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tacrolimus (Envarsus PA / Envarsus / Envarsus XR)

✓ Approved

Paladin Labs, Inc. · FKBP1A · 小分子

什么是 tacrolimus？

tacrolimus 是一种小分子，由Paladin Labs, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Envarsus PA, Envarsus, Envarsus XR
公司Paladin Labs, Inc.
药物类别小分子
分子靶点FKBP1A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Paladin Labs, Inc.

作用机制

分子靶点

tacrolimus 作用于 1 个分子靶点：

FKBP1AFKBP prolyl isomerase 1A (FKBP-12, FKBP12)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

tacrolimus 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Immune system disordersSolid organ transplant rejection✓ Approved

相关研究文献

PubMedAntibodies (Basel, Switzerland)2026-10-26

Primary Mesangial Proliferative Glomerulonephritis: The Forgotten Glomerulopathy.

Filippone Edward J EJ, Farber John L JL

Primary mesangial proliferative glomerulonephritis (MesPGN) refers to the light microscopic description of increased mesangial cells (greater than three cells per mesangial area) without endocapillary proliferation, necrosis, and crescents in the absence of another primary glomerulopathy (e.g., IgA nephropathy) or systemic illness (e.g., lupus). Immunofluorescence may be negative or contain mesangial IgM +/- complement (IgM nephropathy) or C1q + immunoglobulin (C1q nephropathy). The presence of either immune deposits or mesangial proliferation per se connotes a worse prognosis when compared with minimal changes. Segmental sclerosis may be present and imparts a worse prognosis regardless of mesangial proliferation or immune deposits. Primary MesPGN may present clinically as nephrotic syndrome, non-nephrotic proteinuria +/- hematuria, or isolated hematuria. If nephrotic, MesPGN may be considered nosologically as a primary podocytopathy with secondary mesangial cell activation, especially when immunofluorescence is negative. Such podocyte injury may be driven by circulating factors and/or antibodies directed against podocyte-specific antigens. Alternatively, IgM or complement deposits suggest an antibody-driven immune-complex etiology primarily affecting the mesangium with secondary podocyte injury analogous to IgA nephropathy, especially when presenting as non-nephrotic proteinuria or hematuria. No randomized controlled trials have addressed immunosuppression in primary MesPGN. If non-nephrotic or isolated hematuria, supportive care is indicated. If nephrotic, initial immunosuppression should mimic that of the primary podocytopathies (high-dose oral steroids), although tacrolimus may substitute if there is a concern for steroid toxicity. For frequently relapsing/steroid-dependent cases, rituximab is our choice for adults, probably with maintenance dosing. Steroid-resistant cases may be treated with calcineurin inhibition.

PMID 42930038
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PubMedInternational journal of emergency medicine2026-10-26

Low-volume body bag cooling for severe exertional heat stroke in the emergency department: a case report.

Ikeda Takao T, Watase Taketo T, Kondo Takashiro T, Watase Hiroko H et al.

Exertional heat stroke (EHS) is a life-threatening emergency in which delayed or inadequate cooling substantially increases the risk of death and permanent neurological injury. Core temperature reduction to below 39 °C within 30 min is the therapeutic target, and cold-water immersion achieves the fastest cooling rates (0.15-0.35 °C/min) but is frequently unavailable in emergency departments (ED) due to equipment and space limitations. Body bag-based tarp-assisted cooling with oscillation (TACO) has been proposed as an alternative using universally available materials; however, clinical evidence supporting its emergency department use remains limited. A 57-year-old immunocompromised male construction worker (acute myeloid leukemia, status post umbilical cord blood transplantation, maintained on prednisolone and tacrolimus) presented with EHS following 90 min of outdoor labor in ambient conditions of 36 °C and 65% relative humidity. On ED arrival, rectal temperature was 42.0 °C, Glasgow Coma Scale score was 4, blood pressure was 125/80 mmHg, and heart rate was 183 beats/minute. Body bag-based TACO was initiated immediately upon arrival using 15 L of tap water and 15 kg of ice. Endotracheal intubation for airway protection was performed concurrently, demonstrating patient accessibility during cooling. Target temperature (rectal temperature < 39 °C) was achieved in 39 min at a cooling rate of 0.085 °C/min. Glasgow Coma Scale score improved to 14 within 7.5 h of admission. The hospital course was complicated by bacteremia requiring prolonged antimicrobial therapy. The patient was discharged ambulatory on hospital day 42 without neurological sequelae. Body bag-based TACO required substantially less water (15 L) than the water/ice volumes reported in TACO studies (114-151 L) using materials available in any ED. Although the cooling rate achieved (0.085 °C/min) fell below published benchmarks, the patient achieved complete neurological recovery, suggesting that immediate initiation of cooling may help offset a suboptimal rate. While a single case cannot establish equivalence to cold-water immersion, body bag-based TACO offers a practical, low-cost option for initiating cooling when standard infrastructure is unavailable, and merits further comparative evaluation.

