • Immunology • Inflammation • Respiratory Diseases • MYD88 • TLR4

Molecular Mechanisms of Temperature-Regulated Cordycepin Biosynthesis in Cordyceps militaris. (PubMed, J Fungi (Basel)) - "Multi-omics analysis indicated that high temperature promotes cordycepin accumulation through the synergistic regulation of multiple pathways: upregulating genes in the pentose phosphate pathway, purine metabolism, and cordycepin biosynthetic gene cluster (Cns1-Cns3), increasing protective agent pentostatin content, downregulating cordycepin-degrading genes, and enhancing cordycepin transmembrane transport. This study clarifies the molecular mechanism of temperature-mediated cordycepin accumulation, providing a theoretical basis for improving cordycepin production via temperature regulation, optimizing Cordyceps militaris strain quality, and facilitating efficient industrial production."

Journal

Mechanistic insights into cordycepin-enhanced CTLA-4 blockade efficacy via Eubacterium rectale-mediated immunomodulation in colon cancer. (PubMed, Int Immunopharmacol) - "Non-targeted metabolomics analysis using LC-MS identified specific activation of the histidine metabolism pathway, with elevated levels of the key metabolite Cetirizine N-Oxide potentially contributing to enhanced immune activity. Mechanistic studies further revealed that the triple therapy suppresses the activity of the Bcl6 regulatory network, thereby reducing the immunosuppressive function of Tregs and destroying the immunosuppressive interplay between myeloid immune cells and Tregs. These results demonstrate a promising "microbiome-immune" dual-targeting strategy for colon cancer with clinical translational potential."

Journal • Colon Cancer • Colorectal Cancer • Immunology • Oncology • Solid Tumor • BCL6 • CD4

Cordycepin inhibits human extravillous trophoblast invasion by suppressing snail-mediated MMP2 expression. (PubMed, Tissue Cell) - "Functionally, COR treatment inhibited EVT cell invasion, and this effect was mediated by MMP2 downregulation. These findings provide new insights into the molecular mechanisms by which COR regulates EVT cell invasiveness and highlight the potential implications of COR as a health supplement during pregnancy."

Journal • Oncology • MMP2

Clinical Study on the Application of Cordycepin in Combination with Anti-PD-1 for the Treatment of Non-Small Cell Lung Cancer (ChiCTR) - P=N/A | N=9 | Completed | Sponsor: Changzhou No.2 People’s Hospital; Changzhou No.2 People’s Hospital

New trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Predictive Modeling of Cordycepin Content in Cordyceps militaris Using Machine Learning Based on Cultivation Conditions. (PubMed, J Basic Microbiol) - "The developed GUI enables end-users to input cultivation conditions and receive immediate predictions, facilitating data-driven decision-making. This approach offers a scalable and interpretable framework for optimizing bioactive compound production in edible fungi, with potential application in smart bioprocessing and precision fermentation."

Journal

Effect of Cordyceps militaris Extract on Visceral Adipose Tissue Changes After Ovariectomy in Rodents. (PubMed, Int J Endocrinol) - "Moreover, CM increased uterine weight and serum superoxide dismutase in 17β-estradiol-treated OVX rats. These findings suggested that CM, particularly its component cordycepin, holds promise as a natural agent for mitigating weight gain, particularly in the context of postmenopausal obesity."

Journal • Preclinical • Cardiovascular • Genetic Disorders • Obesity • CDKN1A • CEBPA • CEBPB • CYP17A1 • FABP4 • LMNB1 • PPARG

Design, Synthesis, and Anti-Hepatic Fibrosis Evaluation of Cordycepin Derivatives. (PubMed, Molecules) - "The Western blotting result also indicated that 3a could activate the AMPK signaling pathway. Overall, these results suggest 3a may serve as a lead compound for further investigation."

Journal • Fibrosis • Hepatology • Immunology

Protective Effect of Cordyceps militaris Extract Against Cigarette Smoke Extract Induced Neurodegeneration in Zebrafish Model. (PubMed, Neurotox Res) - "CMWE mitigated cigarette smoke-induced behavioral and histological hallmarks of neurodegeneration in zebrafish, likely via synergistic antioxidant and anti-inflammatory mechanisms. These findings support the potential of C. militaris as a natural product-based therapeutic candidate for neurodegenerative disorders, warranting further studies on its individual constituents and mechanisms of action."

Journal • CNS Disorders • Inflammation

Cordycepin Suppressed Ferroptosis to Ameliorate Acute Kidney Injury Through Inhibiting the DNMT1/KLF15/FTH1 Axis. (PubMed, FASEB J) - "COR suppressed ferroptosis by regulating the DNMT1/KLF15/FTH1 axis, thereby improving AKI in vivo. COR suppressed ferroptosis in AKI by depressing DNMT1/KLF15/FTH1 axis."

Journal • Acute Kidney Injury • Cardiovascular • Nephrology • Renal Disease • Reperfusion Injury • DNMT1 • KLF5

Multi-omics and compositional analysis of bidirectional solid fermentation products from Cordyceps militaris and Panax quinquefolius L. (PubMed, J Ginseng Res) - "This study demonstrates that co-culture of American ginseng with C. militaris enables bidirectional biotransformation: fungal enzymes convert ginsenosides into rare ginsenosides, while ginseng nutrients upregulate cordycepin biosynthesis. It offers a novel, eco-friendly approach for targeted transformation and enrichment of active ingredients."

Journal • RB1

RoCi-a single-step multi-copy integration system based on rolling-circle replication. (PubMed, Nucleic Acids Res) - "Using RoCi for cell factory construction resulted in a ∼10-fold increase in production of the specialized metabolite cordycepin and the enzyme β-glucuronidase compared to single-copy strains. Finally, we show that RoCi can also be applied in other fungi like the industrial workhorses A. niger and A. oryzae."

Journal

Cordycepin in cancer therapy: A bibliometric analysis and review of mechanisms. (PubMed, J Food Drug Anal) - "Future research should prioritize pharmacokinetic characterization, investigation of combinatorial therapeutic strategies, and pathways toward clinical translation. Intracellular exposure appears to be shaped by two complementary axes: interference with 3'end polyadenylation and ENT1/ENT2-mediated uptake with ADA-catalyzed deamination."

Journal • Review • Oncology • CDKN1A • SLC29A1

Combination treatment of cordycepin and radiation induces apoptosis accompanied by protective autophagy in TM3 mouse Leydig progenitor cells. (PubMed, J Food Drug Anal) - "Although apoptosis is eventually induced in TM3 cells, protective autophagy is also activated to mitigate the cytotoxic impact of the combination treatment. This finding may provide a reference for the development of safe therapeutic regimen for Leydig cell tumors."

Journal • Preclinical • Oncology • ATG12 • ATG5 • BECN1