Results 11 to 20 of about 423,855 (249)

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

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

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

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

An Ultrafast UPLC–MS/MS Method for Characterizing the In Vitro Metabolic Stability of Acalabrutinib

Molecules, 2023
Acalabrutinib, commercially known as Calquence®, is a pharmacological molecule that has robust inhibitory activity against Bruton tyrosine kinase. The medicine in question was carefully developed by the esteemed pharmaceutical company AstraZeneca.
Mohamed W. Attwa, Ahmed H. Bakheit, Ali S. Abdelhameed, Adnan A. Kadi   +3 more
doaj   +1 more source

Selection of bispecific antibodies with optimal developability using FcRn‑pH‑HPLC as an optimized FcRn affinity chromatography method

mAbs, 2023
A challenge when developing therapeutic antibodies is the identification of candidates with favorable pharmacokinetics (PK) early in development. A key determinant of immunoglobulin (IgG) serum half‑life in vivo is the efficiency of pH-dependent binding ...
Thomas Müller, Carolin Tasser, Michael Tesar, Ivica Fucek, Ute Schniegler-Mattox, Joachim Koch, Kristina Ellwanger   +6 more
doaj   +1 more source

Single daily dosing of antibiotics: importance of in vitro killing rate, serum half-life, and protein binding [PDF]

Antimicrobial Agents and Chemotherapy, 1991
The relative importance of pharmacokinetic and pharmacodynamic parameters for the feasibility of a single daily dose (SDD) of antibiotics remains to be established. Therefore, we studied the relationship between in vitro bacteriological parameters (MIC, MBC, and killing rate [KR], defined as the reduction in the inoculum within 3 h), pharmacokinetic ...
G, Potel, N P, Chau, B, Pangon, B, Fantin, J M, Vallois, F, Faurisson, C, Carbon   +6 more
openaire   +2 more sources

Effects of Flow Hydrodynamics and Eye Movements on Intraocular Drug Clearance

Pharmaceutics, 2022
New in vitro prototypes (PK-Eye™) were tested with and without eye movement to understand diffusion and convection effects on intraocular clearance. Port placement in front ((i) ciliary inflow model) and behind the model lens ((ii) posterior inflow model)
Angeliki Velentza-Almpani, Nkiruka Ibeanu, Tianyang Liu, Christopher Redhead, Peng Tee Khaw, Steve Brocchini, Sahar Awwad, Yann Bouremel   +7 more
doaj   +1 more source

QSPR modelling ofin vitrodegradation half-life of acyl glucuronides

Xenobiotica, 2018
Acyl glucuronidation is an important Phase II biotransformation, which is an efficient detoxification mechanism for the metabolism of carboxylic acid group-containing drugs. However, the reactivity of acyl glucuronide (AG) metabolites associated with short half-lives may be an indication of idiosyncratic drug toxicity.The degradation half-lives of AGs ...
Gulcin Tugcu, Hande Sipahi
openaire   +2 more sources

Control of c-myc mRNA half-life in vitro by a protein capable of binding to a coding region stability determinant. [PDF]

Genes & Development, 1992
Polysome-associated c-myc mRNA is degraded relatively rapidly in cells and in an in vitro mRNA decay system containing extracts from cultured mammalian cells. Using this system, a competition/screening assay was devised to search for factors that bind to specific regions of polysome-associated c-myc mRNA and thereby alter its half-life.
P L, Bernstein, D J, Herrick, R D, Prokipcak, J, Ross   +3 more
openaire   +2 more sources