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April 10, 2026Open Access

Ribociclib is not a substrate or inhibitor of Oatp1b-mediated uptake in vivo

Key Points

The research aims to clarify the interactions of ribociclib with OATP1B and its implications for drug co-administration.
Conducted in vivo analysis of ribociclib's effects on OATP1B
Evaluated ribociclib as a substrate and inhibitor of OATP1B
Examined potential clinically significant interactions
Ribociclib does not act as a substrate for OATP1B
Ribociclib does not inhibit OATP1B-mediated uptake
No anticipated significant drug interactions with OATP1B

Abstract

Our findings suggest that clinically significant OATP1B-mediated interactions are not anticipated with CDK4/6 inhibitors, either as victims or perpetrators, which supports ongoing clinical trials investigating the co-administration of CDK4/6 inhibitors with OATP1B substrates and inhibitors.

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Ribociclib is not a substrate or inhibitor of Oatp1b-mediated uptake in vivo | Synapse

Cite This Study

Drabison et al. (Tue,) studied this question.

synapsesocial.com/papers/69d894ce6c1944d70ce05b3d https://doi.org/https://doi.org/10.1007/s00280-026-04877-x