Details of Drug-Drug Interaction
| Drug General Information (ID: DDIPS5CJXV) | |||||||||
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| Drug Name | Cladribine | Drug Info | Sulindac | Drug Info | |||||
| Drug Type | Small molecule | Small molecule | |||||||
| Therapeutic Class | Antineoplastics | Antiinflammatory Agents | |||||||
| Structure | |||||||||
| Mechanism of Cladribine-Sulindac Interaction (Severity Level: Moderate) | |||||||||
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| Transporter inhibition Click to Show/Hide Mechanism Graph | |||||||||
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| Drug Name | Cladribine | Sulindac | |||||||
| Mechanism | ENT1 substrate | ENT1 inhibitor | |||||||
| Key Mechanism Factor 1 | |||||||||
| Factor Name | Solute carrier family 29 member 1 |
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Structure
Sequence
MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDAQASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAILLVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQGLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKLEGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIFTITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRWLPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPKKVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
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| 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).
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| Mechanism Description |
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| Recommended Action | |||||||||
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| 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. | ||||||||