Dapagliflozin for the Treatment of Metabolic Dysfunction-Associated Steatotic Liver Disease and Steatohepatitis
Author: Dr. Om J Lakhani
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INTRODUCTION
Metabolic dysfunction-associated steatotic liver disease (MASLD), formerly known as non-alcoholic fatty liver disease (NAFLD), and its more severe form metabolic dysfunction-associated steatohepatitis (MASH), formerly known as non-alcoholic steatohepatitis (NASH), represent a spectrum of hepatic disorders characterized by fat accumulation in the liver in the context of metabolic dysfunction [1]. MASLD/MASH has become a leading cause of chronic liver disease worldwide, with a prevalence estimated at 25-30% of the global population and rising [2,3].
Management of MASLD/MASH has primarily focused on lifestyle interventions, including weight loss through diet and exercise [4]. The urgent need for effective pharmacotherapy has driven intense research into various therapeutic targets, including sodium-glucose cotransporter-2 (SGLT2) inhibitors.
This review focuses on the emerging role of dapagliflozin, an SGLT2 inhibitor, in the management of MASLD/MASH, with particular emphasis on recent high-quality evidence from the DEAN trial and related research. We will examine the efficacy, safety, mechanisms of action, and clinical implications of dapagliflozin therapy in this patient population.
PATHOPHYSIOLOGY AND THERAPEUTIC TARGETS
Pathophysiological Mechanisms in MASLD/MASH
MASLD/MASH involves a complex interplay of metabolic dysregulation, insulin resistance, hepatic lipid accumulation, oxidative stress, and inflammatory processes [5]. The progression from simple steatosis (MASLD) to steatohepatitis (MASH) involves hepatocellular injury, inflammation, and eventual fibrosis, which can progress to cirrhosis and hepatocellular carcinoma [6].
Key pathophysiological mechanisms include:
- Insulin resistance leading to increased lipolysis and hepatic de novo lipogenesis
 - Mitochondrial dysfunction and oxidative stress
 - Proinflammatory cytokine production
 - Adipokine dysregulation
 - Gut microbiota alterations [7]
 
SGLT2 Inhibitors as Therapeutic Agents
SGLT2 inhibitors were initially developed for type 2 diabetes mellitus (T2DM) management. They act by inhibiting sodium-glucose cotransporter-2 in the proximal tubule of the kidney, preventing glucose reabsorption and promoting urinary glucose excretion [8]. This mechanism results in improved glycemic control independent of insulin secretion, along with weight loss, blood pressure reduction, and improvements in cardiovascular and renal outcomes [9].
The potential benefits of SGLT2 inhibitors in MASLD/MASH stem from several mechanisms:
- Reduction in insulin resistance
 - Weight loss and visceral fat reduction
 - Improvement in glycemic control
 - Anti-inflammatory effects
 - Reduction in oxidative stress
 - Modulation of energy metabolism in hepatocytes [10,11]
 
CLINICAL EVIDENCE FOR DAPAGLIFLOZIN IN MASLD/MASH
The DEAN Trial: Design and Population
The DEAN (Dapagliflozin Efficacy and Action in NASH) trial represents the most robust evidence to date for dapagliflozin in MASH [12]. This multicenter, double-blind, randomized, placebo-controlled study enrolled 154 adults with biopsy-confirmed MASH. Key population characteristics included:
- Mean age: 35 years
 - Gender distribution: 85% male
 - Type 2 diabetes: Present in 45% of participants
 - Study population: Predominantly Chinese
 - Treatment duration: 48 weeks
 - Intervention: Dapagliflozin 10 mg daily versus placebo [12,13]
 
