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tacrolimus (Envarsus PA / Envarsus / Envarsus XR)

✓ Approved

Paladin Labs, Inc. · FKBP1A · Small Molecule

What is tacrolimus?

tacrolimus is a small molecule developed by Paladin Labs, Inc.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesEnvarsus PA, Envarsus, Envarsus XR
CompanyPaladin Labs, Inc.
Drug ClassSmall Molecule
Molecular TargetFKBP1A
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Paladin Labs, Inc.

Mechanism of Action

Molecular Targets

tacrolimus acts on 1 molecular target:

FKBP1AFKBP prolyl isomerase 1A (FKBP-12, FKBP12)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

tacrolimus is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Immune system disordersSolid organ transplant rejection✓ Approved

Related Research Articles

PubMedFrontiers in cellular and infection microbiology2026-10-15

Etiology, incidence and clinical manifestations of urinary tract infections in evolving population of kidney transplant recipients - a single center 10-year retrospective analysis.

Gołębiewska Justyna E JE, Stefański Krystian K, Pastuszak Krzysztof K, Dębska-Ślizień Alicja A

The aim of the study was to verify how the kidney transplant (KTx) recipient profile changed between 2013 and 2022 and whether these changes influence the incidence, clinical manifestations, and microbiology of urinary tract infections (UTIs). We analyzed clinical data and urine cultures collected during the first posttransplant year in patients who underwent KTx between January 2013 and December 2022. We studied data from 491 patients, who developed 448 episodes of UTIs, including asymptomatic bacteriuria (n=211, 47%), lower UTIs (n=80, 18%), acute graft pyelonephritis (n=97, 22%) and urosepsis (n=60, 13%). During two 5-year time periods (2013-2017 and 2018-2022), the number of recipients aged 70 years or over and 75 years or over increased (p=0.07). Recipients receiving a transplant more recently had higher numbers of mismatching HLA (p=0.001) and maximum CDC-PRA (p=0.001). As a result, in 2018-2022 KTx recipients were more likely to receive induction therapy vs. no induction and tacrolimus vs. cyclosporine-based maintenance immunosuppression (p<0.001). There was a parallel change in the etiology of UTIs, from Escherichia coli being the predominant pathogen (responsible for almost 35% of all UTI episodes in 2013-2017) to Klebsiella pneumoniae, which was isolated in 45% of all UTI episodes between 2018-2022. Klebsiella pneumoniae increased over calendar time (OR/year 1.23, 95% CI 1.08-1.39; p=0.0018). The proportion of highly resistant strains rose from 40.1% in 2013-2017, to 53.4% between 2018-2022 (p=0.008) and also increased in the linear model (p = 0.0369). Over the 10-year period, there was a noticeable change in both KTx recipient and uropathogen characteristics, which requires alteration of antimicrobial prophylaxis and treatment strategies.

PMID 42876619
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PubMedJournal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics2026-10-14

Topical Tacrolimus in Ocular Disease: A Narrative Review of Mechanism of Action and Therapeutic Applications.

Abu Serhan Hashem H, Abu Al-Burak Salem S, Hassan Lameece L, Alshammari Mohammad M et al.

Immune-mediated inflammatory disorders of the ocular surface and anterior segment frequently require sustained immunosuppression, yet prolonged topical corticosteroid use carries the risk of glaucoma, cataract, and infection. Tacrolimus, a macrolide calcineurin inhibitor, has emerged as a steroid-sparing alternative for T-cell-mediated ocular disease. This review summarizes the mechanism of action, ocular pharmacology, clinical applications, and safety profile of topical tacrolimus. Narrative synthesis of the peer-reviewed literature. Tacrolimus binds the immunophilin FK506-binding protein 12; the resulting complex inhibits the phosphatase calcineurin, preventing dephosphorylation and nuclear translocation of the nuclear factor of activated T-cells (NFAT) and thereby suppressing transcription of interleukin-2 and a broad program of pro-inflammatory cytokines. The downstream result is reduced activation across the Th1, Th2, and Th17 lineages, diminished T-follicular helper and B-cell responses, stabilization of mast cells and eosinophils, and anti-angiogenic effects. Compounded topical formulations (typically 0.01%-0.1%) penetrate the cornea and reach therapeutic aqueous concentrations. Topical tacrolimus has shown efficacy in vernal and atopic keratoconjunctivitis, anterior uveitis, scleritis, ocular graft-versus-host disease, cicatrizing conjunctivitis, Thygeson superficial punctate keratitis, autoimmune polyglandular syndrome-1-associated keratitis, and corneal graft rejection. Topical tacrolimus is an effective steroid-sparing immunomodulator for a broad spectrum of T-cell-mediated ocular disease, with a favorable safety profile notable for the absence of steroid-related rises in intraocular pressure or cataractogenesis. Standardized formulations and prospective comparative trials remain priorities.

PMID 42870636
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PubMedTransplantation proceedings2026-10-14

Profound Tacrolimus-Induced Catatonic Encephalopathy in a Kidney Transplant Recipient With Mitochondrial Myopathy: A Cautionary Case of Reversible Neurotoxicity.

