Trends in GPCR drug discovery: new agents, targets and indications.
Level 5 - mechanism / opinion, no new human data
Level is by design analogy (descriptive landscape and database review with no clinical trial intervention data)
PubMed 29075003 · doi:10.1038/nrd.2017.178
What was done
The authors performed an analysis of all GPCR drugs and agents in clinical trials, evaluating trends across molecule types, drug targets, and therapeutic indications.
What was found
A total of 475 drugs (~34% of all FDA-approved drugs) act at 108 unique GPCRs. Approximately 321 agents are in clinical trials, of which ~20% target 66 potentially novel GPCR targets without an approved drug. Biological drugs, allosteric modulators, and biased agonists have increased. Major indications show a shift towards diabetes, obesity, and Alzheimer disease, while central nervous system disorders remain highly represented. In addition, 224 (56%) non-olfactory GPCRs have not yet been tested in clinical trials.
Why it matters
This paper quantifies the contribution of GPCRs to the modern pharmacopeia and identifies that more than half of non-olfactory GPCRs remain completely unexplored in clinical development.
Limits
The abstract does not disclose the specific databases, search strategies, or date ranges used for data extraction. As a descriptive overview, it does not evaluate trial design quality, drug efficacy, or safety outcomes.
Cited by
- supports Approximately 35% of all FDA-approved drugs (around 700 drugs) interact with G-protein coupled receptors (GPCRs).