Quick answer: RGT-075 is an investigational, orally bioavailable, once-daily small-molecule GLP-1 receptor full agonist developed by Regor Therapeutics for obesity and type 2 diabetes. Unlike injectable peptide GLP-1 drugs (semaglutide, liraglutide), RGT-075 is a small synthetic molecule taken as a pill. In a Phase 2a trial, 125 mg once daily produced 5% placebo-adjusted weight loss over 12 weeks with no plateau observed. A larger Phase 2b trial (COMO-1), testing doses up to 225 mg over 36 weeks, is underway with topline data expected in late 2025. RGT-075 is not FDA-approved and remains investigational.
Research Snapshot
| Peptide category | Not a peptide — small-molecule GLP-1 receptor agonist |
| Primary research interest | Obesity / weight management, type 2 diabetes |
| Highest available evidence | Published human Phase 2a topline results (company-reported) |
| Human research available | Yes — Phase 1 (SAD/MAD) and Phase 2a completed; Phase 2b (COMO-1) ongoing |
| Development status | Investigational — Phase 2b in progress as of the sources reviewed for this page |
| Regulatory status | Not approved anywhere; no regulatory filing identified |
| Last reviewed | 2026-09-27 |
Technical Identity
| Primary name | RGT-075 |
| Alternative names | None identified in a primary source reviewed for this page |
| Peptide sequence | Not applicable — RGT-075 is a small synthetic molecule, not a peptide |
| Amino-acid length | Not applicable |
| Molecular formula | Not publicly disclosed in a primary source reviewed for this page |
| Molecular weight | Not publicly disclosed in a primary source reviewed for this page |
| CAS Registry Number | Not publicly disclosed in a primary source reviewed for this page |
| PubChem CID | Not reliably established from a primary source reviewed for this page |
| UNII | Not publicly disclosed |
| DrugBank ID | Not publicly disclosed |
| Chemical modifications | Not applicable — proprietary small molecule structure not disclosed |
| Peptide class | Not applicable — small-molecule GLP-1 receptor full agonist |
| Primary biological target | GLP-1 receptor (full agonist) |
| Developer or originator | Regor Therapeutics |
| Development status | Phase 2b (COMO-1) ongoing |
What Is RGT-075?
RGT-075 is an experimental drug being developed by Regor Therapeutics, a biotechnology company focused on small-molecule alternatives to injectable peptide drugs. It belongs to a wave of “oral GLP-1” candidates — companies including Eli Lilly (orforglipron), Pfizer (formerly danuglipron), AstraZeneca (elecoglipron), and several smaller biotechs are all racing to develop a pill version of the GLP-1 receptor agonist mechanism that made injectable drugs like semaglutide (Ozempic, Wegovy) and tirzepatide (Mounjaro, Zepbound) blockbusters.
Unlike semaglutide or liraglutide, which are modified peptides that must be injected because stomach acid and digestive enzymes would otherwise destroy them, RGT-075 is a small, non-peptide synthetic molecule. Small molecules are generally more resistant to digestion, which is what allows RGT-075 to be taken as a once-daily pill rather than a weekly injection. Regor has not published the detailed chemical structure of RGT-075 in the sources reviewed for this page, so it is described here only by its research code name.
RGT-075 first entered human testing in 2022, with single ascending dose (SAD) and multiple ascending dose (MAD) studies presented as a poster at the American Diabetes Association’s 82nd Scientific Sessions. It progressed into a Phase 2a proof-of-concept obesity trial that reported topline results in January 2025, and Regor has since begun a larger Phase 2b program (COMO-1) evaluating higher doses over a longer duration, with topline data expected toward the end of 2025.
How Does It Work?
Plain-English Explanation
RGT-075 attaches to and activates the GLP-1 receptor, the same receptor targeted by injectable GLP-1 drugs. Activating this receptor slows how quickly the stomach empties, increases the feeling of fullness after eating, and helps the pancreas release insulin more appropriately after meals — all of which combine to reduce food intake and improve blood sugar control. Because RGT-075 is described as a “full agonist,” it is designed to activate the receptor as completely as the body’s own GLP-1 hormone does, rather than only partially.
Technical Explanation
RGT-075 is reported as an orally bioavailable, small-molecule full agonist of the glucagon-like peptide-1 receptor (GLP-1R), a class A G-protein-coupled receptor. In first-in-human single ascending dose testing, mean Cmax and AUC increased in an approximately dose-proportional manner across doses up to 240 mg, with exposure plateauing between the 240 mg and 280 mg cohorts. Renal clearance was reported as low to negligible, and the mean elimination half-life ranged from approximately 6.3 to 11.7 hours across the dose range tested — consistent with once-daily oral dosing. Detailed receptor-binding kinetics, selectivity data versus other receptors, and full pharmacokinetic parameters (e.g., full PK profile at steady state) were not available in the sources reviewed for this page.
