Background: Due to the increasing prevalence of cancer and the inadequacy of current
therapies, the development of novel antitumor pharmaceutics with higher efficacies and lower adverse
effects is considered a fundamental tenet of contemporary cancer management. Poly-
Ethylene-Glycol (PEG) attachment is a novel pharmaceutical technology to improve the efficacy
and safety of chemotherapies. Etirinotecan Pegol (EP), also known as NKTR-102, is the PEGylated
form of Irinotecan (CPT-11), which causes cancer cell apoptosis by inhibiting the topoisomerase
Objectives: The present study reviews and evaluates various reports of the EP’s anti-tumor activity
in various cancers.
Data Sources: Studies were identified using the Scopus database, with no exclusions. The search
terms included Etirinotecan Pegol and NKTR-102, which yielded 125 articles (66 and 59 articles,
respectively). In addition, the clinicaltrials.gov website was used to find ongoing studies, which resulted
in the addition of two studies.
Study Eligibility Criteria: Subsequently, we excluded studies that were published in languages
other than English, duplicate articles, and studies with no data.
Results: This systematic review clarifies that EP possesses numerous advantages over many other
medications, such as safety, efficacy, increased half-life, increased health-related quality of life, increased
overall survival, increased progression-free survival, and decreasing the adverse events in
the treatment of various cancers.
Conclusion: Therefore, Etirinotecan Pegol may represent a major contribution to the treatment of
various cancers in the future.