Current drug metabolism最新文献

{"title":"Mobilising Computational Strategies in Enzyme Inhibition: Reconciling Therapeutic Innovation and Environmental Integrity from Molecular Targets to Ecosystem Disruptors.","authors":"Mallamma T, Jeevan Gowda, Rumaan M, Prakash Goudanavar, Butchi Raju Akondi","doi":"10.2174/0113892002420090251206171649","DOIUrl":"https://doi.org/10.2174/0113892002420090251206171649","url":null,"abstract":"<p><p>Enzyme inhibition has become a cornerstone of modern therapeutics, targeting key molecular pathways implicated in cancer, metabolic disorders, and infectious diseases. This review explores diverse strategies of enzyme inhibition from classical active site-directed inhibitors to innovative biofilm-targeting enzymatic cocktails, emphasising their clinical utility. Beyond medicine, enzyme inhibitors are routinely employed to modulate nitrogen fixation, methanogenesis, and microbial dynamics in industrial and environmental settings. However, this dual-edged sword reveals its paradox: the very agent that heals can also harm. Their ecological persistence and bioaccumulation risks disrupt microbial ecosystems, foster antibiotic resistance, and affect non-target organisms. This review navigates the fine line between pharmaco-logical promise and environmental peril, evaluating risk assessment frameworks, mitigation strategies, and forward-looking approaches such as high-throughput screening, machine learning, and enzyme engineering. Ultimately, it advocates for a symbiotic integration of pharmaceutical innovation and environmental stewardship to create eco-friendly strategies that can enhance therapeutic efficacy without compromising ecological balance.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147764978","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Protective Role of Atriplex halimus L. Against Sodium Benzoate-Induced Fat Benzene Accumulation, Bone Marrow and Liver Alterations in Wistar Rats.","authors":"Khaoula Zeghib, Djahra Ali Boutlelis, Ibtissam Laib, Soumaia Menai, Abderrhmane Bouafia, Sadok Nani, Abdelkrim Rebiai","doi":"10.2174/0113892002430770251208211517","DOIUrl":"https://doi.org/10.2174/0113892002430770251208211517","url":null,"abstract":"<p><strong>Introduction/objective: </strong>This study evaluates the adverse effects of sodium benzoate on the bone marrow and liver of rats, its potential to form benzene, and the protective role of Atriplex halimus extract.</p><p><strong>Methods: </strong>Thirty male albino rats were divided into five groups: control, Atriplex halimus extract alone, sodium benzoate alone, sodium benzoate with preventive Atriplex halimus ex-tract, and sodium benzoate with curative Atriplex halimus extract. Sodium benzoate was administered in drinking water at a dose of 100 mg/kg body weight for 15 weeks. Atriplex halimus extract was administered intragastrically either during the final 30 days (curative) or throughout the entire sodium benzoate exposure period (preventive). Phytochemical analysis of the extract was conducted using LC-MS. Biochemical, histopathological, and oxidative stress markers were assessed.</p><p><strong>Results: </strong>Sodium benzoate exposure led to benzene detection in fat tissues, reduced neutrophil counts, altered hepatic enzyme levels (aspartate aminotransferase, alanine aminotransferase, lactate dehydrogenase), decreased antioxidant defenses (glutathione, catalase, glutathione S-transferase), and increased malondialdehyde levels. Histopathological analysis revealed significant liver degeneration and milder bone marrow damage. Atriplex halimus extract restored biochemical and histological parameters, reversed neutropenia, and reduced benzene accumulation.</p><p><strong>Discussion: </strong>The findings confirm sodium benzoate's toxicity, particularly its oxidative stress and tissue damage effects, and highlight the protective potential of Atriplex halimus extract due to its phenolic compounds and saponins.</p><p><strong>Conclusion: </strong>Atriplex halimus extract exhibits preventive and curative effects against sodium benzoate-induced benzene accumulation in fat, as well as bone marrow and liver injuries.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671147","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Vitro Drug-Drug Interactions between Oxycodone and Commonly Co-Consumed Drugs in Rat and Human Liver Microsomes.","authors":"Weilong Gu, Rachel F Tyndale","doi":"10.2174/0113892002446297260217075246","DOIUrl":"https://doi.org/10.2174/0113892002446297260217075246","url":null,"abstract":"<p><strong>Introduction: </strong>Oxycodone is frequently co-consumed with xylazine, etizolam, di-azepam, and methamphetamine during clinical and/or illicit use.