Tigecycline 中文名称: 替加环素

别名: GAR-936; GAR936; Tigecycline; 220620-09-7; Tygacil; WAY-GAR-936; GAR-936; TYGACL; Tigecycline 替加环素; (4S,4aS,5aR,12aS)-4,7-双(二甲氨基)-9-[(叔丁基氨基)乙酰胺基]-3,10,12,12a-四羟基-1,11-二氧代-1,4,4a,5,5a,6,11,12a-八氢并四苯-2-甲酰胺; 替加环素 USP标准品; 替加环素及其中间体; 2-并四苯甲酰胺,4,7-双(二甲胺基)-9-[[2-[(1,1-二甲基乙基)氨基]乙酰基]氨基]-1,4,4A,5,5A,6,11,12A-八氢-3,10,12,12A-四羟基-1,11-二氧代-,(4S,4AS,5AR,12AS); 9-叔丁基甘氨酰氨基米诺环素

目录号: V5447 纯度: ≥98%

COA 产品数据产品说明书 SDS

替加环素（GAR936；GAR-936；TYGACL）是一种有效的四环素抗生素，具有抑菌作用。

Tigecycline CAS号: 220620-09-7
产品类别: Bacterial

产品仅用于科学研究，不针对患者销售

规格	价格	库存	数量
10 mM * 1 mL in DMSO
1mg
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

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Other Forms of Tigecycline:

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InvivoChem产品被CNS等顶刊论文引用

Nature 2024 Dec 18.

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nat Neurosci 2024, 27:1468-1474.

Nat Metab 2024, 6: 1108-1127.

Cell Stem Cell 2024, 31:106-126.e13.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

Immunity 2024,57:2651-2668.e12.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

纯度/质量控制文件

批次：

纯度: ≥98%

COA

MSDS

NMR

产品说明书

产品描述
生物活性&实验参考方法
化学信息
溶解度数据
计算器
临床试验信息
生物数据图片
相关产品

产品描述

替加环素（GAR936；GAR-936；TYGACL）是一种有效的四环素抗生素，具有抑菌作用。它通过与细菌的 30S 核糖体亚基结合，从而阻止氨酰基-tRNA 在原核翻译过程中进入核糖体 A 位点，从而充当蛋白质合成抑制剂。

生物活性&实验参考方法

靶点	Bacterial protein synthesis; FGFR1 (IC50 = 9.3 nM); FGFR2 (IC50 = 7.6 nM); FGFR3 (IC50 = 22 nM); FGFR4 (IC50 = 290 nM)
体外研究 (In Vitro)	替加环素（0.63-30 μM，预洗脱4天，处理72小时）抑制AML2细胞和HL-60细胞，IC50值分别为4.72±0.54和3.06±0.85 μM（新鲜生产）。偏置前一天，替加环素抑制 HL-60 细胞和 AML2 细胞，IC50 值为 4.27±0.45 μM 和 5.64±0.55 μM。替加环素抑制 AML2，IC50 为 5.02±0.60 和 4.39±0.44 μM（预偏置两天）。细胞和 HL-60 细胞的 IC50 值分别为 4.09±0.41 和 3.95±0.39 μM（预稀释三天）。在盐水中预稀释 4 天后，通过 CellTiter 面粉测量，替加环素抑制 TEX 人类细胞漂白的能力下降（从新鲜合成时的 IC50~5 μM）降至 IC50>50 μM [1]。
体内研究 (In Vivo)	在 NOD/SCID 小鼠中，替加环素（50 mg/kg；腹腔注射；每天两次；持续 11 天）可减少肿瘤体积和重量 [1]。在生理盐水中，替加环素的血药峰浓度(Cmax)、终末半衰期(t1/2)、血药浓度-时间曲线下面积(AUC)、清除率(CL)和分布浓度(Vz)为，分别为22.8μg/mL、108.9min、1912.2minμg/mL、26.1mL/min/kg、4109.4mL/kg。在替加环素制剂（60 mg/mL丙酮酸盐、3 mg/mL抗坏血酸、生理盐水）中，血浆峰浓度（Cmax）、血浆浓度-时间曲线下面积（AUC）、清除率（CL）和分布波形（ Vz)为15.7μg/mL、110.3min、2036.5minμg/mL、24.6mL/min/kg和3906.2mL/kg。
细胞实验	细胞活力测定[1] 细胞类型：人类白血病 OCI-AML2、HL-60 (ATCC) 和 TEX 细胞系测试浓度： 0.63- 30 µM 孵育持续时间：预孵育 4 天，处理 72 小时实验结果：抑制 AML2 细胞和HL-60细胞，IC50分别为4.72±0.54和3.06±0.85μM（新鲜制备）。
动物实验	Animal/Disease Models: NOD/SCID Mouse OCI-AML2 acute myeloid leukemia (AML) xenograft model [1] Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; for 7) [1]. twice (two times) daily; continued for 11 days Experimental Results: Reduction in tumor volume and weight. Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse[1] Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; 360 minutes Experimental Results: peak plasma concentration (Cmax), terminal half-life (t1/2), plasma concentration-time The area under the curve (AUC), clearance (CL) and distribution volume (Vz) were all 22.8 μg/108.9 minutes, 1912.2 minutes*μg/ml, 26.1 ml/minute/kg, and 4109.4 ml/kg respectively.
参考文献	[1]. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281. [2]. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271.
其他信息	Tigecycline is tetracycline in which the hydroxy group at position 5 and the methyl group at position 6 are replaced by hydrogen, and with a dimethylamino substituent and an (N-tert-butylglycyl)amino substituent at positions 7 and 9, respectively. A glycylcycline antibiotic, it has activity against a broad range of Gram-positive and Gram-negative bacteria, including tetracycline-resistant organisms. It is used for the intravenous treatment of complicated skin and skin structure infections caused by susceptible organisms. It has a role as an antibacterial drug. It is a member of tetracyclines and a tertiary alpha-hydroxy ketone. It is a conjugate base of a tigecycline(1+). Tigecycline is a Tetracycline-class Antibacterial. A tetracycline derivative that acts as a protein synthesis inhibitor. It is used as an antibacterial agent for the systemic treatment of complicated skin and intra-abdominal infections. It is also used for the treatment of community-acquired pneumonia. See also: Tigecycline (annotation moved to).