The trial's rigorous design, including paired liver biopsies at baseline and 48 weeks, allowed for definitive assessment of histological outcomes—the gold standard for evaluating MASH therapies.
Primary and Key Secondary Outcomes
Primary Endpoint The primary endpoint was MASH improvement, defined as ≥2-point decrease in the NAFLD Activity Score (NAS) without worsening of fibrosis. This endpoint was achieved in 53% of patients receiving dapagliflozin compared to 30% in the placebo group (risk ratio 1.73, 95% CI 1.16–2.58, P=0.006) [12,13].
Key Secondary Endpoints
- 
MASH resolution (defined as no ballooning, no or minimal inflammation, and steatosis <5%) without fibrosis progression occurred in 23% of dapagliflozin-treated patients versus 8% with placebo [12,13].
 - 
Fibrosis improvement without MASH worsening was observed in 45% of the dapagliflozin group compared to 20% in the placebo group. This effect was particularly pronounced among participants with T2DM [12,13].
 - 
Metabolic parameters showed significant improvements with dapagliflozin, including:
 
- Reduced body weight
 - Decreased waist circumference
 - Reduction in abdominal fat
 - Improved HbA1c levels [12,13,14]
 
- Liver enzymes including alanine aminotransferase (ALT), aspartate aminotransferase (AST), and gamma-glutamyl transferase (γ-GT) showed significant reductions with dapagliflozin compared to placebo [14,15].
 
Subgroup Analyses and Predictors of Response
The DEAN trial provided insights into patient subgroups who might derive particular benefit from dapagliflozin therapy:
- 
Patients with T2DM showed more pronounced benefits in both histological endpoints and metabolic parameters compared to non-diabetic participants [13].
 - 
Patients with significant baseline fibrosis (F2-F3) demonstrated substantial improvements in fibrosis scores, suggesting that dapagliflozin may be effective in patients with more advanced disease [12,13].
 - 
Baseline NAS score was not a significant predictor of response, indicating that patients across the spectrum of MASH severity might benefit from treatment [13].
 
Supporting Evidence from Other Studies
Multiple smaller studies and meta-analyses support the findings from the DEAN trial:
- 
Previous studies have demonstrated significant liver fat reduction with dapagliflozin treatment in patients with MASLD and T2DM, as measured by magnetic resonance imaging-derived proton density fat fraction (MRI-PDFF) [16].
 - 
Mechanistic studies have shown that dapagliflozin reduces hepatic oxidative stress and improves mitochondrial function, which may contribute to its beneficial effects in MASH [15].
 - 
Improvements in serum markers of inflammation and fibrosis including ferritin, high-sensitivity C-reactive protein (hs-CRP), and enhanced liver fibrosis (ELF) score have been reported with dapagliflozin treatment [14,15].
 - 
Beneficial effects on lipid profiles have been observed, including reductions in low-density lipoprotein (LDL) cholesterol and triglycerides [14].
 
SAFETY AND ADVERSE EFFECTS
Overall Safety Profile
The DEAN trial reported an overall favorable safety profile for dapagliflozin. The adverse event rate was numerically lower with dapagliflozin (56%) compared to placebo (64%) [12,13]. This is consistent with the established safety profile of SGLT2 inhibitors in patients with T2DM.
Specific Adverse Effects of Concern
Genitourinary Infections Consistent with the known side effect profile of SGLT2 inhibitors, there was a slightly higher incidence of genital mycotic infections in the dapagliflozin group, although the difference was not statistically significant [12,13].
Reduction in Muscle Mass A notable finding was the reduction in muscle mass and skeletal muscle index (SMI) associated with dapagliflozin treatment [17]. This raises concerns about potential sarcopenia, which is particularly relevant for MASLD/MASH patients who may already be at risk for frailty or who have low baseline muscle mass [17,18].
Volume Depletion and Electrolyte Abnormalities Events related to volume depletion (orthostatic hypotension, dehydration) and electrolyte abnormalities were infrequent and comparable between groups [12].
Diabetic Ketoacidosis No cases of diabetic ketoacidosis were reported in the DEAN trial, although this remains a recognized risk with SGLT2 inhibitor therapy, particularly in patients with T2DM [12,13].
Hypoglycemia The incidence of hypoglycemia was low and not significantly different between treatment groups, consistent with the insulin-independent mechanism of action of dapagliflozin [12].
MECHANISM OF ACTION IN MASLD/MASH
Direct and Indirect Effects on the Liver
The beneficial effects of dapagliflozin in MASLD/MASH are mediated through both direct and indirect mechanisms:
Metabolic Effects
- Improved glycemic control
 - Weight loss and visceral fat reduction
 - Decreased insulin resistance
 - Reduction in free fatty acid flux to the liver [19]
 