Ripa Valeria V, Geffner Stuart R SR, Rosenzweig Matthew G MG, Hanlon Matthew M et al.

Maternally inherited diabetes and deafness (MIDD) is a multisystem mitochondrial disorder most commonly caused by the m.3243A>G pathogenic variant in the MT-TL1 gene. Kidney transplantation in affected individuals presents unique perioperative and immunosuppressive management challenges due to underlying metabolic, neurologic, cardiac, and neuromuscular vulnerability. We report a 64-year-old woman with end-stage renal disease secondary to insulin-dependent diabetes and MIDD (m.3243A>G) who underwent unrelated living donor kidney transplantation. The immediate postoperative period was complicated by diabetic ketoacidosis with lactic acidosis, transient slow graft function, and profound encephalopathy with catatonic features. Neuroimaging showed no acute abnormalities, and electroencephalography demonstrated severe diffuse encephalopathy without epileptiform activity. Tacrolimus levels were supratherapeutic in the early postoperative period. Given concern for calcineurin inhibitor neurotoxicity superimposed on mitochondrial dysfunction, tacrolimus was discontinued, and immunosuppression was switched to cyclosporine. Neurologic status gradually improved, and kidney allograft function fully normalized. This case highlights the substantial perioperative metabolic and neurologic risks associated with kidney transplantation in patients with MIDD. Patients with compensated cardiac dysfunction and manageable neuromuscular impairment should not be excluded from transplantation solely on the basis of mitochondrial cytopathy.

PMID 42875311
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PubMedDiabetes research and clinical practice2026-10-14

Dapagliflozin and 54-week kidney function in kidney transplant recipients with post-transplant diabetes mellitus: a randomized controlled trial.

Li Jinghui J, Fu Zhirong Z, Xu Rongkun R, Zhuang Yanqian Y et al.

To evaluate dapagliflozin effects on kidney function and safety in kidney transplant recipients with post-transplant diabetes mellitus (PTDM). In this single-center, prospective, open-label randomized trial, 68 participants were assigned 1:1 to dapagliflozin 10 mg daily plus standard care or standard care alone. Week-54 observed-data analyses included 27 participants per group; an intention-to-treat multiple-imputation sensitivity analysis included all randomized participants. At week 54, the baseline-adjusted between-group eGFR difference was 6.81 mL/min/1.73 m2 (95 % CI, 1.68 to 11.94; P = 0.010) in the complete-case analysis and 6.05 mL/min/1.73 m2 (95 % CI, 0.99 to 11.11; P = 0.020) after multiple imputation. The estimate was attenuated after additional multivariable adjustment, with the 95 % CI including no difference. Serum magnesium declined less with dapagliflozin, whereas HbA1c and tacrolimus trough concentrations were similar. Observed adverse-event frequencies were similar between groups, although the trial was not powered to assess uncommon safety events. Dapagliflozin showed an exploratory week-54 eGFR signal, but the estimate was sensitive to covariate adjustment and missing-data assumptions. This small trial does not establish a definitive clinically meaningful kidney benefit.

PMID 42874781
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PubMedTransplantation proceedings2026-10-14

Sequential Liver, Kidney, and Heart Transplantation in a Single Recipient: Long-Term Survival Complicated by Chronic Renal Allograft Failure, Lung Cancer, and Recurrent Infection-A Case Report.

Xia Jia-Ni JN, Luo Zhi-Kun ZK, Li Jing-Hao JH, Yu Hang H

Multi-organ transplant recipients face a substantial long-term risk of infection, malignancy, and chronic rejection secondary to prolonged immunosuppression. Sequential liver, kidney, and heart transplantations remain rare, resulting in limited evidence to guide perioperative management and long-term follow-up. A 61-year-old man underwent sequential liver, kidney, and heart transplantations in 2012, 2018, and 2022, respectively. Initial graft function was favorable under an immunosuppressive regimen comprising tacrolimus, mycophenolate mofetil, and corticosteroids. From 2023 onwards, he developed recurrent SARS-CoV-2 infections, lung cancer requiring a segmentectomy, recurrent lower-extremity arteriosclerosis obliterans, and progressive renal allograft failure. He ultimately died from cardiopulmonary arrest precipitated by severe metabolic acidosis and electrolyte derangements complicating renal allograft failure. This case suggests that patients undergoing sequential multi-organ transplantations can achieve meaningful long-term survival with multidisciplinary care and individualized immunosuppression. Nevertheless, complications related to cumulative immunosuppression remain a major challenge, necessitating dynamic follow-up and tailored post-transplant management. Sequential liver, kidney, and heart transplantations are feasible in carefully selected patients. However, the delayed adverse effects of chronic immunosuppression pose a major threat to long-term outcomes, underscoring the absolute necessity for vigilant monitoring and highly individualized pharmacological management.

PMID 42875306
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PubMedDrug design, development and therapy2026-10-13

Interpreting Model-Informed Recommendations for Initial Tacrolimus Dosing in Membranous Nephropathy [Letter].

Fu Wenjing W, Wang Jingyu J

PMID 42866573
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