更新于：2024-06-22
Tacrolimus
他克莫司
更新于：2024-06-22
概要
基本信息
药物类型 小分子化药 |
别名 LCP-TACRO、mdc-GRT、Tacrolimus (INN) + [45] |
靶点 |
作用机制 CaN抑制剂(钙神经素抑制剂) |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (1994-04-08), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国)、孤儿药 (日本) |
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结构
分子式C44H71NO13 |
InChIKeyNWJQLQGQZSIBAF-MLAUYUEBSA-N |
CAS号109581-93-3 |
关联
1,343
项与 他克莫司 相关的临床试验Prospective Case Series of Intestinal and Multivisceral Transplantation for Unresectable Mucinous Carcinoma Peritonei (TRANSCAPE)
High Dose Ruxolitinib and Allogeneic Stem Cell Transplantation in Myelofibrosis Patients With Splenomegaly
A Single Center, Non-Randomized, Phase 1b Study of Orca-T Following Escalated Dose of Total Marrow and Lymphoid Irradiation in Patients With Acute Leukemias and MDS
100 项与 他克莫司 相关的临床结果
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100 项与 他克莫司 相关的转化医学
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100 项与 他克莫司 相关的专利（医药）
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23,965
项与 他克莫司 相关的文献（医药）2024-12-31The Journal of dermatological treatment
Efficacy and safety of 308-nm Excimer lamp combined with Tacrolimus 0.1% ointment vs Tacrolimus 0.1% ointment as monotherapy in treating children with limited vitiligo: a randomized controlled trial
Article
作者: Cork, Michael J ; Ba-Shammakh, Saleh A ; Tashman, Osama ; Alshiyab, Diala ; Al-Qarqaz, Firas ; Al-Fakih, Abdulqudos ; Muhaidat, Jihan ; Sarakbi, Danyah ; Atwan, Ausama
OBJECTIVE:
This study aims to assess the efficacy and safety of combining the 308-nm Excimer lamp with Tacrolimus 0.1% ointment, compared to Tacrolimus 0.1% ointment monotherapy, for treating pediatric vitiligo involving less than 10% of the body surface area.
METHODS:
Fifty pediatric patients with vitiligo were randomly assigned to two groups. Group A received Tacrolimus 0.1% ointment twice daily and Excimer light at 308-nm twice weekly, while Group B received Tacrolimus 0.1% ointment alone, administered twice daily. Repigmentation percentages were evaluated after 30, 90, and 180 days using the rule of nine.
RESULTS:
Group A exhibited a significant improvement in repigmentation, increasing from 10% after one month to 65% after six months. In contrast, Group B observed an increase from 10% to 30% over the same timeframe. The efficacy of the treatment was significantly higher in Group A at both the 3-month and 6-month follow-up points (p-value < .001). Moreover, Group A achieved notably higher repigmentation rates in the face, trunk, and lower limbs.
CONCLUSION:
The combination of Tacrolimus and the 308-nm excimer lamp yielded superior repigmentation results compared to Tacrolimus monotherapy in pediatric vitiligo patients. This combined approach may offer an effective new treatment protocol for pediatric vitiligo.
2024-05-01Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology
Unique association of anti-GABAA receptor encephalitis and myasthenia gravis in a patient with type A thymoma
Article
作者: Duan, Weiwei ; Tan, Hong ; Zhan, Qiong ; Yin, Weifan ; Wu, Feng ; Lu, Wei ; Zeng, Qiuming ; Gu, Wenping ; Ouyang, Song ; Wu, Xiaomei
Association between anti-GABAAR encephalitis and myasthenia gravis is extremely rare with few reported cases. Herein, we report a case of a female patient diagnosed with anti-GABAAR encephalitis and thymoma at the first admission. She was administered glucocorticoids for long-term immunotherapy, and thymectomy with biopsy demonstrated a type A thymoma. After 4 months, the symptoms of encephalitis were relieved, but she then developed post-thymectomy myasthenia gravis with anti-AChR and anti-titin dual positivity. Antibodies to connective tissue (anti-ANA, anti-PCNA) and those characteristics of paraneoplastic syndrome (anti-Ma2/Ta) were also positive. She received oral glucocorticoids and tacrolimus as immunosuppressive therapy, and myasthenic symptoms were stable during a 2-year follow-up. Our case revealed that anti-GABAAR encephalitis and myasthenia gravis can appear in patient with type A thymoma at different periods, which alerts physicians to take long-term follow-up for anti-GABAAR encephalitis with thymoma, even after thymectomy. Concurrent positivity for more than one antibody after thymectomy is rarely observed, and their contribution to the clinical course and treatment decision remains to be further investigated.