Potential Benefits and Research Applications
Weight Loss in Obesity
RGT-075’s primary research application is weight reduction in adults with obesity or overweight. In the Phase 2a trial, 125 mg once daily was investigated for, and has been shown to produce, 5% placebo-adjusted weight loss over 12 weeks, with the weight-loss curve still descending (no plateau) at the end of the study — suggesting further weight loss might occur with longer treatment. This is human clinical-trial evidence, though from a single mid-stage study with topline (not full peer-reviewed) results.
Type 2 Diabetes and Metabolic Markers
RGT-075 is being investigated for type 2 diabetes in addition to obesity, consistent with the broader GLP-1 receptor agonist drug class. In the Phase 2a obesity trial, the drug is reported to have shown improvements in HbA1c (a marker of average blood sugar) and blood pressure as secondary findings, though the trial was not specifically designed or powered to establish diabetes efficacy. This is preliminary human evidence from a topline company announcement rather than a published, peer-reviewed diabetes-specific trial.
What Dosage Information Circulates?
Figures in this section summarize amounts and schedules reported in published research or circulating online. Their inclusion documents what is reported and does not establish that a regimen is verified, safe, effective, or appropriate.
| Reported use or research objective | Route reported | Amount reported | Frequency reported | Reported duration | Evidence or source category |
|---|---|---|---|---|---|
| First-in-human single ascending dose (SAD) study | Oral | 15 mg to 280 mg (seven dose cohorts) | Single dose | Single administration, with follow-up PK sampling | Published human clinical trial (conference poster) |
| Phase 2a obesity proof-of-concept trial | Oral, once daily | 125 mg once daily (target dose); one participant reduced to 60 mg once daily | Once daily | 12 weeks (titration not separately disclosed for this study) | Published human clinical trial (company topline results) |
| Phase 2b obesity trial (COMO-1, ongoing) | Oral, once daily | Multiple doses evaluated, up to 225 mg | Once daily | 36 weeks, including a 12-week titration period | Registered but unpublished human trial (company announcement) |
Explanation of the Reported Figures
The 125 mg once-daily dose is the figure most consistently reported, because it was the target dose used in the completed Phase 2a obesity trial that produced RGT-075’s headline 5% placebo-adjusted weight loss result. That figure comes directly from Regor Therapeutics’ own topline announcement, not from an independent peer-reviewed publication, so it should be read as a company-reported result pending fuller disclosure. The 15 mg–280 mg range comes from the earliest first-in-human SAD study and reflects dose-exploration testing rather than a treatment regimen — pharmacokinetic exposure was reported to plateau between 240 mg and 280 mg, which is likely why the Phase 2a and Phase 2b programs use doses well below that upper bound. The up-to-225 mg figure for Phase 2b (COMO-1) comes from the same company announcement describing that trial’s design; specific per-arm doses within that range have not been disclosed in the sources reviewed for this page. No community, practitioner, or vendor-reported figures for RGT-075 were identified — this compound has not been offered for sale or discussed in research-chemical community channels the way many older peptides have, likely because it is a proprietary small molecule still in company-controlled clinical trials.
Detailed Dosage and Protocol Evidence
Amounts Studied in Human Research
| Research objective | Amount studied | Frequency | Duration | Route | Study population | Source |
|---|---|---|---|---|---|---|
| Safety, tolerability, and PK (SAD) | 15–280 mg across seven cohorts | Single dose | Single dose plus PK follow-up | Oral | Healthy adult volunteers (n=42 treated, per reported AE data) | Regor ADA 2022 SAD poster |
| Obesity, proof-of-concept efficacy | 125 mg once daily (target) | Once daily | 12 weeks | Oral | 73 adults with obesity, ages 18–75, BMI ≥27 kg/m², across 10 US centers | Regor Phase 2a topline press release |
| Obesity, dose-ranging efficacy (COMO-1, ongoing) | Multiple doses up to 225 mg | Once daily | 36 weeks (12-week titration) | Oral | ~240 adults with obesity or overweight | Regor Phase 2b initiation press release |
Amounts Studied in Animal Research
Not consistently reported. No published animal dosing data for RGT-075 were identified in the sources reviewed for this page.
Practitioner and Community-Reported Protocols
Not consistently reported. RGT-075 is a proprietary, patent-protected small molecule still confined to company-sponsored clinical trials; no practitioner-reported or community-reported protocols were identified in the sources reviewed for this page.
Conflicts and Unanswered Questions
The specific per-arm doses being tested within the Phase 2b COMO-1 trial’s “up to 225 mg” range have not been publicly broken out in the sources reviewed for this page. Full pharmacokinetic parameters at steady state, and any titration schedule used in the Phase 2a study specifically, were also not disclosed. Because the Phase 2a and Phase 2b results discussed here are topline company announcements rather than peer-reviewed publications, the underlying full data set — including exact statistical results, confidence intervals, and complete adverse-event tables — has not yet been independently verified.