</p><p><strong>Methods: </strong>We investigated oxycodone metabolism to its two main metabolites, the active ox-ymorphone and the inactive noroxycodone, and potential interactions with these four drugs, using rat (RLM) and human (HLM) liver microsomes.</p><p><strong>Results: </strong>In RLM, Km values were similar for oxymorphone (115 μM) and noroxycodone (128 μM) formation, whereas in HLM, Km values differed for oxymorphone (146 μM) and noroxycodone (1.23 mM) formation. The CLint of oxycodone to noroxycodone was ~4-fold higher than oxycodone to oxymorphone, in both RLM and HLM. Xylazine inhibits (Ki) ox-ymorphone (1.9 μM) and noroxycodone (4.4 μM) formation in RLM more potently than in HLM (313 μM and 247 μM, respectively). Diazepam inhibits oxymorphone (5.0 μM) and no-roxycodone (5.6 μM) formation in RLM more potently than in HLM (1.8 mM and 163 μM, respectively). Etizolam inhibits oxymorphone (14.2 μM) and noroxycodone (16.1 μM) for-mation in RLM more potently than in HLM (550 μM and 129 μM, respectively). Metham-phetamine is not a potent inhibitor of oxymorphone formation (487 μM in RLM and 352 μM in HLM) or noroxycodone formation (5.8 mM in RLM and 2.7 mM in HLM). Similar inhi-bition patterns in RLM for both oxycodone and dextromethorphan, a probe substrate, con-firmed that CYP2D and CYP3A mediate oxymorphone and noroxycodone formation, respec-tively.</p><p><strong>Discussion: </strong>In summary, xylazine, diazepam, and etizolam may cause pharmacokinetic drug-drug interactions (PK-DDIs) with oxycodone in rats but are unlikely to do so in humans.</p><p><strong>Conclusion: </strong>Substantial species differences were observed in both the metabolism of oxyco-done by CYP2D and CYP3A and the inhibition of metabolite formation in RLM versus HLM.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147697578","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Deciphering the Impact of Protein Corona on Biological Fate of Nanomedicine-Loaded Microneedles.","authors":"Junli Zhu, Wenhao Wang, Zhengwei Huang","doi":"10.2174/0113892002459335260311061441","DOIUrl":"https://doi.org/10.2174/0113892002459335260311061441","url":null,"abstract":"<p><p>Due to adsorption of proteins, abundant protein molecules quickly bind to the nano-particles' (NPs) surface when they enter the bloodstream, forming a \"protein corona.\" The protein corona leads to rapid clearance of NPs, thereby impeding efficient drug delivery. Notably, mi-croneedles (MNs) can reduce protein corona formation by altering the route of drug entry and confining the drug within the local tissue microenvironment. This article outlines the relationship between drug-loaded MNs and the protein corona and proposes strategies to suppress its for-mation. Furthermore, it underscores that the synergy between microneedles and stealth nanocar-riers can minimize the detrimental effects associated with protein corona formation.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590509","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Population Pharmacokinetic Models of Oxypurinol in Adults: A Systematic Review.","authors":"Farah Aida A Zairol Azwan, Nor Asyikin Mohd Tahir, Shamin Mohd Saffian, Mohd Makmor-Bakry, Mohd Shahrir Mohamed Said","doi":"10.2174/0113892002439476260101094935","DOIUrl":"https://doi.org/10.2174/0113892002439476260101094935","url":null,"abstract":"<p><strong>Introduction: </strong>Allopurinol and its active metabolite, oxypurinol, reduce uric acid concentrations through xanthine oxidase inhibition by suppressing the conversion of hypoxanthine and xanthine. Oxypurinol plays a prominent role in allopurinol's pharmacological activity due to its longer elimination half-life. Despite decades of clinical use, establishing an optimal dosing strategy to consistently achieve the target serum uric acid concentration lower than 0.36 mmol L-1 remains challenging. This review aimed to summarize the development of population pharmacokinetic modeling for oxypurinol and analyze factors influencing its pharmacokinetic variability.</p><p><strong>Methods: </strong>PubMed, Web of Science, and Scopus were systematically searched from database inception until January 2025, adhering to the PRISMA guideline. Studies were eligible if they involved oxypurinol population pharmacokinetic analyses in adults receiving allopurinol and employed nonlinear mixed-effects modeling.