The New England Journal of Medicine September 22, 2022

Glycemia Reduction in Type 2 Diabetes — Glycemic Outcomes

David M. Nathan, John M. Lachin, Ashok Balasubramanyam, et al. (The GRADE Study Research Group)

Bottom Line

In a head-to-head comparison of second-line diabetes medications added to metformin, liraglutide and insulin glargine were more effective than glimepiride and sitagliptin at achieving and maintaining glycemic control over 5 years.

Key Findings

1. Over a mean follow-up of 5.0 years, the cumulative incidence of the primary outcome (time to confirmed HbA1c ≥7.0%) significantly differed among groups, with a global P-value of <0.001 [4.1.1].
2. Incidence rates for glycemic failure were lowest and similar in the liraglutide (26.1 per 100 participant-years) and insulin glargine (26.5 per 100 participant-years) arms.
3. Glimepiride and sitagliptin were significantly less effective at maintaining glycemic targets, with higher primary outcome incidence rates of 30.4 and 38.1 per 100 participant-years, respectively.
4. The secondary metabolic outcome, time to a confirmed HbA1c >7.5%, followed an identical efficacy hierarchy favoring liraglutide and glargine over the other treatments.
5. Participants assigned to liraglutide experienced greater weight loss but also reported higher frequencies of gastrointestinal side effects compared to the other treatment arms.

Study Design

Design
Randomized Controlled Trial
Open-Label
Sample
5,047
Patients
Duration
5.0 yr
Median
Setting
Multicenter, US
Population Adults with type 2 diabetes of less than 10 years' duration, currently receiving metformin monotherapy, with a baseline HbA1c level of 6.8% to 8.5%.
Intervention Randomized addition of one of four agents to background metformin: insulin glargine U-100, the sulfonylurea glimepiride, the GLP-1 receptor agonist liraglutide, or the DPP-4 inhibitor sitagliptin.
Comparator Head-to-head comparison against the other three active treatment groups.
Outcome Time to a subsequently confirmed glycated hemoglobin (HbA1c) level of 7.0% or higher.

Study Limitations

Sodium-glucose cotransporter-2 (SGLT2) inhibitors were not included as an intervention arm because they were still undergoing regulatory review and not widely approved when the study was designed in 2013 [4.3.9].
The open-label design could introduce performance and reporting biases, particularly regarding adherence, subjective side effects, and subsequent clinical management.
Only a single representative medication from each pharmacological class was tested, meaning the results may not completely generalize to all drugs within those respective classes.

Clinical Significance

The GRADE trial provided essential head-to-head data comparing the most widely prescribed second-line therapies for type 2 diabetes, demonstrating that a GLP-1 receptor agonist (liraglutide) and basal insulin (glargine) provide superior and more durable glycemic control compared to a sulfonylurea (glimepiride) or a DPP-4 inhibitor (sitagliptin). However, the relatively rapid loss of glycemic control across all study arms over the 5.0-year mean follow-up highlights the progressive nature of the disease and the difficulty of maintaining tight HbA1c targets long-term. While the findings support the use of GLP-1 agonists as preferred second-line agents, the trial's applicability to modern practice is somewhat constrained by the lack of an SGLT2 inhibitor arm and the recent emergence of highly potent dual-incretin therapies.

Historical Context

For over two decades, metformin has been the universally agreed-upon first-line pharmacological treatment for type 2 diabetes. However, when metformin monotherapy failed to maintain glycemic targets, clinical guidelines historically offered little consensus on the optimal second-line agent, leaving choices to be driven by cost, side-effect profiles, and clinician preference. The NIH-funded GRADE trial was initiated in 2013 as a landmark comparative effectiveness study to definitively compare the four most commonly used drug classes head-to-head. Although the therapeutic landscape evolved significantly over the trial's duration—most notably with cardiovascular outcome trials shifting guidelines heavily toward SGLT2 inhibitors and newer generation GLP-1 agonists—GRADE remains the largest and longest randomized comparison of these standard second-line options.

Guided Discussion

High-yield insights from every perspective

Med Student
Medical Student

Based on the mechanisms of action of the four drug classes studied in the GRADE trial, why might liraglutide and insulin glargine provide more durable long-term glycemic control compared to sitagliptin and glimepiride?

Key Response

Liraglutide (a GLP-1 receptor agonist) enhances glucose-dependent insulin secretion, suppresses glucagon, and potentially preserves beta-cell function. Insulin glargine directly replaces progressively deficient endogenous basal insulin. In contrast, glimepiride (a sulfonylurea) forces insulin secretion independent of glucose, leading to quicker beta-cell exhaustion, and sitagliptin (a DPP-4 inhibitor) only mildly increases endogenous incretins, making them both less durable as natural beta-cell failure progresses over time.

Resident
Resident

If a patient requires a second-line agent after metformin but has a high risk of hypoglycemia and struggles with obesity, how do the results and safety profiles of the GRADE trial medications guide your choice between liraglutide and insulin glargine?

Key Response

While both liraglutide and insulin glargine maintained glycemic control effectively in the GRADE trial, liraglutide is associated with clinically significant weight loss and carries a very low risk of hypoglycemia. Insulin glargine, conversely, typically causes weight gain and has a higher risk of hypoglycemia. Therefore, liraglutide is the strongly preferred choice for this specific patient phenotype.

