Results 1 to 10 of about 425,696 (264)

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

open access: yesMolecules, 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   +3 more
doaj   +2 more sources

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

open access: yesMolecules, 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   +2 more sources

Evaluation of Violacein Metabolic Stability and Metabolite Identification in Human, Mouse, and Rat Liver Microsomes [PDF]

open access: yesPharmaceutics
Background: Malaria significantly impacts the health of populations living in poverty and vulnerable conditions. Resistance to current antimalarial drugs remains a major challenge and highlights the urgent need for novel, effective, and safer therapies ...
Debora Bressanim de Aquino Calemi   +8 more
doaj   +2 more sources

Metabolic Stability and Metabolite Identification of N-Ethyl Pentedrone Using Rat, Mouse and Human Liver Microsomes [PDF]

open access: yesPharmaceutics
New Psychoactive Substances (NPSs) are defined as a group of substances produced from molecular modifications of traditional drugs. These molecules represent a public health problem since information about their metabolites and toxicity is poorly ...
Alexandre Barcia Godoi   +5 more
doaj   +2 more sources

Assessment of the in vitro metabolic stability of CEP-37440, a selective FAK/ALK inhibitor, in HLMs using fast UPLC–MS/MS method: in silico metabolic lability and DEREK alerts screening [PDF]

open access: yesFrontiers in Chemistry
IntroductionCEP-37440 was synthesized and supplied by the research and development division of Teva Branded Pharmaceutical Products (West Chester, PA, United States). CEP-37440 represents a newly developed compound that exhibits selectivity inhibition of
Mohamed W. Attwa   +3 more
doaj   +2 more sources

CYP2C9 mediates the herb-drug interaction of curcumin with naproxen in rats [PDF]

open access: yesActa Poloniae Pharmaceutica, 2023
Both curcumin and naproxen possess the activity of pain relief, which makes it possible to co-administrate these drugs in the same prescription. This study aimed to assess the potential pharmacokinetic interaction of naproxen with curcumin in rats ...
Yongjun Qiu, Sujun Huang, Minfang Zhu
doaj   +1 more source

Characterization of the metabolism of eupalinolide A and B by carboxylesterase and cytochrome P450 in human liver microsomes

open access: yesFrontiers in Pharmacology, 2023
Eupalinolide A (EA; Z-configuration) and eupalinolide B (EB; E-configuration) are bioactive cis-trans isomers isolated from Eupatorii Lindleyani Herba that exert anti-inflammatory and antitumor effects.
Yingzi Li   +8 more
doaj   +1 more source

Evaluation of Alectinib Metabolic Stability in HLMs Using Fast LC-MS/MS Method: In Silico ADME Profile, P450 Metabolic Lability, and Toxic Alerts Screening

open access: yesPharmaceutics, 2023
Alectinib, also known as Alecensa®, is prescribed for the therapeutic treatment of individuals diagnosed with metastatic non-small cell lung cancer (NSCLC) who have a specific genetic mutation referred to as anaplastic lymphoma kinase (ALK) positivity ...
Mohamed W. Attwa   +3 more
doaj   +1 more source

Metabolite Identification of a Novel Anti-Leishmanial Agent OJT007 in Rat Liver Microsomes Using LC-MS/MS

open access: yesMolecules, 2022
The purpose of this study was to identify potential metabolic pathways and metabolites of OJT007, a methionine aminopeptidase 1 (MetAP1) inhibitor. OJT007 is a novel drug with potent antiproliferative effects against Leishmania Major.
Maria Eugenia Rincon Nigro   +6 more
doaj   +1 more source

Assessment of In Silico and In Vitro Selpercatinib Metabolic Stability in Human Liver Microsomes Using a Validated LC-MS/MS Method

open access: yesMolecules, 2023
Selpercatinib (SLP; brand name Retevmo®) is a selective and potent RE arranged during transfection (RET) inhibitor. On 21 September 2022, the FDA granted regular approval to SLP (Retevmo, Eli Lilly, and Company).
Mohamed W. Attwa   +4 more
doaj   +1 more source

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