Orforglipron

Areas of active research — not promised effects

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Orforglipron (brand name Foundayo, Eli Lilly) received FDA approval on April 1, 2026 under NDA 220934 for chronic weight management as an adjunct to a reduced-calorie diet and increased physical activity in adults with obesity (BMI ≥30) or adults with overweight (BMI ≥27) with at least one weight-related comorbid condition. It is a Schedule-uncontrolled prescription drug dispensed by licensed pharmacies with a valid prescription. A separate NDA for the type 2 diabetes indication was in regulatory review. As an approved drug, it is not subject to the FDA 503A/503B compounding bulk-drug Category-2 restrictions (fda19=false); compounding of an approved drug formulation is generally prohibited without specific FDA guidance.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Orforglipron

Origin

Synthetic non-peptide small molecule (formerly LY3502970) designed by Eli Lilly medicinal chemistry as an orally bioavailable agonist of the class B1 G-protein-coupled GLP-1 receptor. Its core scaffold is a bicyclic pyrazolo[4,3-c]pyridine bearing multiple stereocentred substituents including fluorinated aryl groups and an oxadiazolone moiety (CAS 2212020-52-3, molecular formula C48H48F2N10O5, MW ~883 g/mol). It is structurally unrelated to endogenous GLP-1 peptide or any peptide-based GLP-1 analogue.

Registry IDs

PubChem CID

137319706

CAS

2212020-52-3

InChIKey

USUWIEBBBWHKNI-KHIFEHGGSA-N

DrugBank

DB18964

ChEMBL

CHEMBL4446782

Molecular formula

C48H48F2N10O5

Molar mass

883.0 g/mol

Monoisotopic

882.37772099 Da

InChIKey

USUWIEBBBWHKNI-KHIFEHGGSA-N

Appearance

White to off-white to pale yellow solid powder; the molecular scaffold contains multiple aromatic rings, fluorinated substituents, and a cyclopropyl group consistent with a dense small-molecule API (MW ~883 g/mol, molecular formula C48H48F2N10O5)

Solubility

Oral bioavailability approximately 79% without food restrictions, indicating fav…

Sequence not available in current seed.

Stability: The pyrazolopyridine/oxadiazolone scaffold is subject to CYP3A4-mediated oxidative metabolism in vivo (primary hepatic clearance); fecal elimination accounts fo

Vial sizes

null mg · null mg

Purity grades

pharmaceutical grade (approved product)

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Orforglipron acts as a non-peptide, allosteric agonist at the GLP-1 receptor (GLP-1R), engaging primarily within the transmembrane domain rather than the orthosteric peptide-binding cleft occupied by endogenous GLP-1 and injectable peptide analogues
• Receptor engagement drives Gs-biased signalling, elevating intracellular cAMP and intracellular calcium in a glucose-dependent manner, thereby stimulating insulin secretion from pancreatic beta cells, suppressing postprandial glucagon release, and slowing gastric emptying
• Central GLP-1R activation along appetite-regulatory circuits in the hypothalamus and brainstem reduces food intake and promotes satiety
• Compared with peptide GLP-1RAs, the small-molecule scaffold of orforglipron may confer deeper CNS penetration, reaching reward-related brain regions implicated in food craving suppression

Pharmacokinetics (ADME)

Half-life

Approximately 24–35 hours after single oral doses (0.3–6 mg range); extends to approximately 48–68 hours at steady state during multiple-dose administration (2–24 mg range); supports once-daily oral dosing

Clearance

Primarily hepatic via CYP3A4-mediated oxidative metabolism; fecal elimination accounts for approximately 87% of total radioactivity; urinary excretion minimal (~0.2%)

PK–PD note: Absolute oral bioavailability is approximately 79%, markedly superior to peptide-based oral GLP-1 formulations. Unlike oral semaglutide (Rybelsus), orforglipron absorption is not affected by food or w…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Lütkemeyer et al. 2024 — Effects of once-daily oral orforglipron on weight and metabolic markers: a systematic review and meta-analysis of RCTs (4 RCTs, 815 patients) — Anchoring systematic review; Arch Endocrinol Metab, PMID 39420937
• Karakasis et al. 2023 — Safety and efficacy of oral small-molecule GLP-1 RAs orforglipron and danuglipron: systematic review and meta-analysis of RCTs — Metabolism 2023;148:155710
• Orforglipron: A Comprehensive Review of an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity and Type 2 Diabetes
• Efficacy and Safety of Oral GLP-1 RA Orforglipron on Weight and Glycemic Control According to Diabetes Status: A Systematic Review and Meta-Analysis
• Pandey et al. 2025 — Efficacy and Safety of Orforglipron in Obese Adults With or Without Diabetes: A Systematic Review and Meta-Analysis (5 RCTs, 4410 participants)

5 registered trials — 1 currently recruiting.

