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NK012 + 5-fluorouracil

Development stage
Unknown
Lead developer
Nippon Kayaku
Modality
Small Molecules, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

NK012 + 5-fluorouracil is a combination regimen under investigation for the treatment of advanced solid tumors, particularly colorectal cancer. NK012 is a polymeric micelle formulation that delivers SN-38, the active metabolite of irinotecan (CPT-11), directly to tumor cells. Unlike irinotecan, which requires metabolic activation by enzymes to release SN-38, NK012 releases SN-38 via hydrolysis and accumulates at higher concentrations in tumors. This targeted delivery may reduce certain side effects compared to conventional irinotecan therapy[4][6]. Fluorouracil (also known as 5-FU) is an antimetabolite chemotherapy agent that inhibits DNA synthesis by interfering with thymidylate synthase and RNA function in rapidly dividing cells[1][3][5]. The combination has shown synergistic antitumor activity in preclinical models and early-phase clinical trials for colorectal cancer[6][8].

Other names
fluorouracilSN-38 polymeric micelle (for NK012)
02

Targets

TOP1 (DNA Topoisomerase I)TS (Thymidylate synthase)

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