Afatinib (BIBW2992)

别名: BIBW2992; Afatinib free base; BIBW 2992; BIBW 2992; Afatinib; trade name: Gilotrif, Tomtovok and Tovok 阿法替尼; 阿法替尼杂质; 阿法替尼 BIBW2992; 阿法替尼-D4;阿法替尼标准品; 马来酸阿法替尼;N-[4-[(3-氯-4-氟苯基)氨基]-7-[[(3S)-四氢-3-呋喃基]氧基]-6-喹唑啉基]-4-(二甲基氨基)-2-丁烯酰胺
目录号: V0536 纯度: ≥98%
阿法替尼(原 BIBW 2992;BIBW-2992;商品名:Gilotrif)是一种有效的、共价/不可逆的、口服生物利用的双 (EGFR/ErbB) 受体酪氨酸激酶 (RTK) 抑制剂,具有抗癌活性。
Afatinib (BIBW2992) CAS号: 850140-72-6
产品类别: EGFR
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
1g
Other Sizes

Other Forms of Afatinib (BIBW2992):

  • 阿法替尼双马来酸盐
  • Afatinib-d6 dimaleate (BIBW 2992MA2-d6)
  • 阿法替尼-D6
  • 草酸阿法替尼
  • (R)-Afatinib ((R)-BIBW 2992)
  • Afatinib-d4 (BIBW 2992-d4)
点击了解更多
InvivoChem产品被CNS等顶刊论文引用
顾客使用InvivoChem 产品阿法替尼发表1篇科研文献
纯度/质量控制文件

