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"Time to Reanimate Il-1ra for Sepsis" by Steven P. LaRosa, M.D.

My introduction to the world of clinical trials in sepsis occurred in the 1990’s while I was an Internal Medicine Resident in the MICU at the Cleveland Clinic. My attending physician and ICU director, Charles J. Fisher, Jr, was the lead investigator for the Phase III trial of Interleukin-1 receptor antagonist (IL-1 ra) in patients with sepsis. The basis of the strategy related to the discovery by Charles Dinarello, M.D. of IL-1 and the role it played in the pathophysiology of febrile vasodilatory shock. During this rotation I had the opportunity to enroll a patient of mine into this trial. He was a previously healthy 28 year old male who perforated his bowel as an initial presentation of inflammatory bowel disease. At the time of enrollment the patient was maxed out on vasopressors for septic shock, in ARDS, DIC and acute renal failure. Within 24 hours of beginning the study drug infusion the patient had a miraculous improvement and ultimately survived. When the study blind was broken at the end of the trial my patient had in fact received IL-1ra and I remain convinced that it was the reason for his survival. The results of the trial indicated a non-statistically significant improvement in survival with IL-1 ra and the drug was ultimately abandoned for the treatment of sepsis. The drug, Kineret, has subsequently been approved for rheumatoid arthritis where it works quite well, has a wide therapeutic index, and a good safety profile.

So what went wrong with IL-1ra with respect to sepsis? The major flaw was the assumption that all patients with sepsis have “a cytokine storm” as the main driver of organ failure with IL-1 as a main player. We now know that a hyper-inflammatory response is just one of the many diverse gene expression profiles that occur in patients with sepsis. The second major flaw was the assumption that a clinical phenotype of patients with a systemic inflammatory response due to infection with an organ failure would describe a population with cytokine storm.

Two recent papers by Steve Opal and colleagues raise interesting hypotheses of target subgroups within the sepsis population who may indeed benefit from IL-1 ra. The first analysis was performed because of the benefits that have been described with IL-1ra in patients with Macrophage Activation Syndrome (MAS), previously known as secondary Hemophagocytic Lymphohistiocytosis (HLH). Macrophage Activation Syndrome is essentially a syndrome characterized by cytokine storm and is associated with rheumatologic illnesses such as Still’s Disease, malignancies and infections. Pro-inflammatory cytokines including IL-1 and IL-18 play a key role in this illness which is characterized by bicytopenia, coagulopathy, liver dysfunction, and hemphagocytosis. Opal and colleagues did a post-hoc subgroup analysis of the Phase III IL-ra in patients with Macrophage Activation- like Syndrome (MALS) as bone marrow aspirates looking for hemphagocytosis were not available. The clinical phenotype for MALS was described as sepsis patients with both DIC and hepatobiliary dysfunction. MALS was seen in 43/763 (5.6%) of the trial population however the mortality seen in the IL-1ra population was 34.6% compared with 64.7% in the placebo group; p=0.0071.

A number of caveats come with this data. First, and most importantly, is that this is a post-hoc analysis with a result that did not undergo a Bonferroni correction for the multiplicity of hypotheses being tested raising the possibility that the observed treatment effect could be due to chance alone. The best that can be said is that the result raises a hypothesis that needs to be tested in a confirmatory trial. Secondly, the data are from a trial completed in the 1990’s where the background care was likely different from what occurs today.  Thirdly, data from Giamerellos-Bourboulis and the Hellenic Sepsis Society would suggest that a ferritin level of > 4420 ng/ml may be a more specific marker to define sepsis population with MALS. Finally, The MALS population constitutes ~ 5% of patients with sepsis which raises its own issues. How can you present a business case to the manufacturer on this population? That being said 5% of the estimated 1.7 million hospitalizations with sepsis in the US each year would translate into 85,000 cases with MALS. From clinical trial feasibility one would have to expect a protracted trial and need many sites to complete enrollment. However, if the subgroup data are to believed, you would need to enroll only 40 patents per treatment arm to have 80% power at an alpha of 0.05.

A second post-hoc analysis on the Phase III IL- 1 ra sepsis was performed to examine treatment effect by baseline IL-1ra levels. A total of 529 subjects had baseline plasma samples available. Data from these samples indicated co-linearity between IL-I beta levels and IL-ra levels thus indicating that IL-1 ra is a good surrogate for a population that has IL-1 activation. In the 54% of patients with baseline IL-1 ra levels >2071pg/ml the 28-day mortality was 45.4% in the placebo group and 34.3% in the IL- 1ra treatment group. This constitutes an absolute risk reduction of 12% and a RRR of 74% at a p value of 0.044.
Many of the same caveats regarding the MALS publication can be stated about this data. Again, this is a post-hoc study that was not corrected for the multiplicity of analyses being conducted. The standard of care was different during this trial and the frozen plasma samples assayed were quite old. That being said, this subgroup makes biologic sense as you are describing a population where IL-1 activation is a key feature. A confirmatory trial in this subgroup would be quite feasible and attractive from a business standpoint as it constitutes 50% of the total sepsis population. Based on the observed treatment effect observed in the subgroup, 302 patients per treatment arm would need to be enrolled in a confirmatory, randomized, placebo-controlled study. One would have to develop a “real-time” IL-1ra assay that could be deployed to investigative sites for use as an inclusion criterion.

In summary, two recent post-hoc analyses raise hypotheses of sepsis subgroups that may benefit from IL-1ra treatment. I would implore the manufacturer of the drug to consider revisiting IL-1ra in sepsis given the devastating toll of the disease and the lack of adjuvant treatments.

Disclaimer: I have no financial conflict of interest with respect Swedish Orphan Biovitrum (the maker of Kineret (IL-1ra)

References:
Crit Care Med 2016; 44(2); 44 (2):275-281
Crit Care Med 2018; 46; 21-28

BMC Medicine 2017; 15:172

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