ArticleThe AAPS journal2011
Evaluation of α2-integrin expression as a biomarker for tumor growth inhibition for the investigational integrin inhibitor E7820 in preclinical and clinical studies.
Article in The AAPS journal, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
13 citing papers in PubMed, 19 citations in OpenAlex.
- A phase I, dose escalation, pharmacodynamic, pharmacokinetic, and food-effect study of α2 integrin inhibitor E7820 in patients with advanced solid tumors.Investigational new drugs · 2016Trial
- Beyond DNA damage: 3D tumor models and the integrin mechanobiology of radioresistance.Journal of experimental & clinical cancer research : CR · 2026Review
- Focal adhesion in the tumour metastasis: from molecular mechanisms to therapeutic targets.Biomarker research · 2025Review
- Recent advances in anticancer mechanisms of molecular glue degraders: focus on RBM39-dgrading synthetic sulfonamide such as indisulam, E7820, tasisulam, and chloroquinoxaline sulfonamide.Genes & genomics · 2024Review
- Targeted Therapy for Highly Desmoplastic and Immunosuppressive Tumor Microenvironment of Pancreatic Ductal Adenocarcinoma.Cancers · 2024Review
- Role of integrin α2 in methotrexate-induced epithelial-mesenchymal transition in alveolar epithelial A549 cells.Toxicological research · 2022Article
- Article
- CAM-DR: Mechanisms, Roles and Clinical Application in Tumors.Frontiers in cell and developmental biology · 2021Review
- Antioxidant and anticancer activities of Trigonella foenum-graecum, Cassia acutifolia and Rhazya stricta.BMC complementary and alternative medicine · 2018Article
- Aggretin Venom Polypeptide as a Novel Anti-angiogenesis Agent by Targeting Integrin alpha2beta1.Scientific reports · 2017Article
- Population pharmacokinetic-pharmacodynamic modelling in oncology: a tool for predicting clinical response.British journal of clinical pharmacology · 2015Review
- Optimizing drug development of anti-cancer drugs in children using modelling and simulation.British journal of clinical pharmacology · 2013Review
- Emerging putative biomarkers: the role of alpha 2 and 6 integrins in susceptibility, treatment, and prognosis.Prostate cancer · 2012Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 6 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
E7820 is an orally active inhibitor of α(2)-integrin mRNA expression, currently tested in phases I and II. We aimed to evaluate what levels of inhibition of integrin expression are needed to achieve tumor stasis in mice, and to compare this to the level of inhibition achieved in humans. Tumor growth inhibition was measured in mice bearing a pancreatic KP-1 tumor, dosed at 12.5-200 mg/kg over 21 days. In the phase I study, E7820 was administered daily for 28 days over a range of 0-200 mg, followed by a 7-day washout period. PK-PD models were developed in NONMEM. α(2)-Integrin expression measured on platelets, corresponding to tumor stasis at t = 21 in 50% and 90% of the mice (I(int,50), I(int,90)) were calculated. It was evaluated if these levels of inhibition could be achieved in patients at tolerable doses. One hundred nineteen α(2)-Integrin measurements and 210 tumor size measurements were available from mice. The relationship between PK and α(2)-integrin expression was modeled using an indirect-effect model, subsequently linked to an exponential tumor growth model. I(inh,50) and I(inh,90) were 14.7% (RSE 7%) and 17.9% (RSE 8%). Four hundred sixty two α(2)-integrin measurements were available from 29 patients. Using the schedule of 100 mg qd (MTD), α(2)-integrin expression was inhibited more strongly than the I(int,50) and I(int,90) in greater than 95% and greater than 50% of patients, respectively. Moderate inhibition of α(2)-integrin expression corresponded to tumor stasis in mice, and similar levels could be reached in patients with the dose level of 100 mg qd.
Indexed as
Identifiers
What OpenQuestion holds
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.