纯度: ≥98%

产品描述
阿法替尼(原 BIBW 2992;BIBW-2992;商品名:Gilotrif)是一种有效的、共价/不可逆的、口服生物利用的双 (EGFR/ErbB) 受体酪氨酸激酶 (RTK) 抑制剂,具有抗癌活性。阿法替尼是 FDA 批准的用于治疗非小细胞肺癌 (NSCLC) 的抗癌药物。它在美国以 Gilotrif 品牌销售。它不可逆地结合并抑制 EGFR/HER2,包括 EGFR(wt)、EGFR(L858R)、EGFR(L858R/T790M) 和 HER2,在无细胞测定中 IC50 分别为 0.5 nM、0.4 nM、10 nM 和 14 nM;对吉非替尼耐药的 L858R-T790M EGFR 突变体的活性高 100 倍。
生物活性&实验参考方法
靶点
EGFRL858R (IC50 = 0.4 nM); EGFR (wt) (IC50 = 0.5 nM); ErbB4 (IC50 = 1 nM); EGFRL858R/T790M (IC50 = 10 nM); HER2 (IC50 = 14 nM)
体外研究 (In Vitro)
体外活性:BIBW2992 对野生型和突变型 EGFR 和 HER2 均显示出有效的活性。它针对 L858R EGFR 的效力与吉非替尼相似,但针对吉非替尼耐药的 L858R-T790M EGFR 双突变体的活性高出约 100 倍。 BIBW2992 对体内 EGFR 和 HER2 磷酸化表现出有效的作用。在所有测试的细胞类型中,例如表达 wt EGFR 的人表皮样癌细胞系 A431、转染 wt HER2 的鼠 NIH-3T3 细胞以及乳腺癌细胞系 BT,其与参考化合物(例如 Lapatinib 等)相比均具有优势-474和胃癌细胞系NCI-N87,表达内源性HER2。激酶测定:将人 EGFR 的野生型酪氨酸激酶结构域以及 EGFR L858R/T790M 双突变体的酪氨酸激酶结构域与谷胱甘肽-S-转移酶 (GST) 融合并提取。然后在抑制剂 BIBW2992(在 50% DMSO 中连续稀释)存在的情况下测定酶活性。使用随机聚合物 pEY (4:1) 作为底物,并添加生物素化 pEY (bio-pEY) 作为示踪底物。使用杆状病毒系统克隆 HER2 的激酶结构域,并以与 EGFR 激酶类似的方式进行提取。补充信息中提供了 EGFR、HER2、SRC、BIRK 和 VEGFR2 激酶活性测定的详细信息。细胞测定:将 1 × 104 个 NSCLC 细胞转移至 96 孔板的每个孔中,并在无血清培养基中培养过夜,用于 EGFR 磷酸化测定。第二天添加 BIBW2992 后,将板在 37°C 下孵育 1 小时。 EGF 刺激使用 100 ng/mL 在室温下进行 10 分钟。用冰冷的 PBS 洗涤细胞,每孔用 120 μL HEPEX 缓冲液提取,并在室温下摇动 1 小时。每孔全部 2 × 104 个细胞用于 HER2 磷酸化测定。链霉亲和素预包被板用封闭缓冲液中 1:100 稀释的抗 EGFR-生物素和 c-erb2/HER2 癌蛋白 Ab-5(克隆 N24)-生物素包被。然后将细胞提取物转移至抗体包被的孔中并在室温下孵育1小时。消光在 450 nm 处测量。
体内研究 (In Vivo)
每日口服 20 mg/kg 的 BIBW2992 持续 25 天可导致肿瘤显着消退,累积治疗/对照肿瘤体积比(T/C 比)为 2%。通过组织切片的免疫组织化学染色证实 EGFR 和 AKT 磷酸化的减少。因此,与拉帕替尼和来那替尼一样,BIBW2992是下一代酪氨酸激酶抑制剂(TKI),可不可逆地抑制人表皮生长因子受体2(Her2)和表皮生长因子受体(EGFR)激酶。 BIBW2992 不仅能有效对抗厄洛替尼或吉非替尼等第一代 TKI 靶向的 EGFR 突变,还能对抗那些对这些标准疗法不敏感的患者。
酶活实验
将人 EGFR 野生型和 EGFR L858R/T790M 双突变酪氨酸激酶结构域与 GST 融合并提取。接下来,在使用和不使用抑制剂 BIBW2992 的情况下测量酶活性,BIBW2992 在 50% DMSO 中连续稀释。添加生物素化 pEY (bio-pEY) 作为示踪底物,并使用随机聚合物 pEY (4:1) 作为底物。利用杆状病毒系统,以类似于 EGFR 激酶的方式克隆和提取 HER2 激酶结构域。补充信息包含有关 EGFR、HER2、SRC、BIRK 和 VEGFR2 激酶活性检测的具体信息。
细胞实验
对于 EGFR 磷酸化测试,将 1 × 104 NSCLC 细胞接种到 96 孔板的每个孔中,并在无血清培养基中生长整夜。第二天,添加 BIBW2992 后,将板在 37°C 下孵育一小时。 EGF 刺激在室温下使用 100 ng/mL 进行 10 分钟。在室温下振荡一小时并使用每孔 120 μL HEPEX 缓冲液提取后,用冰冷的 PBS 清洗细胞。 HER2 磷酸化检测每孔总共使用 2 × 104 细胞。 c-erb2/HER2 癌蛋白 Ab-5(克隆 N24)-生物素和抗 EGFR-生物素以 1:100 稀释在封闭缓冲液中包被在链霉亲和素预包被板上。一旦进入抗体包被的孔中,细胞提取物就可以在室温下静置一小时。消光测量发生在 450 nm 处。
动物实验
Athymic NMRI-nu/nu female mice[1]
20 mg/kg
Oral administration
Four bitransgenic mice on continuous doxycycline diets for more than 6 weeks were subjected to MRI (Figure 4) to document the lung tumor burden. Afatinib (BIBW2992) formulated in 0.5% methocellulose-0.4% polysorbate-80 (Tween 80) was administered orally by gavage at 20 mg/kg once daily dosing schedule. Rapamycin was dissolved in 100% ethanol, freshly diluted in 5% PEG400 and 5% Tween 80 before treatment and administered by intraperitoneal injection at 2 mg/kg daily dosage. Mice were monitored by MRI every 1 or 2 weeks to determine reduction in tumor volume and killed for further histological and biochemical studies after drug treatment. For immunohistochemistry staining, three tumor-bearing mice in each group were treated three times with either Afatinib (BIBW2992) (20 mg/kg) alone or Afatinib (BIBW2992) (20 mg/kg) and rapamycin 2 mg/kg at 24 h intervals and killed 1 h after the last drug delivery. All the mice were kept on the doxycycline diet throughout the experiments. Littermates were used as controls.[1]
药代性质 (ADME/PK)
Absorption, Distribution and Excretion
Following oral administration, time to peak plasma concentration (Tmax) is 2 to 5 hours. Maximum concentration (Cmax) and area under the concentration-time curve from time zero to infinity (AUC0-∞) values increased slightly more than dose proportional in the range of 20 to 50 mg. The geometric mean relative bioavailability of 20 mg tablets was 92% as compared to an oral solution. Additionally, systemic exposure to afatinib is decreased by 50% (Cmax) and 39% (AUC0-∞), when administered with a high-fat meal compared to administration in the fasted state. Based on population pharmacokinetic data derived from clinical trials in various tumor types, an average decrease of 26% in AUCss was observed when food was consumed within 3 hours before or 1 hour after taking afatinib.
In humans, excretion of afatinib is primarily via the feces. Following administration of an oral solution of 15 mg afatinib, 85.4% of the dose was recovered in the feces and 4.3% in urine. The parent compound afatinib accounted for 88% of the recovered dose.
The volume of distribution of afatinib recorded in healthy male volunteers is documented as 4500 L. Such a high volume of distribution in plasma suggests a potentially high tissue distribution.
The apparent total body clearance of afatinib as recorded in healthy male volunteers is documented as being a high geometric mean of 1530 mL/min.
Metabolism / Metabolites
Enzyme-catalyzed metabolic reactions play a negligible role for afatinib in vivo. Covalent adducts to proteins were the major circulating metabolites of afatinib.
Biological Half-Life
Afatinib is eliminated with an effective half-life of approximately 37 hours. Thus, steady-state plasma concentrations of afatinib were achieved within 8 days of multiple dosing of afatinib resulting in an accumulation of 2.77-fold (AUC0-∞) and 2.11-fold (Cmax). In patients treated with afatinib for more than 6 months, a terminal half-life of 344 h was estimated.
毒性/毒理 (Toxicokinetics/TK)
Hepatotoxicity
Elevations in serum aminotransferase levels are common during afatinib therapy occurring in 20% to 50% of patients, but rising above 5 times the upper limit of the normal range in only 1% to 2%. Hepatic failure is said to have occurred in 0.2% of patients and to have resulted in several fatalities. Hepatotoxicity appears to be a class effect among protein kinase inhibitors of EGFR2, although liver injury appears to be more frequent and more severe with gefitinib than with afatinib and erlotinib. Specific details of the liver injury associated with afatinib such as latency, serum enzyme pattern, clinical features and course, have not been published. Other EGFR inhibitors, such as erlotinib and gefitinib typically cause liver injury arising within days or weeks of starting therapy and presenting abruptly with hepatocellular enzyme elevations and a moderate-to-severe course. Immunoallergic and autoimmune features are not common. The rate of clinically significant liver injury and hepatic failure is increased in patients with preexisting cirrhosis or hepatic impairment due to liver tumor burden.
Likelihood score: D (possible cause of clinically apparent liver injury).
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the clinical use of afatinib during breastfeeding. Because afatinib is about 95% bound to plasma proteins, the amount in milk is likely to be low. However, its half-life is about 37 hours and it might accumulate in the infant. the manufacturer recommends that breastfeeding be discontinued during afatinib therapy and for 2 weeks after the last dose.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
Protein Binding
In vitro binding of afatinib to human plasma proteins is approximately 95%. Afatinib binds to proteins both non-covalently (traditional protein binding) and covalently.
参考文献