PMID 42928101
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PubMedCureus2026-10-25

Crowned Dens Syndrome Mimicking Septic Arthritis in a Renal Transplant Recipient.

Praveen Nair Harishankar H, Butt Hassan H, Au Marcus M, Heaney Jonathan J

Crowned dens syndrome (CDS) is a rare manifestation of calcium pyrophosphate deposition (CPPD) disease, characterized by crystal deposition surrounding the odontoid process. It typically presents with acute neck pain, restricted cervical movement, and elevated inflammatory markers, frequently mimicking infection or other inflammatory conditions. We report a 66-year-old man with end-stage renal disease secondary to congenital obstructive uropathy and a cadaveric renal transplant, maintained on tacrolimus and prednisolone. He presented with worsening left wrist pain and swelling accompanied by severe neck pain and marked restriction of cervical movement. Elevated inflammatory markers and peripheral joint inflammation initially raised concern for septic arthritis, prompting joint aspiration and empirical intravenous antibiotics. Persistent neck pain led to computed tomography (CT) of the cervical spine, which demonstrated characteristic peri-odontoid calcification consistent with CDS. Magnetic resonance imaging (MRI) demonstrated mild thickening of the cruciate ligaments and excluded cervical cord compression. Radiographs of the left hand and wrist demonstrated soft-tissue calcification consistent with peripheral CPPD. Following multidisciplinary rheumatology and nephrology input, he was treated with colchicine and an increased corticosteroid dose, resulting in rapid clinical improvement and near-complete resolution of symptoms. This case demonstrates an important diagnostic challenge in renal transplant recipients. Chronic immunosuppression increases susceptibility to infection, making prompt exclusion of septic arthritis essential in patients presenting with an acutely swollen joint. However, chronic kidney disease and associated abnormalities of mineral metabolism also predispose to CPPD. CDS should therefore remain an important differential diagnosis when significant neck pain and restriction persist despite initial treatment. CT is particularly valuable for demonstrating characteristic peri-odontoid calcification, while MRI provides complementary assessment when neurological or alternative spinal pathology is suspected. Renal transplantation should not narrow the differential diagnosis to infection alone. CDS should be considered in patients with persistent acute neck pain and risk factors for CPPD once serious infection has been appropriately investigated. Early CT imaging and multidisciplinary management can facilitate diagnosis, enable appropriately tailored anti-inflammatory therapy, and avoid unnecessary prolonged antimicrobial treatment or invasive investigation.

PMID 42924027
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PubMedTherapeutic advances in drug safety2026-10-25

Drug interactions in rheumatoid arthritis: a disparity between electronic database prediction and real-world co-prescription with different large language models.

Lalitkanjanakul Tonson T, Pitidhammabhorn Dhanesh D, Jakramonpreeya Natnicha N, Suechanyapong Werapat W et al.

Rheumatoid arthritis (RA) is a chronic inflammatory disease that often requires multi-drug regimens, which can increase the risk of drug-drug interactions (DDIs). To determine whether polypharmacy contributes to potential DDIs in patients with RA. A retrospective observational study that integrates data from drug interaction databases and medical records, supplemented by artificial intelligence analysis. Twenty-one RA drugs and 54 commonly prescribed medicines were screened for potential DDIs using the Micromedex and WebMD databases and compared with real-world co-prescription at our hospital. The ChatGPT-5 and Gemini 2.5 large language models (LLMs) were also evaluated as "AI judges" versus an expert rheumatologist to assess real-world co-prescription. This study was conducted from January to September 2025. Among 75 frequently prescribed medicines in RA patients, 753 database-predicted potential DDIs were reported, with Micromedex showing 464 DDI pairs and WebMD showing 600 pairs. Both databases classified 47 serious potential DDIs as contraindicated or major, with high concordance. The main predicted DDI mechanisms were immunosuppression (27%), methotrexate toxicity (18%), and nephrotoxicity (12%), with tacrolimus (12%), methotrexate (10%), and infliximab (6%) as major culprit drugs. In real-world co-prescriptions, 259 RA patients showed methotrexate/naproxen (46.4%) and methotrexate/sulfasalazine (29.5%) as the most common real-world co-prescribing patterns with potential DDIs. Brennan-Prediger kappa values indicated fair agreement (0.3161) in the electronic database predictions and conditional agreement (0.9807) among preselected serious DDIs. The LLM evaluation revealed that advanced models (e.g., Gemini 2.5 Pro) provided finesse recommendations highly concordant with expert opinion, whereas simpler models were more conservatively aligned with database alerts. In both real-world co-prescription and database evaluation, serious potential DDIs were associated mainly with methotrexate toxicity. Based on these exploratory findings, advanced LLMs show potential to assist with the contextualizing rigid database alerts and supporting pragmatic clinical decision-making. However, expert clinical judgment and direct patient consultation remain essential to improve RA patient safety and medication adherence.

