Danuglipron

Areas of active research — not promised effects

Each tag links to other compounds with research into that goal. Research use only: these are areas of study, not human-use claims.

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Danuglipron was evaluated under an Investigational New Drug (IND) application throughout its clinical programme but never received FDA approval. Pfizer formally discontinued development in April 2025. The compound has no approved indication, no authorised label, and is not available through commercial or compounding pharmacy channels. It is not a compound subject to the FDA Category-2 503A/503B compounding bulk-drug restrictions (fda19=false); however, manufacture or supply without an active IND is not authorised.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Danuglipron

Origin

Synthetic benzimidazole-carboxylic acid derivative designed by Pfizer medicinal chemistry to function as a non-peptide, orally bioavailable agonist of the class B1 G-protein-coupled GLP-1 receptor; CAS 2230198-02-2. It is structurally unrelated to peptide GLP-1 analogues (e.g., semaglutide, liraglutide) but acts at the same receptor target.

Registry IDs

PubChem CID

134611040

CAS

2230198-02-2

InChIKey

HYBAKUMPISVZQP-DEOSSOPVSA-N

DrugBank

DB16043

ChEMBL

CHEMBL4518483

Molecular formula

C31H30FN5O4

Molar mass

555.6 g/mol

Monoisotopic

555.22818262 Da

InChIKey

HYBAKUMPISVZQP-DEOSSOPVSA-N

Appearance

White to off-white solid powder (typical for benzimidazole small-molecule APIs); molecular formula C31H30FN5O4, MW 555.6 g/mol

Solubility

Small-molecule with fluorobenzyl and oxetane substituents; solubility characteri…

Sequence not available in current seed.

Stability: Benzimidazole carboxylic acid scaffold is susceptible to hydrolysis under extreme pH; fluorobenzyl ether and nitrile substituents are generally stable. Metaboli

Vial sizes

null mg

Purity grades

research grade

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

• Danuglipron binds directly to the extracellular face of the glucagon-like peptide-1 receptor (GLP-1R), a class B1 GPCR, forming critical van der Waals contacts with Trp33 and hydrogen-bonding interactions with extracellular loops 1 and 2
• This orthosteric engagement stabilises an active receptor conformation, driving adenylyl cyclase activation and intracellular cAMP accumulation along with increased intracellular Ca2+ levels — the same downstream cascade activated by native GLP-1 and peptide analogues
• The resulting signalling stimulates glucose-dependent insulin secretion from pancreatic beta cells, suppresses postprandial glucagon release, slows gastric emptying, and engages central satiety circuits to reduce food intake
• Unlike injectable peptide GLP-1RAs, danuglipron's small-molecule scaffold enables oral administration with a pharmacokinetic profile supporting once- or twice-daily dosing

Pharmacokinetics (ADME)

Half-life

Approximately 29–49 hours (dose-dependent); supports once-daily or twice-daily oral dosing in clinical studies

Clearance

Not fully characterised in public disclosures; hepatic/metabolic clearance assumed given small-molecule scaffold and CYP-mediated drug-drug interaction signals identified in phase 1 studies

PK–PD note: Phase 1 PK optimisation studies (NCT04616339, NCT06568731) evaluated modified-release formulations to reduce peak-to-trough variability and gastrointestinal burden. A once-daily modified-release formu…

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

• Karakasis P, et al. Safety and efficacy of the new, oral, small-molecule, GLP-1 receptor agonists orforglipron and danuglipron... systematic review and meta-analysis. Metabolism. 2023 Dec;149:155710 — Anchoring systematic review/meta-analysis; 7 RCTs, 1037 patients; searched Medline/Cochrane/Scopus to Aug 16 2023
• Evaluating Glycemic Control Efficacy and Safety of the Oral Small Molecule GLP-1 RA Danuglipron... Systemic Review and Meta-Analysis. Diabetes Metab Syndr Obes. 2023 — Danuglipron-focused meta-analysis; searched PubMed/Scopus/Cochrane to Aug 2023
• Frontiers Endocrinology 2025 - efficacy and safety of danuglipron and orforglipron... systematic review and meta-analysis
• Ma P, et al. Efficacy and Safety of Danuglipron and Orforglipron in the Treatment of Type 2 Diabetes Mellitus: a Meta-analysis. Chinese General Practice 2025;28(21):2679-2685
• Saxena AR, et al. Efficacy and Safety of Oral Small Molecule GLP-1 RA Danuglipron for Glycemic Control... A Randomized Clinical Trial. JAMA Netw Open. 2023;6(5):e2314493 — Primary phase 2b RCT publication (NCT03985293)

5 registered trials — 0 currently recruiting.