*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性

化学信息 & 存储运输条件

分子式	C29H39N5O8
分子量	585.65
精确质量	585.279
元素分析	C, 59.47; H, 6.71; N, 11.96; O, 21.86
CAS号	220620-09-7
相关CAS号	Tigecycline tetramesylate;Tigecycline hydrochloride;197654-04-9;Tigecycline mesylate;1135871-27-0;Tigecycline hydrate;1229002-07-6;Tigecycline-d9;2699607-86-6
PubChem CID	54686904
外观&性状	Light yellow to yellow solid powder
密度	1.5±0.1 g/cm3
沸点	890.9±65.0 °C at 760 mmHg
熔点	164-166°C
闪点	492.6±34.3 °C
蒸汽压	0.0±0.3 mmHg at 25°C
折射率	1.675
LogP	-1.3
tPSA	205.76
氢键供体(HBD)数目	7
氢键受体(HBA)数目	11
可旋转键数目(RBC)	7
重原子数目	42
分子复杂度/Complexity	1240
定义原子立体中心数目	4
SMILES	CC(C)(C)NCC(=O)NC1=CC(=C2C[C@H]3C[C@H]4[C@@H](C(=O)C(=C([C@]4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C
InChi Key	SOVUOXKZCCAWOJ-HJYUBDRYSA-N
InChi Code	InChI=1S/C29H39N5O8/c1-28(2,3)31-11-17(35)32-15-10-16(33(4)5)13-8-12-9-14-21(34(6)7)24(38)20(27(30)41)26(40)29(14,42)25(39)18(12)23(37)19(13)22(15)36/h10,12,14,21,31,36-37,40,42H,8-9,11H2,1-7H3,(H2,30,41)(H,32,35)/t12-,14-,21-,29-/m0/s1
化学名	(4S,4aS,5aR,12aR)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide
别名	GAR-936; GAR936; Tigecycline; 220620-09-7; Tygacil; WAY-GAR-936; GAR-936; TYGACL; Tigecycline
HS Tariff Code	2934.99.9001
存储方式	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
运输条件	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

溶解度数据

溶解度 (体外实验)	DMSO : ~25 mg/mL (~42.69 mM) H2O : ~8.33 mg/mL (~14.22 mM)
溶解度 (体内实验)	配方 1 中的溶解度: ≥ 2.5 mg/mL (4.27 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。配方 2 中的溶解度:* ≥ 2.08 mg/mL (3.55 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。 20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。 View More* 配方 3 中的溶解度: 36.67 mg/mL (62.61 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶. 请根据您的实验动物和给药方式选择适当的溶解配方/方案： 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、以上所有助溶剂都可在 Invivochem.cn网站购买。

溶解度 (体外实验)

DMSO : ~25 mg/mL (~42.69 mM)
H2O : ~8.33 mg/mL (~14.22 mM)

