Definition and research guide
This page combines a MeSH definition, publication statistics and selected research abstracts. It is a starting point for reading the literature, not a medical textbook or a systematic evidence review.
Content available: 4 complete abstracts (785 words), 10 references. Full article text is not stored or reproduced here; follow the PMID, DOI or PMC links to read the original sources and their access terms.
Definition
A semisynthetic camptothecin derivative that inhibits dna topoisomerase I to prevent nucleic acid synthesis during S phase. It is used as an antineoplastic agent for the treatment of colorectal neoplasms and pancreatic neoplasms.
Definition: NLM Medical Subject Headings (MeSH) scope note (Public domain (U.S. National Library of Medicine); attribution requested). View the MeSH record.
Also known as: Camptothecin-11; Camptothecin 11; Irrinotecan; SN 38 11; SN-38-11; SN3811; 7-Ethyl-10-hydroxycamptothecin; 7 Ethyl 10 hydroxycamptothecin.
Where it fits in the MeSH classification
- Broader topics
- Camptothecin
Related concepts
- Dna Topoisomerase
- Phase
- Colorectal Neoplasms
- Pancreatic Neoplasms
Research landscape
PubMed indexes 9,035 records tagged with the MeSH heading “Irinotecan” (counts retrieved 2026-10-31). 2,041 of them (22.6%) were published from 2020 onward, and the busiest period so far is 2010-2019 with 3,267 records.
Reviews account for 1,146 records (12.7%) and meta-analyses for 126. Randomized controlled trials number 608 (6.7%) as a share of all records on the topic.
Show the data
| Period | Records |
|---|---|
| through 1999 | 542 |
| 2000-2009 | 3,185 |
| 2010-2019 | 3,267 |
| 2020 onward | 2,041 |
Publication-type chart data
| Type | Records | Share |
|---|---|---|
| Reviews | 1,146 | 12.7% |
| Meta-analyses | 126 | 1.4% |
| Randomized controlled trials | 608 | 6.7% |
Method: PubMed query "Irinotecan"[MeSH Terms] with publication-type and date filters, retrieved 2026-10-31.
Reading the evidence in drugs and chemicals
Studies of a chemical or drug can answer very different questions: what it is and how it behaves in cells and animals, how the body handles it, and whether it changes outcomes in people. Laboratory and animal findings often do not carry over to patients, and observational studies of exposures are confounded by who uses a substance and why. Nothing on this page is a recommendation to use, avoid, start or stop any substance or medicine; talk to a qualified clinician or pharmacist about your own situation. Check the dose, the species, the comparison group and whether a patient-relevant outcome was measured.
Evidence from open-access studies
These open-access studies come from PubMed’s best-match results for this heading (papers whose main topic it is), ranked here by citation count, with one recent addition. Each abstract is reproduced in full under its recorded open licence so that you can read the authors’ own words. They illustrate the literature; they are not a systematic summary of it. Citation counts measure attention, not reliability or clinical benefit.
Irinotecan-Still an Important Player in Cancer Chemotherapy: A Comprehensive Overview [1]
Abstract reading summary — source excerpts
- Opening excerpt
- Irinotecan has been used in the treatment of various malignancies for many years.
- Closing excerpt
- We are sure that the article will constitute an important source of information for both new researchers in the field of irinotecan chemotherapy and professionals or clinicians who are interested in the topic.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (145 words)
Irinotecan has been used in the treatment of various malignancies for many years. Still, the knowledge regarding this drug is expanding. The pharmacogenetics of the drug is the crucial component of response to irinotecan. Furthermore, new formulations of the drug are introduced in order to better deliver the drug and avoid potentially life-threatening side effects. Here, we give a comprehensive overview on irinotecan's molecular mode of action, metabolism, pharmacogenetics, and toxicity. Moreover, this article features clinically used combinations of the drug with other anticancer agents and introduces novel formulations of drugs (e.g., liposomal formulations, dendrimers, and nanoparticles). It also outlines crucial mechanisms of tumor cells' resistance to the active metabolite, ethyl-10-hydroxy-camptothecin (SN-38). We are sure that the article will constitute an important source of information for both new researchers in the field of irinotecan chemotherapy and professionals or clinicians who are interested in the topic.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 32664667 · DOI · PMC7404108
Injectable Thermo-Sensitive Chitosan Hydrogel Containing CPT-11-Loaded EGFR-Targeted Graphene Oxide and SLP2 shRNA for Localized Drug/Gene Delivery in Glioblastoma Therapy [2]
Abstract reading summary — source excerpts
- Opening excerpt
- In this study, we aimed to develop a multifunctional drug/gene delivery system for the treatment of glioblastoma multiforme by combining the ligand-mediated active targeting and the pH-triggered drug release features of graphene oxide (GO).
