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Mersana has announced positive results from preclinical studies for its second development candidate, XMT-1107. The studies showed that XMT-1107, a new analogue of fumagillin antiangiogenic conjugated FLEXIM (R) owned by Mersana showed a higher antitumor activity in xenograft tumor models in comparison with other antiangiogenic agents and extended exposure to the drug conjugate, supporting potential clinical utility of XMT-1107 as an anticancer agent.

"We are encouraged by the progress we are seeing today with XMT-1107, which addresses a new mechanism to inhibit proliferation of endothelial cells and has the potential to address a wide variety of angiogenic tumors, dijoJulie Olson, CEO of Mersana. "The first drugs in this class showed a promising activity in clinical practice but was interrupted due to the reversible neurological toxicity. The combination of our new" warhead "from fumagillin to FLEXIM using a specific link technology reduces exposure to the CNS in animal models for detection limits below. We hope moving XMT-1107 in clinical studies in early 2010. "

The study "The antiangiogenic and antitumor activity of XMT-1107, a conjugated polymer derived from fumagillin, and its product release in vivo XMT-1191" showed that XMT-1107 has enhanced the antiangiogenic and antitumor activity in comparison with analogues small molecule delivered without the benefit of FLEXIM. XMT-1107 inhibited human MetAP2 in vitro, was highly active in assays of endothelial cell proliferation in human umbilical vein (HUVEC), and showed activity antiangiogénesis in vivo Matrigel assay. Additionally, XMT-1107 was active in a number of models and xenograft tumor singenésicos. The enhanced antiangiogenic and antitumor activity in vivo of XMT-1107 in comparison with its product release in vivo XMT-1191 clearly demonstrated the benefit of combining with XMT-1191 FLEXIM (R) and supports the potential clinical utility as an agent XMT-1107 anticarcinogenic.

The study entitled "Pharmacokinetics of a new conjugate fumagillin XMT-1107 in rats" to evaluate the pharmacokinetics (PK) of XMT-1107 and its product release conjugate, XMT-1191, the exhibition expanded conjugate XMT-1107 to your product drug release corresponding XMT-1191, while reduced (> 500 times) the maximum plasma XMT-1191 (Cmax).

The data suggest that the slow rate of release of XMT-1191 XMT polymer conjugate-1107 provided a low but consistent exposure to small-molecule highly active XMT-1191, offering an apparent half-life of 22 hours compared with the average life less than five minutes with self-administration of XMT-1191. The data are consistent with activity in vivo significantly higher for the hearing on XMT-1107 XMT-1191 in the activity in a xenograft registered independent poster.