溶解度 (体内实验)

配方 1 中的溶解度: ≥ 2.5 mg/mL (4.27 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

配方 2 中的溶解度: ≥ 2.08 mg/mL (3.55 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

View More

配方 3 中的溶解度: 36.67 mg/mL (62.61 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、以上所有助溶剂都可在 Invivochem.cn网站购买。

制备储备液		1 mg	5 mg	10 mg
	1 mM	1.7075 mL	8.5375 mL	17.0750 mL
	5 mM	0.3415 mL	1.7075 mL	3.4150 mL
	10 mM	0.1708 mL	0.8538 mL	1.7075 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;

3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;

4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。

计算器

质量

浓度

体积

分子量*

计算重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

计算制备已知体积和浓度的溶液所需的化合物的质量
计算将已知质量的化合物溶解到所需浓度所需的溶液体积
计算特定体积中已知质量的化合物产生的溶液的浓度

参见示例

使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？

在分子量（MW）框中输入350.26
在“浓度”框中输入10，然后选择正确的单位（mM）
在“体积”框中输入5，然后选择正确的单位（mL）
单击“计算”按钮
答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。

浓度 (起始)

体积 (起始)

浓度 (终)

体积 (终)

计算重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：

在C1框中输入10，然后选择正确的单位（mM）
在C2框中输入25，然后选择正确的单位（μM）
在V2框中输入25，然后选择正确的单位（mL）
单击“计算”按钮
答案62.5μL（0.1 ml）出现在V1框中

分子式

分子量

g/mol

计算重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4 c12h18n3o4
计算化合物摩尔质量（分子量）的说明：

要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。

分子质量、分子量、摩尔质量和摩尔量的定义：

分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。

配液体积

质量

配液浓度

计算重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

输入试剂的质量、所需的配液浓度以及正确的单位
单击“计算”按钮
答案显示在体积框中

动物体内实验配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg

动物平均体重 g

每只动物给药体积 μL

动物数量

第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。

% DMSO

% Tween 80

% ddH₂O

计算重置

计算结果:

工作液浓度： mg/mL；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意： (1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息

Comparing Tigecycline Vs. Colistimethate in CNS Infections
CTID: NCT06702943
Phase: Status: Not yet recruiting
Date: 2024-11-25

Personalized Treatment of Urogenital Cancers Depends on the Microbiome
CTID: NCT03962920
Phase: N/A Status: Recruiting
Date: 2024-01-30

Study Evaluating The Safety And Effectiveness In Subjects With Tigecycline Treatment
CTID: NCT01072539
Phase: Status: Completed
Date: 2023-12-29

Finding the Optimal Regimen for Mycobacterium Abscessus Treatment
CTID: NCT04310930
Phase: Phase 2/Phase 3 Status: Recruiting
Date: 2023-08-08

Delafloxacin IV and OS Administration Compared to Best Available Therapy in Patients With Surgical Site Infections
CTID: NCT04042077
Phase: Phase 3 Status: Terminated
Date: 2022-02-02

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Antibiotic Therapy for Infectious Diseases
CTID: NCT04937894
Phase: Status: Recruiting
Date: 2021-06-24

A Randomized Controlled Trial Comparing Imipenem and Tigecycline Versus Imipenem and Tigecycline With GM-CSF for the Management of Spontaneous Bacterial Peritonitis Presenting With Septic Shock.
CTID: NCT04208763
Phase: N/A Status: Unknown status
Date: 2021-02-16

Comparative Clinical Study Between Colistin-Tigecycline Combined Therapy Versus Colistin-Meropenem Combined Therapy in Treatment of Blood Stream Infections With Multidrug-Resistant Klebsiella Pneumoniae
CTID: NCT04489459
Phase: Phase 4 Status: Unknown status
Date: 2020-07-29

The Combined Antibiotic Therapy for Carbapenem Resistant Klebsiella Pneumoniae
CTID: NCT03950544
PhaseEarly Phase 1 Status: Unknown status
Date: 2019-05-15

Tygacil Drug Use Investigation
CTID: NCT01789905
Phase: Status: Completed
Date: 2019-02-06

A Study of Plazomicin Compared With Colistin in Patients With Infection Due to Carbapenem-Resistant Enterobacteriaceae (CRE)
CTID: NCT01970371
Phase: Phase 3 Status: Completed
Date: 2018-10-16

Pharmacokinetics and Safety of Tigecycline in the Treatment of Clostridium Difficile Associated Diarrhea (CDAD)
CTID: NCT01401023
Phase: N/A Status: Completed
Date: 2018-07-10

