NCIt definition : A polymeric prodrug of camptothecin (CPT) with potential antineoplastic activity.
Polymeric camptothecin prodrug XMT-1001 consists of CPT conjugated to the 60-70 kDa,
inert, bio-degradable, hydrophilic copolymer poly[1-hydroxymethylene hydroxymethyl
formal] (PHF). Through a dual-phase, non-enzymatic release mechanism, CPT is first
released in plasma from XMT-1001 as the lipophilic prodrugs CPT-SI (a succinimidoglycinate
derivative) and CPT-SA (a succinamidoyl glycinate derivative), which are then hydrolyzed
within tissues to release the lactone form of CPT. CPT inhibits the catalytic activity
of DNA topoisomerase I, thereby inhibiting DNA replication and inducing apoptosis.
This agent may exhibit a more favorable pharmacokinetic profile than other agents
in the same class.;
Semantic type(s)