GPR109A agonist
- Suppresses adipocyte lipolysis → altered lipid handling
- Raises HDL and lowers triglycerides
- Prostaglandin release through the same receptor causes the flushing
Drugs with this mechanism (3)
- Dimethyl fumarate — Oral MS drug acting through Nrf2; limited by flushing and lymphopenia.
- Diroximel fumarate — Dimethyl fumarate reformulated for less GI upset; same active metabolite.
- Niacin — Vitamin B3; NAD precursor and lipid agent, causes GPR109A-mediated flushing.
Self-check
- Which adipocyte process does niacin receptor activation suppress?
Lipolysis. - What causes niacin-related flushing through the same receptor?
Prostaglandin release.
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