C-kit controls blood-brain barrier permeability by regulating caveolae-mediated transcytosis after chronic cerebral hypoperfusion
This study provides evidence that C-kit is a key BBB permeability regulator through caveolae-mediated transcytosis in EC after CCH.PMID:38141279 | DOI:10.1016/j.biopha.2023.115778 (Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie)
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - December 23, 2023 Category: Drugs & Pharmacology Authors: Junkui Shang Wei Li Huiwen Zhang Wan Wang Ning Liu Dandan Gao Fengyu Wang Xi Yan Chenhao Gao Ruihua Sun Haohan Zhang Kai Ma Fengmin Shao Jiewen Zhang Source Type: research
Cancers, Vol. 16, Pages 90: NK3.3-Derived Extracellular Vesicles Penetrate and Selectively Kill Treatment-Resistant Tumor Cells
uth
Cancer treatments often become ineffective due to the development of tumor resistance, leading to metastasis and relapse. Treatments may also fail because of their inability to access cells deep within the tumor tissue. When this occurs, new therapeutic agents are needed. We previously reported that NK3.3EVs, extracellular vesicles (EVs) derived from the normal human natural killer (NK) cell line, NK3.3, have strong cytotoxic activity against leukemia and breast cancer cell lines, without harming normal cells. Here, we used a three-dimensional (3D) MCF7 breast cancer mammosphere model to reproduce a more physiologi...
Source: Cancers - December 23, 2023 Category: Cancer & Oncology Authors: Allyson McCune Jacki Kornbluth Tags: Article Source Type: research
Pharmacokinetic Interaction Between Imatinib and Metformin in Rats
ConclusionWith both single and multiple co-administration doses, metformin significantly changed the pharmacokinetic parameters of imatinib andN-desmethyl imatinib. The results suggest that care should be taken when metformin and imatinib are co-administered. (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - December 23, 2023 Category: Drugs & Pharmacology Source Type: research
Real-World Effectiveness of Dasatinib Versus Imatinib in Newly Diagnosed Patients With Chronic Myeloid Leukemia
CONCLUSIONS: Patients with CML-CP treated with 1L dasatinib achieved higher rates of, with shorter times to, MMR and DMR versus 1L imatinib. These clinically meaningful improvements were observed across subgroups.PMID:38135632 | DOI:10.1016/j.clml.2023.10.005 (Source: Clinical Lymphoma and Myeloma)
Source: Clinical Lymphoma and Myeloma - December 22, 2023 Category: Cancer & Oncology Authors: Andrew J Klink Scott J Keating John Brokars Bruce Feinberg Elias Jabbour Source Type: research
Identification of oral therapeutics using an AI platform against the virus responsible for COVID-19, SARS-CoV-2
Conclusion: This research underscores the potential of repurposing existing compounds for treating COVID-19. Our preliminary findings underscore the therapeutic promise of several compounds, notably Mebendazole, in both in vitro and in vivo settings against SARS-CoV-2. Several of the drugs explored, especially Mebendazole, are off-label medication; their cost-effectiveness position them as economical therapies against SARS-CoV-2. (Source: Frontiers in Pharmacology)
Source: Frontiers in Pharmacology - December 22, 2023 Category: Drugs & Pharmacology Source Type: research
Successful Prediction of Fetal Exposure to Dual BCRP/P-gp Drug Substrates Using the Efflux Ratio-Relative Expression Factor Approach and PBPK M & amp;S
Clin Pharmacol Ther. 2023 Dec 20. doi: 10.1002/cpt.3157. Online ahead of print.ABSTRACTTo inform fetal drug safety, it is important to determine or predict fetal drug exposure throughout pregnancy. The former is not possible in the 1st or 2nd trimester. In contrast, at the time of birth, fetal drug exposure, relative to maternal exposure, can be estimated as Kp,uu (unbound fetal umbilical venous [UV] plasma AUC/unbound maternal plasma [MP] AUC), provided the observed UV/MP values, spanning the dosing interval, are available from multiple maternal-fetal dyads. However, this fetal Kp,uu cannot be extrapolated to other drugs....
Source: Clinical Pharmacology and Therapeutics - December 21, 2023 Category: Drugs & Pharmacology Authors: Ankit Balhara Mengyue Yin Jashvant D Unadkat Source Type: research
Successful Prediction of Fetal Exposure to Dual BCRP/P-gp Drug Substrates Using the Efflux Ratio-Relative Expression Factor Approach and PBPK M & amp;S
Clin Pharmacol Ther. 2023 Dec 20. doi: 10.1002/cpt.3157. Online ahead of print.ABSTRACTTo inform fetal drug safety, it is important to determine or predict fetal drug exposure throughout pregnancy. The former is not possible in the 1st or 2nd trimester. In contrast, at the time of birth, fetal drug exposure, relative to maternal exposure, can be estimated as Kp,uu (unbound fetal umbilical venous [UV] plasma AUC/unbound maternal plasma [MP] AUC), provided the observed UV/MP values, spanning the dosing interval, are available from multiple maternal-fetal dyads. However, this fetal Kp,uu cannot be extrapolated to other drugs....
