Quick answer: CT-996 is an investigational, once-daily oral small-molecule GLP-1 receptor agonist being developed by Roche, via its Carmot Therapeutics acquisition, for obesity and type 2 diabetes. It is a “biased” GLP-1 agonist engineered to activate one signaling pathway (cAMP) while minimizing another (beta-arrestin recruitment), a design intended to improve tolerability. In an early Phase 1 trial, a rapid dose-escalation schedule produced 6.1% placebo-adjusted weight loss in just four weeks, though at the cost of a high rate of nausea; a slower escalation schedule was much better tolerated but showed little benefit over placebo in that short window. CT-996 is not approved and remains in early-stage human testing.
Research Snapshot
| Peptide category | Not a peptide — small-molecule, biased GLP-1 receptor agonist |
| Primary research interest | Obesity / weight management, type 2 diabetes |
| Highest available evidence | Published human Phase 1 topline results (company-reported) |
| Human research available | Yes — Phase 1 (CT-996-201) completed in participants with and without type 2 diabetes; Phase 2 planned |
| Development status | Investigational — early-stage; Phase 2 development was planned to begin in 2025 per the sources reviewed for this page |
| Regulatory status | Not approved anywhere; no regulatory filing identified |
| Last reviewed | 2026-09-27 |
Technical Identity
| Primary name | CT-996 |
| Alternative names | None identified in a primary source reviewed for this page |
| Peptide sequence | Not applicable — CT-996 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 | Engineered as a “biased” GLP-1 receptor agonist — activates cAMP signaling with minimal-to-no beta-arrestin recruitment, unlike the natural GLP-1 hormone |
| Peptide class | Not applicable — small-molecule, biased GLP-1 receptor agonist |
| Primary biological target | GLP-1 receptor (biased agonism favoring cAMP signaling) |
| Developer or originator | Carmot Therapeutics (acquired by Roche/Genentech, December 2023, for approximately $2.7 billion) |
| Development status | Phase 1 completed; Phase 2 planned |
What Is CT-996?
CT-996 is an investigational, once-daily, oral small-molecule GLP-1 receptor agonist originally developed by Carmot Therapeutics, a company Roche (through its Genentech subsidiary) acquired in December 2023 for approximately $2.7 billion, largely to gain access to Carmot’s obesity and diabetes pipeline. CT-996 is one part of that acquired portfolio; another, more advanced Carmot-derived asset, the injectable dual GLP-1/GIP agonist CT-388, has since reported positive Phase 2 results and is covered in its own entry on this site.
CT-996 is designed as a “biased” GLP-1 receptor agonist — a molecule engineered to selectively activate one intracellular signaling pathway (cAMP production) downstream of the GLP-1 receptor while minimizing activation of another (beta-arrestin recruitment). The scientific rationale behind this approach is that beta-arrestin recruitment may be more closely linked to certain side effects, so a molecule that favors cAMP signaling might, in principle, deliver similar metabolic benefits with better tolerability — though this hypothesis has not yet been definitively proven in large human trials for CT-996 specifically.
The drug completed a Phase 1 trial (CT-996-201, registered as NCT05814107) with results announced by Roche in July 2024, and a further cohort in participants with type 2 diabetes was planned to begin later in 2024. As of the sources reviewed for this page, Roche has indicated Phase 2 development was planned to begin in 2025, with CT-996 envisioned as a potential oral maintenance therapy that could be used to sustain weight loss achieved with an injectable drug.
How Does It Work?
Plain-English Explanation
Like other GLP-1 receptor agonists, CT-996 activates the GLP-1 receptor to reduce appetite, increase fullness, and slow digestion. What sets it apart is that it is engineered to trigger the receptor’s signals in a more selective way than the body’s natural GLP-1 hormone does — the idea being to keep the beneficial appetite and blood-sugar effects while dialing down signals that might contribute to side effects like nausea.
Technical Explanation
CT-996 is reported as a biased agonist of the GLP-1 receptor that activates cAMP signaling with minimal-to-no recruitment of beta-arrestin, in contrast to the balanced signaling profile of endogenous GLP-1. Pharmacokinetically, blood levels of CT-996 were reported to be largely unaffected by fasting versus a standardized high-fat meal, which — if it holds up in larger trials — would allow flexible dosing without regard to meal timing, a potential convenience advantage over some other oral GLP-1 candidates. Full receptor-binding kinetics, selectivity data, and steady-state pharmacokinetic parameters were not available in the sources reviewed for this page.
