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Genentech terminates phase II trial of GDC-8264 for cardiac surgery-associated acute kidney injury

Genentech, Inc., a wholly owned subsidiary of Hoffmann-La Roche, has terminated its Phase II GDC-8264 clinical trial evaluating the selective RIPK1...

Genentech Terminates Phase II Trial of RIPK1 Inhibitor GDC-8264 for Cardiac Surgery-Associated Acute Kidney Injury

Genentech, Inc., a wholly owned subsidiary of Hoffmann-La Roche, has terminated its Phase II GDC-8264 clinical trial evaluating the selective RIPK1 inhibitor for the prevention of acute kidney injury in patients undergoing cardiac surgery. According to the ClinicalTrials.gov registry update for NCT06602453, the sponsor cited that the study was "unlikely to demonstrate a statistically significant clinical benefit" as the basis for the early stop. The trial, which had enrolled 67 participants across sites in the United States, Europe, Australia, New Zealand, South Korea, and Canada, was designed to test whether perioperative RIPK1 inhibition could reduce kidney complications following cardiopulmonary bypass procedures. No results have been posted to the registry.

The termination marks the end of clinical development for GDC-8264 — also known as flizasertib or RO7288817 — which Genentech removed from its pipeline in Q1 2025. The decision follows a separate setback for the same molecule in acute graft-versus-host disease, where a Phase Ib trial (NCT05673876) was also discontinued after an interim analysis indicated futility.

How the Acute Kidney Injury Clinical Trial Was Designed

The Phase II study was a randomized, double-blind, placebo-controlled trial conducted in two sequential parts. Genentech designed the study to enroll adults aged 40 and older who were scheduled for non-emergent cardiac surgery requiring cardiopulmonary bypass — including isolated coronary artery bypass grafting, surgical aortic or mitral valve replacement or repair, and combined procedures. Eligible participants had to carry at least one or two predefined risk factors for acute kidney injury, depending on the type of surgery. These risk factors included age over 70, a history of chronic kidney disease with estimated glomerular filtration rate below 60 mL/min/1.73 m², diabetes requiring pharmacotherapy, chronic obstructive pulmonary disease on medical therapy, left ventricular ejection fraction below 40%, or preoperative anemia with hemoglobin below 10 g/dL.

The trial's primary endpoint was the percentage of participants who developed major adverse kidney events within 90 days of surgery, a composite measure known as MAKE90. A co-primary endpoint tracked the number of participants experiencing adverse events over the same period, reflecting the study's dual focus on efficacy and safety. Secondary endpoints included change from baseline in estimated glomerular filtration rate at days 30, 60, and 90 post-surgery; the percentage of participants developing acute kidney injury within seven days of surgery; the incidence of MAKE30 and MAKE60; and the number of participants with new or worsened chronic kidney disease by day 90.

Quadruple masking was employed — participants, care providers, investigators, and outcomes assessors were all blinded. The study used a parallel intervention model, with participants randomized to receive either GDC-8264 or matching placebo administered as film-coated tablets according to a pre-defined dosing regimen. The trial spanned more than 30 sites across 12 countries, with facilities including Duke University Medical Center, Mayo Clinic, Columbia University Irving Medical Center, Yale New Haven Hospital, Stanford University Medical Center, Royal Infirmary of Edinburgh, Hôpital de la Pitié-Salpêtrière in Paris, and Severance Hospital in Seoul.

The study began enrolling on 17 January 2025. The primary completion date was listed as 3 March 2026, but the trial was terminated before reaching that milestone. Of the 67 participants enrolled, several sites had withdrawn prior to termination, including Ronald Reagan UCLA Medical Center and Columbia University Irving Medical Center, suggesting operational challenges alongside the scientific ones.

Why Genentech Stopped the GDC-8264 Acute Kidney Injury Program

The registry states that the Genentech GDC-8264 program was halted because the trial was unlikely to demonstrate statistically significant clinical benefit. The sponsor has not disclosed interim efficacy data, safety signals, or the specific analysis that triggered the decision. A separate published source (Pajulas et al., Frontiers in Immunology, 2025) characterized the termination as being "for business reasons," which may reflect the broader strategic calculus behind the decision but does not contradict the registry's stated rationale of anticipated futility.

