- Reaction score
- 732
Per the BAY patent:Let's hope SMI will be enough but I'm not sure as pegasus already stated before:
There is SMI-1 and SMI-6 that @FollicleGuardian found for a cheap price. It's not the same though. Per the patent, competitive antagonists of the receptor are ineffective in the hair follicle because concentrations of prolactin are too high since it's produced within the hair follicle, and prolactin has a higher binding affinity for the receptor than the antagonists.
This might be why the small molecule antagonists don't include hair loss as a potential indication in the patent.
The antibody is a non-competitive inhibitor, meaning that it doesn't have to outcompete prolactin for receptor binding. It can bind to the receptor along with prolactin and still silence it.
I think the competitive antagonists are likely better than nothing, but they won't give the kind of regrowth the antibody does
competitive PRLR antagonists are not effective in neutralizing local PRL signaling in the hair follicle due to their negative characteristics which are
1) a reduced PRLR inhibition in the presence of increasing PRL concentrations due to the competitive mechanism of action
2) reduced half-life
3) reduced affinity to the PRLR if compared to PRL.
SMI has already solved no 2. It also has very strong affinity to the PRL receptor. Kd= 3.3. It remains to be seen if it is enough to solve 1, and 3.