Braf-Inhibitoren
Encorafenib
| Molekulargewicht | 540,01 g/mol |
| Halbwertszeit | > 24 h (Lemech et al. 2013) |
| Mechanismus / Effekt | induces sustained mitogen-activated protein kinase (MAPK) pathway inhibition and has selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E |
| Erkrankung / Tumorentität | 6 mg/kg in human melanoma xenograft models, unresectable or metastatic melanoma |
| IC 50 | EC50 = 4nM (Darrin D Stuart et al. 2012) |
| ? | c(t=1,9h) = 1527 ng/mL (200 mg, n = 1) (Sparidans et al 2016) |
| eigene Forschungsergebnisse | kaum Unterschied +2Gy (M. Steck Vortrag DEGRO 2017) |
| Literatur | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3724517/ http://link.springer.com/article/10.1007%2Fs40265-013-0049-8 |