Bleomycin

Summary

Bleomycin is a mixture of glycopeptide antibiotics derived from Streptomyces verticillus, used primarily as an antineoplastic agent. It is a key component of combination chemotherapy regimens for Hodgkin lymphoma, testicular germ cell tumors, and squamous cell carcinomas. Its notable adverse effect profile includes pulmonary toxicity, which can be dose-limiting.

Mechanism of Action

Bleomycin binds to DNA and, in the presence of Fe(II) and molecular oxygen, generates free radicals that cause single- and double-strand DNA breaks, leading to cell cycle arrest (G2/M phase) and apoptosis in rapidly dividing cells.

Routes of Administration

Goals & Uses

• Testicular germ cell tumor treatmentOncologyHigh
• Ovarian germ cell tumor treatmentOncologyModerate
• Hodgkin lymphoma treatmentOncologyHigh
• Squamous cell carcinoma treatmentOncologyModerate
• Malignant pleural effusion sclerotherapyPalliative OncologyModerate
• Non-Hodgkin lymphoma treatmentOncologyModerate

Contraindications

• Severe pulmonary diseaseRespiratoryHigh
• Prior severe bleomycin pulmonary toxicityDrug Toxicity HistoryHigh
• Severe renal impairmentOrganModerateKidney function concerns
• Hypersensitivity to bleomycinAllergy/immunologyHigh
• Cumulative dose >400 unitsOncology/safetyHigh

Adverse Effects

• Cutaneous toxicity (skin thickening, hyperpigmentation, alopecia)DermatologicCommon
• Pulmonary fibrosis/pneumonitisRespiratoryUncommon
• Fever and chillsConstitutionalCommon
• Nausea and vomitingGastrointestinalCommon
• MyelosuppressionHematologicUncommon
• Anaphylactoid/idiosyncratic reactionsImmunologicUncommon

Drug Interactions

• Supplemental oxygen (high FiO2)High
• DigoxinLow
• PhenytoinModerate
• CisplatinModerate
• Granulocyte colony-stimulating factors (G-CSF)Moderate

Population Constraints

• SmokersLifestyleRelative
• Elderly patients (≥70 years)AgeRelative
• Patients undergoing general anesthesiaPerioperativeRelative
• Patients with renal impairmentOrgan ImpairmentRelative
• Pregnant womenReproductiveRelative

Regulatory Status

• European UnionApprovedApproved: Hodgkin lymphoma, Testicular germ cell tumors, Squamous cell carcinomaAvailable as generic bleomycin sulfate across EU member states; national-level approvals.
• United StatesApprovedApproved: Hodgkin lymphoma, Non-Hodgkin lymphoma, Testicular carcinoma, Squamous cell carcinoma of head and neck, cervix, and skin, Malignant pleural effusion (sclerotherapy)FDA-approved; listed in USP. Brand name Blenoxane; multiple generic formulations available.
• United KingdomApprovedApproved: Hodgkin lymphoma, Testicular germ cell tumors, Squamous cell carcinoma, Malignant pleural effusionAvailable via MHRA-approved generics; used per NICE-aligned oncology guidelines.

FDA-approved since 1973 (Blenoxane). Approved in EU and UK under various generic formulations. Pulmonary toxicity has led to strict cumulative dose limits (typically ≤400 units lifetime).

Evidence & Sources

No sources recorded yet.