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doxorubicin (doxorubicin, Nanox / Doxonax)

✓ Approved

Nanox · TOP2A · 小分子

什么是 doxorubicin？

doxorubicin 是一种小分子，由Nanox研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)。

药物档案

商品名doxorubicin, Nanox, Doxonax
公司Nanox
药物类别小分子
分子靶点TOP2A
给药途径Injectable (Others)
状态Approved
来源： ClinicalTrials.gov, Nanox

作用机制

分子靶点

doxorubicin 作用于 1 个分子靶点：

TOP2ADNA topoisomerase II alpha (TOP2alpha, TOPIIA)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

doxorubicin 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Kaposi's sarcoma✓ Approved

相关研究文献

PubMedSignal transduction and targeted therapy2026-07-27

Bacteria-mimicking cancer cells reprogram macrophages via multiple pattern recognition receptor pathways for cancer immunotherapy.

Song Seoyoon S, Yu Dongjun D, Kang Haneul H, Lee Deborah D et al.

Although macrophages are a powerful cell-based platform for cancer immunotherapy, their antitumor functions, such as phagocytosis and inflammatory responses, are limited by the immunosuppressive tumor microenvironment. Here, we show that decorating cancer cell membranes with bacteria-derived pathogen-associated molecular patterns (PAMPs) initiates phagocytosis and inflammatory responses of macrophages toward cancer cells involving various pattern-recognition receptor signaling pathways. Bacteria-derived PAMPs were formulated into membrane-decorating nanoparticles, and these nanoparticles reprogrammed immunosuppressive macrophages into inflammatory phenotypes. Cancer cell membrane-attached PAMP nanoparticles maintained their immunostimulatory responses, stimulating macrophages' antitumor functions. The fraction of phagocytic macrophages significantly increased when coincubated with membrane-decorated cancer cells, along with an increased secretion of inflammatory cytokines such as interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α). Transcriptomic gene ontology analysis revealed that the response of macrophages to PAMP-decorated cancer cells resembled their response to bacteria, involving signaling pathways including inflammatory response and innate immune response. In a mouse model, locally injected membrane-decorating PAMP nanoparticles suppressed tumor growth. The therapeutic effect was more pronounced in combination with the chemotherapeutic drug doxorubicin. Median survival days significantly increased in both the PAMP nanoparticle and the PAMP nanoparticle plus doxorubicin combination group with complete remission cases, compared to the doxorubicin group. Our findings provide insights into the use of macrophages as a cancer immunotherapy modality.

PMID 42503515
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PubMedACS nano2026-07-27

Anti-PEG Single-Chain Variable-Fragment Antibody-Assisted In Vivo Process Decoding of PEGylated Nanomedicines.

Pan Feng F, Xu Qingyuan Q, Tian Kaisong K, Luo Gan G et al.

Clinical translation of nanomedicines is greatly hindered by insufficient understanding of their in vivo process, yet a key challenge lies in quantifying the encapsulated versus free drug forms in tissues and cells. Herein, we present a facile, versatile anti-PEG single-chain variable-fragment antibody (PEG-scFv)-based method enabling quantitative measurement of both forms in various biofluids (e.g., interstitial fluid, cytoplasm). By this method, we map the in vivo process of PEGylated liposomal doxorubicin (sLip/Dox) at unprecedented resolution. In the bloodstream, doxorubicin remains largely encapsulated in liposomes (>99%). In liver as the main organ for drug elimination, less drug was distributed in the interstitium (>80% encapsulated) but more in liver cells (mainly in Kupffer cells) released in a time-dependent manner, accompanying doxorubicin transferred to hepatocytes most in free form by 12 h postinjection. After extravasation into tumors, there was a limited access of sLip/Dox to tumor cells, confining most of the drug in the interstitium mainly being encapsulated (more than 75%), and the internalized fraction underwent a gradual release process in both tumor-associated macrophages and tumor cells. These findings revealed that for sLip/Dox, which primarily underwent drug release intracellularly, cellular internalization rates could be the key factor in determining its in vivo performance. Given widespread PEGylation on developing nanomedicines and the cost-effectiveness of scFv production, PEG-scFv offers a broadly applicable tool for dissecting in vivo processes of nanomedicines to establish dose-effect relationships like small-molecule drugs, further to guide rational nanotherapeutic design.

