Mathew Thomas

TL;DR: Design and preclinical evaluation of AP24534, a potent, orally available multitargeted kinase inhibitor active against T315I and other BCR-ABL mutants, and clinical evaluation ofAP24534 as a pan-BCR-ABl inhibitor for treatment of CML are reported.

TL;DR: The inhibitory mechanism exemplified by ponatinib may have broad relevance to designing inhibitors against other kinases with mutated gatekeeper residues, and the extensive network of optimized molecular contacts found in the DFG‐out binding mode leads to high potency and renders binding less susceptible to disruption by single point mutations.

TL;DR: Brigatinib represents the most clinically advanced phosphine oxide-containing drug candidate to date and is currently being evaluated in a global phase 2 registration trial.

TL;DR: An investigator-driven, multicenter, open label, randomized study to establish whether the source of factor VIII (FVIII) replacement affects the rate of inhibitory alloantibodies in previously untreated patients with severe hemophilia A.

TL;DR: Analysis of plasma levels of each drug showed that AP26113 had equivalent efficacy to PF1066 at 4- to 10-fold lower levels of exposure (AUC and 24 h trough plasma levels) and support the clinical evaluation of AP26 113 in patients with ALK-driven tumors.