Fellow
Fellow

The GRADE study focused heavily on glycemic outcomes, but modern diabetes management emphasizes cardiorenal risk reduction. How do the cardiovascular outcomes observed in the GRADE trial align with dedicated cardiovascular outcome trials (CVOTs) for GLP-1 RAs, and why is this critical when choosing a second-line agent?

Key Response

In GRADE, liraglutide showed a numerical advantage in cardiovascular outcomes, though the study was not primarily powered for MACE like dedicated CVOTs (e.g., LEADER). Fellows must recognize that while glargine and liraglutide have similar glycemic durability, liraglutide provides proven ASCVD risk reduction independent of A1c lowering, making GLP-1 RAs vastly superior second-line choices in patients with or at high risk for cardiovascular disease.

Attending
Attending

Given the robust durability of glycemic control demonstrated by liraglutide and insulin glargine in the GRADE trial, how should clinicians balance these clinical benefits against the higher costs and access barriers of GLP-1 RAs compared to the inexpensive but less durable sulfonylureas?

Key Response

Attendings must navigate the tension between evidence-based efficacy and real-world affordability. While glimepiride is cheap, its rapid loss of efficacy and higher rate of hypoglycemia and weight gain often lead to downstream costs and complications. The teaching point is to advocate for GLP-1 RAs or basal insulin for long-term durability and safety, reserving sulfonylureas only when access strictly precludes other options, while engaging in shared decision-making regarding out-of-pocket costs.

Scholarly Review

Critical appraisal through the lens of expert reviewers and guideline development

PhD
PhD

The GRADE trial utilized a pragmatic, comparative effectiveness design. What are the statistical and methodological challenges in interpreting time-to-event data for the primary metabolic outcome (A1c > 7.0%), and how does missing data or differential non-adherence over 5 years impact the validity of these Kaplan-Meier estimates?

Key Response

In a 5-year pragmatic trial, differential dropout and medication non-adherence are major threats. Using a primary outcome of time to A1c > 7.0% requires robust intention-to-treat analysis and proportional hazards assumptions. The critique focuses on how informative censoring or varying rates of treatment discontinuation (e.g., due to GI side effects of GLP-1 RAs vs. hypoglycemia of SUs) might bias the comparative durability estimates, necessitating sophisticated sensitivity analyses like inverse probability weighting.

Journal Editor
Journal Editor

SGLT2 inhibitors were not included as a primary comparative arm in the GRADE trial due to their lack of availability at the trial's inception. As an editor reviewing this manuscript, how does the omission of this now-pillar drug class affect the contemporary relevance of the study, and how should the authors contextualize this limitation?

Key Response

A critical reviewer would flag that the landscape of diabetes management shifted dramatically during the trial's long execution phase. The omission of SGLT2 inhibitors threatens the contemporary external validity of the findings. The authors must transparently acknowledge this and frame their findings specifically as comparative durability among the included classes, while editorial contextualization is needed to remind readers that SGLT2 inhibitors are now standard-of-care second-line agents for many patients.

Guideline Committee
Guideline Committee

Current ADA/EASD guidelines prioritize GLP-1 RAs and SGLT2 inhibitors for patients with high cardiorenal risk. Does the GRADE trial provide sufficient Level A evidence to formally downgrade sulfonylureas and DPP-4 inhibitors to third- or fourth-line therapies even in patients without established cardiovascular disease?

Key Response

Yes. GRADE provides definitive, high-quality comparative effectiveness evidence that sulfonylureas and DPP-4 inhibitors have inferior long-term glycemic durability compared to GLP-1 RAs and basal insulin. This supports strengthening ADA/EASD guideline recommendations that explicitly deprioritize SUs and DPP-4is in favor of GLP-1 RAs for glycemic maintenance in general type 2 diabetes populations, updating algorithms to reflect durability, weight, and hypoglycemia profiles as primary decision drivers rather than just initial A1c lowering.

Clinical Landscape

Noteworthy Related Trials

1998

UKPDS Trial

n = 3,867 · Lancet

Tested

Intensive blood-glucose control with sulfonylureas or insulin

Population

Newly diagnosed T2DM patients

Comparator

Conventional treatment with diet

Endpoint

Microvascular and macrovascular complications

Key result: Intensive glycemic control significantly reduced the risk of microvascular complications but not macrovascular disease initially.
2006

ADOPT Trial

n = 4,360 · NEJM

Tested

Initial monotherapy with rosiglitazone, metformin, or glyburide

Population

Recently diagnosed drug-naive T2DM patients

Comparator

Active comparators among the three drugs

Endpoint

Time to monotherapy failure

Key result: Rosiglitazone provided greater durability of glycemic control compared to metformin and glyburide, though with more adverse effects.
2008

ACCORD Trial

n = 10,251 · NEJM

Tested

Intensive glycemic control target HbA1c below 6.0 percent

Population

T2DM patients with high CV risk

Comparator

Standard glycemic control target HbA1c 7.0 to 7.9 percent

Endpoint

Nonfatal MI, nonfatal stroke, or CV death

Key result: Intensive therapy increased all-cause mortality and did not significantly reduce major cardiovascular events.

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