Bosutinib is an anti-cancer drug in the form of coated tablets used to treat chronic myeloid leukemia (CML) with a Philadelphia chromosome (Ph+). It inhibits kinases and is used when imatinib, nilotinib, and dasatinib are intolerable or ineffective.

Indications

The drug is prescribed for the treatment of CML Ph+ in the chronic, accelerated, or blast crisis phase if previous therapy is ineffective or causes side effects.

Dosage form

Bosutinib is available as yellow, oval, film-coated tablets. The tablets are white with a yellowish or brown tint. Each tablet contains 500 mg of the active ingredient.

Administration and dosage

The recommended dose is 500 mg once daily with food. Treatment should be continued until the disease progresses or intolerable side effects occur.

In case of moderate renal insufficiency (creatinine clearance 30-50 ml/min), the dose is reduced to 400 mg, and in case of severe renal insufficiency (creatinine clearance <30 ml/min), the dose is reduced to 300 mg.

Contraindications

The drug should not be taken in case of:

• hypersensitivity to bosutinib;
• use of potent or moderate CYP3A inhibitors or inducers;
• pregnancy and breastfeeding;
• under the age of 18.

With caution

Bosutinib should be used with caution in the following cases:

• when using weak CYP3A inhibitors or inducers;
• when taking P-glycoprotein substrates or proton pump inhibitors;
• when having arrhythmias, factors that prolong the QTc interval, and cardiovascular diseases;
• when using medications that cause QT interval prolongation.

Side effects

Possible side reactions include:

• cardiovascular system: pericardial effusion;
• hearing system: tinnitus;
• digestive system: diarrhea, vomiting, abdominal pain, gastritis, pancreatitis;
• liver: hepatotoxicity, liver dysfunction;
• nervous system: headache, dizziness, altered taste;
• respiratory system: shortness of breath, cough, pleural effusion, pulmonary edema;
• skin: rash, itching, hives, acne;
• urinary system: renal failure;
• musculoskeletal system: joint and back pain, myalgia;
• other: fatigue, swelling, fever, asthenia.

Special instructions

• In the first three months of treatment, and if necessary, liver function should be checked monthly. If liver enzyme levels increase, the dose may need to be adjusted or the medication may need to be discontinued.
• Diarrhea, nausea, and vomiting may occur during treatment. In such cases, anti-diarrheal and anti-emetic agents are prescribed.
• Every two weeks during the first two months of treatment, and then monthly and as needed, the blood count and electrocardiogram are checked. If necessary, the levels of potassium and magnesium are adjusted.
• The medication should be taken one hour before a meal or two hours after a meal. It is not recommended to take it with grapefruit juice.
• During treatment and for three months after treatment, reliable methods of contraception should be used.
• If you experience dizziness, you should refrain from driving or operating machinery.

Drug Interactions

Bosutinib should not be combined with strong or moderate CYP3A inhibitors, such as ritonavir, itraconazole, ketoconazole, clarithromycin, grapefruit juice, and others. This can increase the concentration of the drug in the blood.

Before using bosutinib, please consult your doctor. Self-medication is dangerous.