Important Published Research
First-in-Human Single Ascending Dose Study (ADA 2022 Poster)
Study type: Phase 1, single ascending dose, presented as a poster at the American Diabetes Association’s 82nd Scientific Sessions (May 2022).
Subjects: Healthy adult volunteers across seven dose cohorts (15–280 mg), with approximately 42 subjects reported to have received active treatment.
Findings: RGT-075 exposure (Cmax and AUC) increased in an approximately dose-proportional manner up to 240 mg, with exposure plateauing at 280 mg. Renal clearance was low to negligible. Elimination half-life ranged from about 6.3 to 11.7 hours. No serious adverse events or deaths occurred; roughly half of treated subjects experienced an adverse event, most commonly mild nausea, vomiting, or headache; a maximum tolerated dose was not reached.
Limitations: This was a poster presentation of a small, short-duration safety and PK study, not a full peer-reviewed publication, and it was not designed to assess efficacy.
In plain English: The drug is absorbed and cleared from the body in a way that supports once-daily dosing, and healthy volunteers tolerated single doses reasonably well up to the highest levels tested, with nausea and vomiting as the main side effects.
Phase 2a Obesity Proof-of-Concept Trial (Topline Results, January 2025)
Study type: Phase 2a, presumed randomized and placebo-controlled based on standard trial design for this stage (specific randomization and blinding details were not fully spelled out in the press release reviewed for this page).
Subjects: 73 adults with obesity, ages 18–75, BMI ≥27 kg/m², across 10 US clinical centers.
Findings: 125 mg once daily produced 5% placebo-adjusted weight loss over 12 weeks with no plateau in the weight-loss curve, plus reported improvements in HbA1c and blood pressure. No treatment-related serious adverse events occurred; the discontinuation rate due to adverse events was 4%, identical between active treatment and placebo; only one participant (2%) required a dose reduction (to 60 mg). Nausea occurred in about 40% of treated participants and vomiting in about 24%.
Limitations: This is a topline company announcement, not a peer-reviewed publication — full statistical detail, confidence intervals, and the complete data set have not been independently verified. The 12-week duration is short relative to the 36-plus-week trials typically used to establish long-term weight-loss efficacy for this drug class.
In plain English: In a fairly small, short study, the drug produced meaningful weight loss with side effects (mainly nausea and vomiting) similar in pattern to other GLP-1 drugs, and most people tolerated it well enough to stay on treatment.
Timing, Duration, and Research Variables
RGT-075 is dosed once daily by mouth. In the Phase 2b (COMO-1) trial, dosing follows a 12-week titration period before reaching the target maintenance dose, over a total treatment duration of 36 weeks — a titration approach broadly similar to that used for injectable GLP-1 drugs, intended to reduce gastrointestinal side effects like nausea as the dose is increased gradually. Specific week-by-week titration steps have not been disclosed in the sources reviewed for this page. Elimination half-life of roughly 6–12 hours is consistent with, but somewhat shorter than, the multi-day half-lives of injectable GLP-1 peptide drugs, which is part of why RGT-075 is dosed daily rather than weekly.
Combinations and Related Research
No formally studied combination trials involving RGT-075 and another investigational or approved drug were identified in the sources reviewed for this page. As a GLP-1 receptor full agonist, RGT-075 is mechanistically comparable to other oral small-molecule GLP-1 candidates in development, including orforglipron, elecoglipron (AZD5004), and TERN-601, though no head-to-head trials between these compounds were identified. No practitioner-reported or community-reported combination protocols were identified, consistent with RGT-075 remaining confined to company-sponsored clinical trials.
Side Effects, Risks, and Limitations
The most commonly reported side effects across RGT-075’s Phase 1 and Phase 2a studies are gastrointestinal: nausea (reported in about 40% of Phase 2a participants) and vomiting (about 24%), consistent with the class-wide GI side-effect profile of GLP-1 receptor agonists. Headache was also reported in the single ascending dose study. No treatment-related serious adverse events or deaths have been reported in the studies reviewed for this page, and discontinuation due to adverse events was low (4% in Phase 2a, matching placebo). A maximum tolerated dose was not reached in single-dose testing up to 280 mg.
Because RGT-075 is not an approved product, it is not manufactured, packaged, or quality-controlled for consumer purchase, and no legitimate supply of RGT-075 for personal use exists outside of Regor’s controlled clinical trials. Long-term safety beyond roughly 36 weeks of exposure has not yet been studied. As with any investigational compound still in Phase 2, unknown risks — including rare adverse effects that would only appear in larger, longer trials or in cardiovascular outcome studies — cannot be ruled out.
