Verzenios ® (abemaciklib)

För fullständig produktresumé för Verzenios se FASS.

Denna information är endast avsedd för sjukvårdspersonal verksam i Sverige och som svar på din fråga. Informationen nedan är på engelska

Verzenios® ▼ (abemaciclib): Verkningsmekanism

Verzenios (abemaciclib) är en hämmare av cyklinberoende kinaser 4 och 6 (CDK4 och CDK6) vilken med kontinuerlig exponering resulterade i senescens och apoptos.

Detailed Information

Abemaciclib is an inhibitor of CDK4 and CDK6. These kinases are activated upon binding to D-cyclins. In breast cancer cell lines, cyclin D1/CDK4  has been shown to promote phosphorylation of the Rb, cell proliferation, and tumor growth. Abemaciclib prevents Rb phosphorylation, blocking progression from G1 into S phase of the cell cycle, leading to suppression of tumor growth in preclinical models following short duration target inhibition. In ER+ breast cancer cell lines, sustained target inhibition by abemaciclib prevents rebound of Rb phosphorylation and cell cycle reentry, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption at clinically relevant concentrations, as a single agent or in combination with antiestrogens, resulted in reduction of tumor size.1,2

Reference

1. Data on file, Eli Lilly and Company and/or one of its subsidiaries.

2. Verzenios [summary of product characteristics]. Eli Lilly Nederland B.V., The Netherlands.

Glossary

CDK = cyclin-dependent kinase

HR+ = hormone receptor-positive

Rb = retinoblastoma protein

This medicinal product is subject to additional monitoring. This will allow quick identification of new safety information. Healthcare professionals are asked to report any suspected adverse reactions.

Datum fӧr senaste ӧversyn 2018 M10 11

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