… II glucuronidation metabolism on abacavir bioactivation to the protein-reactive aldehyde …
a candidate drug such as abacavir (daily dose = 600 mg) by monitoring systemic (and excreta) …

… recognized to underlie the bioactivation of many substituted … α,β-unsaturated aldehyde
metabolite of abacavir, did react … span in humans of ~120 days, also has been used to monitor …

… The widespread use of metabolic stability screening in drug … ADH and ALDH are involved in
the bioactivation of abacavir (ABC)… bioactivation to form a reactive α,β-unsaturated aldehyde …

… of these aldehyde RM in human plasma samples obtained during drug monitoring. Docking
… originating from the metabolic transformation, often called bioactivation, of particular …

… candidate is bioactivated to a reactive metabolite, several in … mechanisms of toxicity were
monitored in a panel consisting … For example, we now know that antigens derived from abacavir …

… bioactivation of drugs to chemically reactive metabolites (CRMs) as a possible causal factor
… Figure 17 (adapted from [159] ) Covalent binding of drugs and metabolites in human liver …

… indicated phase I bioactivation in human liver microsomes, … generation of a reactive aldehyde
metabolite that did not form … scans such as selected reaction monitoring (SRM), precursor …

… mitigated the formation of the electrophilic aldehyde metabolite, and was a more potent …
In vitro metabolism studies were conducted on human tissue acquired from a third party that …

… of metabolic liabilities, identification of any bioactivation to reactive … , and metabolic stability
testing of metabolites during lead … However, a proposed aldehyde oxidase metabolite of one …

… well as with a bioactivated version of abacavir, leading to a … active in reactive metabolite
formation are alcohol/aldehyde … area to date has focused on monitoring clinical samples. The …