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NKTR-102 (PEG-Irinotecan) Demonstrates Significant Tumor Growth Inhibition In Multiple Preclinical Tumor Models
Date:10/25/2007

ffective halflife of the metabolite was increased from 15 hours with irinotecan to 6 days with NKTR-102.

This increased and prolonged metabolite exposure following administration of NKTR-102 was associated with its anti-tumor activity in lung and colorectal models using pharmacokinetic (PK) and pharmacodynamic (PD) modeling. Further, PK/PD simulations performed with irinotecan administration show that a continuous infusion of irinotecan at 240 mg/kg would be required to achieve the equivalent tumor exposure of the active metabolite and associated tumor growth inhibition found with NKTR-102. This 240 mg/kg dose of irinotecan would be expected to cause significant mortality in mice.

Data Presentations

The two poster presentations made today at the AACR-NCI-EORTC International Conference, and prior presentations for NKTR-102, can be found on Nektar's website at http://www.nektar.com/wt/page/nktr102media

C10: "NKTR-102, a novel polyethylene glycol conjugate of irinotecan, has improved antitumor activity in three mouse xenograft models"

C157: "NKTR-102, a novel PEGylated-irinotecan conjugate, results in sustained tumor growth inhibition in mouse models of human colorectal and lung tumors that is associated with increased and sustained SN38 exposure"

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 1 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.

Nektar PEGylation Platform

Nektar PEGylation technology can enhance the properties of therapeutic a
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SOURCE Nektar Therapeutics
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