Abemaciclib inhibits renal tubular secretion without changing glomerular filtration rate.

07:00 EST 17th November 2018 | BioPortfolio

Summary of "Abemaciclib inhibits renal tubular secretion without changing glomerular filtration rate."

Abemaciclib, an inhibitor of cyclin dependent kinases 4 and 6, is indicated for metastatic breast cancer treatment. Reversible increases in serum creatinine levels of approximately 15%-40% over baseline have been observed following abemaciclib dosing. This study assessed the in vitro and clinical inhibition of renal transporters by abemaciclib and its metabolites using metformin (a clinically relevant transporter substrate), in a clinical study that quantified glomerular filtration and iohexol clearance, In vitro, abemaciclib inhibited metformin uptake by OCT2, MATE1 and MATE2-K transporters with an IC50 of 0.4-3.8 μM. Clinically abemaciclib significantly increased metformin exposure but did not significantly affect measured glomerular filtration rate, serum NGAL, serum cystatin C or the urinary markers of kidney tubular injury, NGAL and KIM-1,. This article is protected by copyright. All rights reserved.


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This article was published in the following journal.

Name: Clinical pharmacology and therapeutics
ISSN: 1532-6535


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