A Study To Determine The Efficacy And Safety Of Tigecycline Compared With Imipenem/Cliastatin to Treat Complicated Intra-Abdominal Infection
CTID: NCT01721408
Phase: Phase 4 Status: Completed
Date: 2018-04-09

Tigecycline for Treatment of Rapidly Growing Mycobacteria
CTID: NCT00600600
Phase: Phase 2 Status: Completed
Date: 2017-05-23

Pharmacokinetics Of Tigecycline In Morbidly Obese Subjects
CTID: NCT01560143
Phase: Phase 4 Status: Completed
Date: 2017-02-09

Study of Tigecycline Pharmacokinetics in Patients Undergoing Continuous Renal Replacement Therapy(CRRT)
CTID: NCT02931526
Phase: Status: Unknown status
Date: 2016-10-13

Impact of Treatment With Colistin on Mortality Bacteremia Multiresistant Acinetobacter Baumannii Sensitive Colistin in Patients Critical
CTID: NCT02573064
Phase: Status: Completed
Date: 2015-10-09

Safety Study Evaluating Intravenous Infusions of Tigecycline to Treat Acute Myeloid Leukemia
CTID: NCT01332786
Phase: Phase 1 Status: Completed
Date: 2015-04-15

Safety and Efficacy Study of a Fluoroquinolone to Treat Complicated Skin Infections
CTID: NCT00719810
Phase: Phase 2 Status: Completed
Date: 2014-07-14

Study Comparing Tigecycline Versus Ceftriaxone Sod
A B-D-GLUCAN DRIVEN ANTIFUNGAL STEWARDSHIP APPROACH TO MANAGE EMPIRICAL THERAPY IN PATIENTS AT VERY HIGH RISK FOR INVASIVE CANDIDIASIS: A RANDOMIZED CONTROLLED TRIAL
CTID: null
Phase: Phase 4 Status: Ongoing
Date: 2017-01-11

Pharmacokinetics of Tigecycline in Patients Receiving Continuous Renal Replacement Therapy
CTID: null
Phase: Phase 4 Status: Completed
Date: 2014-01-14

Perioperative complications in obese and non-obese patients: Prevention and treatment of wound infections and post-operative pain.
CTID: null
Phase: Phase 3 Status: Completed
Date: 2013-05-13

Investigation on the peritoneal tissue concentrations of antibiotics in surgical patients with peritonitis using microdialysis. Example: linezolide, tigecycline
CTID: null
Phase: Phase 4 Status: Completed
Date: 2013-01-22

An Open-Label, Randomized, Multicenter, Phase III Study of Ceftazidime Avibactam (CAZ-AVI) and Best Available Therapy for the Treatment of Infections Due to Ceftazidime Resistant Gram Negative Pathogens
CTID: null
Phase: Phase 3 Status: Completed
Date: 2012-09-11

Target site pharmacokinetics of linezolid or tigecycline in patients with severe skin and skin structure infections (SSSI) associated with chronic fistulas.
CTID: null
Phase: Phase 4 Status: Prematurely Ended
Date: 2011-03-17

A Phase 3, Multicenter, Randomized, and Double-blind Study to Evaluate the Safety of Tigecycline versus a Ceftriaxone Regimen in the Treatment of Complicated Intra-abdominal Infections and Community-acquired Pneumonia in Pediatric Subjects Ages 8 to 17 Years Old
CTID: null
Phase: Phase 3 Status: Completed
Date: 2009-09-15

A Phase 3, Multicenter, Randomized, Double-blind Study to Evaluate the Safety and Efficacy of Tigecycline Versus Comparator (Clindamycin or Vancomycin) for the Treatment of Complicated Skin and Skin Structure Infections, Including Those due to MRSA, in Pediatric Subjects Ages 8 to 17 Years Old
CTID: null
Phase: Phase 3 Status: Completed
Date: 2009-03-20

A Multicenter, Open-Label, Ascending Multiple-Dose Study to Assess the
CTID: null
Phase: Phase 2 Status: Completed
Date: 2008-10-29

A PHASE 2, MULTICENTER, RANDOMIZED, DOUBLE-BLIND, COMPARATIVE STUDY OF THE SAFETY AND EFFICACY OF 2 DOSES OF TIGECYCLINE VERSUS IMIPENEM/CILASTATIN FOR THE TREATMENT OF SUBJECTS WITH HOSPITAL-ACQUIRED PNEUMONIA
CTID: null
Phase: Phase 2 Status: Completed, Prematurely Ended
Date: 2008-09-17

