ABSTRACT
Introduction: A PEGylated form of irinotecan, a topoisomerase I inhibitor, is now available in commerce; its safety and efficacy have been tested in platinum resistant/refractory ovarian cancer (PROC) patients. This novel agent is known as Etirinotecan Pegol (EP). EP, like irinotecan, exerts its action through its principal metabolite SN-38.
Areas covered: This drug evaluation article focuses on the most recent investigations and clinical progress regarding EP, a long-acting polymer conjugate of irinotecan for the treatment of PROC.
Expert opinion: EP provides prolonged and continuous exposure of SN-38 in tumors, when compared to its parent drug irinotecan. Results from phase II studies are comparable in terms of efficacy to other agents of proven use in PROC. A limitation of the use of EP is the schedule-dependent toxicities (mainly diarrhea and dehydration). In the future, EP could be investigated in association with other agents, even in attempts to restore sensitivity to other treatments. PROC remains a very difficult setting and EP might be a valid agent for patients with good performance status that have exhausted therapeutic options. In such a setting, participation in clinical trials is strongly encouraged.
Article Highlights
Platinum resistant/refractory ovarian cancer (PROC) represents up to 30–45% of epithelial ovarian cancer (OC).
PROC is treated mainly with sequential, single-agent, palliative chemotherapy that offer similar objective response rates (10%–20%), median PFS (3–4 months), and overall survival (12 months) with different toxicity profiles.
Etirinotecan Pegol (EP) is a long-acting polymer conjugate of irinotecan, whose active metabolite is SN-38.
EP was developed to reduce maximal exposure to SN-38 to normal tissues, while providing an increased and continuous exposure in tumors, thus reducing adverse effects while maintaining efficacy.
Results of Phase II studies of EP were comparable with other agents used in PROC in terms of PFS and OS.
Schedule-dependent toxicities are the main limitation to the use of EP.
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Declaration of interest
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Reviewer disclosures
Peer reviewers on this manuscript have no relevant financial or other relationships to disclose