- Reaction score
- 3,656
He only used it 3xW, assumedly this has strong effect through suppression of AR geneexpression or it acts systemically. I doubt the effect comes from only local blocking AR, since I dont think the effect can be sustained 2 days without going systemic.
I wonder if longer half-life in anti-androgen means longer blockage of the receptor independt the drugconcentration at receptor site. What are the factors for how long time a drug block a receptor? I guess affinity and ofc receptor at concentration site, but anyone that can explain this further?
Enzalutamide lacks the partial agonist activity notable with other non-steroidal anti-androgens, and given its activity not just as an inhibitor of the androgen receptor, but pre-clinically to inhibit nuclear translocation of the AR and inhibit the association of AR with DNA, further differentiates it from other anti-androgens (figure1).
SOURCE: http://clincancerres.aacrjournals.o...rly/2013/01/08/1078-0432.CCR-12-2910.full.pdf
No data about how long it binds to the receptors sadly.