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QuickView for Bleomycin (compound)

Summary
General Info

PubChem

PubChem Compound 11980859

PubChem Compound 11980859

Name:	Bleomycin
PubChem Compound ID:	11980859
Description:	A complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2. It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors.
Molecular formula:	C₁₁₀H₁₆₈N₃₇O₄₂S₅⁺
Molecular weight:	2841.07 g/mol
Synonyms:	NSC125066; Bleomycin sulfate; 11056-06-7

DrugBank

Identification

Name:	Bleomycin
Name (isomeric):	DB00290
Drug Type:	small molecule
Description:	A complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2. It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors.
Synonyms:	Bleomycin A2; Bleomycinum [INN-Latin]; Bleomycin B2; BLM; Bleomycine [INN-French]; Bleomicina [INN-Spanish]; Bleomycin sulfate; Bleomicin; Bleocin
Brand:	Blenoxane, Bleo
Category:	Antimetabolites, Antibiotics, Antineoplastic
CAS number:	11056-06-7

Pharmacology

Indication:	For palliative treatment in the management malignant neoplasm (trachea, bronchus, lung), squamous cell carcinoma, and lymphomas.
Pharmacology:	Bleomycin is an antibiotic which has been shown to have antitumor activity. Bleomycin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of mitomycin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. Bleomycin... show more » Bleomycin is an antibiotic which has been shown to have antitumor activity. Bleomycin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of mitomycin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. Bleomycin has been shown in vitro to inhibit B cell, T cell, and macrophage proliferation and impair antigen presentation, as well as the secretion of interferon gamma, TNFa, and IL-2. The antibiotic antitumor drugs are cell cycle-nonspecific except for Bleomycin (which has major effects in G2 and M phases). show less «
Mechanism of Action:	Although the exact mechanism of action of bleomycin is unknown, available evidence would seem to indicate that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. DNA cleavage by bleomycin depends on oxygen and metal ions, at least in vitro. It is believed that bleomycin c... show more » Although the exact mechanism of action of bleomycin is unknown, available evidence would seem to indicate that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. DNA cleavage by bleomycin depends on oxygen and metal ions, at least in vitro. It is believed that bleomycin chelates metal ions (primarily iron) producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA. show less «
Absorption:	Systemic absorption is approximately 45%.
Protein binding:	1%
Biotransformation:	Hepatic
Route of elimination:	It was reported that patients with moderately severe renal failure excreted less than 20% of the dose in the urine.
Half Life:	115 minutes
Toxicity:	Excessive exposure may cause fever, chills, nausea, vomiting, mental, confusion, and wheezing. Bleomycin may cause irritation to eyes, skin and respiratory tract. It may also cause a darkening or thickening of the skin. It may cause an allergic reaction.
Affected organisms:	Humans and other mammals

Interactions

Drug interaction:

Natalizumab	Immunosuppressants like bleomycin may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Patients receiving natalizumab should not use concurrent immunosuppressants.
Trastuzumab	Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Fosphenytoin	The antineoplasic agent decreases the effect of hydantoin
Tacrolimus	Tacrolimus (Topical) may enhance the adverse/toxic effect of Immunosuppressants. Avoid use of tacrolimus ointment in patients receiving immunosuppressants.
Leflunomide	Immunosuppressants like bleomycin may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Consider eliminating the use of a leflunomide loading dose in patients who are receiving other immunosuppressants in order to reduce the risk for serious adverse events such as hematologic toxicity.

Targets

Enzymes

Bleomycin hydrolase