</p><p><strong>Results: </strong>Eight studies met the inclusion criteria, mostly involving adult gout patients. Pharmacokinetic analyses of oxypurinol employed a one-compartment model, incorporating firstorder absorption and elimination, reporting clearance value of 0.60-1.74 L h-1 and volume of distribution 38.1-59.3 L. Covariates associated with oxypurinol clearance included creatinine clearance, body weight, normal fat mass, fat-free mass, ethnicity, genetic polymorphisms, and concomitant diuretics; whereas, total body weight was found as significant predictors for volume of distribution.</p><p><strong>Discussions: </strong>Reported values for oxypurinol clearance and volume of distribution varied across studies. The small sample sizes and underrepresentation of certain populations, particularly Asians, restrict the generalizability of these findings.</p><p><strong>Conclusion: </strong>Further research involving larger, more diverse cohorts is needed to refine therapeutic drug monitoring and identify potential covariates across different populations to optimize allopurinol therapy.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147510285","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development and Evaluation of a Baicalin-Loaded Phytosomal Transdermal Patch for Type 2 Diabetes Mellitus.","authors":"Priya Singhal, Rupa Mazumder, Anjna Rani, Abhijit Debnath","doi":"10.2174/0113892002437368260113092840","DOIUrl":"https://doi.org/10.2174/0113892002437368260113092840","url":null,"abstract":"<p><strong>Introduction: </strong>Type 2 diabetes management remains challenging because of low bioavailability, side effects, and poor compliance with oral therapies. Transdermal delivery methods offer a non-invasive therapeutic approach with sustained delivery, which avoids first-pass metabolism.</p><p><strong>Methods: </strong>A total of 207 different phytochemicals were virtually screened using i-dock against the diabetic target, PPAR-γ. Subsequently, three matrix-type transdermal patches were developed: a patch containing pure baicalin, a standard patch containing metformin, and a baicalin-loaded phytosomal patch. Phytosomes loaded with baicalin were optimized by using Central Composite Design and evaluated for their physicochemical properties, drug content, physical strength, in vitro, and ex vivo studies. In vivo antidiabetic efficacy was also studied in diabetic Wistar rats over 21 days, followed by a comparison of all formulations, including histopathological analysis of pancreatic tissue.</p><p><strong>Results: </strong>Molecular docking studies showed promising results; baicalin has a high binding affinity for PPAR-γ (-9.8 kcal/mol). The optimized phytosomal patch confirmed a uniform drug content (91.4 ± 0.12 %) and showed sustained release over 12 hours. The ex vivo permeation study showed a significantly higher skin flux for the phytosomal patch (83.6%). In vivo studies confirmed that baicalin-loaded phytosomal patches showed significant blood glucose reductions (223 ± 0.32 to 96 ± 0.38 levels by Day 21), a comparable efficacy to standard metformin patches (224 ± 0.37mg/dL to 94 ± 0.34 mg/dL by Day 21).</p><p><strong>Discussion: </strong>The enhanced skin permeation, penetration, and sustained-release exhibited by the phytosomal transdermal patch can be explained by the phospholipid-based shell structure, leading to better affinity with the skin, facilitating retention of the drug. The comparable glycemic control observed with metformin indicates that baicalin-loaded phytosomal transder-mal patches can achieve effective therapeutic concentrations via transdermal delivery, which is corroborated across two studies. These observations are consistent with previous literature documenting improved solubility and bioavailability of plant-derived actives utilizing phyto-some-based systems, which have applicability for chronic metabolic diseases such as T2DM.</p><p><strong>Conclusion: </strong>The developed phytosomal transdermal patch showed sustained release, better permeation, and potent antidiabetic activity; thus, it offers an alternative to conventional T2DM therapies.