Source: Clinical Pharmacology and Therapeutics - December 21, 2023 Category: Drugs & Pharmacology Authors: Ankit Balhara Mengyue Yin Jashvant D Unadkat Source Type: research
Successful Prediction of Fetal Exposure to Dual BCRP/P-gp Drug Substrates Using the Efflux Ratio-Relative Expression Factor Approach and PBPK M & amp;S
Clin Pharmacol Ther. 2023 Dec 20. doi: 10.1002/cpt.3157. Online ahead of print.ABSTRACTTo inform fetal drug safety, it is important to determine or predict fetal drug exposure throughout pregnancy. The former is not possible in the 1st or 2nd trimester. In contrast, at the time of birth, fetal drug exposure, relative to maternal exposure, can be estimated as Kp,uu (unbound fetal umbilical venous [UV] plasma AUC/unbound maternal plasma [MP] AUC), provided the observed UV/MP values, spanning the dosing interval, are available from multiple maternal-fetal dyads. However, this fetal Kp,uu cannot be extrapolated to other drugs....
Source: Clinical Pharmacology and Therapeutics - December 21, 2023 Category: Drugs & Pharmacology Authors: Ankit Balhara Mengyue Yin Jashvant D Unadkat Source Type: research
The SNP rs460089 in the gene promoter of the drug transporter OCTN1 has prognostic value for treatment-free remission in chronic myeloid leukemia patients treated with imatinib
Leukemia, Published online: 21 December 2023; doi:10.1038/s41375-023-02109-2The SNP rs460089 in the gene promoter of the drug transporter OCTN1 has prognostic value for treatment-free remission in chronic myeloid leukemia patients treated with imatinib (Source: Leukemia)
Source: Leukemia - December 21, 2023 Category: Hematology Authors: Katerina Machova Polakova Ali Albeer Vaclava Polivkova Monika Krutska Katerina Vlcanova Nikola Curik Alice Fabarius Hana Klamova Birgit Spiess Cornelius F. Waller Tim H. Br ümmendorf Jolanta Dengler Volker Kunzmann Andreas Burchert Petra Belohlavkova Sat Source Type: research
Molecules, Vol. 29, Pages 67: An Efficient Synthesis of 1-(1,3-Dioxoisoindolin-2-yl)-3-aryl Urea Analogs as Anticancer and Antioxidant Agents: An Insight into Experimental and In Silico Studies
san
The present investigation reports the efficient multistep synthesis of 1-(1,3-dioxoisoindolin-2-yl)-3-aryl urea analogs (7a–f) in good yields. All the 1-(1,3-dioxoisoindolin-2-yl)-3-aryl urea analogs (7a–f) were characterized by spectroscopic techniques. Five among the six compounds were tested against 56 cancer cell lines at 10 µM as per the standard protocol. 1-(4-Bromophenyl)-3-(1,3-dioxoisoindolin-2-yl)urea (7c) exhibited moderate but significant anticancer activity against EKVX, CAKI-1, UACC-62, MCF7, LOX IMVI, and ACHN with percentage growth inhibitions (PGIs) of 75.4...
Source: Molecules - December 21, 2023 Category: Chemistry Authors: Obaid Afzal Mohamed Jawed Ahsan Tags: Article Source Type: research
Identification of common genes and pathways underlying imatinib and nilotinib treatment in CML: a Bioinformatics Study
Nucleosides Nucleotides Nucleic Acids. 2023 Dec 20:1-21. doi: 10.1080/15257770.2023.2296021. Online ahead of print.ABSTRACTImatinib (IMA) and nilotinib are the first and second generations of BCR-ABL tyrosine kinase inhibitors, which widely applied in chronic myeloid leukemia (CML) treatment. Here we aimed to provide new targets for CML treatment by transcriptome analysis. Microarray data GSE19567 was downloaded and analyzed from Gene Expression Omnibus (GEO) to identify common genes, which are downregulated or upregulated in K562-imatinib and K562-nilotinib treated cells. The differentially expressed genes (DEGs) were ass...
Source: Nucleosides, Nucleotides and Nucleic Acids - December 20, 2023 Category: Biochemistry Authors: Yalda Hekmatshoar Yalda Rahbar Saadat Tulin Ozkan Sureyya Bozkurt Aynur Karadag Gurel Source Type: research
Tyrosine Kinase Inhibitors in pediatric chronic myeloid leukemia: a focused review of clinical trials
Tyrosine Kinase Inhibitors (TKIs) is revolutionizing the management of pediatric Chronic Myeloid Leukemia (CML), offering alternatives to Allogeneic Hematopoietic Stem Cell Transplantation (AHSCT). We conducted a comprehensive review of 16 Randomized Controlled Trials (RCTs) encompassing 887 pediatric CML patients treated with TKIs including Imatinib, Dasatinib, and Nilotinib. The median patient age ranged from 6.5 to 14 years, with a median white blood cell count of 234 x 10^9/uL, median hemoglobin level of 9.05 g/dL, and median platelet count of 431.5 x 10^9/µL. Imatinib seems to be predominant first line TKI, with the ...
Source: Frontiers in Oncology - December 20, 2023 Category: Cancer & Oncology Source Type: research
Metabolic pseudoprogression in a patient with metastatic KIT exon 11 GIST after 1 month of first-line imatinib: a case report
ConclusionsThis report aims to highlight the existence of this metabolic pseudoprogression in GIST at the beginning of imatinib therapy in order to avoid early treatment discontinuation. Therefore, an early metabolic progression during a molecular targeted therapy always deserves to be evaluated in the context of the disease molecular profiling, and in case of a discordant finding between functional imaging and molecular background, a short-term longitudinal control should be suggested. (Source: Frontiers in Oncology)
Source: Frontiers in Oncology - December 20, 2023 Category: Cancer & Oncology Source Type: research
