Retsevmo ® (selperkatinib)

För fullständig produktresumé för Retsevmo se FASS.

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

Vilken verkningsmekanism har Retsevmo® ▼ (selperkatinib)?

Selperkatinib är en hämmare av RET-tyrosinkinasreceptorn (RET = rearranged during transfection). Selperkatinib hämmade vildtyp-RET och flera muterade RET-isoformer.

Mechanism of Action

Selpercatinib is a kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC50 values ranging from 0.92 nM to 67.8 nM. 1

In other enzyme assays, selpercatinib also inhibited FGFR 1, 2, and 3 at higher concentrations that were still clinically achievable.1

Certain point mutations in RET or chromosomal rearrangements involving in-frame fusions of RET with various partners can result in constitutively activated chimeric RET fusion proteins that can act as oncogenic drivers by promoting cell proliferation of tumor cell lines. In in vitro and in vivo tumor models, selpercatinib demonstrated anti-tumor activity in cells harboring constitutive activation of RET protein resulting from gene fusions and mutations, including

  • CCD6-RET

  • KIF5B-RET

  • RET V804M, and

  • RET M918T.1

Selpercatinib showed antitumor activity in mice intracranially implanted with a patient-derived RET fusion positive tumor.1

References

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

Glossary

CCDC6 = coiled-coil domain containing 6

FGFR = fibroblast growth factor receptor

IC50 = half maximal inhibitory concentration 

KIF5B = kinesin family member 5B

RET = rearranged during transfection

VEGFR = vascular endothelial growth factor receptor

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 January 21, 2021


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