Onzeald (etirinotecan pegol; Nektar Therapeutics) is a polyethylene glycol (PEG) conjugate of irinotecan, a prodrug that is metabolized via enzymatic cleavage into the biologically active metabolite 10-hydroxy-7-ethyl camptothecin, also known as SN-38. SN-38 inhibits DNA topoisomerase 1 during the S-phase of the mitotic cycle, which results in the formation of covalent and nonreversible Top1-DNA complexes. When the DNA replication fork collides with these complexes, lethal DNA lesions are formed. The cleavable ester-based linkages in Onzeald are slowly hydrolyzed in vivo, decreasing the toxicity of irinotecan by providing continuous exposure to lower doses.
Expression of Trop-1 is associated with poor prognosis of several human cancers, including oral, pancreatic, gastric, ovarian, colorectal, breast, and lung tumors. Approximately 11–18% of metastatic triple-negative breast cancer patients present with brain metastases and up to 35% of all breast cancer patients will eventually develop brain metastases during the course of the disease.
4 Drug Overview
5 Product Profiles
5 Onzeald : Breast cancer: triple-negative
LIST OF FIGURES
10 Figure 1: Datamonitor Healthcare’s drug assessment summary of Onzeald for TNBC
10 Figure 2: Datamonitor Healthcare’s drug assessment summary of Onzeald for TNBC
LIST OF TABLES
6 Table 1: Onzeald drug profile
8 Table 2: Late-phase trials of Onzeald for TNBC
9 Table 3: Onzeald for TNBC – SWOT analysis
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