I came across a protocol by Dmitry Kats, who claims to have a PhD in epidemiology and is selling his capsules via purebulk.com. The protocol is basically intended to upregulate the GPR109a niacin receptor pathway with this promise: "to prevent along with revert disease, promote health forward, even 'anti-age,' and so much more." It involves a starting dose of 4 grams of nicotinic acid (a truly punishing dose) with proportionate amounts of folic acid and n-acetylglutamine (https://hom3ostasis.com/protocol/). There seems to be a lack of evidence-based rationale for the combination of supplements or their strict ratio. Kats advises on his protocol website: “Try to avoid Rx &/or wean off. This is VERY possible.” – an obvious red flag. Apparently Twitter banned him but he seems to have a new Twitter account and is back to making outlandishly questionable statements e.g., about the COVID vaccine being spiked with drugs.
Despite the above concerns, the GPR109a pathway has promise e.g., in areas such as neuroinflammation, but the folic acid and acetylglutamine in the Kats protocol may not add much. There should be a protocol for GPR109a but not this one.
Aside from niacin, there may be GPR109a agonists that are flush-free and reduce niacin’s flush while having unique benefits that round out niacin’s effect. For example, moderate dose niacin could be combined with GPR109a-targeting Beta-hydroxybutyrate (BHB) as well as butyrate-producing probiotics.
I don’t think a GPR109a protocol should aim to max out the receptor, due to apparent hormesis. One caveat reminiscent of other protocols:
Our results suggest that strong GPR109A agonists, if developed, may have a narrow therapeutic dose range for anti-inflammatory activity without causing cell death.
Any thoughts on boosting GPR109a?