- Closing excerpt
- The in situ forming hydrogel will not only provide extended drug release but also combine the advantages offered by the chitosan-based copolymer structure for siRNA delivery to broaden treatment modalities in cancer therapy.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (308 words)
In this study, we aimed to develop a multifunctional drug/gene delivery system for the treatment of glioblastoma multiforme by combining the ligand-mediated active targeting and the pH-triggered drug release features of graphene oxide (GO). Toward this end, we load irinotecan (CPT-11) to cetuximab (CET)-conjugated GO (GO-CET/CPT11) for pH-responsive drug release after endocytosis by epidermal growth factor receptor (EGFR) over-expressed U87 human glioblastoma cells. The ultimate injectable drug/gene delivery system was designed by co-entrapping stomatin-like protein 2 (SLP2) short hairpin RNA (shRNA) and GO-CET/CPT11 in thermosensitive chitosan-g-poly(N-isopropylacrylamide) (CPN) polymer solution, which offers a hydrogel depot for localized, sustained delivery of the therapeutics after the in situ formation of CPN@GO-CET/CPT11@shRNA hydrogel. An optimal drug formulation was achieved by considering both the loading efficiency and loading content of CPT-11 on GO-CET. A sustained and controlled release behavior was found for CPT-11 and shRNA from CPN hydrogel. Confocal microscopy analysis confirmed the intracellular trafficking for the targeted delivery of CPT-11 through interactions of CET with EGFR on the U87 cell surface. The efficient transfection of U87 using SLP2 shRNA was achieved using CPN as a delivery milieu, possibly by the formation of shRNA/CPN polyplex after hydrogel degradation. In vitro cell culture experiments confirmed cell apoptosis induced by CPT-11 released from acid organelles in the cytoplasm by flow cytometry, as well as reduced SLP2 protein expression and inhibited cell migration due to gene silencing. Finally, in vivo therapeutic efficacy was demonstrated using the xenograft of U87 tumor-bearing nude mice through non-invasive intratumoral delivery of CPN@GO-CET/CPT11@shRNA by injection. Overall, we have demonstrated the novelty of this thermosensitive hydrogel to be an excellent depot for the co-delivery of anticancer drugs and siRNA. The in situ forming hydrogel will not only provide extended drug release but also combine the advantages offered by the chitosan-based copolymer structure for siRNA delivery to broaden treatment modalities in cancer therapy.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 32993166 · DOI · PMC7583917
Tumour-on-chip microfluidic platform for assessment of drug pharmacokinetics and treatment response [3]
Abstract reading summary — source excerpts
- Opening excerpt
- Microphysiological in vitro systems are platforms for preclinical evaluation of drug effects and significant advances have been made in recent years.
- Closing excerpt
- We demonstrate here that our microfluidic tumour-on-chip platform can successfully predict the efficacy from in vivo studies and therefore represents an innovative tool to guide drug dose and schedules for optimal efficacy and pharmacodynamic assessment, while reducing the need for animal studies.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (173 words)
Microphysiological in vitro systems are platforms for preclinical evaluation of drug effects and significant advances have been made in recent years. However, existing microfluidic devices are not yet able to deliver compounds to cell models in a way that reproduces the real physiological drug exposure. Here, we introduce a novel tumour-on-chip microfluidic system that mimics the pharmacokinetic profile of compounds on 3D tumour spheroids to evaluate their response to the treatments. We used this platform to test the response of SW620 colorectal cancer spheroids to irinotecan (SN38) alone and in combination with the ATM inhibitor AZD0156, using concentrations mimicking mouse plasma exposure profiles of both agents. We explored spheroid volume and viability as a measure of cancer cells response and changes in mechanistically relevant pharmacodynamic biomarkers (γH2AX, cleaved-caspase 3 and Ki67). We demonstrate here that our microfluidic tumour-on-chip platform can successfully predict the efficacy from in vivo studies and therefore represents an innovative tool to guide drug dose and schedules for optimal efficacy and pharmacodynamic assessment, while reducing the need for animal studies.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 34429505 · DOI · PMC8385015
Cyclic Peptide-Polymer Conjugate Nanotubes for Delivery of SN-38 in Treatment of Colorectal Cancer Model [4]
Abstract reading summary — source excerpts
- Opening excerpt
- Cyclic peptide-polymer conjugate nanotubes have been shown to be powerful drug delivery vectors, due to their propensity for dynamic self-assembly, high aspect ratio morphology and structural interchangeability.
- Closing excerpt
- Herein, the self-assembly, in vitro efficacy and in vivo pharmacokinetic and anti-tumor pharmacodynamics of these nanotubes in colorectal cancer models, comparing the potent topoisomerase inhibitor SN-38 with its clinically-used parent pro-drug irinotecan, is explored.
- Interpretation limits
- Verbatim excerpts from the authors’ abstract; the closing excerpt may describe a finding, limitation or recommendation. Design, population, effect size and uncertainty have not been independently extracted or appraised. Read the complete abstract and linked paper before interpreting the findings.