Monozentrische, prospektive, offene Studie zur Untersuchung der „steady state“-Pharmakokinetik von Tigecyclin im Plasma, im ELF und in Alveolarmakrophagen bei Intensivpatienten mit tiefer Atemwegsinfektion.
CTID: null
Phase: Phase 3 Status: Prematurely Ended
Date: 2007-05-16

A Multicenter, Randomized, Double-Blind, Comparison Study of the Safety and Efficacy of a Once-Daily Dose of Tigecycline versus Ertapenem for the Treatment of Foot Infections in Subjects with Diabetes
CTID: null
Phase: Phase 3 Status: Prematurely Ended, Completed
Date: 2006-12-20

A MULTICENTER, RANDOMIZED, OPEN-LABEL COMPARISON OF THE SAFETY
CTID: null
Phase: Phase 4 Status: Completed
Date: 2006-09-22

A Multicenter, Open-Label, Randomized Comparative Study of Tigecycline vs Ceftriaxone Sodium Plus Metronidazole for the Treatment of Hospitalized Subjects With Complicated Intra-abdominal Infection.
CTID: null
Phase: Phase 3 Status: Completed
Date: 2005-12-12

生物数据图片

Ascorbic acid and pyruvate stabilize tigecycline in saline solution. Tigecyline (1 mg/mL) was dissolved in saline solution with or without supplementation with various excipients and incubated in the light. Tigecycline concentrations were detected over time by HPLC and expressed as a relative percentage of that detected immediately following fresh dilution in saline ( = 100%). Tigecycline was dissolved in (A) saline with or without 0.6 mg/mL ascorbic acid, 6 mg/mL pyruvate, 50 mg/mL 2-hydroxypropyl-β-cyclodextrin (HPCD), 0.3 U/mL Oxyrase with 20 mM sodium lactate, 6 mg/mL EDTA sodium, 5% (w/v) glucose, 5% (w/v) mannitol, 10% (v/v) ethanol, 10 mM sodium phosphate (Na-PO4) buffer pH 6.9, or 10 mM sodium bicarbonate (Na-HCO3) buffer pH 6.8; (B) saline containing 0–30 mg/mL ascorbic acid; or (C) saline containing 0–300 mg/mL pyruvate; (D) Iscove's modified Dulbecco's medium (IMDM). In all panels, data indicate the mean ± standard deviation of 3 independent experiments.[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.

Tigecycline is stabilized in solution under novel formulation conditions for up to 7 days. Following dissolution in saline or a novel stabilizing formulation containing ascorbic acid (3 mg/mL) and pyruvate (60 mg/mL) in saline, adjusted to pH 7, tigecycline concentrations were detected by HPLC and expressed as a relative percentage of that detected following fresh dilution in saline ( = 100%). (A) Tigecycline (1 mg/mL) dissolved in saline or the novel formulation was incubated under light or dark conditions, demonstrating light sensitivity. (B) Increasing concentrations of tigecycline were dissolved in the novel formulation and incubated in the dark. Tigecycline stability in solution was reduced at concentrations greater than 1 mg/mL. In all panels, data indicate the mean ± standard deviation of 3 independent experiments.[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.

The novel ascorbic acid- and pyruvate-containing formulation displays efficacy in AML cells grown in vivo. (A) Mice were administered 50/kg tigecycline or 50 mg/kg novel tigecycline formulation by intraperitoneal injection and plasma was collected at increasing times after treatment. Plasma tigecycline concentration was determined using HPLC. The peak plasma concentration (C max), the terminal half-life (t 1/2), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) were evaluated using WinNonlin 6.2.1. Data represent the mean ± standard deviation of a representative experiment with 3 mice per group. Human leukemia OCI-AML2 cells were injected subcutaneously into the flank of NOD/SCID mice. Eleven days after injection, once tumors were palpable, mice were treated with 50 mg/kg of tigecycline, novel formulation of tigecycline, or vehicle controls (saline or formulation) by intraperitoneal injection twice a day for 11 days (n = 9 per group). Tigecycline in each formulation was prepared fresh twice a day. (B) Tumor volume was monitored over time. Eleven days after injection, mice were sacrificed and tumors excised. (C) Tumor weight was measured. ** indicates p<0.01 and * indicates p<0.05 as determined by Tukey's post-test and one-way ANOVA analysis. Lines represent median. (D) Total proteins were extracted and analyzed by immunoblotting for Cox-1, Cox-2 and Cox-4 expression. PVDF membrane was stained with 0.1% Amido Black.[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.