Cardiovascular

Myeloperoxidase inhibition with mitiperstat in heart failure with preserved or mildly reduced ejection fraction: a randomized phase 2b trial.

TL;DR

Mitiperstat was safe and well tolerated but did not improve symptoms or exercise function in chronic heart failure with preserved or mildly reduced ejection fraction.

Key Findings

Mitiperstat (pooled doses) did not significantly improve the co-primary endpoint of Kansas City Cardiomyopathy Questionnaire Total Symptom Score (KCCQ-TSS) at 16 weeks compared to placebo.

  • Placebo-corrected difference in mean change from baseline was -1.4 points (95% CI -3.9, 1.2; P = 0.29)
  • 711 patients were randomized 1:1:1 to mitiperstat 2.5 mg, mitiperstat 5 mg, or placebo
  • Trial was multicenter, randomized, double-blind, placebo-controlled, three-arm, parallel-group phase 2b design
  • 45% of enrolled patients were women

Mitiperstat (pooled doses) did not significantly improve the co-primary endpoint of 6-minute walk distance (6MWD) at 16 weeks compared to placebo.

  • Placebo-corrected difference in mean change from baseline was 3.8 m (95% CI -3.1, 10.8; P = 0.28)
  • 6MWD was evaluated at 16 weeks as one of the two co-primary endpoints
  • Neither the 2.5 mg nor the 5 mg dose achieved significance

Mitiperstat did not improve any secondary endpoints, including natriuretic peptides, inflammatory markers, or echocardiographic parameters.

  • Secondary endpoints included changes in natriuretic peptides and inflammatory markers assessed up to 48 weeks
  • Echocardiographic parameters were assessed up to 24 weeks
  • No secondary endpoint showed significant improvement with mitiperstat versus placebo

Adverse and serious adverse events, including infections, were similar between mitiperstat and placebo groups, with the exception of maculopapular rash.

  • Maculopapular rash occurred in 3.6% of mitiperstat-treated patients versus 0.4% of placebo-treated patients
  • Overall rates of adverse events and serious adverse events were similar across groups
  • Infection rates were comparable between mitiperstat and placebo groups
  • The authors concluded mitiperstat was 'safe and well tolerated'

The trial was designed to test whether MPO inhibition could improve outcomes in heart failure with ejection fraction greater than 40%, based on the mechanistic rationale that MPO-derived oxidants reduce nitric oxide bioavailability and promote coronary microvascular dysfunction, cardiomyocyte stiffening, and interstitial fibrosis.

  • Patients had heart failure with preserved or mildly reduced ejection fraction (EF >40%)
  • Treatment duration was 48 weeks
  • Co-primary endpoints were assessed at 16 weeks
  • MPO inhibition was hypothesized to address mechanisms specifically implicated in HFpEF/HFmrEF pathogenesis

The trial enrolled 711 patients randomized across three arms over a 48-week treatment period.

  • Randomization was 1:1:1 to mitiperstat 2.5 mg, mitiperstat 5 mg, or placebo
  • The study was registered at ClinicalTrials.gov as NCT04986202
  • The trial was multicenter with international participation including centers in multiple countries based on the author affiliations

What This Means

This research tested whether a drug called mitiperstat, which blocks an enzyme called myeloperoxidase (MPO), could help people with a type of heart failure where the heart muscle pumps adequately but is too stiff. The idea behind the treatment was that MPO produces harmful chemical substances that reduce the availability of nitric oxide, stiffen heart muscle cells, and cause scarring — all of which are thought to contribute to this type of heart failure. The study enrolled 711 patients and randomly assigned them to receive one of two doses of mitiperstat or a placebo (inactive treatment) for 48 weeks, measuring whether symptoms and exercise ability improved after 16 weeks. The results showed that mitiperstat did not improve patients' heart failure symptoms as measured by a standard patient questionnaire (KCCQ-TSS), nor did it improve how far patients could walk in 6 minutes. Additionally, no improvements were seen in any of the other measures tested, including markers of heart stress in the blood (natriuretic peptides), inflammatory markers, or heart structure and function on ultrasound. The drug was generally well tolerated — side effects and serious complications were similar between the mitiperstat and placebo groups — though a skin rash occurred more often in patients taking mitiperstat (3.6%) compared to placebo (0.4%). This research suggests that blocking MPO with mitiperstat, despite a strong biological rationale, does not translate into clinical benefit for patients with this form of heart failure. These findings highlight how difficult it remains to develop effective treatments for heart failure with preserved ejection fraction, and raise questions about whether MPO inhibition is an effective therapeutic target for this condition, or whether different patient populations, doses, or treatment strategies might need to be explored.

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Citation

Lund L, Lam C, Pizzato P, Michaëlsson E, Mattsson A, Ericsson H, et al.. (2026). Myeloperoxidase inhibition with mitiperstat in heart failure with preserved or mildly reduced ejection fraction: a randomized phase 2b trial.. Nature medicine. https://doi.org/10.1038/s41591-026-04615-z