Tacrolimus shows promise in treatment of dermatologic conditions with risk factors

Key takeaways:

• Tacrolimus may be promising for patients with psoriasis or atopic dermatitis who also have cardiovascular risk factors.
• In dermatologic indications, voclosporin has only been used in psoriasis treatment.

Compared with the systemic calcineurin inhibitor standard cyclosporine, tacrolimus shows promise for numerous dermatologic conditions, whereas the literature on voclosporin is limited, according to a study.

“Systemic calcineurin inhibitors (CNIs), cyclosporine, tacrolimus and voclosporin, are immunosuppressive drugs commonly used in organ transplantation,” Annie Dai, MD, and Soo Jung Kim, MD, PhD, both of the department of dermatology at Baylor College of Medicine, wrote. “CNIs’ main immunomodulatory mechanism is inhibiting interleukin-2 and disrupting T-cell activation.”

While cyclosporine was FDA approved in 1997 for severe psoriasis, tacrolimus and voclosporin are newer with “increased potency and relatively more favorable side effects,” according to the study. Currently, there are no approved dermatologic uses for, or studies regarding the use of, systemic tacrolimus and voclosporin.

In this study, Dai and Kim examined the published literature for tacrolimus and voclosporin to discuss possible monitoring guidelines for dermatologic indications.

Tacrolimus

Tacrolimus was FDA approved in 1994 as a cyclosporine alternative for preventing liver transplant rejection. Tacrolimus is 100 times more effective at suppressing T-cell activation and may lower the risk for cardiovascular disease in at-risk patients compared with cyclosporine, according to the study.

As a result, the researchers found that tacrolimus may be more suitable for patients with psoriasis or atopic dermatitis who also have cardiovascular risk factors. Studies have also reported that tacrolimus could be used as a short-term treatment while transitioning to a long-term treatment.

Tacrolimus also has better intestinal absorption than cyclosporine making it a promising alternative treatment for patients with pyoderma gangrenosum and irritable bowel syndrome and for patients with intestinal Behçet’s disease, according to the study.

Voclosporin

Voclosporin was FDA approved in 2021 for the treatment of active lupus nephritis. Compared with cyclosporine, voclosporin can be used at a lower dosage yet will yield similar results due to its metabolite profile, according to the study.

Researchers believe that voclosporin has the best safety profile of all the CNIs; however, further studies are needed to confirm this hypothesis.

Voclosporin is also currently being studied for its potential antiviral role in COVID-19-positive kidney transplants.

In dermatologic indications, voclosporin has only been used for the treatment of psoriasis. One phase 2 and one phase 3 trial have confirmed that voclosporin reduces psoriasis severity; however, the drug did not outperform cyclosporine.

Adverse events associated with voclosporin most commonly include gastrointestinal upset, headaches and infections, according to the study.

Recommendations

While both drugs show promise for dermatologic indications, the authors recommend that dermatologists should continue to exercise caution when prescribing these medications, limiting their uses to less than 1 year.

“More studies are needed to appropriately determine the efficacy of tacrolimus and voclosporin for off-label dermatologic uses and to develop clinical guidelines,” Dai and Lee wrote.

Reference

• Novel Drug Approvals for 2021. Updated June 13, 2021. Accessed June 13, 2023. https://www.fda.gov/drugs.