PMID 42503863
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PubMedJournal of biochemical and molecular toxicology2026-07-27

Morroniside Attenuates Doxorubicin-Induced Cardiotoxicity by Activating the PI3K/AKT/Nrf2/HO-1 Pathway to Inhibit Ferroptosis and Oxidative Stress.

Lin Zhi-Hui ZH, Lin Xing-Yu XY, Lu Wen-Jie WJ, Wu Meng-Qi MQ et al.

Cardiotoxicity induced by doxorubicin (Dox) significantly contributes to increased mortality among cancer patients, yet available pharmacological interventions remain scarce. Recent studies suggest that ferroptosis is a key mechanism in the development of Dox-induced cardiotoxicity (DIC). Morroniside (Mor), an active iridoid glycoside isolated from Cornus officinalis, exhibits multiple pharmacological properties such as antioxidant, anti-ferroptotic, and anti-inflammatory activities. Given this multi-target profile, Mor shows potential as a treatment option for reducing DIC. This work was designed to examine the association between Mor and DIC. In vivo DIC model, C57BL/J mice received 5 mg/kg/d Mor via oral gavage for 5 weeks. In vitro DIC model, H9c2 cells were exposed to 10 μM Mor over a 48-h period. Cardiac injury markers were quantified in serum and cell culture supernatants. Biochemical assays, western blotting, cellular immunofluorescence, and DHE/ROS staining were employed to evaluate ferroptosis and oxidative stress. Mor administration substantially reduced the levels of cardiac injury biomarkers while simultaneously attenuating ferroptosis and oxidative stress in vivo. In cellular models, Mor exhibited potent anti-ferroptotic and antioxidant effects through Nrf2 pathway activation. Further mechanistic studies identified PI3K/AKT pathway as the upstream regulator of Nrf2 activation in response to Mor treatment. Our study provided the first evidence for Mor's cardioprotective effects against DIC. Mechanistically, Mor attenuated DIC by suppressing ferroptosis and reducing oxidative stress via activation of the PI3K/AKT/Nrf2/HO-1 signaling pathway.

PMID 42504915
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PubMedJournal of drug targeting2026-07-27

Cathepsin B-Activated Vitamin E Prodrugs Target Cancer Stem Cells and Enhance Chemotherapy Response in Triple-Negative Breast Cancer with Minimal Cardiotoxicity.

Pandurangi Raghu R, Tomasetti Marco M, Verapazham Sekar T ST, Paulmurugan Ramasamy R et al.

Triple-negative breast cancer (TNBC) remains one of the most difficult malignancies to treat owing to high relapse, enrichment of cancer stem cells (CSCs), and constitutive activation of pro-survival signaling such as NF-κB. We conceived a new therapeutic concept-A Priori Activation of Apoptosis Pathways (AAAPT)-designed to pre-empt and circumvent tumor tactics that desensitize cells to diverse interventions by restoring apoptotic checkpoints while suppressing dysregulated survival pathways (e.g., NF-κB) that are upregulated in resistant clones. CSCs and therapy-refractory TNBC subpopulations overexpress Cathepsin B and exhibit organelle fragility in lysosomes and mitochondria. To target these liabilities, we designed Cathepsin B-cleavable vitamin E analogs (AAAPT leading drugs: AMP-001/002/003) that selectively release active agents inside tumor and CSC populations.In vitro, AMP-001/002/003 showed selective cytotoxicity toward Cathepsin B-positive TNBC cells, inhibited mammosphere formation (a functional surrogate for CSC self-renewal), and spared non-malignant epithelial cells and human iPSC-derived cardiomyocytes. Combination studies revealed strong synergy with doxorubicin, lowering its effective IC50. In vivo, AMP-001 significantly reduced TNBC xenograft burden without overt systemic or cardiac toxicity, consistent with the in-vitro safety profile.These findings support Cathepsin B-activated vitamin E analogs as tumor-selective chemosensitizers that address key TNBC liabilities-CSCs, NF-κB-mediated resistance, and organelle-level stress responses-while mitigating doxorubicin-associated cardiotoxicity.

PMID 42506946
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PubMedACS applied bio materials2026-07-27

Thermosensitive Block Copolymer Hydrogel with Embedded Catanionic Vesicles as a Localized Doxorubicin Delivery Platform for Melanoma.

