Idiosyncratic Drug Toxicity-View from Pharmacokinetics and Drug Metabolism-

[Front-line research of idiosyncratic drug toxicity].

Role of Bioactivation in Idiosyncratic Drug Toxicity: Structure–Toxicity Relationships

Adverse drug reactions (ADRs) continue to be a significant contributor to overall attrition statistics in the pharmaceutical industry. ADRs pose a significant health problem since they contribute to patient morbidity and mortality and represent one of the most common causes for pharmaceutical product recalls and black-box warning labels. Of a total of 548 drugs approved in the period from 1975 ...

Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib.

Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant antitumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and drug-drug interaction (DDI) profile of carfilzomib. The PK of carfilzomib, infused over 2-10 minutes, was evaluated in patients with solid tumors ...

New horizons in drug metabolism, pharmacokinetics and drug discovery.

Along with minimal toxicity, good drug metabolism and pharmacokinetic (DMPK) properties are essential for the clinical success of a drug candidate. A major cause of failure of orally administered drugs during their development is the discovery that in humans they have low intestinal absorption and/or high clearance causing low and variable bioavailability. In addition, drug interactions and the...

Advanced knowledge in drug metabolism and pharmacokinetics

Drug metabolism and transport in human organs, such as in the liver, intestine, and kidney, control the concentrations of a drug and its metabolites in the circulating system and target organs in a certain period of time following drug administration. The pharmacokinetic properties will consequently determine therapeutic efficacy and influence toxicological effects. Changes of drug metabolism a...