From the Journals

UC: Tofacitinib tied to modest, reversible lipid increases, infrequent CV events

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Important initial step

Tofacitinib has several well-described effects on lipid metabolism, increasing levels of LDL cholesterol, HDL cholesterol, and total cholesterol. The clinical consequences of these lipid changes remains uncertain in ulcerative colitis (UC), for which there may be an increased risk of cardiovascular events.

In this study, Sands and colleagues used the largest cohort to date to quantify the effect of tofacitinib-associated lipid profile changes, their association with inflammatory markers, and the risk of major adverse cardiovascular events (MACEs). Using pooled data from multiple controlled, open-label studies of tofacitinib in UC, the authors appreciated a significant association between the rise in HDL cholesterol, LDL cholesterol, and total cholesterol levels and declines in C-reactive protein. They noted only four MACEs, an incidence rate similar to that seen in prior anti–tumor necrosis factor trials, and no change in a commonly used risk score for cardiovascular events.

These results are an important initial step in quantifying the cardiovascular risk associated with tofacitinib, but should be interpreted with caution. A significant proportion of individuals evaluated were from induction studies, with only 8 weeks of exposure. Only one dose of tofacitinib was required for inclusion. The median age in the OCTAVE trials, which contributed the majority of the data for this cohort, was only 41 years, and the baseline cardiovascular risk was low. While these data and rheumatologic literature are reassuring, further research with longitudinal follow-up, the assessment of time-varying exposures, and stratification by baseline cardiovascular risk will be required to better understand the association between tofacitinib and MACEs.

Frank I. Scott, MD, MSCE, assistant professor of medicine, Crohn’s and Colitis Center, codirector of clinical research/DART, director of GI fellowship research, division of gastroenterology and hepatology, University of Colorado at Denver, Aurora. He has received research funding and consulting fees from Takeda, and Janssen, and consulting fees from Merck.


 

FROM CLINICAL GASTROENTEROLOGY AND HEPATOLOGY

Serum lipid increases seen after 8-61 weeks of tofacitinib treatment for ulcerative colitis are modest, reversible, and correlated with reduced systemic inflammation, according to results of an analysis including more than 1,000 patients.

Major adverse cardiac events (MACE) were “infrequent” following treatment, according to the authors of the analysis, with an incidence rate similar to what has been reported for tofacitinib in rheumatoid arthritis and for other agents in ulcerative colitis.

That said, the period of observation in the analysis is “relatively short,” and so may not provide an accurate risk estimate for MACE, noted the investigators, led by Bruce E. Sands, MD, of the division of gastroenterology at the Icahn School of Medicine at Mount Sinai, New York.

“Longer-term studies, involving a larger number of patients, will be needed to further assess MACE risk in patients with ulcerative colitis,” Dr. Sands and coinvestigators wrote in their report on the observational analysis, which appears in Clinical Gastroenterology and Hepatology.

“It is noteworthy that no increase in MACE risk and no dose relationship with tofacitinib have been observed in a larger rheumatoid arthritis cohort with over 8.5 years of observation and more than 19,000 patient-years of collective exposure,” they continued.

The present analysis included 1,157 patients with ulcerative colitis who participated in 8-week phase 2 and 3 tofacitinib induction studies, a phase 3 maintenance study, and a long-term extension study that is ongoing.

Reversible and dose-dependent increases in both LDL cholesterol and HDL cholesterol were observed after 8 weeks of treatment with tofacitinib at the recommended induction dose of 10 mg twice daily, the investigators found.

Increases in LDL cholesterol, HDL cholesterol, and total cholesterol correlated with decreases in high-sensitivity C-reactive protein, suggesting any potential impact of lipid increases on cardiovascular events might be offset by reduced inflammation, according to the investigators.

“Previous studies in RA and inflammatory bowel disease have shown an inverse relationship between active inflammation and serum lipid profiles, suggesting that inflammation lowers lipid concentrations, and that treatment of the underlying inflammatory disease may, therefore, increase them,” Dr. Sands and colleagues wrote.

The lipid changes also correlated with increases in body mass index, possibly because of better nutrition, reduced protein loss, and less catabolism following tofacitinib treatment, along with the corticosteroid taper required in these studies of the drug, they added.

Lipid increases generally stayed elevated through 61 weeks of treatment, while in patients randomized to placebo after 8 weeks of tofacitinib treatment, lipid levels fell back toward baseline, which suggests a reversal of the increases after tofacitinib withdrawal, the investigators wrote.

A total of 4 MACEs were seen among the 1,157 patients in the analysis, for an incidence rate of 0.24 (95% confidence interval, 0.07-0.62), according to the report. Those events included an acute coronary syndrome, an MI, an aortic dissection, and a hemorrhagic stroke. All four occurred in tofacitinib-treated patients, though the investigators noted that the aortic dissection and hemorrhagic stroke are events typically associated with genetics or other nonlipid factors.

In any case, that MACE incidence rate was “similar” to infliximab (Remicade) for what has been observed in tumor necrosis factor antagonist treatment of ulcerative colitis within a U.S. claims database study. In that analysis, including patients treated with infliximab, golimumab, and adalimumab, the incidence rate was 0.51 (95% CI, 0.31-0.79), the investigators noted.

These findings, taken together, support recommendations in tofacitinib prescribing information that call for monitoring of lipid concentrations 4-8 weeks after treatment is started, according to Dr. Sands and coauthors.

Funding for the study came from Pfizer. The study authors disclosed potential conflicts of interest related to Pfizer, AbbVie, Amgen, Bristol-Myers Squibb, Celgene, Janssen, MedImmune (AstraZeneca), Millennium Pharmaceuticals, Prometheus Laboratories, Takeda, and 4D Pharma, among others.

SOURCE: Sands BE et al. Clin Gastroenterol Hepatol. 2019 May 8. doi: 10.1016/j.cgh.2019.04.059.

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