Machado Rui L RL, Zoco Aitana A, Oliveira Isabel S IS, Silva Bruna B et al.

Skin cancer, particularly melanoma, remains a major therapeutic challenge due to its high metastatic potential and limited efficacy of systemic chemotherapy. Localized and controlled delivery of chemotherapeutic agents such as doxorubicin (DOX) represents a promising alternative to systemic treatments and costly immunotherapies. Hybrid hydrogels that integrate polymeric scaffolds with embedded nanostructures (e.g., vesicles, micelles, or nanoparticles) have emerged as particularly effective platforms for enhancing therapeutic performance. Herein, we report the development of a thermosensitive hybrid hydrogel for potential melanoma drug delivery applications, obtained by dispersing DOX-loaded, pH-sensitive 12-2-12/SLSar catanionic vesicles within a poloxamer 237 (F87) scaffold. The system was comprehensively characterized in terms of rheological behavior, biocompatibility, drug-release kinetics, and in vitro anti-melanoma activity in 2D monolayer cell cultures and 3D spheroids. In parallel, molecular-level interactions between the F87 matrix and the surfactant-based vesicles were investigated. Strong polymer-surfactant interactions were observed, leading to the formation of mixed polymer/surfactant micelles and vesicles, and inducing significant modifications in aggregate physicochemical properties, particularly surface charge. These interactions were found to be thermally driven and strongly dependent on the polymer-to-surfactant ratio. The catanionic vesicles exhibited high DOX encapsulation efficiency and remained stably dispersed within the F87 scaffold. The resulting hybrid hydrogel demonstrated controlled release kinetics, offering potential advantages for localized drug delivery compared with vesicle-only formulations. Moreover, the hybrid system demonstrated excellent biocompatibility and significantly outperformed neat F87 hydrogels in enhancing DOX internalization and inducing melanoma cell death in vitro. Overall, this work presents a versatile and tunable strategy for integrating catanionic vesicles into thermosensitive polymeric scaffolds, providing a promising platform for localized melanoma drug delivery.

PMID 42504495
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PubMedMedical sciences (Basel, Switzerland)2026-07-27

Empagliflozin Protects Against Doxorubicin Cardiotoxicity: Integrative Assessment of Cardiac Kinetics and Electrophysiology Using Machine Learning in a Rat Model.

Goje Iacob-Daniel ID, Ordodi Valentin Laurențiu VL, Bojin Florina Maria FM, Goje Greta-Ionela GI et al.

Background/Objectives: Anthracycline-induced cardiotoxicity remains a major challenge in cancer treatment, and researchers are showing interest in artificial intelligence (AI) to improve the prediction and detection of cancer therapy-related cardiac dysfunction (CTRCD). Current surveillance strategies rely mainly on left ventricular ejection fraction and, more recently, global longitudinal strain. Methods: The present study was designed to evaluate cardiac performance in a rat model of doxorubicin-induced cardiotoxicity and empagliflozin-mediated cardioprotection using a machine learning-based analytical framework. Eighteen adult male Sprague-Dawley rats were assigned to five experimental groups. We aimed to quantify ventricular wall dynamics and contractility using an advanced image-processing and object-detection model that has not been previously used to distinguish normal from impaired cardiac kinetics. During real-time recording, simultaneous electrocardiogram monitoring was performed, enabling direct correlation between deep learning-based ventricular wall motion metrics and cardiac electrical activity. The cardioprotective effects of empagliflozin were further validated by immunofluorescence staining (cTnI, vimentin, α-SMA, and Cx43) of rat cardiomyocytes and paraffin-embedded cardiac tissue, demonstrating attenuation of cellular injury and structural remodeling. Results: The integrated analysis of cardiac kinetic patterns derived via machine learning distinguishes not only extreme cardiotoxicity, but also tracks a graded pattern consistent with ECG-derived severity and treatment-related functional preservation. These findings indicate that the algorithm captures the gradient of empagliflozin's cardioprotective effect within this internally validated preclinical setting. Additionally, immunofluorescence results validated the benefits of SGLT2 inhibition on myocardial integrity. Conclusions: The novelty of the present work lies at the intersection of advanced cardiac kinetic analysis using AI, preclinical modeling, and SGLT2-mediated cardioprotection in cardio-oncology.

PMID 42506311
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