Phase 1
NCT06023095
A Study of LY3502970 in Chinese Participants With Obesity or Are Overweight With Weight-related Comorbidities

COMPLETED

Phase 3
NCT06672939
A Study of Orforglipron (LY3502970) in Adolescent Participants With Obesity, or Overweight With Related Comorbidities

RECRUITING

Phase 1
NCT05841238
A Multiple Dose Study of LY3502970 in Healthy Overweight and Obese Participants

COMPLETED

Phase 1
NCT05051566
A Multiple Dose Study of LY3502970 in Healthy Participants

COMPLETED

Phase 1
NCT06824051
A Study of Orforglipron (LY3502970) in Adult Participants With Obesity or Overweight

COMPLETED

Summary (literature)

The safety profile of orforglipron in Phase 3 trials is consistent with the GLP-1 receptor agonist drug class. The most common adverse reactions reported at a frequency of 5% or greater in the approved indication include nausea (up to ~36%), constipation (~30%), diarrhea (~27%), …

WADA status

GLP-1 receptor agonists as a class (specifically semaglutide and tirzepatide) entered the WADA 2026 Monitoring Program effective January 1, 2026, to detect pote…

Dominant research route: PO (oral)

Phase 1a single/multiple ascending dose, Phase 1 food-effect, Phase 1 absolute bioavailability, Phase 2 dose-response, and Phase 3 (ATTAIN-1, ATTAIN-2) trials in humans (healthy adults and patients with obesity/T2D)

Bioavailability: Mean absolute oral bioavailability 79.1% ± 16.8% measured versus IV microtracer in healthy participants (Morse et al., Clin Pharmacol Drug Dev 2026); earlier preclinical/early-clinical reviews cited ~20–40%. Food lowers AUC/Cmax by ~18–24% (not considered clinically meaningful). Half-life ~24.6–35.3 h (single dose) and ~48–67 h (Day 28).

Orforglipron (LY3502970) is a non-peptide small-molecule GLP-1 receptor agonist designed for once-daily oral administration without food/liquid restrictions or absorption enhancers. Oral is the only route administered therapeutically across all clinical trials.

IV microtracer reference dose administered to healthy participants in a Phase 1 absolute-bioavailability study (Study A) for PK mass-balance only

Bioavailability: Used solely as the reference comparator to calculate absolute oral bioavailability (79.1% ± 16.8%); not a therapeutic route.

IV was used only as a microtracer route in the disposition/absolute-bioavailability study to enable mass-balance and bioavailability calculation; orforglipron is not developed or administered as an IV therapeutic.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Weekly median $/mg from the live vendor crawl.

Researched storefront prices, bucketed

p25 $0.368 · median $0.372 · p75 $0.387 · 6 researched vendors

Legit, COA-backed band: $0.350–$0.450/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$4

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Independent labs cited for this compound

No FDA recalls, market withdrawals, or safety alerts specific to Foundayo (orforglipron) were found in the FDA Enforcement Reports or Recalls databases as of the search date; the product was approved April 1, 2026 and no recall events have been published.

Buyer red-flag checklist

• Orforglipron is a newly approved (April 1, 2026) prescription drug; no FDA-approved generic exists — any 'generic orforglipron' offered online is fraudulent and potentially counterfeit.
• Oral tablet form is easier to counterfeit than injectable GLP-1s (pill press + powders), increasing risk of falsified product with incorrect dose, incorrect active ingredient, or no active ingredient.
• Foreign-sourced orforglipron API is subject to FDA Detention Without Physical Examination under Import Alert 66-80 unless the manufacturer is on the Green List.
• FDA found 21% of 48 evaluated GLP-1 API manufacturing sites noncompliant with CGMP, indicating heightened adulteration risk for bulk GLP-1 substances used in compounding.
• Compounded or 'research-use-only' orforglipron is not FDA-approved and has not been evaluated for safety, purity, or potency; no USP reference standard exists for orforglipron.

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No independent third-party lab tests (Janoshik, MZ Biolabs, Finnrick, or equivalent) of orforglipron were located. Orforglipron is a small-molecule (non-peptide) GLP-1 receptor agonist supplied as FDA-approved Foundayo tablets rather than as a gray-market research peptide, so the peptide-purity/underdosing testing ecosystem does not currently apply.

• Detention Without Physical Examination (DWPE) of Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Bulk Drug Substances. Revised 06/22/2026 to add Orforglipron API and FDA Product Code 61P[][]77 (Anti-Diabetic). FDA evaluated 48 GLP-1 API sites and found 21% noncompliant under section 501 of the FD&C Act (CGMP failures or failure to respond to 704(a)(4) records requests); foreign-sourced GLP-1 APIs are subject to DWPE based on appearance of adulteration except firms/products on the Green List.66-80
• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Not on the WADA 2026 Prohibited List; GLP-1 receptor agonists are included in WADA's 2026 Monitoring Program (in-competition monitoring to detect patterns of misuse). Orforglipron is not specifically named but falls within the GLP-1 receptor agonist class under monitoring.

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• Manufacturer-affiliated channels (Lilly official YouTube, LillyDirect) present in discourse
• Trial-participant self-selection bias in anecdotal reports
• Newly approved drug (April 2026) — limited long-term real-world data
• US-centric access/insurance framing

Manually researched from reddit, youtube— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
• Free base vs acetate
• Understanding evidence grades

FDA-approved oral small-molecule GLP-1 receptor agonist (Foundayo, Eli Lilly) for chronic weight management in adults; first pill-form GLP-1RA with no food or water dosing restrictions. Approximately 92 articles are indexed (literature last scanned 2026-05-29). US regulatory status: FDA-approved prescription drug (Foundayo) — April 1, 2026. Research use only.

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