Bleomycin !

A Streptomyces glycopeptide that uses iron and oxygen to cut DNA. Used in testicular cancer and Hodgkin lymphoma; it spares the marrow but can scar the lungs.

Updated 2026-11-01

Class: Antitumour antibiotics
Target: DNA (oxidative strand cleavage)
ATC code: L01DC01
WHO Model List of Essential Medicines

DNA (oxidative strand cleavage)Bleomycin

NMR structure of bleomycin A2 bound to DNA; the metal in the structure is cobalt, used as a stable stand-in for the iron bleomycin uses in cells.

Target in 3D: DNA (oxidative strand cleavage). PDB structure 1MXK (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Bleomycin has one part that binds DNA and another that holds a metal ion. With ferrous iron and oxygen the complex becomes activated and generates oxygen radicals that break DNA strands, mostly single-strand breaks and some double-strand breaks. Cells pile up in the G2 phase. The drug is inactivated by bleomycin hydrolase, an enzyme that is scarce in lung and skin, the two tissues it harms most.

Bleomycin binds DNA and chelates iron
Iron plus oxygen produce oxygen radicals
Single- and double-strand DNA breaks
Cells stall in G2; lung and skin lack the inactivating enzyme

Pharmacokinetics

Absorption: Given IV, IM, SC or into the pleural space; well absorbed by the IM route.
Distribution: Wide; enters the brain poorly.
Metabolism: Inactivated by bleomycin hydrolase in most tissues except skin and lung.
Elimination: Mostly by the kidneys; levels rise sharply in kidney failure, so the dose is reduced.
Half-life: About 2 hours with normal kidney function.

Indications

Testicular germ-cell carcinoma (embryonal, choriocarcinoma, teratocarcinoma), in combination. Testicular cancer →
Squamous cell carcinoma of the head and neck. Head and neck squamous cell carcinoma (oral cavity and oropharynx, HPV) →
Squamous cell carcinoma of the cervix, vulva and penis. Cervical cancer →
Hodgkin and non-Hodgkin lymphoma.
Malignant pleural effusion, as a sclerosing agent.

Adverse effects

Common

Skin changes: hyperpigmentation, thickening, redness, striae, nail changes
Fever (hyperthermia) after the dose
Mouth sores and hair loss
Little bone-marrow suppression

Contraindications

Previous hypersensitivity or idiosyncratic reaction to bleomycin
Used with extreme caution in significant kidney impairment or reduced lung function

Key interactions

Cisplatin: Cisplatin kidney damage reduces bleomycin clearance; fatal bleomycin lung toxicity has occurred this way.
High inspired oxygen (anaesthesia, respiratory therapy): Can trigger lung injury in people who have received bleomycin, even at concentrations usually safe.
Vinblastine: Raynaud phenomenon has been reported with the combination.

What is monitored

Breathing symptoms (dry cough, breathlessness) and chest examination for fine crackles
Chest X-rays during treatment; diffusing capacity (DLCO) may be followed
Kidney function before each dose
Temperature and blood pressure after the first doses in lymphoma

Administration and safety

Routes: intravenous, intramuscular, subcutaneous or intrapleural; the route on the order is checked.
Bleomycin amounts are expressed in units, not milligrams; the unit on the order is checked.
Before surgery the anaesthesia team is told about bleomycin so that inspired oxygen is kept close to room air.
Hazardous drug: prepared and given following hazardous-drug handling procedures (impervious gloves, no skin contact) and disposed of as cytotoxic waste.

Nursing care

Independent double check of drug, patient, route and cycle before giving it (high-alert medicine).
After the first doses in lymphoma, watch closely for fever, chills, low blood pressure, confusion and wheeze.
Ask about cough and breathlessness at every visit and listen to the lung bases.
Teaching: tell any future anaesthetist or emergency team about bleomycin; report new cough or breathlessness.

Pregnancy and breastfeeding

Can cause fetal harm (teratogenic in rats); pregnancy is avoided during treatment.

Test yourself

Think of the answer, then tap the question to see it.

What is the most serious toxicity of bleomycin, and what are its risk factors?

Pneumonitis progressing to pulmonary fibrosis; risk rises with age, total dose, kidney impairment, lung disease and high inspired oxygen.

Why is bleomycin useful in combination chemotherapy for testicular cancer and Hodgkin lymphoma?

It causes little myelosuppression, so its toxicity does not overlap with marrow-suppressive drugs.

Which enzyme inactivates bleomycin, and why does it matter?

Bleomycin hydrolase; it is scarce in lung and skin, which explains why those organs are injured.

A patient treated with bleomycin needs surgery. What must the anaesthesia team know?

High inspired oxygen can trigger bleomycin lung injury, so oxygen is kept near room-air concentrations and fluids are managed carefully.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - BLEOMYCIN- bleomycin sulfate powder, for solution (DailyMed (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 70 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).

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Representative model, for educational purposes only.