ArticleInvestigational new drugs2012
A phase I study of continuous infusion cilengitide in patients with solid tumors.
Article in Investigational new drugs, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 30 citations in OpenAlex.
- Serum C-Telopeptide Collagen Crosslinks and Plasma Soluble VEGFR2 as Pharmacodynamic Biomarkers in a Trial of Sequentially Administered Sunitinib and Cilengitide.Clinical cancer research : an official journal of the American Association for Cancer Research · 2015Trial
- Allosteric regulation of fibronectin binding by the anti-β1 integrin antibody TS2/16.PNAS nexus · 2026Article
- Unlocking Lung Cancer Cell Dormancy: An Epigenetic Perspective.International journal of molecular sciences · 2025Review
- Switching Roles─Exploring Concentration-Dependent Agonistic versus Antagonistic Behavior of Integrin Ligands.Journal of medicinal chemistry · 2025Article
- Cilengitide sensitivity is predicted by overall integrin expression in breast cancer.Breast cancer research : BCR · 2024Article
- Review
- Targeting TGFβ signal transduction for cancer therapy.Signal transduction and targeted therapy · 2021Review
- Modulating Tumor Cell Functions by Tunable Nanopatterned Ligand Presentation.Nanomaterials (Basel, Switzerland) · 2020Review
- Cell Adhesion Molecules and Their Roles and Regulation in the Immune and Tumor Microenvironment.Frontiers in immunology · 2019Review
- Integrins as Therapeutic Targets: Successes and Cancers.Cancers · 2017Review
- In vitro and in vivo drug disposition of cilengitide in animals and human.Pharmacology research & perspectives · 2016Article
- Insulin-like growth factor binding protein-3 inhibits cell adhesion via suppression of integrin β4 expression.Oncotarget · 2015Article
- Iodine-125-labeled cRGD-gold nanoparticles as tumor-targeted radiosensitizer and imaging agent.Nanoscale research letters · 2015Article
- Article
- Cilengitide inhibits attachment and invasion of malignant pleural mesothelioma cells through antagonism of integrins αvβ3 and αvβ5.PloS one · 2014Article
- Combating resistance to anti-IGFR antibody by targeting the integrin β3-Src pathway.Journal of the National Cancer Institute · 2013Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
backgroundCilengitide (EMD121974) is a cyclized pentapeptide that is a potent and selective integrin antagonist which has shown activity in malignant gliomas. In all previous studies, cilengitide has been administered in an intermittent fashion. However, cilengitide has a short half-life of 3-5 h with no evidence of drug accumulation. These data prompted the initiation of this phase I study of continuous infusion cilengitide.
methodsCilengitide was administered as a continuous infusion without break in 4-week cycles. Plasma samples for pharmacokinetic studies were obtained weekly in cycle 1 immediately prior to and 2 h after infusion bag change.
resultsThirty-five patients were treated (median age 56; 23 males) at dose levels of 1, 2, 4, 8, 12, 18, 27, and 40 mg/h. Toxicities were limited to grade ≤ 2 and showed no relation to dose. Fatigue was most common (17%), while all other toxicities were reported in <10% of patients. No dose-limiting toxicities were observed, and therefore the maximum tolerated dose was not reached. Pharmacokinetic analysis showed that values for clearance and volume of distribution were comparable across dose levels, and the steady-state concentration increased proportionally with dose.
conclusionsCilengitide can be safely administered as a continuous infusion at doses up to at least 40 mg/h, which represents the maximum feasible dose due to drug solubility and delivery limitations. The pharmacokinetics of continuous infusion cilengitide are linear and consistent with the results obtained using a twice weekly infusion.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.