Joseph A. Ware

TL;DR: Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling.

TL;DR: A review of the available clinical literature describing the extent of the interaction between 15 orally administered, small‐molecule targeted anticancer therapies and acid‐reducing agents suggests that the magnitude of this DDI is largest for compounds whose in vitro solubility varies over the pH range 1–4.

TL;DR: Pictilisib was safely administered with a dose-proportional pharmacokinetic profile, on-target pharmacodynamic activity at dose levels ≥100 mg and signs of antitumor activity.

TL;DR: The clinical pharmacokinetics and in vitro inhibition of digoxin were examined to predict the P‐glycoprotein (P‐gp) component of drug–drug interactions and found that digoxin is likely to show the highest perturbation, via inhibition of P‐gp, because of the absence of metabolic clearance.

TL;DR: A series of compounds were designed and synthesized as antagonists of cIAP1/2, ML-IAP, and XIAP based on the N-terminus, AVPI, of mature Smac to lead to decreased viability of breast cancer cells without affecting normal mammary epithelial cells.