Results 51 to 60 of about 53,097 (209)

Pharmacokinetic profiling of imatinib in relation to CYP3A4 activity in leukaemia patients

British Journal of Clinical Pharmacology, EarlyView.
Aim Imatinib pharmacokinetics exhibit large interindividual variability because of differences in CYP3A4 activity—the main imatinib‐metabolizing enzyme. While therapeutic drug monitoring is effective, it requires steady‐state conditions and frequent sampling.
Anna Sofie Buhl Rasmussen, Mathilde Rønne Koch, Cecilie Utke Rank, Christen Lykkegaard Andersen, Allan Weimann, Maria Thastrup, Tianwu Yang, Trine Meldgaard Lund, Ib Jarle Christensen, Flemming Nielsen, Tore Bjerregaard Stage, Sara Bisgaard Jensen, Mette Klarskov Andersen, Kjeld Schmiegelow, Kim Dalhoff   +14 more
wiley   +1 more source

The effect of mild and moderate hepatic impairment on the pharmacokinetics, safety and tolerability of balcinrenone

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aim Balcinrenone (previously AZD9977) is a novel selective non‐steroidal mineralocorticoid receptor antagonist (MRA) with a differential mechanism of action relative to approved MRAs. The aim of this trial was to assess the pharmacokinetics, safety and tolerability of balcinrenone in participants with mild and moderate hepatic impairment ...
Anna L. Eriksson, Deeyen Karsanji, Bonifride Tuyishimire, Joanna Parkinson, Maria Heijer, Tadeusz Pawlik, Judith Hartleib‐Geschwindner, Maria Leonsson‐Zachrisson, Hans Ericsson   +8 more
wiley   +1 more source

Imatinib and hypophosphatemia: Case report and review of literature

Journal of Oncological Sciences, 2017
Imatinib mesylate is a potent inhibitor of the BCR-Abl kinases, c-Kit, PDGFR, and fms. Imatinib used for treatment of chronic myeloid leukemia and gastrointestinal stromal tumor. Imatinib has been well tolerated.
Erdem Şen, İrem Öner, Özlem Ata
doaj   +1 more source

A Study of the Identification, Fragmentation Mode and Metabolic Pathways of Imatinib in Rats Using UHPLC-Q-TOF-MS/MS

Journal of Analytical Methods in Chemistry, 2021
In this study, The metabolites, metabolic pathways, and metabolic fragmentation mode of a tyrosine kinase inhibitor- (TKI-) imatinib in rats were investigated.
Sijiang Liu, Zhaojin Yu
doaj   +1 more source

Control of Gemcitabine Activity With Blue and Red Light

Chemistry – A European Journal, EarlyView.
Treating cancer with chemotherapy is generally associated with many side effects, which can be addressed by selectively releasing the desired drugs with visible light. Sixteen new blue light‐activatable cytostatics were introduced, with the gemcitabine derivative exhibiting ideal properties.
Nils F. Kersten, Konstantin L. Stock, Marius Hyprath, Hannah Weisser, Timo Weinrich, Dieter Steinhilber, Alexander Heckel   +6 more
wiley   +1 more source

Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib

Clinical Pharmacology &Therapeutics, EarlyView.
Repurposing drugs whose clinical safety has been established offers a valuable approach to reduce the cost and time associated with the development of new drugs for malaria. Here, we investigate the potential to repurpose the anticancer kinase inhibitor berzosertib for the treatment of malaria, by assessing whether a predicted efficacious human dose ...
Devasha Redhi, Mwila Mulubwa, Mmakwena M. Mmonwa, Mathew Njoroge, Liezl Krugmann, Kelly Chibale   +5 more
wiley   +1 more source

The role of mutation testing in patients with chronic myeloid leukemia in chronic phase after imatinib failure and their outcomes after treatment modification: Single-institutional experience over 13 years

Indian Journal of Medical and Paediatric Oncology, 2017
Introduction: BCR-ABL1 kinase domain mutations represent the most frequent mechanism of resistance to tyrosine kinase inhibitor (TKI) therapy, being detected in 40%–50% of imatinib-resistant patients with chronic myeloid leukemia in chronic phase (CML-CP)
Puligundla Krishna Chaitanya, Karnam Ashok Kumar, Bala Stalin, Gundeti Sadashivudu, Maddali Lakshmi Srinivas   +4 more
doaj   +1 more source

Chronic myeloid leukemia patients sensitive and resistant to imatinib treatment show different metabolic responses. [PDF]

PLoS ONE, 2010
The BCR-ABL tyrosine kinase inhibitor imatinib is highly effective for chronic myeloid leukemia (CML). However, some patients gradually develop resistance to imatinib, resulting in therapeutic failure.
Jiye A, Sixuan Qian, Guangji Wang, Bei Yan, Sujiang Zhang, Qing Huang, Lingna Ni, Weibin Zha, Linsheng Liu, Bei Cao, Ming Hong, Hanxin Wu, Hua Lu, Jian Shi, Mengjie Li, Jianyong Li   +15 more
doaj   +1 more source

Characterization of Lysosomal Hydrolases and Transporters and Their Age‐Dependent Variability: Relevance to Drug Metabolism and Transport of Small Molecule and Biologic Drugs

Clinical Pharmacology &Therapeutics, EarlyView.
Lysosomes play a key role in the accumulation, catabolism, and transport of endogenous and exogenous metabolites and proteins and are involved in drug metabolism and prodrug activation. However, the protein abundance and interindividual variability of lysosomal drug‐metabolizing enzymes and transporters (DMETs) remain underexplored.
Darshak Gadara, Dilip Kumar Singh, Sandhya Subash, Guihua Yue, Deepak Ahire, Chris Bohl, Maciej Czerwinski, Stephanie Helmstetter, Scott Heyward, Robert S. Jones, Cyrus Khojasteh, Ryota Kikuchi, Priyanka Kulkarni, Bin Ma, Bernard Murray, Chris Seib, Bill Smith, David M. Stresser, Mitchell E. Taub, Ting Wang, Bhagwat Prasad   +20 more
wiley   +1 more source

Maternal and Neonatal Complications Associated with Breast Cancer Systemic Treatments—A VigiBase Disproportionality Analysis Study

Clinical Pharmacology &Therapeutics, EarlyView.
Pregnancy‐associated breast cancer (PrBC) presents therapeutic challenges. Understanding maternal–fetal safety of systemic anticancer therapies is critical. We performed a case/non‐case disproportionality analysis using the WHO global pharmacovigilance database up to January 2024, to evaluate maternal–fetal outcomes associated with breast cancer (BC ...
Rayan Kabirian, Floriane Jochum, Elise Dumas, Florence Coussy, Kevin Bihan, Bénédicte Lebrun‐Vignes, Barbara Pistilli, Marc‐Antoine Benderra, Lise Selleret, Laurent Chouchana, Fabien Reyal, Anne‐Sophie Hamy, Paul Gougis   +12 more
wiley   +1 more source