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147510333","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lymphatic Drug Delivery System and Lipid-based Nanoformulations: Savior to Save for Patients Receiving Highly Hepatotoxic Drugs.","authors":"Vishal Kumar Vishwakarma, Prabhat Kumar Upadhyay, Nandini Dubey, Aditya Singh, Harlokesh Narayan Yadav","doi":"10.2174/0113892002395927251205235609","DOIUrl":"https://doi.org/10.2174/0113892002395927251205235609","url":null,"abstract":"<p><p>The liver plays a vital role in regulating normal physiological processes in the body. Liver dysfunction can lead to mild to severe pathological conditions and, in some cases, death. To date, more than 900 drugs, toxins, and herbs have been identified with the potential to cause various liver diseases, including acute liver damage, cholestatic jaundice, hepatic granulomas, active chronic hepatitis, and hepatic tumors. A wide range of liver dysfunction results from drug consumption and is referred to as drug-induced liver injury (DILI). DILI significantly contributes to the immediate withdrawal of drugs from the mar-ket. Due to its numerous advantages, the oral route has long been the preferred method of drug administration, although these medicines increase the risk of liver damage. Novel drug delivery approaches, such as the lymphatic drug delivery system and lipid-based nanofor-mulations-including solid lipid nanoparticles (SLNs) and nanostructured lipid carriers-can bypass the liver, reducing the toxic effects of various drugs. Therefore, SLNs represent a promising strategy for lymphatic drug delivery, particularly for hepatocompromised pa-tients and those taking hepatotoxic drugs. This review summarizes how lymphatic drug delivery systems and lipid-based nanoformulations can benefit hepatocompromised pa-tients and individuals on hepatotoxic medications.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147490884","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological Complexities of Herbal Medicinal Extracts: A Review of Bioavaila-bility, Interactions, and Standardization.","authors":"Manoj Madanahalli Ramesh, Sneha Dinesh, Annegowda Hardur Venkatappa, Richard Lobo","doi":"10.2174/0113892002430015251201072618","DOIUrl":"https://doi.org/10.2174/0113892002430015251201072618","url":null,"abstract":"<p><p>Herbal medicines have gained remarkable popularity due to their natural origins and potential medicinal value. Nevertheless, they are chemically complex and pose signifi-cant pharmacological challenges. This review focuses on the key aspects influencing their clinical use: their variable bioavailability, complex pharmacokinetics (ADME), and potential for interactions. A primary concern is herb-drug interactions, with special emphasis on the modulation of drug-metabolizing enzymes by specific phytoconstituents, which can alter drug concentrations to an extent that may be life-threatening, causing either increased toxicity or therapeutic failure. The pharmacological profile is further complicated by the complex effects of constituents, such as synergistic or antagonistic actions, which make predicting therapeutic response and safety difficult. A critical challenge in this field is the frequent dis-connect between in vitro findings and in vivo outcomes, underscoring the importance of phar-macokinetic data, particularly bioavailability, for accurate clinical risk assessment. Safety is a paramount concern, as it is often compromised by inconsistent standardization and quality control, leading to batch-to-batch variability, potential adulteration, and contamination. The absence of stringent regulation impairs therapeutic consistency and introduces health risks. To address these issues, advanced approaches are being employed to improve bioavailability, including novel drug delivery systems that enhance solubility and stability. This review em-phasizes that a rigorous, phytoconstituent-centric approach is essential for navigating the complexities of herbal medicine. By addressing challenges in pharmacokinetics, interactions, safety, standardization, and bioavailability through rigorous scientific investigation and em-bracing future perspectives, such as in silico modeling and improved regulatory frameworks, the quality, safety, and effectiveness of herbal treatments can be ensured, supporting their responsible integration into modern, evidence-based medical systems.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147490844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Zebrafish as a Model Organism to Study Neurotoxicity: A Potential Tool for Neuroprotective Drug Discovery.","authors":"Rajneesh Kumar, Poonam Dhiman, Damanpreet Singh","doi":"10.2174/0113892002418502251128110509","DOIUrl":"https://doi.org/10.2174/0113892002418502251128110509","url":null,"abstract":"<p><strong>Introduction: </strong>Danio rerio, the zebrafish, serves as an excellent model in neuroprotective drug discovery due to its conserved nervous system organization, neurotransmitter pathways, antioxidant de-fenses, and genomic similarity to mammals.