Results 11 to 20 of about 103,612 (260)

A Sensitive, Green, and Fast LC–MS/MS Analytical Method for the Quantification of Ribociclib: Evaluation of the Metabolic Stability in HLMs

Separations, 2023
Ribociclib (Kisqali®) is a pharmacological agent that has great selectivity as a cyclin-dependent kinase 4/6 inhibitor. It has received regulatory approval for its application in the treatment of breast cancer.
Mohamed W. Attwa, Ali S. Abdelhameed, Adnan A. Kadi   +2 more
doaj   +1 more source

A Fast LC-MS/MS Methodology for Estimating Savolitinib in Human Liver Microsomes: Assessment of Metabolic Stability Using In Vitro Metabolic Incubation and In Silico Software Analysis

Separations, 2023
Savolitinib (Orpathys®), was developed by (HUTCHMED (Shanghai, China) and, AstraZeneca (Gaithersburg, Maryland, USA), is an inhibitor of the c-Met receptor tyrosine kinase that is orally bioavailable.
Mohamed W. Attwa, Haitham AlRabiah, Ali S. Abdelhameed, Adnan A. Kadi   +3 more
doaj   +1 more source

A Rapid and Sensitive UPLC-MS/MS Method for Quantifying Capmatinib in Human Liver Microsomes: Evaluation of Metabolic Stability by In Silico and In Vitro Analysis

Separations, 2023
Capmatinib (CMB) is an orally bioavailable mesenchymal–epithelial transition (MET) inhibitor approved by the US-FDA to treat metastatic non-small cell lung cancer (NSCLC) patients, with MET exon 14 skipping mutation.
Mohamed W. Attwa, Ali S. Abdelhameed, Aishah M. Alsibaee, Adnan A. Kadi   +3 more
doaj   +1 more source

Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs. [PDF]

PLoS ONE, 2018
Two chemotypes were examined in vitro with CYPs 3A4 and 2C19 by molecular docking, metabolic profiles, and intrinsic clearance deuterium isotope effects with specifically deuterated form to assess the potential for enhancement of pharmacokinetic ...
Hao Sun, David W Piotrowski, Suvi T M Orr, Joseph S Warmus, Angela C Wolford, Steven B Coffey, Kentaro Futatsugi, Yinsheng Zhang, Alfin D N Vaz   +8 more
doaj   +1 more source

Development of a Fast and Sensitive UPLC–MS/MS Analytical Methodology for Fenebrutinib Estimation in Human Liver Microsomes: In Vitro and In Silico Metabolic Stability Evaluation

Separations, 2023
Fenebrutinib (GDC-0853; FNB) is an oral small molecule that was developed by Roche Pharmaceuticals to slow multiple sclerosis progression. FNB is a reversible bruton tyrosine kinase (BTK) inhibitor, which showed the maximum potency of BTK inhibitors in ...
Mohamed W. Attwa, Aishah M. Alsibaee, Haya I. Aljohar, Ali S. Abdelhameed, Adnan A. Kadi   +4 more
doaj   +1 more source

A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation [PDF]

Royal Society Open Science, 2019
Spebrutinib (SBT) is a Bruton's tyrosine kinase inhibitor. SBT is currently in phase II and phase I clinical trials for the management of rheumatoid arthritis and chronic lymphocytic leukaemia, respectively.
Ali S. Abdelhameed, Mohamed W. Attwa, Nasser S. Al-Shaklia, Adnan A. Kadi   +3 more
doaj   +1 more source

An UPLC–ESI–MS/MS Bioanalytical Methodology for the Quantification of Gilteritinib in Human Liver Microsomes: Application to In Vitro and In Silico Metabolic Stability Estimation

Separations, 2023
Gilteritinib (Xospata®) is a tyrosine kinase inhibitor (TKI) that works by inhibiting numerous receptor tyrosine kinases, involving AXL and FMS-like tyrosine kinase 3 (FLT3).
Mohamed W. Attwa, Haitham AlRabiah, Aishah M. Alsibaee, Ali S. Abdelhameed, Adnan A. Kadi   +4 more
doaj   +1 more source

Rapid LC-MS/MS Bosutinib Quantification with Applications in Metabolic Stability Estimation

Molecules, 2023
Bosutinib (BOS) is FDA approved drug for the treatment of chronic phase (CP) Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML).
Mohamed W. Attwa, Mohammed M. Alanazi
doaj   +1 more source

Development and Validation of a Rapid LC-MS/MS Method for Quantifying Alvocidib: In Silico and In Vitro Metabolic Stability Estimation in Human Liver Microsomes

Molecules, 2023
Alvocidib (AVC; flavopiridol) is a potent cyclin-dependent kinase inhibitor used in patients with acute myeloid leukemia (AML). The FDA has approved orphan drug designation to AVC for treating patients with AML.
Mohamed W. Attwa, Haitham AlRabiah, Adnan A. Kadi   +2 more
doaj   +1 more source

Intrinsic Clearance Assay Incubational Binding: A Method Comparison [PDF]

Drug Metabolism and Disposition, 2017
The fraction of unbound drug (fuinc) in in vitro intrinsic clearance (CLint) incubation is an important parameter in the pursuit of accurate clearance predictions and is often predicted using algorithms based on drug lipophilicity measures. However, analysis of an AstraZeneca database suggests that simple lipophilicity alone is a relatively poor ...
Sofia, Chen, Luna, Prieto Garcia, Fredrik, Bergström, Pär, Nordell, Ken, Grime   +4 more
openaire   +2 more sources