{"id":"6ff70aee-5ef5-5352-a373-a630ac53f6e2","stable_key":"1bbf9d44-8d2b-5b35-8f82-f6876558b0b3:cyclosporine-inhibits-oatp1b1","predicate":"inhibits","statement":"Cyclosporin A inhibited OATP2-mediated uptake of labelled cerivastatin in transporter-expressing MDCKII cells with a Ki of 0.2 micromolar.","claim_class":"mechanistic","status":"source_derived_draft","evidence_grade":"ungraded","direction":"negative","is_public":true,"mechanism_event_id":"9d549946-46b5-507f-9843-9596bcf0dfd5","mechanism_event_label":"Cyclosporin A inhibited OATP2-mediated uptake of labelled cerivastatin in transporter-expressing MDCKII cells with a Ki of 0.2 micromolar.","subject":{"id":"b199063a-fae6-5c5c-9cb4-22c10453bbac","slug":"cyclosporine","display_name":"Cyclosporine","entity_type_key":"drug"},"object":{"id":"38b2f200-15ca-5db6-8d7e-2b78ee490eda","slug":"slco1b1","display_name":"Human OATP1B1 / SLCO1B1","entity_type_key":"protein"},"evidence_count":1,"mechanism_event":{"id":"9d549946-46b5-507f-9843-9596bcf0dfd5","stable_key":"1bbf9d44-8d2b-5b35-8f82-f6876558b0b3:cyclosporine-inhibits-oatp1b1-event","event_type":"biochemical_relationship","label":"Cyclosporin A inhibited OATP2-mediated uptake of labelled cerivastatin in transporter-expressing MDCKII cells with a Ki of 0.2 micromolar.","description":"Hepatic sinusoidal uptake transport","status":"provisional","compartment":null,"participants":[{"entity":{"id":"b199063a-fae6-5c5c-9cb4-22c10453bbac","slug":"cyclosporine","display_name":"Cyclosporine","entity_type_key":"drug"},"role":"acting component","stoichiometry":null,"state_label":"","sequence_order":0,"notes":""},{"entity":{"id":"38b2f200-15ca-5db6-8d7e-2b78ee490eda","slug":"slco1b1","display_name":"Human OATP1B1 / SLCO1B1","entity_type_key":"protein"},"role":"component the finding is about","stoichiometry":null,"state_label":"","sequence_order":1,"notes":""}]},"contexts":[{"dimension":"duration","value_text":"Not stated here","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"evidence_access","value_text":"Primary PubMed abstract and indexed metadata reviewed. Full-text method details not stated here remain unresolved.","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"experimental_model","value_text":"Human OATP2 (OATP1B1 / SLCO1B1) expressed in MDCKII cells","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"exposure","value_text":"Cyclosporin A","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"limitations","value_text":"The transporter is named OATP2 in this 2003 report, which is the protein now called OATP1B1 and encoded by SLCO1B1; the same entity is reused here rather than forked. The Ki is for cerivastatin as the probe substrate and does not transfer unchanged to other OATP1B1 substrates.","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"organism","value_text":"Human OATP2 (OATP1B1 / SLCO1B1) expressed in MDCKII cells","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"plain_language","value_text":"Cyclosporin A inhibited OATP2-mediated uptake of labelled cerivastatin in transporter-expressing MDCKII cells with a Ki of 0.2 micromolar.","comparator":null,"unit":null,"notes":"","entity":null},{"dimension":"primary_references","value_text":"Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. 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No reference carries a recorded retraction, erratum or expression of concern. Each of the seven is a separate laboratory and each carries its own lineage key, so none of them can be counted twice as independent support. Study-specific concentrations, kinetic constants and limitations retained. Not publisher full text.","file_path":"","sha256":"499d00555a629cba2271c3888d7e93627949891d565c4c78c843610de2913080","revision_id":"263ee68a-4184-51d0-a977-197d7ddb7a4d","review_status":"unverified_draft","notes":""}}],"relations":[],"conflicts":[],"corrections":[],"research":null}