</p><p><strong>Methods: </strong>A systematic literature search following PRISMA 2020 guidelines was conducted across Pub-Med, Scopus, Web of Science, and Google Scholar. Studies published between 2020 and 2025 were pri-oritized, with earlier key papers included for context. The data on larval, adult, and genetically modified zebrafish models were analyzed for neurotoxic effects, focusing on study design, toxicants, and neurobe-havioral or molecular outcomes.</p><p><strong>Results: </strong>Neurotoxicants such as chlorpyrifos, bisphenol, triphenyl phosphate, aluminum, ammonium ac-etate, arsenic, zinc, acrylamide, methylmercury, and tris (1,3-dichloro-2-propyl) phosphate were shown to cross the zebrafish blood-brain barrier. These exposures caused significant behavioral alterations, neu-rotransmitter imbalances, oxidative stress, and gene or protein expression changes related to brain func-tion. Analysis of the transgenic zebrafish revealed notable alterations in neuronal development and axonal morphology upon exposure to various neurotoxic chemicals.</p><p><strong>Discussion: </strong>Zebrafish display neurotoxic responses with a close resemblance to mammals, supporting their translational value in neurotoxicity and drug discovery studies. However, limitations such as a less complex brain compared to mammals, quick neuronal regeneration, limited tissue access, and difficulties in drug absorption quantification warrant refinements in zebrafish models.</p><p><strong>Conclusion: </strong>Zebrafish offer a versatile, cost-effective, and genetically tractable system for neurotoxicity and neuroprotection research. This systematic review highlights their crucial role in neuroprotective drug discovery while emphasizing the need for improved methodological approaches to enhance translational reliability.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147462725","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Advances in Carbon Nanotubes: Revolutionizing Cancer Diagnosis and Targeted Therapy.","authors":"Bharat Veer, Shatrudhan Prajapati, Shikha Yadav","doi":"10.2174/0113892002382741251212100251","DOIUrl":"https://doi.org/10.2174/0113892002382741251212100251","url":null,"abstract":"<p><p>Nanotechnology has been applied to the diagnostic and therapeutic treatment of cancer, with Carbon Nanotubes (CNTs) serving as an effective platform for these processes. In addition to their known physicochemical characteristics, such as high surface area, mechanical strength, and ease of functionali-zation, CNTs possess pharmacokinetic properties that enable their use in targeted drug-delivery and diag-nostic systems. Through functionalization, biodistribution, cellular uptake, and circulatory time can be modulated, thereby overcoming the limitations of traditional therapies, such as low bioavailability and systemic toxicity, and enabling more robust absorption, distribution, metabolism, and excretion profiles. Targeted CNT formulations can reduce off-target exposure and improve therapeutic efficiency through targeted delivery and controlled release. Besides, conjugation of CNTs to imaging or diagnostic agents enables improved assessment of biodistribution and metabolic characteristics, which justify their use as theranostic platforms. This review describes the new developments in CNT-based drug delivery systems for cancer treatment, with particular regard to their interactions with metabolism and the importance of these interactions on drug excretion. The fact that CNTs cross biological barriers and can boost drug bio- availability highlights the importance of these nanoparticles in enhancing the effectiveness of treatment procedures and minimizing toxicity. However, safety issues, including toxicity, long-term safety, and bi- ocompatibility, are also significant impediments to clinical translation. There will be a need to address such issues by systematizing pharmacokinetic and metabolic studies to assist in developing CNT-based solutions for precision oncology.</p>","PeriodicalId":10770,"journal":{"name":"Current drug metabolism","volume":" ","pages":""},"PeriodicalIF":1.8,"publicationDate":"2026-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147456194","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}