III. Contraindications

  1. Active malignancy
  2. Moderate to severe Renal Insufficiency
  3. Moderate to severe hepatic insufficiency
  4. Acute infections
  5. Chronic Infections (exclude before administration)
    1. HIV Infection
    2. Hepatitis BVirus
    3. Hepatitis CVirus
    4. Tuberculosis

IV. Mechanism

  1. Purine Nucleoside antimetabolite analog
  2. Cladribine is metabolized intracellularly to 2-CdATP (Cladribine triphosphate, an active metabolite)
  3. 2-CdATP incorporates into DNA
    1. Results in DNA single strand breaks
  4. Also depletes energy molecules
    1. Nicotinamide Adenine Dinucleotide (NAD)
    2. Adenosine Triphosphate (ATP)
  5. Selectively more toxic to cancerous Lymphocytes and Monocytes
    1. Cladribine is resistant to Adenosine deaminase (therefore selective for Lymphocytes and Monocytes)
    2. Noncancerous Lymphocytes and Monocytes are less responsive to Cladribine

V. Medications

  1. Leustatin IV Solution: 10 mg per 10 ml vials (Hairy Cell Leukemia)
  2. Mavenclad oral tablets: 10 mg (Multiple Sclerosis)

VI. Dosing

  1. See other references for disease specific dosing protocols

VII. Adverse Effects

  1. Alopecia
  2. Fever
  3. Headache
  4. Impaired future fertility
  5. Myelosuppression (with prolonged drop in CD4 Count)
  6. Nephrotoxicity
  7. Neurotoxicity
  8. Hepatotoxicity
  9. Rash
  10. Secondary malignancy

VIII. Safety

  1. Avoid in Pregnancy (any trimester)
    1. Men and women should use reliable Contraception for at least 6 months after last dose
  2. Avoid in Lactation
    1. Avoid Breast Feeding for at least 10 days after last dose
  3. Monitoring
    1. MRI Brain
      1. Risk of Progressive Multifocal Leukoencephalopathy
      2. Baseline within first 3 months of starting Cladribine
    2. Complete Blood Count
      1. Lymphocytes should be in normal range before first treatment
      2. Lymphocytes should be >800 cells/uL before second treatment (may required delayed course)
    3. Renal Function tests
    4. Liver Function Tests

IX. Drug Interactions

  1. Live attenuated Vaccinations
    1. Give all Live Vaccines at least 4 to 6 weeks before starting Cladribine

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Related Studies

Ontology: Cladribine (C0092801)

Definition (NCI_NCI-GLOSS) An anticancer drug that belongs to the family of drugs called antimetabolites.
Definition (NCI) A purine nucleoside antimetabolite analogue. Cladribine triphosphate, a phosphorylated metabolite of cladribine, incorporates into DNA, resulting in single-strand breaks in DNA, depletion of nicotinamide adenine dinucleotide (NAD) and adenosine triphosphate (ATP), and apoptosis. Because this agent is resistant to adenosine deaminase, an enzyme that inactivates some antineoplastic agents, it is selectively toxic to lymphocytes and monocytes which exhibit little deoxynucleotide deaminase activity. (NCI04)
Definition (MSH) An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia.
Definition (CSP) adenosine deaminase-resistant congener of deoxyadenosine with selective toxicity towards lymphocytes and monocytes; used as an immunosuppressive in treating certain leukemias, lymphomas, and autoimmune disorders.
Definition (PDQ) A purine nucleoside antimetabolite analogue. Cladribine triphosphate, a phosphorylated metabolite of cladribine, incorporates into DNA, resulting in single-strand breaks in DNA, depletion of nicotinamide adenine dinucleotide (NAD) and adenosine triphosphate (ATP), and apoptosis. Because this agent is resistant to adenosine deaminase, an enzyme that inactivates some antineoplastic agents, it is selectively toxic to lymphocytes and monocytes which exhibit little deoxynucleotide deaminase activity. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41184&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=41184&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C1336" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
MSH D017338
SnomedCT 108800000, 386916009
English 2'-Deoxy-2-chloroadenosine, 2-Chloro-2'-deoxyadenosine, 2-Chlorodeoxyadenosine, Adenosine, 2-chloro-2'-deoxy-, cladribine, Cladribina, 2-Chloro-2-Deoxyadenosine, CHLORODEOXYADENOSINE 02 02, CHLORODEOXYADENOSINE 02, chlorodeoxyadenosine, cladribine (medication), CLADRIBINE, Cladribine [Chemical/Ingredient], 2-chloro-2'-deoxyadenosine, cda, cdas, Cladribine product, Cladribine (product), Cladribine (substance), Cladribine, 2-chlorodeoxyadenosine, CdA, 2-CdA, 2CDA
Swedish Kladribin
Czech 2-chlorodeoxyadenosin
Finnish Kladribiini
Russian KLADRIBIN, 2-KHLORODEOKSIADENOZIN, 2-KHLORO-2-DEOKSIADENOZIN, 2-ХЛОРО-2-ДЕОКСИАДЕНОЗИН, 2-ХЛОРОДЕОКСИАДЕНОЗИН, КЛАДРИБИН
Japanese クラドリビン, 2-クロロデオキシアデノシン, ロイスタチン, 2-クロロ-2'-デオキシアデノシン
Italian 2'-Deossi-2-cloroadenosina, 2-Cloro-2’-deossiadenosina, 2-Clorodeossiadenosina, Cladribina
German CHLORDESOXYADENOSIN 02 02, CHLORDESOXYADENOSIN 02, 2-Chlor-2'-Desoxyadenosin, 2-Chlordesoxyadenosin, Cladribin
Polish Kladrybina
Spanish cladribina (producto), cladribina (sustancia), cladribina, 2-Cloro-2'-desoxiadenosina, 2-Clorodesoxiadenosina, Cladribina
French Chloro-2 désoxyadénosine
Portuguese 2-Cloro-2'-desoxiadenosina, 2-Clorodesoxiadenosina, Cladribina