@article {YU2541, author = {NING Y. YU and COLLEEN CONWAY and RHONEIL L.S. PENA and JOY Y. CHEN}, title = {STEALTH{\textregistered} Liposomal CKD-602, a Topoisomerase I Inhibitor, Improves the Therapeutic Index in Human Tumor Xenograft Models}, volume = {27}, number = {4B}, pages = {2541--2545}, year = {2007}, publisher = {International Institute of Anticancer Research}, abstract = {Background: CKD-602, a topoisomerase I inhibitor, has antitumor activity in a broad spectrum of tumor types. STEALTH{\textregistered} liposomal CKD-602 (S-CKD602) prolongs circulation of CKD-602 in plasma, increases drug exposure in tumors and improves efficacy compared with free drug. Materials and Methods: Different dosing regimens of S-CKD602, free CKD-602 and topotecan were compared for antitumor activity in female athymic nude mice bearing human A375 melanoma, ES-2 ovarian, H82 SCLC or HT-29 colon tumor xenografts. Results: S-CKD602 was more efficacious than free drug in all tumor types studied. The therapeutic index (TI) of S-CKD602 was estimated to be ~6-fold greater than that of free CKD-602 in ES-2 and ~3-fold greater in H82 tumors. TI of S-CKD602 was ~2-fold greater than that of free CKD-602 and ~5-fold greater than that of topotecan in A375, and >=3-fold greater in HT-29 tumors. In A375 tumors, once-weekly dosing of S-CKD602 was superior to once every 2 weeks or twice weekly schedules. Conclusion: The therapeutic index of S-CKD602 was greater than that of free CKD-602 and topotecan in several human tumor types. Copyright{\textcopyright} 2007 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved}, issn = {0250-7005}, URL = {https://ar.iiarjournals.org/content/27/4B/2541}, eprint = {https://ar.iiarjournals.org/content/27/4B/2541.full.pdf}, journal = {Anticancer Research} }