patupilone (EPO 906) / Novartis - LARVOL DELTA

High-throughput chemical screen identifies epothilone B in modulating inflammatory bowel disease by triggering neutrophil apoptosis. (PubMed, Genes Dis) - "Mechanistically, Epo B selectively stimulates neutrophil apoptosis by targeting and enhancing Caspase-3 cleavage, thereby inhibiting neutrophilic inflammation. This study underscores the utility of in vivo high-throughput drug screening in IBD and highlights Epo B as a promising candidate for drug repurposing in IBD treatment, offering a novel therapeutic strategy by targeting neutrophil apoptosis."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • CASP3

Endophytic Aspergillus glaucus as a novel epothilone B producer: Antiproliferative activity and in silico analysis. (PubMed, Appl Microbiol Biotechnol) - "• The purified epothilone has plausible antiproliferative, apoptotic, and antimetastatic activities. • The epothilone had coherent multitarget interactions with key oncogenic kinases and β-tubulin taxane site."

Journal • Oncology • CDC37 • EGFR • HSP90AA1 • JAK2 • PIK3CA

Development and validation of an m6A and autophagy related lncRNAs signature for predicting survival and modulating the immune microenvironment in esophageal squamous cell carcinoma. (PubMed, Front Immunol) - "Pharmacogenomic analysis identified nine compounds (Shikonin, Bicalutamide, Bryostatin-1, Epothilone-B, JNK-9L, LFM-A13, QS11, VX-680, and Z-LLNle-CHO) exhibiting differential sensitivity between the dichotomous risk strata. This study yields findings that hold significant clinical implications for refining prognostic stratification and deciphering the immune landscape in ESCC. Moreover, they offer novel perspectives that may pave the way for more precise prognostic assessment and the formulation of targeted therapeutic interventions."

Biomarker • IO biomarker • Journal • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • LAIR1 • TNFRSF18

Phase I/II Study of Celebrex and EPO906 in Patients With Metastatic Colorectal Cancer (clinicaltrials.gov) - P1/2 | N=75 | Completed | Sponsor: University of Southern California | Unknown status ➔ Completed

Trial completion • Colon Adenocarcinoma • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor

Paclitaxel, Carboplatin, and Bevacizumab or Paclitaxel, Carboplatin, and Temsirolimus or Ixabepilone, Carboplatin, and Bevacizumab in Treating Patients With Stage III, Stage IV, or Recurrent Endometrial Cancer (clinicaltrials.gov) - P2 | N=349 | Active, not recruiting | Sponsor: National Cancer Institute (NCI) | Trial completion date: Mar 2026 ➔ Mar 2027

Trial completion date • Carcinosarcoma • Endometrial Adenocarcinoma • Endometrial Cancer • Endometrial Serous Adenocarcinoma • Oncology • Sarcoma • Solid Tumor • Uterine Cancer • AKT1

Microtubule-stabilizing drugs suppress convulsions in a C. elegans model of CAMSAP disorders. (PubMed, Epilepsy Res) - "We found that animals with genetically disrupted ptrn-1 (the C. elegans homolog of CAMSAP1) exhibited elevated convulsion frequency relative to wild type, and that Epothilone B and Valproic Acid reduced convulsions. We also found that Paclitaxel increased convulsions, and Davunetide produced variable outcomes. These results suggest that pharmacologic microtubule stabilization is a promising strategy for diseases caused by genetic disruption to CAMSAP function."

Journal • CNS Disorders • Epilepsy • Psychiatry

Dimeric Anthraquinone Rugulosin A Induces Apoptosis in Lung Adenocarcinoma and Targets PI3K/AKT/MAPK Pathways In Silico. (PubMed, ACS Omega) - "Although less potent than the nanomolar-range reference drug Epothilone B (IC50 < 0.1 μM), rugulosin A showed submicromolar-to-low micromolar efficacy with notable selectivity toward cancer cells, which is considered significant for an unoptimized natural product scaffold. Its antiproliferative activity against K562 cells (GI50 = 3.69 μM), benchmarked against Imatinib (GI50 = 0.373 μM), also falls within the active range of natural product leads...Molecular docking revealed strong binding energies (-10.1, -9.8, and -11.0 kcal/mol), along with a stable molecular dynamics simulations data. These findings highlight rugulosin A (3) as a promising anticancer lead that modulates major apoptosis signaling pathways."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • AKT1 • CASP3 • MAPK14 • PIK3CA

Ixabepilone and Temsirolimus in Treating Patients With Solid Tumors That Are Metastatic or Cannot Be Removed by Surgery (clinicaltrials.gov) - P1 | N=22 | Active, not recruiting | Sponsor: National Cancer Institute (NCI) | Trial completion date: Mar 2026 ➔ Mar 2027

