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cladribine (Leustatin)
Chemotherapy Agents

How it is administered

Cladribine is most commonly administered as an intravenous (IV) infusion. It is supplied in single-use vials containing 10 mg (1 mg/mL) of cladribine. The usual recommended dose for treating active Hairy Cell Leukemia is a single course given by continuous infusion for 7 consecutive days at a dose of 0.09 mg/kg/day. The medication must be diluted with 0.9% Sodium Chloride Injection before administration.

Cladribine is also available as an oral tablet for other indications (such as multiple sclerosis), but for blood cancers, the IV infusion is the standard method.

How it works

Cladribine is a synthetic antineoplastic (anti-cancer) agent that targets certain types of white blood cells, particularly lymphocytes and monocytes. It works by mimicking a natural building block of DNA, but with a slight chemical difference. Once inside the cell, cladribine is converted into its active form by cellular enzymes. This active form accumulates in cells that have high levels of a specific enzyme (deoxycytidine kinase) and low levels of another (deoxynucleotidase), which is typical for lymphocytes and monocytes.

The active cladribine disrupts the cell's ability to repair and replicate DNA, leading to cell death. This is especially effective against both actively dividing and resting (quiescent) lymphocytes and monocytes, making it a powerful treatment for certain blood cancers like Hairy Cell Leukemia. By selectively targeting these cells, cladribine helps reduce the abnormal cell population that characterizes the disease.

Common side effects

Common side effects of cladribine (as reported in clinical trials for Hairy Cell Leukemia) include:

  • Fatigue (31%)
  • Fever (33%)
  • Nausea (22%)
  • Headache (14%)
  • Rash (16%)
  • Vomiting (9%)
  • Diarrhea (7%)
  • Cough (7%)
  • Decreased appetite (8%)
  • Dizziness (6%)
  • Myalgia (muscle pain, 6%)
  • Asthenia (weakness, 6%)
  • Administration site reactions (11%)
  • Insomnia (3%)

Serious side effects can include severe bone marrow suppression, infections (bacterial, viral, or fungal), and prolonged low blood counts. Some patients may also experience prolonged depression of immune cells (CD4 lymphocytes).

Who Should take it

Cladribine is indicated for the treatment of active Hairy Cell Leukemia. This includes patients who have clinically significant anemia, neutropenia (low white blood cell count), thrombocytopenia (low platelet count), or other disease-related symptoms. It can be used as a first-line treatment or in patients who have received prior therapies.

Patients with active disease who require therapy due to symptoms or abnormal blood counts are the primary candidates. Cladribine has shown high response rates, even in patients who have previously been treated with other agents, including interferon or deoxycoformycin.

Who should not take it

Cladribine should not be used in patients who are hypersensitive to cladribine or any of its components. It is also contraindicated in pregnant women, as it can cause harm to the fetus, and in women who are breastfeeding, as it is unknown if the drug passes into breast milk.

Caution is advised in patients with known or suspected renal or hepatic insufficiency, and it should not be administered to patients with active infections or severe bone marrow impairment. Live attenuated vaccines should not be given during treatment due to the risk of infection.

Commonly used with

Cladribine is often used as a single agent for Hairy Cell Leukemia. However, in some cases, it may be used in combination with supportive treatments such as antibiotics (to prevent or treat infections), transfusions (for anemia or low platelets), or growth factors (to stimulate blood cell production).

It is important to avoid using cladribine with other drugs that cause immunosuppression or myelosuppression unless specifically directed by your doctor, as this can increase the risk of infections and other complications.

Commonly tested with

Cladribine has been tested in combination with other chemotherapeutic agents, especially in research settings for bone marrow transplant conditioning regimens (such as with cyclophosphamide and total body irradiation). However, for Hairy Cell Leukemia, it is most commonly tested and used as a single agent.

In clinical trials, cladribine has also been compared to other treatments like interferon and deoxycoformycin, particularly in patients who have relapsed or are refractory to first-line therapies.

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