Drug General Information (ID: DDIQCJ3TMZ)
  Drug Name Cladribine Drug Info Cilostazol Drug Info
  Drug Type Small molecule Small molecule
  Therapeutic Class Antineoplastics Vasodilator Agents
  Structure

 Mechanism of Cladribine-Cilostazol Interaction (Severity Level: Moderate)
     Transporter inhibition Click to Show/Hide Mechanism Graph
Could Not Find 2D Structure
      Drug Name Cladribine Cilostazol
      Mechanism ENT1 substrate ENT1 inhibitor
      Key Mechanism Factor 1
Factor Name Solute carrier family 29 member 1
×
Structure Sequence
MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDAQASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAILLVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQGLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKLEGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIFTITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRWLPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPKKVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
Gene Name ENT1
Uniprot ID S29A1_HUMAN
KEGG Pathway hsa:2030
Protein Family SLC29A/ENT transporter (TC 2.A.57) family
Protein Function
Mediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive (ES) to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (NBMPR) and is sodium-independent. It has a higher affinity for adenosine. Inhibited by dipyridamole and dilazep (anticancer chemotherapeutics drugs).
    Click to Show/Hide
      Mechanism Description
  • Decreased clearance of Cladribine due to the transporter inhibition by Cilostazol 

Recommended Action
      Management Coadministration of potent ENT1, CNT3, or BCRP transporter inhibitors should be avoided during the 4 to 5-day oral cladribine treatment cycles. If coadministration is required, consider concomitant alternatives that exhibit no or minimal inhibition of ENT1, CNT3, or BCRP. If this is not possible, dose reduction to the minimum mandatory dose, separation in the timing of administration, and careful patient monitoring is recommended.

References
1 Cerner Multum, Inc. "Australian Product Information.".
2 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
3 Product Information. Leustatin (cladribine). Ortho Biotech Inc, Raritan, NJ.