Ghrelin Receptor Blocker for Alcohol Use Disorder Doesn't Disrupt Other Hormones
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.
Quick Facts
What This Study 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.
Key Numbers
13 hormones measured; largely unaffected during dosing and alcohol challenge; Phase 1b placebo-controlled
How They Did This
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.
Why This Research 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 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.
What This Study Doesn't 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.
Questions This Raises
- ?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?
Trust & Context
- Key Stat:
- 13 hormones unchanged Insulin, GLP-1, cortisol, thyroid, leptin, and 8 others unaffected by ghrelin receptor blockade
- Evidence Grade:
- Moderate — placebo-controlled human trial but small Phase 1b with focus on safety/endocrine endpoints rather than efficacy.
- Study Age:
- Published in 2020; ghrelin-targeted therapies for addiction remain in early clinical development.
- Original Title:
- 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.
- Published In:
- Neuropharmacology, 170, 107788 (2020)
- Authors:
- Lee, Mary R(3), Farokhnia, Mehdi(8), Cobbina, Enoch, Saravanakumar, Anitha, Li, Xiaobai, Battista, Jillian T, Farinelli, Lisa A, Akhlaghi, Fatemeh, Leggio, Lorenzo
- Database ID:
- RPEP-04934
Evidence Hierarchy
Frequently Asked Questions
How does blocking ghrelin help with alcohol problems?
Ghrelin, the "hunger hormone," also drives alcohol cravings. Blocking its receptor may reduce the urge to drink.
Is this drug available for use?
No — it's still in early clinical trials. This study focused on confirming it doesn't cause hormonal side effects.
Read More on RethinkPeptides
Cite This Study
https://rethinkpeptides.com/research/RPEP-04934APA
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
MLA
Lee, Mary R, et al. "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, 2020. https://doi.org/10.1016/j.neuropharm.2019.107788
RethinkPeptides
RethinkPeptides Research Database. "Endocrine effects of the novel ghrelin receptor inverse agon..." RPEP-04934. Retrieved from https://rethinkpeptides.com/research/lee-2020-endocrine-effects-of-the
Access the Original Study
Study data sourced from PubMed, a service of the U.S. National Library of Medicine, National Institutes of Health.
This study breakdown was produced by the RethinkPeptides research team. We analyze and report published research findings without making health recommendations. All interpretations are based solely on the published abstract and study data.