Busulfan

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Busulfan

Busulfan is a chemotherapy

Chemotherapy

Chemotherapy, in its most general sense, refers to treatment of disease by chemicals that kill cells, specifically those of micro-organisms or cancer....
drug that is a cell cycle non-specific alkylating antineoplastic agent

Alkylating antineoplastic agent

An alkylating antineoplastic agent is an alkylating agent that attaches an alkyl group to DNA.Since cancer cells generally proliferate unrestrictively more than healthy cells do, cancer cells are more sensitive to DNA damage - such as being alkylated....
(slows the growth of cancer cells). More specifically it belongs to a subclass of alkylating agents known as alkyl sulfonates. It is marketed in the U.S. by GlaxoSmithKline

GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
under the brand name Myleran, and has been in clinical use since 1959. Busulfan is also available in an IV formulation marketed as Busulfex by PDL BioPharma, Inc.

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Encyclopedia

Busulfan is a chemotherapy

Chemotherapy

Alkylating antineoplastic agent

GlaxoSmithKline

History

Busulfan used to be the standard of treatment for Chronic Myeloid Leukemia (CML) until it was replaced with the new gold standard, Imatinib

Imatinib

Imatinib is a medication used to treat certain types of cancer. It is currently marketed by Novartis as Gleevec or Glivec as its mesylate salt, imatinib mesilate ....
.

Indications

Currently, its main uses are in bone marrow transplantation, especially in chronic myelogenous leukemia

Chronic myelogenous leukemia

Chronic myelogenous leukemia , also known as chronic granulocytic leukemia , is a form of leukemia characterized by the increased and unregulated growth of predominantly myeloid cells in the bone marrow and the accumulation of these cells in the blood....
(CML), where it is used as a conditioning drug. Busulfan can control tumor burden but cannot prevent transformation or correct cytogenic abnormalities. Though not as common, it may also be used for Chronic Lymphocytic Leukemia (CLL). The drug was recently used in a study to examine the role of platelet-transported serotonin

Serotonin

Serotonin is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system and enterochromaffin cells in the gastrointestinal tract of animals including humans....
in liver

Liver

The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
regeneration.

Availabilty

Myleran is supplied in white film coated tablets with 2mg of Busulfan per tablet.

Side effects

Toxicity may include interstitial pulmonary fibrosis, hyperpigmentation

Hyperpigmentation

In dermatology, hyperpigmentation is the darkening of an area of skin or nail caused by increased melanin....
, seizures, hepatic (veno-occlusive disease) and wasting syndrome. Phenytoin

Phenytoin

Phenytoin sodium is a commonly used antiepileptic. Phenytoin acts to dampen the unwanted, runaway brain activity seen in seizure by reducing electrical conductance among brain cells by stabilizing the inactive state of voltage gated sodium channels....
may be used concurrently to prevent the seizures.

1,4-Butanediol dimethanesulfonate is listed by the IARC

IARC

IARC may refer to:* International Aerial Robotics Competition* International Agency for Research on Cancer* International Arctic Research Center...
as a Group 1 carcinogen

Carcinogen

The term carcinogen refers to any substance, radionuclide or radiation that is an agent directly involved in the promotion of cancer or in the increase of its propagation....
.

Pharmacology

Its mechanism of action through alkylation

Alkylation

Alkylation is the transfer of an alkyl group from one molecule to another. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion or a carbene ....
produces Guanine

Guanine

Guanine is one of the five main nucleobases found in the nucleic acids DNA and RNA, the others being adenine, cytosine, thymine, and uracil. In DNA, guanine is paired with cytosine....
-Guanine intrastrand crosslinks. This occurs through an SN2 reaction in which the relatively nucleophilic guanine N7 attacks the carbon adjacent to the mesylate

Mesylate

In chemistry, a mesylate is any salt or ester of methanesulfonic acid . In salts, the mesylate is present as the CH3SO3- anion....
leaving group. This kind of damage cannot be repaired by cellular machinery and thus the cell undergoes apoptosis

Apoptosis

Apoptosis is the process of programmed cell death that may occur in multicellular organisms. Programmed Cell death involves a series of biochemical events leading to a characteristic cell Morphology and death, in more specific terms, a series of biochemical events that lead to a variety of morphological changes, including Bleb , changes...
. Busulfan also induces thrombocytopenia

Thrombocytopenia

Thrombocytopenia is the presence of relatively few platelets in blood.Generally speaking, in humans, a normal platelet count ranges from 150,000 and 450,000 per mm3....
, a condition of lowered blood platelet

Platelet

Platelets, or Thrombocyte, are small, irregularly shaped anuclear cells, 2-4?m in diameter, which are derived from fragmentation of precursor megakaryocytes....
count and activity.

External links

(PDF prescribing information)
(PDF prescribing information)