2024-05-01Biochimica et biophysica acta. Proteins and proteomics
Propagation of conformational instability in FK506-binding protein FKBP12
Article
作者: Hernández, Griselda ; Bashir, Qamar ; LeMaster, David M
FKBP12 is the archetype of the FK506 binding domains that define the family of FKBP proteins which participate in the regulation of various distinct physiological signaling processes. As the drugs FK506 and rapamycin inhibit many of these FKBP proteins, there is need to develop therapeutics which exhibit selectivity within this family. The long β4-β5 loop of the FKBP domain is known to regulate transcriptional activity for the steroid hormone receptors and appears to participate in regulating calcium channel activity for the cardiac and skeletal muscle ryanodine receptors. The β4-β5 loop of FKBP12 has been shown to undergo extensive conformational dynamics, and here we report hydrogen exchange measurements for a series of mutational variants in that loop which indicate deviations from a two-state kinetics for those dynamics. In addition to a previously characterized local transition near the tip of this loop, evidence is presented for a second site of conformational dynamics in the stem of this loop. These mutation-dependent hydrogen exchange effects extend beyond the β4-β5 loop, primarily by disrupting the hydrogen bond between the Gly 58 amide and the Tyr 80 carbonyl oxygen which links the two halves of the structural rim that surrounds the active site cleft. Mutationally-induced opening of the cleft between Gly 58 and Tyr 80 not only modulates the global stability of the protein, it promotes a conformational transition in the distant β2-β3a hairpin that modulates the binding affinity for a FKBP51-selective inhibitor previously designed to exploit a localized conformational transition at the homologous site.
100 项与 他克莫司 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 间质性肺疾病 | 日本 | 2013-06-14 | |
| 小肠移植排斥 | 日本 | 2011-07-26 | |
| 溃疡性结肠炎 | 日本 | 2009-07-07 | |
| 粘膜炎 | 日本 | 2008-01-25 | |
| 同种异体移植排斥反应 | 欧盟 | 2007-04-23 | |
| 同种异体移植排斥反应 | 冰岛 | 2007-04-23 | |
| 同种异体移植排斥反应 | 列支敦士登 | 2007-04-23 | |
| 同种异体移植排斥反应 | 挪威 | 2007-04-23 | |
| 肝移植排斥反应 | 欧盟 | 2007-04-23 | |
| 肝移植排斥反应 | 冰岛 | 2007-04-23 | |
| 肝移植排斥反应 | 列支敦士登 | 2007-04-23 | |
| 肝移植排斥反应 | 挪威 | 2007-04-23 | |
| 狼疮性肾炎 | 日本 | 2007-01-26 | |
| 胰腺移植排斥反应 | 日本 | 2005-01-19 | |
| 肺移植排斥反应 | 日本 | 2003-01-31 | |
| 心脏移植排斥反应 | 日本 | 2001-06-20 | |
| 重症肌无力 | 日本 | 2000-09-20 | |
| 特应性皮炎 | 日本 | 1999-06-16 | |
| 骨髓移植排斥反应 | 日本 | 1999-04-30 | |
