Drug intelligence / Profile preview

doxorubicin

Development stage
Approved
Lead developer
Farmitalia
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Doxorubicin is an anthracycline antibiotic and cytotoxic chemotherapy agent used to treat a wide range of cancers, including breast cancer, bladder cancer, lung cancer, ovarian cancer, stomach cancer, thyroid cancer, soft tissue and bone sarcomas, Hodgkin lymphoma and non-Hodgkin lymphoma (including multiple myeloma), acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), neuroblastoma and Wilms' tumor[1][2][3][4][5]. It is administered intravenously. Doxorubicin works primarily by intercalating into DNA and inhibiting the enzyme topoisomerase II. This prevents DNA replication and transcription by stabilizing the topoisomerase II complex after it has broken the DNA chain for replication[3][5]. Additionally, it generates reactive oxygen species that cause further cellular damage[3][8]. Doxorubicin can also induce histone eviction from chromatin and alter gene expression through mechanisms involving ceramide synthesis and regulated intramembrane proteolysis[6]. The drug was first approved in 1974. Its use is limited by dose-dependent cardiotoxicity.

Brand names
AdriamycinRubexAdriamycin RDFAdriamycin PFS
Other names
doxorubicin hydrochloride
02

Targets

DNA polymerase familyTOP1 (DNA Topoisomerase I)Pol III (Dna-directed RNA polymerase III)TOP2A (DNA topoisomerase II)DNATOP2B (DNA topoisomerase II beta)

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