Potential Benefits and Research Applications
Weight Loss in Obesity
CT-996 has been shown, in a Phase 1 trial using a rapid dose-escalation schedule, to produce 6.1% placebo-adjusted weight loss within just four weeks (7.3% in the active-treatment group versus 1.2% with placebo, p<0.001). This is an early but statistically significant human result. Notably, a separate, more gradual dose-escalation schedule tested in the same program produced only 2.3% weight loss at four weeks with no statistically significant advantage over placebo — meaning the impressive headline weight-loss figure is specific to the rapid-escalation regimen and was not seen with gentler titration in this short time frame.
Type 2 Diabetes
CT-996 is being investigated for type 2 diabetes as well as obesity. A Phase 1 cohort specifically in participants with obesity and type 2 diabetes was planned to begin later in 2024, but detailed efficacy results for that population were not available in the sources reviewed for this page.
Potential Role as Maintenance Therapy
Roche has been reported to be investigating CT-996’s potential use as an oral maintenance therapy — a pill that could help patients sustain weight loss initially achieved with an injectable GLP-1 or GLP-1/GIP drug. This is a proposed research direction rather than an established, tested use, and has not been established through the clinical evidence reviewed for this page.
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 |
|---|---|---|---|---|---|
| Phase 1, single ascending dose (Part 1) | Oral | Not broken out by specific dose in the sources reviewed for this page | Single dose | Single administration plus PK follow-up | Published human clinical trial (company topline results) |
| Phase 1, rapid dose-escalation cohort (Part 2, obesity) | Oral, once daily | Initial 10 mg, increased roughly every 3–7 days to a peak of 120 mg | Once daily | 4 weeks | Published human clinical trial (company topline results) |
| Phase 1, gradual dose-escalation cohort (Part 2, obesity) | Oral, once daily | Slower titration schedule; specific per-step doses not disclosed in the sources reviewed for this page | Once daily | 4 weeks | Published human clinical trial (company topline results) |
| Phase 1, obesity with type 2 diabetes (Part 3) | Oral, once daily | Not disclosed in the sources reviewed for this page | Once daily | Not disclosed in the sources reviewed for this page | Registered but results not fully disclosed at time of review |
Explanation of the Reported Figures
The most important figure reported for CT-996 is not a single dose but a comparison between two escalation strategies: a rapid schedule (10 mg starting dose, stepped up every 3–7 days to a 120 mg peak) that produced strong four-week weight loss but a high rate of nausea (around 85% of participants), versus a gradual schedule that was much better tolerated but showed little advantage over placebo in the same four-week window. Both figures come from Roche’s own topline Phase 1 announcements and follow-up reporting — no independent peer-reviewed publication with the full dataset was identified in the sources reviewed for this page. This dose-escalation contrast is a genuinely important and distinctive piece of information about CT-996, since it suggests the eventual approved (if any) titration schedule will need to balance efficacy against tolerability more carefully than the rapid-escalation arm did. No community, practitioner, or vendor-reported figures for CT-996 were identified — it has not circulated outside company-sponsored trials.
Detailed Dosage and Protocol Evidence
Amounts Studied in Human Research
| Research objective | Amount studied | Frequency | Duration | Route | Study population | Source |
|---|---|---|---|---|---|---|
| Safety/PK, single ascending dose | Not broken out by specific dose in the sources reviewed for this page | Single dose | Single dose plus PK follow-up | Oral | 40 participants (Part 1) | Roche July 2024 Phase 1 topline press release |
| Efficacy/tolerability, obesity, rapid vs. gradual titration | Rapid: 10 mg to 120 mg peak; Gradual: slower step-up, doses not fully disclosed | Once daily | 4 weeks | Oral | 75 participants with obesity, no type 2 diabetes, across three cohorts (Part 2) | Roche press release; BioSpace and PharmExec coverage |
| Obesity with type 2 diabetes | Not disclosed in the sources reviewed for this page | Once daily | Not disclosed in the sources reviewed for this page | Oral | 60 participants across two cohorts (Part 3, planned to begin later in 2024) | PharmExec coverage of Roche Phase 1 program |
Amounts Studied in Animal Research
Not consistently reported. No published animal dosing data for CT-996 were identified in the sources reviewed for this page.
Practitioner and Community-Reported Protocols
Not consistently reported. CT-996 is a proprietary compound confined to Roche-sponsored clinical trials; no practitioner-reported or community-reported protocols were identified.
