The ghrelin receptor inverse agonist PF-5190457 did not significantly alter levels of 13 other hormones in heavy drinkers, supporting its safety profile for alcohol use disorder treatment.
13 hormones unchangedInsulin, GLP-1, cortisol, thyroid, leptin, and 8 others unaffected by ghrelin receptor blockade
What the researchers found
PF-5190457 did not significantly alter blood levels of 13 hormones (including insulin, GLP-1, cortisol, thyroid hormones, and leptin) during dosing or alcohol co-administration.
Why it matters
For a drug targeting the ghrelin system (which intersects with appetite, growth hormone, and metabolism), showing minimal hormonal side effects is critical for clinical development.
The numbers in context
13 hormones measured; largely unaffected during dosing and alcohol challenge; Phase 1b placebo-controlled
How the study worked
Placebo-controlled Phase 1b human laboratory study in heavy drinkers. PF-5190457 dosed to steady state, then alcohol challenge administered. Blood drawn for 13 hormone panels at multiple timepoints.
Who was studied
Heavy drinking individuals (human)
What this study cannot tell us
Small Phase 1b study (exact N not specified); short-term dosing only; endocrine safety over months/years of use unknown; efficacy for reducing drinking not reported here.
How to read the evidence
Moderate — placebo-controlled human trial but small Phase 1b with focus on safety/endocrine endpoints rather than efficacy.
When this study was published
Published in 2020; ghrelin-targeted therapies for addiction remain in early clinical development.
The bigger picture
There are currently no FDA-approved drugs targeting the ghrelin system. If PF-5190457 proves effective for alcohol use disorder with a clean safety profile, it would represent a novel treatment approach.
Questions still open
- Does PF-5190457 actually reduce alcohol consumption or cravings in larger trials?
- Would long-term ghrelin receptor blockade affect growth hormone or metabolism?
- Could this drug help with other ghrelin-related conditions like binge eating?
Common questions
How does blocking ghrelin help with alcohol problems?
Is this drug available for use?
Read the original research
Endocrine effects of the novel ghrelin receptor inverse agonist PF-5190457: Results from a placebo-controlled human laboratory alcohol co-administration study in heavy drinkers.
Neuropharmacology, 170, 107788
Citation
Lee, Mary R; Farokhnia, Mehdi; Cobbina, Enoch; Saravanakumar, Anitha; Li, Xiaobai; Battista, Jillian T; Farinelli, Lisa A; Akhlaghi, Fatemeh; Leggio, Lorenzo. (2020). Endocrine effects of the novel ghrelin receptor inverse agonist PF-5190457: Results from a placebo-controlled human laboratory alcohol co-administration study in heavy drinkers.. Neuropharmacology, 170, 107788. https://doi.org/10.1016/j.neuropharm.2019.107788