A Comprehensive Monograph on Doxorubicin: Chemistry, Pharmacology, and Clinical Application

Part I: Foundational Characteristics

Section 1: Introduction and Drug Identification

1.1. Overview and Historical Context

Doxorubicin is a cytotoxic anthracycline antibiotic that has served as a cornerstone of cancer chemotherapy for over half a century.[1] Its broad spectrum of activity against both hematologic malignancies and solid tumors has cemented its role in numerous first-line and salvage treatment regimens. The drug's development is a landmark in the history of oncology, representing a pivotal moment in the discovery of potent antineoplastic agents from natural sources. It is recognized as such a critical medication that it is included on the World Health Organization's List of Essential Medicines.[1]

The story of doxorubicin begins in the 1950s with a concerted effort by Farmitalia Research Laboratories in Italy to discover anticancer compounds from soil-dwelling microorganisms.[4] This search led to the isolation of a novel strain of

Streptomyces peucetius from a soil sample collected near the 13th-century Castel del Monte in Apulia, Italy.[4] This bacterium produced a vibrant red pigment, an antibiotic that demonstrated significant activity against tumors in murine models. Concurrently, researchers at Rhône-Poulenc in France isolated the same compound, which they named Rubidomycin due to its ruby color.[6] The two teams ultimately combined their nomenclature to create the generic name

daunorubicin, a portmanteau of "Dauni," a pre-Roman tribe from the Italian region of discovery, and "rubis," the French word for ruby.[5] Clinical trials in the 1960s confirmed daunorubicin's efficacy in treating acute leukemia and lymphoma, but by 1967, its potential to induce fatal cardiac toxicity became a significant clinical concern.[4]