PMID 42923782
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PubMedJournal of clinical pharmacology2026-10-23

Population Pharmacokinetic Analysis of Tacrolimus in Time-Dependent Increase of Clearance for Patients with Living-Donor Liver Transplantation: A Prospective Observational Study.

Matsumoto Naoya N, Oda Kazutaka K, Shimata Keita K, Hirukawa Kazuya K et al.

Tacrolimus is a first-line immunosuppressant used to prevent rejection in living donor liver transplantation (LDLT) and is subject to therapeutic drug monitoring due to its concentration-dependent effects and side effects. Metabolism of tacrolimus is reduced by the CYP3A5*3 allele. In addition, liver regeneration over time leads to increased tacrolimus clearance. The purpose of this study was to develop a tacrolimus population pharmacokinetic (popPK) model that takes into consideration the CYP3A5*3 allele and the time-dependent increase in clearance. To develop the popPK model, we used data from 25 recipients and 25 donors who received LDLT and tacrolimus at Kumamoto University Hospital. The measured data consisted of four blood concentration points including peak values at 12 h after the first dose of tacrolimus, and trough blood concentrations obtained by TDM on consecutive days. Nonlinear mixed-effects modeling method was used to develop the popPK model, and i-Densy by ARKRAY Co., Ltd. was used for CYP3A5 gene polymorphism analysis. The popPK model was developed as a one-compartment model incorporating a time-dependent sigmoidal model for clearance. Total bilirubin value was found to be a predictor of volume of distribution and rate constant of absorption, while aspartate transaminase was found to be a predictor of volume of distribution. The CYP3A5*3 allele was not found to be a predictor of tacrolimus pharmacokinetics. We developed a popPK model that includes a time-dependent increase in CL of tacrolimus for patients with LDLT.

PMID 42910779
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PubMedFrontiers in immunology2026-10-23

Clinical study of eculizumab with or with not tacrolimus in the treatment of generalized myasthenia gravis.

Yang Bin B, Wang Jing J, Zhao Xiuli X, Jing Chuya C et al.

Eculizumab, an antibody that inhibits the complement system, and the immunosuppressant Tacrolimus are both authorized for treating patients with generalized myasthenia gravis (GMG). This study seeks to evaluate and compare the clinical effectiveness of Eculizumab with or with not Tacrolimus in the treatment of generalized myasthenia gravis. A retrospective study was performed involving 95 patients with GMG treated with Eculizumab at three hospitals in China. Among them, 80 patients were included in the analysis: 57 received Eculizumab alone, while 23 were treated with a combination of Eculizumab and Tacrolimus. The main outcome assessed was the percentage of GMG patients who reached Minimal Symptom Expression (MSE). Secondary outcomes included changes in MG-Activities of Daily Living (MG-ADL) scale, Quantitative Myasthenia Gravis (QMG) score, CH50 concentration, and doses of pyridostigmine and prednisolone. Additionally, the safety profiles of both treatment groups were examined. In the main outcome, a higher proportion of patients reached MSE status when treated with a combination of Eculizumab and Tacrolimus compared to Eculizumab alone (Eculizumab: 29 patients, 50.9% vs Eculizumab and Tacrolimus: 18 patients, 78.3%; p<0.05). Regarding secondary outcomes, both treatment groups showed significant improvements in clinical symptoms, as indicated by notable reductions in QMG and MG-ADL scores, along with a significant reduction in prednisolone dosage. Furthermore, analysis of secondary outcome parameters revealed no significant differences between the two groups (p>0.05). The decrease in complement CH50 concentration is accompanied by a decrease in QMG and MG-ADL scores, indicating that Eculizumab treats GMG through the mechanism of complement system. In terms of security, hyperuricemia was more commonly associated with the combination therapy of Eculizumab and Tacrolimus than with Eculizumab alone. Our research indicates that Eculizumab can effectively reduce disability in GMG patients by inhibiting complement system activation under real-world clinical conditions in China. We observed a correlative link between Eculizumab and Tacrolimus combination treatment and an increased probability of achieving MSE status, in comparison with Eculizumab monotherapy. However, combination therapy is associated with a higher risk of elevated serum uric acid among GMG patients, which necessitates regular close monitoring of renal function.

PMID 42908923
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