Conflicts and Unanswered Questions
The exact per-step doses used in the gradual (slower) titration cohort have not been fully disclosed in the sources reviewed for this page, only that they resulted in a lower peak nausea rate and lower efficacy than the rapid-escalation cohort over the same four weeks. Results from the Part 3 cohort in participants with type 2 diabetes had not been publicly reported as of the sources reviewed for this page. Because all available efficacy data covers only a four-week window, it remains unclear how weight loss, tolerability, or the efficacy gap between titration schedules would evolve over the longer treatment durations (12+ weeks) typically used to establish this drug class’s real-world value.
Important Published Research
Roche Phase 1 Topline Results (CT-996-201, NCT05814107; announced July 2024)
Study type: Multi-part, randomized, double-blind, placebo-controlled Phase 1 trial in otherwise-healthy overweight or obese adults, with and without type 2 diabetes.
Subjects: Part 1 (single ascending dose): 40 participants. Part 2 (multiple ascending dose, obesity without diabetes): 75 participants across three cohorts. Part 3 (multiple ascending dose, obesity with type 2 diabetes): 60 participants across two cohorts, planned to begin later in 2024.
Findings: In the rapid dose-escalation cohort (10 mg starting dose, increased roughly every 3–7 days to a 120 mg peak), participants lost 7.3% of body weight at four weeks versus 1.2% with placebo — a 6.1% placebo-adjusted difference (p<0.001). A gradual dose-escalation cohort produced only 2.3% weight loss at four weeks, not significantly different from placebo, but was much better tolerated. Nausea occurred in roughly 85% of participants on the rapid-escalation schedule; other common effects included GERD, vomiting, constipation, and abdominal distention. All adverse events were reported as mild or moderate across all cohorts, no unexpected safety signals were observed, and no participants discontinued the study due to drug-related toxicity. CT-996 blood levels were reported to be largely unaffected by fasting versus a high-fat meal.
Limitations: This is a topline company announcement covering only a four-week efficacy window from an early-stage trial, not a full peer-reviewed publication. The high nausea rate in the rapid-escalation cohort illustrates a real efficacy-versus-tolerability trade-off that has not yet been resolved with a titration schedule shown to deliver both good efficacy and good tolerability.
In plain English: Pushing the dose up quickly produced strong weight loss fast, but caused a lot of nausea; easing into the dose more slowly avoided the nausea but also mostly avoided the weight loss, at least within the first month. Roche will likely need to find a middle-ground titration schedule in later trials.
Timing, Duration, and Research Variables
CT-996 is dosed once daily by mouth. The key research variable studied so far is the pace of dose escalation itself: a rapid schedule reaching a 120 mg peak within roughly 2–3 weeks produced strong short-term weight loss but high rates of nausea, while a more gradual schedule over the same four-week observation period produced minimal weight loss beyond placebo but was much better tolerated. All efficacy data currently available covers only a four-week treatment window; how these two approaches would compare over the 12-to-36-week durations typically used in later-stage obesity trials has not yet been reported. CT-996’s apparent lack of sensitivity to food timing (fasting vs. a high-fat meal) is a notable pharmacokinetic feature that, if confirmed in larger trials, could simplify dosing instructions relative to oral drugs that require strict fasting.
Combinations and Related Research
No formally studied combination trials involving CT-996 and another drug were identified. CT-996 was acquired by Roche alongside CT-388, a further-along injectable dual GLP-1/GIP receptor agonist from the same Carmot Therapeutics pipeline that has already reported positive Phase 2 results — Roche has discussed CT-996 as a potential future oral maintenance option that could follow initial treatment with an injectable like CT-388, though this specific sequential-use strategy has not itself been tested in a published trial. No practitioner-reported or community-reported combination protocols exist, as CT-996 remains confined to Roche-sponsored trials.
Side Effects, Risks, and Limitations
The dominant side effects reported for CT-996 are gastrointestinal and clearly tied to how quickly the dose is increased: nausea occurred in roughly 85% of participants on the rapid dose-escalation schedule, along with gastroesophageal reflux (GERD), vomiting, constipation, and abdominal distention. Roche has stated that all adverse events across all cohorts were mild or moderate, that no unexpected safety signals emerged, and that no participant discontinued the study because of drug-related toxicity. This GI side-effect pattern is broadly consistent with the wider GLP-1 receptor agonist drug class, and the sharp contrast between the rapid- and gradual-escalation cohorts underscores how much titration speed affects tolerability for this compound specifically.
Because CT-996 is not an approved product, it is not manufactured or sold for consumer use, and no legitimate supply exists outside Roche’s controlled clinical trials. Longer-term safety data beyond the four-week window reported so far, and full safety data from the type 2 diabetes cohort, were not available in the sources reviewed for this page.
