Additive Anti-Tumor Activity of NKTR-102 in Combination With Bevacizumab Highlighted in Positive Preclinical Data Presented at AA...(rgrowth by up to 97% in an irinotecan-re...),Health

Date:4/14/2008

r growth by up to 97% in an irinotecan-resistant mouse xenograft model of colorectal cancer (HT29), which was greater than monotherapy with either NKTR-102 or bevacizumab. NKTR-102 at 46 mg/kg, co-administered with bevacizumab, also resulted in eight partial tumor regressions and one complete tumor regression. This compares to no tumor regressions observed with bevacizumab monotherapy, and two partial regressions and one complete regression with NKTR-102 monotherapy. NKTR-102 alone, and in combination with bevacizumab, was well-tolerated, with minimal weight loss.

NKTR-102 also exhibited superior pharmacokinetics in a repeated dose study in dogs, with a 6-fold increase in exposure (AUC) and a 4-fold lower peak plasma concentration (Cmax) of SN38, the active metabolite of irinotecan, as compared to the equivalent dosing of irinotecan. The lower peak plasma concentration of NKTR-102 was associated with a superior tolerability profile, with less gastrointestinal and hematopoietic toxicity than comparable doses of irinotecan.

In animal models, NKTR-102 had a markedly improved safety and tolerability profile when compared to irinotecan in animal models. Both the incidence and severity of diarrhea and neutropenia were lower in dogs treated with NKTR-102 as compared to irinotecan. Diarrhea and neutropenia are the most common side effects associated with irinotecan treatment, and can limit treatment with the therapy.

Data Presentations

The three poster presentations made this week at the AACR Annual Meeting can be found on Nektar's website at http://www.nektar.com/wt/page/nktr102media

#766: "Enhanced anti-tumor activity of NKTR-102, a novel

PEGylated-irinotecan, when administered in combination with bevacizumab

in a mouse model of human colorectal tumors"

#5741: "NKTR-102, a novel PEGylated-irinotecan, has an enhanced

pharmacokinetic
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SOURCE Nektar Therapeutics Copyright©2008 PR Newswire. All rights reserved

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