Regulatory and Developmental Status
RGT-075 is investigational and has not been approved by the FDA or any other regulatory authority for any use. It is currently in Phase 2b clinical development (the COMO-1 trial) for obesity, with topline data expected toward the end of 2025 per Regor’s public statements as of the sources reviewed for this page. No regulatory filing (such as an NDA or equivalent) has been identified. Development status may have changed since this page was last reviewed; readers should check Regor Therapeutics’ own communications or clinicaltrials.gov for the most current status.
Frequently Asked Questions
What is RGT-075?
RGT-075 is an investigational, orally bioavailable, once-daily small-molecule GLP-1 receptor full agonist developed by Regor Therapeutics for obesity and type 2 diabetes. It is not a peptide and not approved for any use.
How does RGT-075 work?
It activates the GLP-1 receptor, slowing stomach emptying, increasing fullness, and supporting insulin release after meals — the same core mechanism as injectable GLP-1 drugs like semaglutide, but delivered as a once-daily pill instead of an injection.
What dosage has been studied for RGT-075?
Single doses from 15 mg to 280 mg were tested in early Phase 1 safety studies. The completed Phase 2a obesity trial used 125 mg once daily. The ongoing Phase 2b (COMO-1) trial is testing multiple doses up to 225 mg once daily.
Is there a dosage that commonly circulates online?
125 mg once daily is the figure most often cited, because it was the target dose in Regor’s completed Phase 2a obesity trial. This is a company-reported clinical trial dose, not a community- or vendor-reported figure — RGT-075 has not circulated in research-chemical or community channels.
How frequently is RGT-075 dosed?
Once daily, by mouth, in every study identified for this page.
What route of administration is used?
Oral (tablet or capsule form specifics not disclosed in the sources reviewed for this page) — this is a key selling point versus injectable GLP-1 drugs.
How long do reported protocols last?
The completed Phase 2a trial ran 12 weeks. The ongoing Phase 2b (COMO-1) trial runs 36 weeks, including a 12-week titration period.
Has RGT-075 been studied in humans?
Yes. It has completed Phase 1 (single and multiple ascending dose) and Phase 2a obesity trials, and is currently in a Phase 2b obesity trial (COMO-1).
What side effects have been reported?
Mainly gastrointestinal — nausea (about 40% of Phase 2a participants) and vomiting (about 24%) — plus headache in earlier dose-finding studies. No treatment-related serious adverse events have been reported.
Is RGT-075 approved?
No. It is investigational and has not been approved by the FDA or any other regulator.
How strong is the evidence?
Moderate for a Phase 2 investigational drug: the weight-loss and safety data come from a company-reported topline readout of a controlled human trial, not yet a full peer-reviewed publication, and the Phase 2b confirmatory trial is still ongoing.
What remains unknown?
Full peer-reviewed data from the Phase 2a trial, specific per-arm doses within the Phase 2b trial’s tested range, the drug’s exact chemical structure and identifiers, and longer-term safety and efficacy data beyond 36 weeks.
Bottom Line
RGT-075 is one of several oral small-molecule GLP-1 receptor agonists in development as a pill alternative to injectable weight-loss and diabetes drugs. Its strongest evidence so far is a completed Phase 2a trial showing 5% placebo-adjusted weight loss over 12 weeks at a 125 mg once-daily dose, with a side-effect profile (nausea, vomiting) typical of the GLP-1 drug class and no treatment-related serious adverse events reported. What is genuinely published is limited to a conference poster (Phase 1 PK/safety) and company topline press releases (Phase 2a efficacy and Phase 2b design) — full peer-reviewed data has not yet been identified. Dosage information that “circulates” about RGT-075 is essentially limited to these same company-disclosed clinical trial doses; no independent community or practitioner protocols exist because the compound remains confined to Regor’s controlled trials. Major limitations include the short 12-week duration of the only completed efficacy trial, the lack of independently verified full data, and undisclosed chemical identity details. RGT-075 remains investigational, currently in Phase 2b development, with topline Phase 2b data expected around late 2025.
Sources
- Regor Therapeutics — “Regor Releases Phase 2a Topline Results for RGT-075, an Oral Once-daily Small Molecule GLP-1R Agonist, and Begins Phase 2b Study in the US for the Treatment of Obesity” — PR Newswire, January 2025 — Company press release
- Regor Therapeutics — “Regor Initiates Phase 2 Study of Oral Once-daily GLP-1 Agonist RGT-075 for the Treatment of Obesity” — PR Newswire, 2024 — Company press release
- Regor Therapeutics — “A First-in-Human Study of RGT-075” — Single Ascending Dose (SAD) poster, ADA 82nd Scientific Sessions, May 2022 — Conference poster PDF
- Drug Topics — “Oral GLP-1 Shows Significant Weight Loss in Patients With Obesity” — news coverage of Phase 2a results — News article