All you need to know about Bosutinib

Bosutinib is a src tyrosine kinase inhibitor that is used in the treatment of chronic myelogenous leukemia, which has resistance intolerance to prior therapy. Bosutinib inhibits the activity of platelet-derived growth factor and vascular endothelial growth factor.

On September 4, 2012, and 27 March 2013, Bosutinib was approved by US FDA and EU European Medicines Agency approval
respectively in order to treat adult patients with Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance, or intolerance to prior therapy.

Dosage and Administration: 

Bosutinib tablets are present in two different concentrations that are 100 mg and 500 mg. The recommended dose of Bosutinib tablets is 500 mg daily. Hepatic impairment reduces the dose of the bosutinib tablets to 200 mg.
The dose is adjustable in case of hematologic and non- hematologic toxicity.

Side effects of Bosutinib: 

Some common side effects of the bosutinib 500mg tablet are:

• Diarrhoea 
• Nausea
• Vomiting
• Abdominal pain
• Rash
• Anemia
• Fatigue 
• Thrombocytopenia

On the other hand, some common side effects as Drug hypersensitivity, Dehydration, Hyperkalaemia (high blood potassium), low blood phosphate, Dizziness, Dysgeusia (distorted sense of taste), Pericardial effusion, Pleural effusion, QT interval prolongation, Shortness of breath, Gastritis (stomach swelling), Hepatotoxicity (liver dysfunction/damage), Abnormal LFTs, Elevated blood bilirubin levels, GGT increased, Acne, Itchiness, Hives, Myalgia (muscle aches), Back pain, Kidney failure, Chest pain, Muscle weakness, Increased blood creatinine, Increased lipase, Increased blood amylase level and Elevated blood creatine phosphokinase

Some serious adverse reactions of the bosutinib tablets are

• Gastrointestinal toxicity: if any symptom of toxicity appears then the drug use is discontinued.
• Myelosuppression: blood count measurement is necessary
• Hepatic toxicity:  monitor of the Liver enzyme is very necessary
• Embryo-fetal toxicity: causes damage to fetal and main cause toxicity.

How Does Bosutinib work: 

Bosutinib 500 mg is an ATP-competitive Bcr-Abl tyrosine kinase inhibitor with an additional inhibitory effect on SRc family kinases (including Src, Lyn, and Hck). This drug has enough potential against the receptors for vascular endothelial growth factor and platelet derived growth factor.
This medication basically inhibited imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines. The ratio is about 16 of 18 but did not inhibit V299L and T315I mutant cells. Bosutinib is metabolized through CYP3A4.

Drug Interactions:

• Drugs containing Proton pump inhibitors decrease the amount of Bosutinib 500 mg in the human body.
• Should be avoided the concurrent use of this medication with moderate Or strong CYP3A inhibitors and inducers.
• Bosutinib 500mg  is not recommended to be used in a person who has a problem of hypersensitivity.
• Bosutinib is basically known as the substrate and also an inhibitor of CYP3A4 and P-glycoprotein (P-gp). Hence CYP3A4 inhibitors and P-gp are able to increase the plasma levels of bosutinib. In this way, CYP3A4 inducers may reduce the existing plasma concentrations of bosutinib 500 mg. It can also alter the metabolism and uptake of other drugs that are substrates for CYP3A4 and P-gp. 

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