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 a potent and selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6), and most active against Cyclin D1/CDK4 in enzymatic assays. Abemaciclib prevents retinoblastoma protein (Rb) phosphorylation, blocking cell cycle progression from the G1 to the S‑phase of cell division, leading to suppression of tumour growth. In oestrogen receptor‑positive breast cancer cell lines, sustained target inhibition with abemaciclib prevented rebound of Rb phosphorylation resulting in cell senescence and apoptosis. In vitro, Rb-negative and Rb-depleted cancer cell lines are generally less sensitive to abemaciclib. In breast cancer xenograft models, abemaciclib dosed daily without interruption at clinically relevant concentrations alone or in combination with anti-oestrogens resulted in reduction of tumour size.1

Verzenios is indicated for the treatment of women with hormone receptor positive (HR+), human epidermal growth factor receptor 2 (HER2) negative locally advanced or metastatic breast cancer in combination with an aromatase inhibitor or fulvestrant as initial endocrine-based therapy, or in women who have received prior endocrine therapy.1

Reference

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

Glossary

CDK = cyclin-dependent kinase

HER2 = human epidermal growth factor receptor 2

HR+ = hormone receptor-positive

LHRH = luteinising hormone-releasing hormone

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 2017 M08 17

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