Radgocitabine (DB11667): A Comprehensive Profile of an Investigational Nucleoside Analogue for Advanced Colorectal Cancer and Hematologic Malignancies

I. Introduction

Radgocitabine, identified by DrugBank Accession Number DB11667 and CAS Number 135598-68-4, is an investigational small molecule nucleoside analogue.[1] Chemically known as 2'-cyano-2'-deoxy-1-(beta-D-arabinofuranosyl)cytosine, it is also referred to by synonyms such as CNDAC, TAS-109, and DFP-10917.[1] Radgocitabine has been evaluated in clinical trials for the treatment of various malignancies, most notably advanced colorectal cancer and, more recently, acute myeloid leukemia (AML).[1] This report provides a comprehensive overview of Radgocitabine, encompassing its chemical properties, preclinical pharmacology with a focus on its unique mechanism of action, pharmacokinetic profile, clinical development journey including efficacy and safety findings across different indications, drug interaction potential, and current regulatory status. The development of Radgocitabine illustrates a strategic evolution, moving from initial studies in solid tumors to a more focused investigation in hematologic cancers, where it shows considerable promise.

II. Background and Identification

Radgocitabine is classified as an investigational small molecule drug.[1] It belongs to the chemical groups of arabinonucleosides, pyrimidine nucleosides, and more specifically, pyrimidine 2'-deoxyribonucleosides.[1] These are compounds characterized by a pyrimidine base linked to a ribose sugar moiety that lacks a hydroxyl group at the 2' position.[1] Radgocitabine is structurally an analogue of the naturally occurring nucleoside deoxycytidine.[2]