Safety and clinical activity of the Notch inhibitor, crenigacestat (LY3039478), in an open-label phase I trial expansion cohort of advanced or metastatic adenoid cystic carcinoma

Conclusion The crenigacestat RP2D regimen induced manageable toxicity and limited clinical activity, without confirmed responses, in heavily pretreated patients with ACC.
Source: Investigational New Drugs - Category: Drugs & Pharmacology Source Type: research

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Cancer Biomark. 2021 Jul 20. doi: 10.3233/CBM-203043. Online ahead of print.ABSTRACTBy using a meta-analytical approach, this study aimed to analyse the diagnostic capacity of protein-based biomarkers in saliva for the differential diagnosis of oral potentially malignant disorders (OPMDs) and oral squamous cell carcinoma (OSCC) from healthy individuals as control group (HCG).Articles on protein-based biomarkers in saliva, which provided quantitative expression in individuals with clinical and histopathological diagnosis of OPMD or oral leukoplakia (OL) were considered eligible. Searches were conducted in eight electronic d...
Source: Cancer Biomarkers - Category: Cancer & Oncology Authors: Source Type: research
Eur J Pharmacol. 2021 Jul 29:174400. doi: 10.1016/j.ejphar.2021.174400. Online ahead of print.ABSTRACTOral squamous cellular carcinoma (OSCC) is considered a life-threatening disease with detection in late stages, which forces us to opt for dangerous treatment with a combination of chemotherapy and radiotherapy. Herbal components such as piperine and quercetin are derived from edible sources, proving their anticancer potential against oral cancer cells in vitro. Encapsulation into lipid matrix-mediated nanostructured lipid carriers (NLCs) can make both drugs bio-accessible. NLCs were synthesised using the high shear homoge...
Source: European Journal of Pharmacology - Category: Drugs & Pharmacology Authors: Source Type: research
Patterns of failure after treatment of oral and squamous cell carcinomas (OSCC) are diversified, with recurrences being one of the common causes. A special group of patients are sometimes encountered in the ou...
Source: BMC Cancer - Category: Cancer & Oncology Authors: Tags: Research article Source Type: research
Bioorg Chem. 2021 Jul 24;115:105205. doi: 10.1016/j.bioorg.2021.105205. Online ahead of print.ABSTRACTInhibiting the Dihydrofolate reductase (DHFR) enzyme has been validated in multiple clinical manifestations related to bacterial infection, malaria, and multiple types of cancer. Herein, novel series of 3-methyl-imidazo[2,1-b] thiazole-based analogs were synthesized and biologically evaluated for their in vitro inhibitory profile towards DHFR. Compounds 22 and 23 exhibited potent inhibitory profile targeting DHFR (IC50 0.079 and 0.085 µM, respectively comparable to MTX IC50 0.087 µM). Compounds 22 and 23 showed...
Source: Bioorganic Chemistry - Category: Chemistry Authors: Source Type: research
Mol Med Rep. 2021 Oct;24(4):685. doi: 10.3892/mmr.2021.12325. Epub 2021 Jul 30.ABSTRACTOral squamous cell carcinoma (OSCC) is a cancer associated with high mortality (accounting for 3.1/100,000 deaths per year in Brazil in 2013) and a high frequency of amplification in the expression of the epidermal growth factor receptor (EGFR). Treatment with the EGFR inhibitor cetuximab leads to drug resistance in patients with OSCC due to unknown mechanisms. Galectin‑3 (Gal‑3) is a β‑galactoside binding lectin that regulates multiple signaling pathways in cells. The present study aimed to investigate the effect of Gal‑3 i...
Source: Molecular Medicine Reports - Category: Molecular Biology Authors: Source Type: research
Oral Oncol. 2021 Jul 27;121:105451. doi: 10.1016/j.oraloncology.2021.105451. Online ahead of print.ABSTRACTOral cavity squamous cell carcinoma (OCSCC) is the most common malignancy of the oral cavity. The substantial risk factors for OCSCC are the consumption of tobacco products, alcohol, betel quid, areca nut, and genetic alteration. However, technological advancements have occurred in treatment, but the survival decreases with late diagnosis; therefore, new methods are continuously being investigated for treatment. In addition, the rate of secondary tumor formation is 3-7% yearly, which is incomparable to other malignanc...
Source: Cell Research - Category: Cytology Authors: Source Type: research
Bioorg Chem. 2021 Jul 24;115:105205. doi: 10.1016/j.bioorg.2021.105205. Online ahead of print.ABSTRACTInhibiting the Dihydrofolate reductase (DHFR) enzyme has been validated in multiple clinical manifestations related to bacterial infection, malaria, and multiple types of cancer. Herein, novel series of 3-methyl-imidazo[2,1-b] thiazole-based analogs were synthesized and biologically evaluated for their in vitro inhibitory profile towards DHFR. Compounds 22 and 23 exhibited potent inhibitory profile targeting DHFR (IC50 0.079 and 0.085 µM, respectively comparable to MTX IC50 0.087 µM). Compounds 22 and 23 showed...
Source: Bioorganic Chemistry - Category: Chemistry Authors: Source Type: research
Mol Med Rep. 2021 Oct;24(4):685. doi: 10.3892/mmr.2021.12325. Epub 2021 Jul 30.ABSTRACTOral squamous cell carcinoma (OSCC) is a cancer associated with high mortality (accounting for 3.1/100,000 deaths per year in Brazil in 2013) and a high frequency of amplification in the expression of the epidermal growth factor receptor (EGFR). Treatment with the EGFR inhibitor cetuximab leads to drug resistance in patients with OSCC due to unknown mechanisms. Galectin‑3 (Gal‑3) is a β‑galactoside binding lectin that regulates multiple signaling pathways in cells. The present study aimed to investigate the effect of Gal‑3 i...
Source: Molecular Medicine Reports - Category: Molecular Biology Authors: Source Type: research
Utilizing digital pathology algorithms for the objective quantification of immunohistochemical staining, this study aimed to identify robust prognostic biomarkers for oral cancer. Tissue microarrays with specimens of a large cohort of oral squamous cell carcinoma (n=222) were immunohistochemically stained to determine the expression of PD-L1, EGFR, and COX-2 and the amount of infiltrating NK cells and CD8-positive T cells. Immunoreactivity scores were assessed using both a classical manual scoring procedure and a digital semi-automatic approach using QuPath. Digital scoring was successful in quantifying the expression leve...
Source: Frontiers in Oncology - Category: Cancer & Oncology Source Type: research
Clin Cancer Res. 2021 Jul 27:clincanres.1061.2021. doi: 10.1158/1078-0432.CCR-21-1061. Online ahead of print.ABSTRACTPURPOSE: The role of chemotherapy in adenoid cystic carcinoma (ACC) is controversial because ACC is usually stable without chemotherapy and lack of randomized trials. Here, we conducted the first randomized trial to evaluate the efficacy of axitinib as compared to observation in ACC.PATIENTS AND METHODS: In this multicenter, prospective phase II trial, we enrolled patients with recurrent or metastatic ACC whose cancer had progressed within the past 9 months. Patients were randomly assigned to either axitinib...
Source: Clinical Lung Cancer - Category: Cancer & Oncology Authors: Source Type: research
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