Small molecule
PubChem CID 31703
Doxorubicin
Adriamycin
- Mechanism of action
- Topoisomerase II inhibitor / DNA intercalator
- In plain language
- Wedges itself into a cancer cell's DNA and jams the enzyme the cell needs to untangle and copy it, so the cell can't divide — and dies instead.
- How it works
- Doxorubicin, an anthracycline, intercalates between base pairs of the DNA double helix, distorting its structure and blocking DNA- and RNA-dependent polymerases from proceeding along the strand. It also binds and poisons topoisomerase II, stabilizing the transient enzyme-DNA cleavable complex that normally lets the double helix relax and reseal after strand cleavage, so unrepaired double-strand breaks accumulate. The drug additionally undergoes redox cycling to generate reactive oxygen species that cause further DNA, lipid, and protein damage — a process implicated in its dose-dependent cardiotoxicity. Together these effects halt replication and transcription in rapidly dividing malignant cells and drive them into apoptosis.
- Therapeutic applications
- Indicated as a component of multi-agent adjuvant chemotherapy for women with axillary lymph node involvement following resection of primary breast cancer, and for treatment of acute lymphoblastic leukemia, acute myeloblastic leukemia, Hodgkin lymphoma, non-Hodgkin lymphoma, metastatic breast carcinoma, metastatic Wilms' tumor, neuroblastoma, metastatic soft tissue and bone sarcoma, metastatic ovarian carcinoma, metastatic transitional cell bladder carcinoma, metastatic thyroid carcinoma, metastatic gastric carcinoma, and metastatic bronchogenic carcinoma.
- Class
- Small molecule
- Therapeutic area
- Oncology
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