Results 81 to 90 of about 192,321 (311)

Utility of in vitro systems and preclinical data for the prediction of human intestinal first-pass metabolism during drug discovery and preclinical development [PDF]

, 2013
A growing awareness of the risks associated with extensive intestinal metabolism has triggered an interest in developing robust methods for its quantitative assessment.
Karlsson, Fredrik, Bouchene, Salim, Hilgendorf, Constanze,, Dolgos, Hugues, Karlsson, Fredrik,, Dolgos, Hugues,, Hilgendorf, Constanze, Peters, Sheila Annie, Bouchene, Salim,, Peters, Sheila Annie,   +9 more
core   +1 more source

Mechanism-based Preclinical Approaches for the Evaluation of Drug-Drug Interactions.

Drug Metabolism and Pharmacokinetics, 2000
Pharmacokinetic drug-drug interactions (PDDI), in which the pharmacokinetic clearance of one drug is altered by a co-administered drug, can be divided mechanistically into two general categories: 1. inhibitory PDDI, the inhibition of the metabolic clearance of one drug by a co-administered drug; and 2.
openaire   +2 more sources

Proteasome inhibitor, ixazomib prevents topoisomerase‐I degradation and reverses irinotecan resistance in colorectal cancer

Molecular Oncology, EarlyView.
Ixazomib inhibits proteasome‐mediated degradation of topoisomerase I induced by irinotecan, thereby restoring drug sensitivity and promoting tumor cell death in colorectal cancer. Irinotecan, a topoisomerase I (topoI) inhibitor, is widely used for colorectal cancer, but resistance remains a major clinical challenge.
Yuho Ebata, Koji Ando, Hirofumi Hasuda, Koshi Mimori, Elizabeth C. Unan, Siddhartha Pulukuri, Aahana Tiku, Allison Berger, Eiji Oki, Ajit Bharti, Tomoharu Yoshizumi   +10 more
wiley   +1 more source

In vitro studies and in vivo evaluation of novel diamidines for 2nd stage sleeping sickness [PDF]

, 2014
Summary: African sleeping sickness is one of the most neglected tropical diseases. Transmitted by the tsetse fly it exclusively occurs in sub-Saharan Africa.
Wenzler, Tanja
core   +1 more source

Preclinical Models of Restenosis and Their Application in the Evaluation of Drug-Eluting Stent Systems [PDF]

Veterinary Pathology, 2009
Coronary arterial disease (CAD) is the leading cause of death in the United States, the European Union, and Canada. Percutaneous coronary intervention (PCI) has revolutionized the treatment of CAD, and it is the advent of drug-eluting stent (DES) systems that has effectively allayed much of the challenge of restenosis that has plagued the success of ...
openaire   +2 more sources

Stimulator of interferon genes agonist augmented antitumor immunity of osimertinib in Egfr‐mutated lung cancer

Molecular Oncology, EarlyView.
Combining osimertinib with the STING agonist ADU‐S100 activates innate and adaptive immunity to overcome the non‐inflamed microenvironment of Egfr‐mutant lung cancer. This combination increases NK and CD8+ T‐cell infiltration, associated with activation of the STING‐IRF3 pathway and local immunogenic cell death.
Jun Nishimura, Tadahiro Kuribayashi, Johannes Brägelmann, Sachi Okawa, Masataka Taoka, Shunta Mori, Tomoka Nishimura, Takaaki Tanaka, Go Makimoto, Kiichiro Ninomiya, Kammei Rai, Eiki Ichihara, Ryohei Katayama, Katsuyuki Hotta, Masahiro Tabata, Yosuke Togashi, Yoshinobu Maeda, Martin L. Sos, Katsuyuki Kiura, Kadoaki Ohashi   +19 more
wiley   +1 more source

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

The role of the anaesthetised guinea-pig in the preclinical cardiac safety evaluation of drug candidate compounds [PDF]

, 2012
Despite rigorous preclinical and clinical safety evaluation, adverse cardiac effects remain a leading cause of drug attrition and post-approval drug withdrawal. A number of cardiovascular screens exist within preclinical development. These screens do not,
Borland, Samantha, Kirk, Sarah, Skinner, Matthew, Borland, Samantha; id_orcid, Philp, Karen, Ewart, Lorna, Valentin, Jean-Pierre, Marks, Louise, Lainée, Pierre   +8 more
core   +1 more source

Epigenetic heterogeneity and plasticity in therapy‐induced tumor states through single‐cell multi‐omics

Molecular Oncology, EarlyView.
Single‐cell multi‐omics reveals epigenetic heterogeneity across therapy‐adaptive tumor states, including quiescent/dormant, drug‐tolerant persister, and EMT‐like phenotypes. By linking regulatory features with state‐associated biomarkers, these approaches inform biomarker‐guided therapeutic strategies for evolving tumors.
Hee Jung Kim, Hwiyeong Lee, Jin Hong, Daechan Park   +3 more
wiley   +1 more source

First-generation and preclinical evaluation of an EphA5-targeted antibody-drug conjugate in solid tumors [PDF]

Contemporary cancer treatment strategies are shifting toward targeted therapies to improve efficacy and minimize toxicity. Here, we report the design and preclinical evaluation of MBRC-101, a first-in-class antibody-drug conjugate (ADC) targeting EphA5 ...
Christopher Markosian, Stephen C. Alley, Ethan R. Chen, Kirstin F. Barnhart, Renata Pasqualini, Yongjian Wu, Wadih Arap, Isan Chen, Fenny H.F. Tang, Sun-Young Kim, Daniela I. Staquicini, Fernanda I. Staquicini, Vanessa de Oliveira, J. Kellogg Parsons   +13 more
core   +1 more source