The scientific hypothesis underpinning the trial was that RIPK1-mediated necroptosis — a pro-inflammatory form of regulated cell death — plays a central role in renal ischemia-reperfusion injury during cardiac surgery. Preclinical studies, including work by Linkermann et al. (Kidney International, 2012), had demonstrated that RIPK1 inhibition reduced tubular cell necroptosis and preserved renal function in murine models of kidney injury. GDC-8264 had shown potent on-target pharmacodynamic activity in a Phase I healthy volunteer study, where it rapidly and completely inhibited release of CCL4, a downstream chemokine marker of RIPK1 pathway activation (Jones et al., Clinical Pharmacology & Therapeutics, 2023).

The gap between preclinical promise and clinical outcome is not unusual in this therapeutic area. Cardiac surgery-associated acute kidney injury affects up to 30% of surgical patients and is linked to increased mortality, prolonged hospitalization, and progression to chronic kidney disease. Yet no pharmacological intervention has been approved to prevent it. The pathophysiology involves multiple overlapping mechanisms — hemodynamic instability, inflammation, oxidative stress, nephrotoxin exposure — making it difficult to achieve clinically meaningful benefit by targeting a single pathway.

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A Pattern of Setbacks for RIPK1 Inhibitors

The termination of the GDC-8264 clinical trial in NCT06602453 extends a pattern of clinical disappointments for the RIPK1 inhibitor class. GDC-8264 had previously failed in acute graft-versus-host disease, where the Phase Ib trial was stopped after an interim futility analysis. That setback prompted Genentech's pivot to the cardiac surgery-associated acute kidney injury indication — a mechanistically distinct application that leveraged the same core biology of necroptotic cell death during ischemia-reperfusion injury.

Beyond Genentech, other sponsors have encountered similar difficulties. GlaxoSmithKline's GSK2982772, the first RIPK1 inhibitor to enter clinical research in 2014, was eventually returned to the research stage and is no longer listed in the company's active pipeline. Sanofi scrapped its last remaining Denali Therapeutics-partnered RIPK1 inhibitor in January 2025. No RIPK1 inhibitor has achieved regulatory approval for any indication.

Sanofi remains the most active sponsor in the RIPK1 space, with several molecules under investigation in early-phase trials. SAR443122 has been evaluated in Phase II for cutaneous lupus erythematosus and in a Phase Ib study in severe COVID-19. SAR443060 entered a Phase Ib trial in amyotrophic lateral sclerosis. China-based GenFleet Therapeutics has advanced GFH312 into a Phase I study. All of these programs remain in early development, and none has yet generated late-phase efficacy data.

The field appears to be shifting away from broad acute indications — such as organ protection during surgery — toward more mechanistically defined populations in autoimmune and neurodegenerative disease, where RIPK1-driven necroinflammation may play a more tractable role. Whether this recalibration will yield clinical success remains to be determined.

Key Takeaways

  • Cardiac surgery-associated acute kidney injury remains an area with no approved preventive pharmacotherapy, despite affecting up to 30% of patients undergoing cardiopulmonary bypass procedures. The multifactorial pathophysiology — spanning hemodynamic, inflammatory, and nephrotoxic mechanisms — has made single-target interventions difficult to translate from preclinical models to clinical outcomes.

  • The RIPK1 inhibitor class has now accumulated multiple clinical failures across different indications: Genentech's GDC-8264 terminated in both acute graft-versus-host disease and acute kidney injury prevention; GSK's GSK2982772 returned to research stage; Sanofi discontinued its Denali-partnered program. No RIPK1 inhibitor has reached Phase III or received regulatory approval.

  • Remaining clinical activity in the RIPK1 space is concentrated in early-phase trials led by Sanofi (SAR443122 in cutaneous lupus, SAR443060 in ALS) and GenFleet Therapeutics (GFH312 in Phase I), with a strategic pivot toward autoimmune and neurodegenerative indications rather than acute organ injury. The translational gap between preclinical necroptosis biology and clinical efficacy continues to challenge the field.


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