Trial completion date • Oncology • Solid Tumor

Epothilone B stabilizes microtubules via Tau to protect retinal ganglion cells and promote axon regeneration. (PubMed, Cell Commun Signal) - No abstract available

Journal

Microtubule-stabilizer epothilone B counteracts anesthetic-induced slowed swimming in Tetrahymena pyriformis. (PubMed, Exp Cell Res) - "We first extend previous findings with other volatile anesthetics, to show that isoflurane also reversibly slows swimming speed in Tetrahymena. Our present results are thus consistent with the hypothesis that all ciliates are sensitive to volatile anesthetics, and support conserved molecular mechanisms of anesthetic action in single-celled organisms and mammals. Moreover, our preparation enables inexpensive high-throughput testing of the functional roles played by specific candidate molecular targets of volatile anesthetics in ciliates."

Journal • Anesthesia

Synthesis and Early Assessment of Epothilone-Derived Fluorescent Probes for Microtubule Imaging. (PubMed, ChemMedChem) - "Building on a tested strategy for the synthesis of epothilone-type structures, an analog of epothilone B with an extended C(6) substituent terminating in an alkyne group has been prepared. A Huisgen [3 + 2] cycloaddition of this analog with azide-functionalized derivatives of Alexa Fluor 488 and Janelia Fluor 646 gave bright fluorescent probes emitting in the green and far-red spectral range, respectively. Both probes bind to microtubules with high affinity and specifically label the microtubule network in A549 cells."

Journal

Brain-penetrant microtubule-stabilizer epothilone B delays isoflurane-induced unconsciousness in mice. (PubMed, Neuropharmacology) - "Our findings support the Orchestrated Objective Reduction (Orch OR) model that posits consciousness as a property of a quantum physical state of neural MTs. We also discuss possible sex differences in anesthetic mechanisms suggested by our data."

Journal • Preclinical • Anesthesia

Rational design of a bifunctional glycosyltransferase for enhanced substrate promiscuity and thermostability. (PubMed, J Biotechnol) - "Structural dynamics analyses revealed that mutation-induced global conformational rigidity and localized hydrogen-bond network optimization primarily drove thermostability improvement and substrate affinity enhancement, respectively. This work establishes a closed-loop engineering paradigm of "computational prediction → rational mutagenesis → mechanistic decoding", providing a scalable framework for precision engineering of GTs and glycoside biomanufacturing."

Journal

AI-driven multi-omics integration of cancer-associated fibroblasts for prognostic modeling and therapeutic target discovery in head and neck squamous cell carcinoma. (PubMed, NPJ Precis Oncol) - "Furthermore, therapeutic vulnerabilities were explored by integrating drug sensitivity prediction, AI-assisted cMAP screening, and molecular docking validation, which identified Epothilone B as a promising agent targeting HBEGF. Overall, this research shows that understanding the heterogeneity of CAFs with AI-enabled multi-omics modeling can reveal prognostic biomarkers and therapeutic targets for overcoming resistance, with the ultimate goal of improving precision oncology for HNSCC."

Journal • Tumor mutational burden • Head and Neck Cancer • Microsatellite Instability • Oncology • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Carcinoma of Head and Neck • HBEGF • MSI • TMB

Fast-adapting graph neural network with prior knowledge for drug response prediction across preclinical and clinical data. (PubMed, J Pharm Anal) - "Additionally, metaDRP's inherent interpretability offers reliable insights into drug mechanisms of action, such as elucidating the pathways and molecular targets of drugs like epothilone B and pemetrexed. This work provides a promising approach to overcoming data scarcity and out-of-distribution challenges in drug response prediction, while promoting the integration of few-shot learning in this field."

Clinical data • Journal • Preclinical • Oncology

In Vivo Local Administration of Para-Amino-Bebblistatin to the Injured Spinal Cord Fails to Improve the NaChBac-Expressing DRGs Transplantation. (PubMed, Int J Mol Sci) - "We employ, alone or in combination, blebbistatin and epothilone B, tested in vitro...Nevertheless, when applied in vivo in a model of SCI, local and single para-amino-blebbistatin (a stable analogue of blebbistatin) administration and the transplanted NaChBac expressing sensory neurons limit the functional recovery enabled by neuronal transplantation alone. Thus, despite the beneficial outputs of isolated neuronal cultures that allow selection of in vivo combinatory strategies, the multifaced characteristics of CNS injuries limit the potential success of single and local treatment administration, demanding extended and sustained treatments."

Journal • Preclinical • CNS Disorders • Orthopedics • Transplantation

In situ structural mechanism of epothilone-B-induced CNS axon regeneration. (PubMed, Nature) - "These microtubule shoots serve as scaffolds for various types of vesicles and endoplasmic reticulum, facilitating the supply of materials necessary for axon repair until membrane tension normalizes. We demonstrate the unexpected ability of neuronal cells to adjust to strain induced by epothilone B, which creates homeostatic imbalances and activates axons to regeneration mode."

