Crizotinib is an oral tyrosine kinase inhibitor approved for treating patients with non-small cell lung cancer (NSCLC) containing an anaplastic lymphoma kinase (ALK) rearrangement. We used knockout mice to study the roles of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) in plasma pharmacokinetics and brain accumulation of oral crizotinib, and the feasibility of improving crizotinib kinetics using coadministration of the dual ABCB1/ABCG2 inhibitor elacridar. In vitro, crizotinib was a good transport substrate of human ABCB1, but not of human ABCG2 or murine Abcg2. With low-dose oral crizotinib (5 mg/kg), Abcb1a/1b(-/-) and Abcb1a/1b;Abcg2(-/-) mice had an approximately twofold higher plasma AUC than wild-type mice, and ...
BACKGROUND AND PURPOSE: Pralsetinib is an FDA-approved oral small-molecule inhibitor for treatment o...
Mitogen/extracellular signal-regulated kinase (MEK) inhibitors have been tested in clinical trials f...
Vemurafenib (PLX4032) is a novel tyrosine kinase inhibitor that has clinical efficacy against metast...
Contains fulltext : 138290.pdf (Publisher’s version ) (Closed access)Crizotinib is...
Tyrosine kinase inhibitors (TKIs) are small molecule inhibitors that selectively interfere with the ...
We aimed to clarify the roles of the multidrug transporters ABCB1 and ABCG2 in oral availability and...
Brigatinib is an FDA-approved oral anaplastic lymphoma kinase (ALK) inhibitor for treatment of metas...
P-Glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) are two efflux transporters at t...
Lorlatinib (PF-06463922) is a promising oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor cur...
Sotorasib (Lumakras™) is the first FDA-approved KRASG12C inhibitor for treatment of patients with no...
Ponatinib is an oral BCR-ABL1 inhibitor for treatment of advanced leukemic diseases that carry the P...
EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth fac...
Lorlatinib, a novel generation oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor with high me...
Quizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acu...
BACKGROUND AND PURPOSE: Pralsetinib is an FDA-approved oral small-molecule inhibitor for treatment o...
Mitogen/extracellular signal-regulated kinase (MEK) inhibitors have been tested in clinical trials f...
Vemurafenib (PLX4032) is a novel tyrosine kinase inhibitor that has clinical efficacy against metast...
Contains fulltext : 138290.pdf (Publisher’s version ) (Closed access)Crizotinib is...
Tyrosine kinase inhibitors (TKIs) are small molecule inhibitors that selectively interfere with the ...
We aimed to clarify the roles of the multidrug transporters ABCB1 and ABCG2 in oral availability and...
Brigatinib is an FDA-approved oral anaplastic lymphoma kinase (ALK) inhibitor for treatment of metas...
P-Glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) are two efflux transporters at t...
Lorlatinib (PF-06463922) is a promising oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor cur...
Sotorasib (Lumakras™) is the first FDA-approved KRASG12C inhibitor for treatment of patients with no...
Ponatinib is an oral BCR-ABL1 inhibitor for treatment of advanced leukemic diseases that carry the P...
EAI045 is a fourth-generation allosteric tyrosine kinase inhibitor (TKI) of the epidermal growth fac...
Lorlatinib, a novel generation oral anaplastic lymphoma kinase (ALK) and ROS1 inhibitor with high me...
Quizartinib, a second-generation FLT3 inhibitor, is in clinical development for the treatment of acu...
BACKGROUND AND PURPOSE: Pralsetinib is an FDA-approved oral small-molecule inhibitor for treatment o...
Mitogen/extracellular signal-regulated kinase (MEK) inhibitors have been tested in clinical trials f...
Vemurafenib (PLX4032) is a novel tyrosine kinase inhibitor that has clinical efficacy against metast...