Some transformations of tacrolimus, an immunosuppressive drug

Skytte, Dorthe Mondrup; Jaroszewski, Jerzy W.; Johansen, Kenneth T.; Hansen, Steen Honoré; Hansen, Lars P.; Nielsen, Peder Bo; Frydenvang, Karla

doi:10.1016/j.ejps.2012.12.001

Cited by 19 publications

(20 citation statements)

References 35 publications

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“…TAC inhibits activation of nuclear factor T (nuclear factor of activated T cells), which is essential for transcription of cytokine genes in T cells, thereby blocking transcription of IL-2 and IFN-γ and ultimately exerting a strong effect on immune suppression. 42 …”

Section: Discussionmentioning

confidence: 99%

Efficacy and safety of tacrolimus combined with glucocorticoid treatment for IgA nephropathy: a meta-analysis

Zhang

Luo

et al. 2018

J Int Med Res

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ObjectiveAs a classical immunosuppressant, tacrolimus (TAC) has been widely used in organ transplantation therapy, but the general benefits of TAC for the treatment of IgA nephropathy (IgAN) remain uncertain. We conducted a meta-analysis to examine the effects of TAC combined with glucocorticoid on IgAN.MethodsWe searched the information databases PubMed/Medline, Embase, Science Citation Index, Chinese Biomedical Literature and the Chinese databases VIP, CNKI and Wan Fang for randomized controlled trials of TAC combined with glucocorticoid as a therapy for IgAN.ResultsTen relevant studies involving 472 patients were included in a meta-analysis. Overall, the TAC group showed a significant decrease in proteinuria compared with the control group (MD: −0.18 g/d, 95% CI: −0.32 to −0.04). No increased risk of adverse events was observed (OR: 0.93, 95% CI: 0.65 to 1.33). In general, the TAC group showed good tolerance.ConclusionEvidence to date clearly indicates that TAC combined with glucocorticoid is quite effective in reducing proteinuria and albuminuria in patients with IgAN. Moreover, we found that patients receiving TAC therapy did not show an increased risk of side effects compared with control group patients. TAC combined with glucocorticoid is a promising medication and merits further research.

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Section: Discussionmentioning

confidence: 99%

Efficacy and safety of tacrolimus combined with glucocorticoid treatment for IgA nephropathy: a meta-analysis

Zhang

Luo

et al. 2018

J Int Med Res

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“…TAC (also known as FK506 or fujimycin) inhibits the activation of a transcription factor essential for the transcription of cytokine genes in T cells, causing the production of cytokines such as IL-2 and IFN-γ to be reduced, and ultimately resulting in immune suppression (29). Since the activation of T cells plays a crucial role in the pathogenesis of inflammatory glomerular diseases (30).…”

Section: Discussionmentioning

confidence: 99%

Tacrolimus combined with low-dose corticosteroids is an effective and safe therapeutic option for refractory IgA nephropathy

Wan

et al. 2016

Experimental and Therapeutic Medicine

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Tacrolimus (TAC) has been shown to improve remission from proteinuria in patients with refractory IgA nephropathy (IgAN); however, the efficacy and safety of TAC in such patients have not been fully explored. Therefore, the present study was conducted to evaluate the tolerance to and efficacy of TAC combined with low-dose corticosteroids in patients with refractory IgAN. This was a single-center retrospective study. A total of 28 patients with refractory IgAN were randomly included and received TAC plus corticosteroid; 26 patients received TAC and prednisone, and 2 patients received TAC and methylprednisolone. In addition, all patients were treated with an angiotensin inhibitor. Total urinary protein excretion, serum albumin, blood glucose, complete remission (CR), partial remission (PR), cholesterol, low-density lipoprotein (LDL), serum creatinine (Scr) and estimated GFR (eGFR) were tested at baseline and at 3, 6 and 12 months after the initiation of treatment in all patients. The primary endpoints were CR and PR. Secondary endpoints included changes of Scr, eGFR, clinical data and adverse events. After 12 months, CR was achieved in 40.1% of patients and PR in 43.4%, yielding a total response rate of 83.5%, and the total urinary protein excretion, serum albumin, cholesterol and LDL results were improved significantly compared with those at baseline. Proteinuria and serum albumin results were significantly improved by month 3 of treatment. Two patients relapsed during months 3-6 of follow-up. At the 12-month follow-up, renal function was improved compared with the baseline level as evidenced by eGFR and Scr, respectively. The blood glucose level was stable. One case of pneumococcal pneumonia developed in a patient treated with TAC plus low-dose methylprednisolone and one case of upper gastrointestinal hemorrhage was found in a patient treated with TAC plus low-dose prednisone; both cases completely recovered after treatment. In conclusion, TAC combined with low-dose corticosteroids may be an effective and safe therapeutic option for the treatment of refractory IgAN. However, given the small number of patients in this study, further prospective randomized controlled trials are required with a larger sample of participants and longer follow-up period.

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“…Although there is extensive literature on the determination and characterization of tacrolimus process related compounds and some potential degradation products [17,18,[23][24][25][26][27][28][29], practically no attention has been paid to the impurities that originate from drug-excipient interactions. The main purpose of this work was to investigate influence of commonly used excipients on degradation of TAC.…”

Section: Introductionmentioning

confidence: 99%

Solid state compatibility study and characterization of a novel degradation product of tacrolimus in formulation

Peterka¹,

Grahek²,

Hren³

et al. 2015

Journal of Pharmaceutical and Biomedical Analysis

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Some transformations of tacrolimus, an immunosuppressive drug

Cited by 19 publications

References 35 publications

Efficacy and safety of tacrolimus combined with glucocorticoid treatment for IgA nephropathy: a meta-analysis

Efficacy and safety of tacrolimus combined with glucocorticoid treatment for IgA nephropathy: a meta-analysis

Tacrolimus combined with low-dose corticosteroids is an effective and safe therapeutic option for refractory IgA nephropathy

Solid state compatibility study and characterization of a novel degradation product of tacrolimus in formulation

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