Phase 1
NCT04616339
STUDY TO COMPARE PHARMACOKINETICS (PK) OF SINGLE ORAL DOSES OF DIFFERENT PF-06882961 FORMULATIONS IN PARTICIPANTS WHO ARE OVERWEIGHT OR HAVE OBESITY

COMPLETED

Phase 2
NCT04617275
A 12-WEEK TITRATE STUDY TO EVALUATE SAFETY, TOLERABILITY AND PHARMACODYNAMICS OF PF-06882961 IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND IN NON-DIABETIC ADULTS WITH OBESITY

COMPLETED

Phase 1
NCT06568731
A Study to Learn How Different Amounts of the Study Medicine Danuglipron Are Taken up Into the Blood in Otherwise Healthy Adults With Overweight or Obesity

COMPLETED

Phase 1
NCT04839393
A Drug-Drug Interaction Study Between PF-06882961 and PF-06865571 in Healthy Adult Participants and Overweight Adults or Adults With Obesity Who Are Otherwise Healthy

COMPLETED

Phase 1
NCT06541678
A Study to Learn if the Study Medicines Called Itraconazole and Cyclosporine Change How the Body Processes the Other Study Medicine Called Danuglipron in Healthy Adults.

COMPLETED

Summary (literature)

The most prevalent adverse effects in phase 2 clinical trials were gastrointestinal in nature: nausea (reported in up to ~73% of participants at higher doses), vomiting (~47%), and diarrhoea (~25%). Discontinuation rates driven by GI adverse events were high — exceeding 50% in so…

WADA status

Not specifically listed by name on the 2026 WADA Prohibited List. Danuglipron is a non-peptide small-molecule GLP-1 receptor agonist and does not fall within th…

Dominant research route: Oral (PO)

Human Phase 1, Phase 2a, Phase 2b RCTs; animal PK in Wistar rats and cynomolgus monkeys

Bioavailability: Orally bioavailable small-molecule GLP-1R agonist; dose-proportional increases in plasma exposure at steady state observed in human Phase 1; similar plasma exposure and t½ when administered fed versus fasted, indicating danuglipron can be dosed without regard to food

Dominant research route. Administered orally twice-daily in Phase 1 (NCT03538743, 98 T2D patients, 28 days) and Japanese Phase 1 (40/80/120 mg BID, 8 weeks). Phase 2a evaluated dose-escalation schemes to target doses of 80–200 mg BID. Once-daily modified-release formulations were also clinically evaluated (NCT06153758, NCT06567327, NCT06568731). Animal oral PK characterized in male Wistar rats and male cynomolgus monkeys with oral plasma concentration peaking at ~3 h.

Animal PK only — male Wistar rats and male cynomolgus monkeys

Bioavailability: IV administration used as reference for oral bioavailability determination in preclinical species; no human IV data reported

IV PK was characterized in male Wistar rats and male cynomolgus monkeys alongside oral (PO) administration to determine oral bioavailability in preclinical models. No human IV studies have been reported. Danuglipron increased insulin levels in primates but not rodents, explained by a primate-specific tryptophan-33 residue in the GLP-1R binding pocket.

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

Danuglipron is a Pfizer investigational small molecule; the immediate-release program was de-prioritized in 2023 with a modified-release formulation still in development. No consumer grey-market 'research peptide' channel exists; pricing is set by biochemical reagent distributors and has been stable. Limited public time-series data.

Researched storefront prices, bucketed

p25 $13.60 · median $16.00 · p75 $40.00 · 5 researched vendors

Legit, COA-backed band: $7.36–$40.00/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)

$74

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

None found. Danuglipron was an investigational (unapproved) small-molecule oral GLP-1 receptor agonist never marketed; no FDA recalls, market withdrawals, or enforcement actions specific to danuglipron were identified.

Buyer red-flag checklist

• Investigational only — never approved by FDA or any health authority; not legally marketed (Pfizer, Dec 2023)
• Development discontinued April 14, 2025 after a participant experienced potential drug-induced liver injury (Pfizer)
• Phase 2b twice-daily formulation not advanced to Phase 3 due to >50% discontinuation rates across all doses (Pfizer, Dec 2023)
• Small-molecule (non-peptide) oral GLP-1RA; absent from grey-market peptide testing databases, so no independent purity/underdosing data exists
• High gastrointestinal adverse-event rates in Phase 2b (up to 73% nausea, 47% vomiting, 25% diarrhea) (Pfizer, Dec 2023)

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

Underdosing / mislabeling: No independent lab tests (Janoshik / MZ Biolabs / Finnrick aggregates) were found for danuglipron. It is an investigational small molecule (not a peptide) and was not identified in grey-market peptide testing channels; underdosing prevalence is therefore not applicable/unsourced.

• 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 prohibited; GLP-1 receptor agonists (semaglutide, tirzepatide) included in WADA 2026 Monitoring Program effective 1 January 2026. Danuglipron is not individually named and is an investigational, discontinued (April 2025) non-approved GLP-1 RA; no WADA Prohibited List entry found for danuglipron.

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

• News-event-driven sentiment (April 2025 discontinuation dominates discourse)
• Investigational/discontinued compound — limited first-hand user reports
• Pfizer corporate news cycle amplification

Manually researched from reddit, x, 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

Oral small-molecule GLP-1 receptor agonist (Pfizer PF-06882961) studied for type 2 diabetes and obesity; development discontinued in April 2025 due to a liver safety signal. Approximately 38 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Investigational — development discontinued; no FDA approval. Research use only.

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