Direct Hepatic Effects
- Modulation of hepatic energy metabolism
 - Activation of AMP-activated protein kinase (AMPK)
 - Reduction in hepatic de novo lipogenesis
 - Enhancement of fatty acid oxidation [15,19]
 
Anti-inflammatory and Antifibrotic Effects
- Suppression of proinflammatory cytokines
 - Reduction in oxidative stress
 - Decreased activation of hepatic stellate cells
 - Improvement in mitochondrial function [15]
 
Comparative Effects with Other SGLT2 Inhibitors
While the DEAN trial focused specifically on dapagliflozin, evidence suggests that beneficial effects on MASLD/MASH may be a class effect of SGLT2 inhibitors:
- 
Empagliflozin has shown similar liver fat reduction and improvements in liver enzymes in patients with MASLD and T2DM [20].
 - 
Canagliflozin has demonstrated reductions in liver enzymes and improved fibrosis markers in patients with T2DM and MASLD [21].
 - 
Comparative studies between different SGLT2 inhibitors in MASLD/MASH are limited, and it remains unclear whether significant differences in efficacy exist within this class [22].
 
CLINICAL APPLICATIONS AND PATIENT SELECTION
Current Position in Therapeutic Algorithm
The DEAN trial provides high-quality evidence supporting dapagliflozin as among the first agents to meet histological endpoints for MASH improvement [12,13,23].
Based on current evidence, dapagliflozin could be considered in the following context:
- As an adjunct to lifestyle modifications (diet and exercise)
 - Particularly in patients with concomitant T2DM
 - In patients with histologically confirmed MASH, especially with early-stage fibrosis (F2-F3)
 - As part of a multidisciplinary approach to MASLD/MASH management [23]
 
Optimal Patient Selection
Evidence suggests that the following patient characteristics may identify those most likely to benefit from dapagliflozin therapy:
Favorable Candidates
- Patients with coexisting T2DM and MASLD/MASH
 - Patients with obesity or metabolic syndrome
 - Patients with early-stage fibrosis (F2-F3)
 - Patients without significant sarcopenia or frailty [12,13,23]
 
Less Favorable Candidates
- Patients with low muscle mass or sarcopenia
 - Elderly patients at high risk for falls or fractures
 - Patients with advanced fibrosis or cirrhosis (limited evidence)
 - Patients with recurrent genitourinary infections [17,18,23]
 
Practical Recommendations for Clinical Implementation
Baseline Assessment
- Comprehensive metabolic evaluation
 - Assessment of liver disease severity (imaging, non-invasive fibrosis markers, or biopsy in select cases)
 - Measurement of baseline muscle mass and strength
 - Evaluation for sarcopenia risk factors [23,24]
 
Monitoring During Treatment
- Regular assessment of liver enzymes
 - Monitoring of glycemic control in patients with T2DM
 - Body composition analysis to detect changes in muscle mass
 - Surveillance for adverse effects (genitourinary infections, volume depletion) [23,24]
 
Complementary Interventions
- Structured physical activity programs, including resistance training
 - Nutritional strategies to preserve muscle mass
 - Adequate protein intake (1.2-1.5 g/kg/day)
 - Vitamin D supplementation if deficient [17,18,24]
 
LIMITATIONS AND KNOWLEDGE GAPS
Generalizability of Current Evidence
The DEAN trial provides robust evidence for dapagliflozin in MASH, but several limitations should be noted:
- 
The study population was predominantly young (mean age 35), male (85%), and Chinese, which may limit generalizability to older, female, or ethnically diverse populations [12,13].
 - 
The treatment duration was 48 weeks, which may be insufficient to fully assess long-term outcomes such as progression to cirrhosis, hepatocellular carcinoma, or mortality [12,13].
 - 
The trial included a significant proportion of patients with T2DM (45%), and the relative efficacy in non-diabetic versus diabetic MASH remains incompletely characterized [12,13].
 