Journal

Targeted environmental enrichment is more effective than bipedal treadmill training after thoracic spinal cord injury. (PubMed, Brain Commun) - "Our findings indicate that targeted environmental enrichment outperforms bipedal training across several behavioural measures which produced a ceiling effect that epothilone B could not overcome. Therefore, these results suggest that targeted environmental enrichment may be a more effective rehabilitation approach than B-TMT and should be considered for application in models of severe spinal cord injury."

Journal • CNS Disorders • Musculoskeletal Diseases • Orthopedics

Expression of Concern: Epothilone B Benefits Nigrostriatal Pathway Recovery by Promoting Microtubule Stabilization After Intracerebral Hemorrhage. (PubMed, J Am Heart Assoc) - "The editors and Scientific Publishing Committee are in communication with the authors regarding the integrity of the image data, and Loma Linda University has confirmed the concerns are being reviewed. While we await the outcome of this review, we are publishing this Expression of Concern to indicate that the data and statements in the article may not be reliable."

Journal • Cerebral Hemorrhage • Hematological Disorders

Prognostic risk model of gastric adenocarcinoma based on exosome-related genes. (PubMed, Medicine (Baltimore)) - "Drug sensitivity analysis indicated that bortezomib, docetaxel, and epothilone B were more effective in the high-risk group. The exosome-related risk model constructed in this study can effectively predict the prognosis of patients with STAD."

Biomarker • Journal • Gastric Adenocarcinoma • Gastric Cancer • Oncology • Solid Tumor • APOA1 • APOD • SERPINE1

Construction of a prognostic model for hepatocellular carcinoma based on necrosis by sodium overload-related genes and identification of ANKRD13B as a new prognostic marker. (PubMed, Funct Integr Genomics) - "Drug sensitivity analysis identified eight chemotherapeutic agents with heightened sensitivity in high-risk patients: BI.2536, Bleomycin, Cisplatin, Doxorubicin, Epothilone B, Gemcitabine, Mitomycin C, and Paclitaxel. We established a novel NECSO prognostic model demonstrating good predictive capacity for HCC prognosis and therapeutic responsiveness. This model helps with personalized clinical management."

Biomarker • IO biomarker • Journal • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor

Machine learning-based characterization of a PANoptosis-associated model for enhancing prognosis and immunotherapy response in lung adenocarcinoma patients. (PubMed, Discov Oncol) - "The present study developed a PRS using 101 machine learning combination algorithms, which could aid in risk stratification and prognosis for LUAD patients. The candidate drugs and target may provide new insights in the treatment of high PRS group patients."

IO biomarker • Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • TRPA1

m6A-Mediated Methylation Patterns and Their Association With Obstructive Sleep Apnea in Lung Adenocarcinoma. (PubMed, Cancer Rep (Hoboken)) - "Analyses confirmed m6A modification's role in LUAD progression, immune regulation, and outcomes. The m6A score is a valuable prognostic marker associated with survival, OSAHS incidence, and drug sensitivity. These findings highlight m6A's potential as a therapeutic target and biomarker, particularly for LUAD patients with OSAHS."

Biomarker • IO biomarker • Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Obstructive Sleep Apnea • Oncology • Respiratory Diseases • Sleep Disorder • Solid Tumor

Epothilone B from Aspergillus fumigatus with a strong antiproliferative and anti-tubulin polymerizing activities; apoptosis, and cell cycle analyses. (PubMed, BMC Microbiol) - "The level of released LDH of HepG-2 cells was increased exponentially with the Epothilone concentration, ensuring their negative effect on the plasma membrane permeability. From the docking results, the binding energy of Epothilone B with the tubulin-β was -9.96 kcal/mol, that was lower than Taxol (-7.87 kcal/mol), ensuring the higher affinity of Epothilone B to bind with the β-tubulin protein."

Journal • Oncology • CASP9

Machine learning-based diagnostic and prognostic models for breast cancer: a new frontier on the clinical application of natural killer cell-related gene signatures in precision medicine. (PubMed, Front Immunol) - "Furthermore, drug sensitivity analysis indicated that high-risk patients were more sensitive to Thapsigargin, Docetaxel, AKT inhibitor VIII, Pyrimethamine, and Epothilone B, while showing higher resistance to drugs such as I-BET-762, PHA-665752, and Belinostat. This study provides a comprehensive analysis of NRGs in BC and establishes reliable ML-based diagnostic and prognostic models. The findings highlight the clinical relevance of NRGs in BC progression, immune regulation, and therapy response, offering potential targets for personalized treatment strategies."

Biomarker • Gene Signature • IO biomarker • Journal • Breast Cancer • Oncology • Solid Tumor • CD2 • IL21 • PRDX1 • ULBP2