Patrick Daly

DocwireNews

Recently, the novel Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor, belumosudil, was approved for the treatment of chronic graft-versus-host disease (GVHD) in patients who failed at least 2 prior lines of therapy. However, the effects of belumosudil on the pharmacokinetics of other immunosuppressive therapies (ISTs) are unknown, according to a presentation at the <a href="https://www.hematology.org/Meetings/Annual-Meeting" target="_blank" rel="noopener">64th ASH Annual Meeting and Exposition</a>.
Researchers, led by Eric Gaskill, examined plasma concentrations of tacrolimus or sirolimus in patients with chronic GVHD who received belumosudil and determined it had a clinically significant impact on IST pharmacokinetics, requiring dose adjustments.
<h3>Belumosudil Impacts Tacrolimus or Sirolimus Concentration</h3>
The study retrospectively enrolled 30 patients with chronic GVHD who received belumosudil concurrently with tacrolimus (n=12) or sirolimus (n=26) at the Moffitt Cancer Center between February 2019 and July 2022. Authors noted tacrolimus and sirolimus typically had target concentration ranges of 3-7 ng/mL and 5-10 ng/mL, respectively. Concentration to dose (C-D) ratios were measured at baseline and at 3 points during treatment.
Of note, patients on sirolimus (P&lt;.001) or tacrolimus (P=.014) who initiated belumosudil had significant increases in mean C-D ratio from baseline to all points during concurrent belumosudil treatment. In addition, a higher proportion of patients on concurrent belumosudil had supratherapeutic levels (tacrolimus, 25%; sirolimus, 62%). Researchers found most tacrolimus levels returned to therapeutic ranges after dose adjustments; however, sirolimus levels were more likely to remain at supratherapeutic levels even after dose adjustments.
Due to the different tacrolimus and sirolimus C-D ratios at each point during belumosudil treatment, the authors suggested this combination may require multiple dose adjustments. They also determined a “significant risk” if this drug interaction is left unsupervised, as 12 of the 26 sirolimus patients had sirolimus concentrations &gt;15 ng/mL.
Ultimately, the authors proposed that “empiric dose reductions of at least 25% for [sirolimus] and [tacrolimus] should be considered with co-administration of [belumosudil], with close monitoring of IST levels at baseline and periodically during initial months of concurrent therapy.”
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Belumosudil Significantly Affects IST Serum Concentrations

ASH Annual Meeting 2022

Recently, the novel Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor, belumosudil, was approved for the treatment of chronic graft-versus-host disease ...

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