Ongoing Knowledge Gaps
Several important questions remain unanswered:
- 
Long-term outcomes: Effects on mortality, progression to cirrhosis, hepatocellular carcinoma, and quality of life with dapagliflozin in MASLD/MASH remain uncertain [23,25].
 - 
Muscle mass concerns: The risk-benefit ratio regarding muscle mass loss in broader populations, especially the elderly and those with baseline sarcopenia, needs further exploration [17,18].
 - 
Combination therapies: The potential synergistic effects of dapagliflozin with other emerging therapies (such as FXR agonists, GLP-1 receptor agonists) are not well established [23,25].
 - 
Post-treatment durability: Whether the beneficial effects of dapagliflozin on MASH histology persist after treatment discontinuation remains unknown [23].
 - 
Comparative effectiveness: Direct comparisons with other SGLT2 inhibitors or metabolic drugs are lacking [22,23].
 
Ongoing and Future Studies
Several ongoing clinical trials may address current knowledge gaps:
- Studies evaluating longer treatment durations and post-treatment follow-up
 - Trials investigating combination therapies with other agents (GLP-1 receptor agonists, FXR agonists)
 - Studies focusing on special populations (elderly, non-diabetic MASH, cirrhotic patients)
 - Research specifically addressing the impact on muscle mass and strategies to mitigate this effect [23,25]
 
SUMMARY AND RECOMMENDATIONS
Key Evidence-Based Conclusions
- 
Efficacy: Dapagliflozin demonstrates significant efficacy in improving histological features of MASH, with 53% of treated patients achieving ≥2-point reduction in NAS without worsening fibrosis compared to 30% with placebo [12,13].
 - 
MASH Resolution: Complete resolution of MASH without fibrosis progression was observed in 23% of dapagliflozin-treated patients versus 8% with placebo [12,13].
 - 
Fibrosis Improvement: Improvement in fibrosis without worsening of MASH occurred in 45% of dapagliflozin recipients compared to 20% with placebo, with more pronounced effects among those with T2DM [12,13].
 - 
Metabolic Benefits: Significant improvements in weight, waist circumference, abdominal fat, and glycemic control were observed with dapagliflozin [12,13,14].
 - 
Safety: The overall safety profile was favorable, with a numerically lower adverse event rate with dapagliflozin (56%) compared to placebo (64%), though muscle mass reduction is a concern [12,13,17].
 
Practical Recommendations
Based on current evidence, the following practical recommendations can be made:
- 
Consider dapagliflozin as an adjunctive therapy in patients with biopsy-proven MASH, particularly those with coexistent T2DM, obesity, or metabolic syndrome.
 - 
Monitor closely for muscle loss, especially in patients with risk factors for sarcopenia. Baseline and follow-up assessments of muscle mass and strength are advisable.
 - 
Implement nutritional and physical activity strategies to counteract potential sarcopenia risk, including resistance training and adequate protein intake.
 - 
Use as part of a comprehensive approach to MASLD/MASH management, including lifestyle modifications, metabolic risk factor control, and addressing comorbidities.
 - 
Recognize that dapagliflozin currently lacks regulatory approval for MASLD/MASH, and its use for this indication would be off-label, necessitating appropriate patient counseling.
 - 
Individualize therapy based on patient-specific risk-benefit analysis, with particular caution in elderly patients or those with baseline sarcopenia.
 
Evidence Strength and Future Directions
The DEAN trial provides robust data for the efficacy of dapagliflozin in MASH, but further research is needed to address long-term outcomes, optimal patient selection, and strategies to mitigate muscle mass loss.
As the treatment landscape for MASLD/MASH continues to evolve, dapagliflozin represents a promising option, particularly for patients with concomitant metabolic dysfunction. Ongoing clinical trials and real-world evidence will further refine its role in the management of this increasingly prevalent liver disease.
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