NO. 020 · INCRETIN
ORAL GLP-1 RECEPTOR MIMETIC
Small-molecule receptor activator
ALIASES
oral-glp1-receptor-mimetic, LY3502970, oral GLP-1 small molecule
CLASS
Non-peptide oral GLP-1 receptor allosteric agonist (the originator pharma sponsor)
FORMULA
Small molecule · oral bioavailable
HALF-LIFE
~24-30 hours (once-daily oral)
ROUTES
Oral (Phase 3 clinical)
MECHANISM OF ACTION
the originator pharma sponsor oral non-peptide small-molecule GLP-1 receptor agonist (LY3502970). First oral GLP-1 designed for once-daily tablet dosing, bypassing the injection requirement of peptide GLP-1s. ACHIEVE-1 Phase 3 readout expected 2026.
EVIDENCE GRADES
Wharton 2023 NEJM · placebo-subtracted weight loss ~14.7% at 45 mg/day in 36-week Phase 2.
Frias 2023 NEJM · HbA1c reduction up to ~2.1%.
SAFETY
Side effects
- GI: nausea, diarrhea, vomiting (titration-dependent)
- Decreased appetite
Drug interactions
- Standard GLP-1 class · oral medication absorption (delayed gastric emptying)
Contraindications
- History of MTC or MEN2 (class precaution)
REGULATORY STATUS
FDA · Investigational. Phase 3 ACHIEVE/ATTAIN programs ongoing.
WADA · Not currently listed on the WADA Prohibited List.
STORAGE
Lyophilized · n/a · tablet formulation
Reconstituted · n/a
PEER-REVIEWED EVIDENCE
- Wharton S, et al.. Daily Oral GLP-1 Receptor Agonist the oral GLP-1 receptor mimetic for Adults with Obesity. N Engl J Med 2023. PMID 37364188. link →
FAQ · 6 QUESTIONS
▶ What is the oral GLP-1 receptor mimetic?
the oral GLP-1 receptor mimetic (LY3502970) is an orally bioavailable non-peptide small-molecule allosteric agonist of the GLP-1 receptor developed by the originator pharma sponsor. It is the first oral GLP-1 candidate that does not require the specialized absorption formulation used by oral the long-acting GLP-1 agonist.
▶ How is the oral GLP-1 receptor mimetic different from the long-acting GLP-1 agonist?
the oral GLP-1 receptor mimetic is a small molecule taken orally without dietary restriction. the long-acting GLP-1 agonist is a peptide that requires subcutaneous injection or a specialized oral formulation taken on an empty stomach with limited water and at least 30 minutes before eating.
▶ What weight loss has Phase 2 shown?
Phase 2 obesity (Wharton 2023 NEJM) reported up to ~14.7% placebo-subtracted weight loss at 45 mg daily over 36 weeks. Phase 3 enrolling.
▶ Is the oral GLP-1 receptor mimetic FDA-approved?
Not yet as of 2026-05. Phase 3 ACHIEVE-1 (T2D) and ATTAIN-1 (obesity) programs are ongoing.
▶ How does it work?
the oral GLP-1 receptor mimetic is a positive allosteric modulator of the GLP-1 receptor. It binds outside the orthosteric peptide-binding pocket and stabilizes the active receptor conformation, producing functional agonist activity.
▶ Daily dose in trials?
Phase 2 used daily oral doses of 12 mg to 45 mg. This wiki does not recommend any human dose.
SIGNATURE MOVES
Skips injection. Once-daily tablet.
ACHIEVE-1 Phase 3 program. Body-weight reduction.
SOURCED FROM GIGACOMPOUNDS
Reference compounds documented on this page are available as research-grade material at GigaCompounds · ≥99% purity · per-batch Certificate of Analysis. For laboratory research use only. No human dose is recommended by this wiki.
▶ LAST UPDATED · 2026-05-19