XMT-1107 inhibited human MetAP2 in vitro, was highly active in human umbilical vein endothelial cell (HUVEC) proliferation assays, and showed anti-angiogenesis activity in vivo in the Matrigel plug assay. Additionally, XMT-1107 was active in a number of syngeneic and xenograft tumor models. The enhanced antiangiogenic and in vivo anti-tumor activity of XMT-1107 compared to its in vivo release product XMT-1191 clearly demonstrated the benefit of conjugating XMT-1191 to Fleximer(R) and supports the potential clinical utility of XMT-1107 as an anti-cancer agent.
"Pharmacokinetics of a novel fumagillol conjugate XMT-1107 in the rat"
By Alex Yurkovetskiy, Dana L. Shkolny, Laura C. Akullian, Mao Yin, Laraine L. Meyers, Robert J. Fram, Timothy B. Lowinger.
This study evaluated the pharmacokinetics (PK) of XMT-1107 and its conjugate release product, XMT-1191, in rats. The XMT-1107 conjugate extended exposure to its corresponding drug release product, XMT-1191, while significantly reducing (> 500 fold) maximum XMT-1191 plasma levels (Cmax).
The data suggest that the slow rate of release of XMT-1191 from the polymer conjugate XMT-1107 provided a low but consistent exposure to the highly active XMT-1191 small molecule, providing an apparent half life of 22 hours compared with a half life of less than five minutes with free XMT-1191 administration. The data are consistent with the significantly higher in vivo activity seen for XMT-1107 relative to XMT-1191 in xenograft activity reported in a separate poster.
About Mersana Therapeutics, Inc.
Mersana, a privately held, venture backed company, utilizes its proprietary technology platform to transform existing and experimental anti-cancer agents into new, patentable drugs with superior pharmaceutical properties. Mersana's lead compound, XMT-1001, is currently in Phase I trials in cancer patients. Mersana's secon
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