Read complete abstract (159 words)
Cyclic peptide-polymer conjugate nanotubes have been shown to be powerful drug delivery vectors, due to their propensity for dynamic self-assembly, high aspect ratio morphology and structural interchangeability. Building upon previous studies that demonstrate the shielding abilities of the polymeric corona of nanotubes to enhance pro-drug bond stabilities and modulate hydrolysis, here the concept of a hydrophobic core building block with multiple drug units to improve drug loading capacity and overall efficiency of the nanotube carriers is utilized. By leveraging the intermolecular features of the drug core to strengthen assembly, it is hypothesized that these nanotubes have the potential as a responsive supramolecular delivery system whereby upon full hydrolysis of the labile drug, these core forming interactions disappear, and nanotubes can fall apart and undergo clearance. Herein, the self-assembly, in vitro efficacy and in vivo pharmacokinetic and anti-tumor pharmacodynamics of these nanotubes in colorectal cancer models, comparing the potent topoisomerase inhibitor SN-38 with its clinically-used parent pro-drug irinotecan, is explored.
Abstract reproduced from the open-access article under the recorded cc by licence; © the authors. PMID 41070822 · DOI · PMC12836451
Key reviews and meta-analyses
The most cited review-type papers among PubMed’s best-match results for this heading, listed with bibliographic details only. Follow the links for the full text and access terms.
- Research article Irinotecan: 25 years of cancer treatment [5]
- Research article Individualization of Irinotecan Treatment: A Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics [6]
- Research article Antibody-drug conjugates targeting TROP-2 and incorporating SN-38: A case study of anti-TROP-2 sacituzumab govitecan [7]
- Research article Liposomal irinotecan (Onivyde): Exemplifying the benefits of nanotherapeutic drugs [8]
- Research article Intestinal bacterial β-glucuronidase as a possible predictive biomarker of irinotecan-induced diarrhea severity [9]
- Research article Liposomal Irinotecan: A Review in Metastatic Pancreatic Adenocarcinoma [10]
References
- Kciuk M, Marciniak B, Kontek R. Irinotecan-Still an Important Player in Cancer Chemotherapy: A Comprehensive Overview. . 2020. PMID 32664667 · DOI · PMC7404108
- Lu YJ, Lan YH, Chuang CC, Lu WT, Chan LY, Hsu PW, et al.. Injectable Thermo-Sensitive Chitosan Hydrogel Containing CPT-11-Loaded EGFR-Targeted Graphene Oxide and SLP2 shRNA for Localized Drug/Gene Delivery in Glioblastoma Therapy. . 2020. PMID 32993166 · DOI · PMC7583917
- Petreus T, Cadogan E, Hughes G, Smith A, Pilla Reddy V, Lau A, et al.. Tumour-on-chip microfluidic platform for assessment of drug pharmacokinetics and treatment response. . 2021. PMID 34429505 · DOI · PMC8385015
- Hill SK, Zeng M, Rajendrakumar SK, Dallmann R, Perrier S. Cyclic Peptide-Polymer Conjugate Nanotubes for Delivery of SN-38 in Treatment of Colorectal Cancer Model. . 2026. PMID 41070822 · DOI · PMC12836451
- Bailly C. Irinotecan: 25 years of cancer treatment. Pharmacol Res. 2019. PMID 31415916 · DOI
- de Man FM, Goey AKL, van Schaik RHN, Mathijssen RHJ, Bins S. Individualization of Irinotecan Treatment: A Review of Pharmacokinetics, Pharmacodynamics, and Pharmacogenetics. Clin Pharmacokinet. 2018. PMID 29520731 · DOI · PMC6132501
- Goldenberg DM, Sharkey RM. Antibody-drug conjugates targeting TROP-2 and incorporating SN-38: A case study of anti-TROP-2 sacituzumab govitecan. MAbs. 2019. PMID 31208270 · DOI · PMC6748572
- Milano G, Innocenti F, Minami H. Liposomal irinotecan (Onivyde): Exemplifying the benefits of nanotherapeutic drugs. Cancer Sci. 2022. PMID 35445479 · DOI · PMC9277406
- Chamseddine AN, Ducreux M, Armand JP, Paoletti X, Satar T, Paci A, et al.. Intestinal bacterial β-glucuronidase as a possible predictive biomarker of irinotecan-induced diarrhea severity. Pharmacol Ther. 2019. PMID 30831128 · DOI
- Frampton JE. Liposomal Irinotecan: A Review in Metastatic Pancreatic Adenocarcinoma. Drugs. 2020. PMID 32557396 · DOI · PMC7347682
About this article
- Sources
- NLM Medical Subject Headings (definition, synonyms); NCBI PubMed (counts, identifiers); Europe PMC (open-access abstracts and citation counts).
- Verification
- Every reference was resolved against PubMed on 2026-10-31; title, year and DOI matched.
- Review state
- automated source verified; no human expert review has been recorded yet.
- Version
- 1, last updated 2026-10-31.
See how EvidenceLib is built. Spotted an error? Email support@evidencehelix.com.
Evidence strength
EvidenceHelix's computed view of the study designs behind this topic: how common meta-analyses, randomized trials and reviews are, how recent the literature is, and a plain-language reading. It describes the design mix of the literature. It is not a quality appraisal of any study, and it is not medical advice.