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Additive Anti-Tumor Activity of NKTR-102 in Combination With Bevacizumab Highlighted in Positive Preclinical Data Presented at AACR Meeting
Date:4/14/2008

profile with reduced gastrointestinal and hematopoietic

toxicity compared to irinotecan with repeat dosing in dogs"

#5742: "NKTR-102, a novel PEGylated-irinotecan, has a superior acute

safety, tolerability, and pharmacokinetic profile compared to irinotecan

in rats and dogs"

Prior data presentations on the anti-tumor activity and pharmacokinetics of NKTR-102 in mouse xenograft models of colorectal, breast and lung cancer can be found at http://www.nektar.com/wt/page/nktr102media.

About NKTR-102

Nektar is developing NKTR-102, a PEGylated form of irinotecan, which was invented by Nektar using its world-leading small molecule PEGylation technology platform. The product is currently in Phase 2 clinical development. Irinotecan is an important chemotherapeutic agent used for the treatment of solid tumors, including colorectal and lung cancers. By applying Nektar's small molecule PEGylation technology to irinotecan, NKTR-102 may prove to be a more powerful and tolerable anti-tumor agent. Preclinical studies show that treatment with NKTR-102 results in significant suppression of tumor growth in an irinotecan-resistant mouse colorectal tumor model and in similar models of breast and lung cancer. Administration of NKTR-102 in an animal model also results in a markedly improved time-concentration profile for SN38, the active metabolite of irinotecan, as compared to treatment with irinotecan.

Nektar PEGylation Platform

Nektar PEGylation technology can enhance the properties of therapeutic agents by increasing drug circulation time in the bloodstream, decreasing immunogenicity and dosing frequency, increasing bioavailability and improving drug solubility and stability. It can also be used to modify pharmaceutical agents to preferentially target certain systems within the body. It is a technique in which non-toxic polyethylene glycol (PEG) polyme
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SOURCE Nektar Therapeutics
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