Regulatory and Developmental Status
CT-996 is investigational and has not been approved by the FDA or any other regulatory authority. It completed a Phase 1 trial (CT-996-201) with topline results announced in July 2024, and Roche has indicated Phase 2 development was planned to begin in 2025. No regulatory filing has been identified. Development status may have changed since this page was last reviewed; readers should check Roche’s or Genentech’s own communications, or clinicaltrials.gov, for the most current status.
Frequently Asked Questions
What is CT-996?
CT-996 is an investigational, once-daily oral small-molecule GLP-1 receptor agonist being developed by Roche (via its Carmot Therapeutics acquisition) for obesity and type 2 diabetes. It is not approved for any use.
How does CT-996 work?
It activates the GLP-1 receptor in a “biased” way — favoring cAMP signaling over beta-arrestin recruitment — which is intended to preserve appetite-reducing and blood-sugar benefits while potentially improving tolerability compared with less selective GLP-1 activation.
What dosage has been studied for CT-996?
A rapid escalation schedule (10 mg starting dose, increased every 3–7 days to a 120 mg peak) and a slower, gradual escalation schedule were both tested over four weeks in a Phase 1 obesity cohort. Specific doses for the single ascending dose and type 2 diabetes cohorts were not disclosed in the sources reviewed for this page.
Is there a dosage that commonly circulates online?
The 10 mg to 120 mg rapid-escalation schedule is the figure most associated with CT-996’s headline weight-loss result, but it comes from Roche’s own Phase 1 trial reporting, not community or vendor sources — CT-996 has not circulated in research-chemical or community channels.
How frequently is CT-996 dosed?
Once daily, by mouth, in every study identified.
What route of administration is used?
Oral, and reportedly usable without regard to meal timing based on early PK data.
How long do reported protocols last?
The only efficacy data reported so far covers a four-week Phase 1 treatment window. Longer trials have not yet reported results.
Has CT-996 been studied in humans?
Yes. It has completed a Phase 1 trial in participants with and without type 2 diabetes, with topline results reported by Roche in July 2024.
What side effects have been reported?
Mainly gastrointestinal — nausea (about 85% of participants on the rapid-escalation schedule), GERD, vomiting, constipation, and abdominal distention. All adverse events were reported as mild or moderate, with no discontinuations due to drug-related toxicity.
Is CT-996 approved?
No. It is investigational and has not been approved by the FDA or any other regulator.
How strong is the evidence?
Early-stage: the available weight-loss and safety data come from a company-reported topline Phase 1 readout covering only four weeks, not a full peer-reviewed publication or a longer, more definitive trial.
What remains unknown?
Whether a titration schedule can be found that captures the rapid-escalation cohort’s efficacy without its high nausea rate; results from the type 2 diabetes cohort; the drug’s exact chemical structure and identifiers; and efficacy and safety data beyond four weeks.
Bottom Line
CT-996 is an early-stage investigational oral small-molecule GLP-1 receptor agonist from Roche’s Carmot Therapeutics acquisition, engineered as a “biased” agonist intended to improve tolerability relative to less selective GLP-1 activation. Its strongest evidence so far is a Phase 1 trial showing that a rapid dose-escalation schedule can produce 6.1% placebo-adjusted weight loss in just four weeks — but at the cost of a high nausea rate (around 85% of participants), while a gentler titration schedule tested in the same trial avoided most of the nausea but also most of the weight-loss benefit within that short window. What is genuinely published is limited to Roche’s own Phase 1 topline announcements and subsequent news coverage; no independent peer-reviewed publication with the complete dataset was identified. Dosage information “circulating” about CT-996 is essentially limited to these same company-disclosed clinical-trial figures. Major limitations include the very short four-week efficacy window, the unresolved trade-off between titration speed and tolerability, and undisclosed chemical identity details. CT-996 remains investigational, with Phase 2 development planned to begin in 2025 per the sources reviewed for this page.
Sources
- Roche — “Ad hoc announcement pursuant to Art. 53 LR: Roche announces positive Phase I results of its oral GLP-1 receptor agonist CT-996 for the treatment of people with obesity” — July 2024 — Company press release
- BioSpace — “Roche’s Obesity Pill Candidate Hit With Safety Concerns Despite Strong Efficacy Data” — coverage of the rapid vs. gradual dose-escalation cohort results — News article
- PharmExec — “CT-996 Demonstrates Significant Weight Loss in Patients with Obesity and Type 2 Diabetes” — News article