| 肾移植排斥反应 | 日本 | 1996-04-16 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 新型冠状病毒感染 | 临床3期 | 西班牙 | 2020-04-01 | |
| 肺损伤 | 临床3期 | 西班牙 | 2020-04-01 | |
| 霍奇金淋巴瘤 | 临床3期 | 美国 | 2009-06-01 | |
| 霍奇金淋巴瘤 | 临床3期 | 美国 | 2009-06-01 | |
| 非霍奇金淋巴瘤 | 临床3期 | 美国 | 2009-06-01 | |
| 非霍奇金淋巴瘤 | 临床3期 | 美国 | 2009-06-01 | |
| 皮肌炎 | 临床3期 | 日本 | 2007-07-01 | |
| 皮肌炎 | 临床3期 | 日本 | 2007-07-01 | |
| 肺炎 | 临床3期 | 日本 | 2007-07-01 | |
| 肺炎 | 临床3期 | 日本 | 2007-07-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 125 | Tacrolimus continuous infusion | 糧鹹醖範鑰鹽糧繭顧餘(壓衊憲網鏇鑰鑰餘窪構) = 鑰醖觸壓憲齋鬱廠範淵 壓襯鹹鑰鑰願顧繭齋築 (齋廠糧夢糧願繭網鑰壓 ) 更多 | 积极 | 2024-05-14 | ||
临床2期 | 8 | 繭淵淵獵餘鏇憲餘遞網(遞糧廠餘鏇齋衊願觸窪) = none 夢鏇襯構壓壓壓鬱廠築 (簾鹽選艱夢繭願製襯鹽 ) 更多 | 积极 | 2024-04-15 | |||
临床2期 | 20 | 製遞積憲觸齋廠醖餘廠(夢廠衊糧膚淵製鑰壓鹽) = 願衊簾鹽簾蓋鏇鏇窪襯 蓋膚獵觸衊蓋窪廠獵鹹 (鏇範鏇觸淵淵鏇積蓋衊, 餘襯蓋蓋淵壓鏇夢構鑰 ~ 襯鑰淵繭築構顧淵廠選) 更多 | - | 2024-03-12 | |||
临床2期 | 61 | Umbilical Cord Blood Transplantation+Fludarabine Phosphate+Busulfan+CYCLOPHOSPHAMIDE+Melphalan+Tacrolimus+Ruxolitinib+mycophenolate mofetil+Methotrexate | 構餘製淵夢壓醖範範網(觸構獵夢壓網獵蓋壓顧) = 觸築齋構製醖製鹽鏇繭 齋醖鹽範選淵繭鏇蓋鑰 (夢餘廠餘鏇範淵鹹膚鬱, 醖鹽觸壓繭壓範範膚齋 ~ 願網鏇膚衊築積糧繭願) 更多 | - | 2024-03-05 | ||
临床2期 | - | 41 | (Envarsus XR) | 鬱齋艱膚遞遞糧願襯鏇(糧獵選構製鹽鬱鬱夢夢) = 繭觸構構蓋廠簾衊醖壓 襯蓋鏇網選鹽選齋淵鹽 (糧鹽製鏇觸蓋壓壓鑰壓, 願憲憲製鬱廠糧壓顧繭 ~ 鏇壓鹹繭構鑰選繭夢鏇) 更多 | - | 2024-01-22 | |
(IR Tacrolimus (Historical Control)) | 構遞選築蓋齋遞齋鑰壓(遞願壓繭鹹製夢艱夢鑰) = 願窪衊襯構齋壓鏇壓襯 積艱壓願膚繭鬱齋窪鹽 (獵構憲構糧廠鏇淵鏇壓, 鹽製鏇構齋願膚選齋壓 ~ 鹹窪遞鏇衊繭觸鏇壓積) 更多 | ||||||
GlobeNewswire 人工标引  | 临床2期 | 4 | TFF TAC | 製鹽糧鏇願鏇襯襯夢觸(齋簾鑰範簾窪範蓋襯獵) = No clinical evidence of acute rejection，No signs and symptoms suggestive of acute rejection，No use of pulse corticosteroids，No deterioration in spirometry，No chest X-ray findings suggestive of acute rejection 簾積鹹醖壓範齋鏇憲鑰 (壓憲鹹夢鹽構衊膚餘製 ) 更多 | 积极 | 2024-01-19 | |
临床2期 | 11 | (Matched Sibling Donor Group) | 製餘願遞餘襯鏇顧襯願(衊遞獵顧衊網廠膚築壓) = 範憲膚構蓋製淵構網顧 鹹築壓艱鏇鏇齋鏇憲廠 (觸築構糧蓋蓋獵艱壓鏇, 構範淵範願願醖繭艱蓋 ~ 顧範憲憲網齋積網鏇淵) 更多 | - | 2024-01-17 | ||
Stem Cell Infusion+Clofarabine+Fludarabine+Busulfan+Cyclophosphamide+Decitabine+Tacrolimus+mycophenolate mofetil+cytarabine+Idarubicin (Haploidentical Donor Group) | 製餘願遞餘襯鏇顧襯願(衊遞獵顧衊網廠膚築壓) = 製窪願鬱衊鏇網淵襯製 鹹築壓艱鏇鏇齋鏇憲廠 (觸築構糧蓋蓋獵艱壓鏇, 憲壓鏇鹹鹽鏇淵蓋膚蓋 ~ 築築蓋壓鬱鹹構窪範獵) 更多 | ||||||
临床3期 | 431 | 構齋餘鏇淵鑰鬱選鏇鹽(遞鏇淵淵鏇繭鹹鑰網淵) = 襯餘壓鏇窪鹽醖衊壓鏇 蓋繭壓壓繭襯鹽鑰鑰選 (簾繭憲艱鑰觸積構衊鹹, 鹽獵膚選網膚衊築鬱願 ~ 鬱淵積鹽夢獵鹹衊鹽遞) 更多 | - | 2024-01-12 | |||
N/A | - | 249 | 壓艱廠鑰鑰積網鬱窪鑰(簾製範衊廠繭獵觸廠窪) = 顧糧壓範淵鑰憲襯鹽鹹 蓋範觸積夢齋壓鑰襯觸 (襯願網願衊選鹹蓋繭膚, 31 ~ 48) 更多 | 积极 | 2024-01-01 | ||
壓艱廠鑰鑰積網鬱窪鑰(簾製範衊廠繭獵觸廠窪) = 窪網構範簾獵選壓膚窪 蓋範觸積夢齋壓鑰襯觸 (襯願網願衊選鹹蓋繭膚, 8 ~ 21) 更多 | |||||||
N/A | - | 鬱窪遞蓋範廠憲襯襯壓(糧窪製襯糧壓膚衊衊醖) = 築蓋鹹衊醖觸構齋壓製 積衊製壓齋餘觸繭鑰膚 (觸憲齋鹽襯顧製範壓鬱, 0.19 ~ 0.28) 更多 | - | 2023-12-11 |
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