[1]. Oncogene . 2008 Aug 7;27(34):4702-11.

[2]. Expert Opin Investig Drugs . 2014 Jan;23(1):135-43.

其他信息
Pharmacodynamics
Aberrant ErbB signaling triggered by receptor mutations, and/or amplification, and/or receptor ligand overexpression contributes to the malignant phenotype. Mutation in EGFR defines a distinct molecular subtype of lung cancer. In non-clinical disease models with ErbB pathway deregulation, afatinib as a single agent effectively blocks ErbB receptor signaling resulting in tumor growth inhibition or tumor regression. NSCLC tumors with common activating EGFR mutations (Del 19, L858R) and several less common EGFR mutations in exon 18 (G719X) and exon 21 (L861Q) are particularly sensitive to afatinib treatment in non-clinical and clinical settings. Limited non-clinical and/or clinical activity was observed in NSCLC tumors with insertion mutations in exon 20. The acquisition of a secondary T790M mutation is a major mechanism of acquired resistance to afatinib and gene dosage of the T790M-containing allele correlates with the degree of resistance in vitro. The T790M mutation is found in approximately 50% of patients' tumors upon disease progression on afatinib, for which T790M targeted EGFR TKIs may be considered as a next line treatment option. Other potential mechanisms of resistance to afatinib have been suggested preclinically and MET gene amplification has been observed clinically. At the same time, the effect of multiple doses of afatinib (50 mg once daily) on cardiac electrophysiology and the QTc interval was evaluated in an open-label, single-arm study in patients with relapsed or refractory solid tumors. Ultimately, no large changes in the mean QTc interval (i.e., >20 ms) were detected in the study.
*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
C24H25CLFN5O3
分子量
485.94
精确质量
485.162
元素分析
C, 59.32; H, 5.19; Cl, 7.30; F, 3.91; N, 14.41; O, 9.88
CAS号
850140-72-6
相关CAS号
Afatinib dimaleate;850140-73-7;Afatinib-d6;1313874-96-2;Afatinib oxalate;1398312-64-5;(R)-Afatinib;439081-17-1;Afatinib-d4
PubChem CID
10184653
外观&性状
White to light yellow solid powder
密度
1.4±0.1 g/cm3
沸点
676.9±55.0 °C at 760 mmHg
熔点
100 - 102 °C
闪点
363.2±31.5 °C
蒸汽压
0.0±2.1 mmHg at 25°C
折射率
1.668
LogP
3.59
tPSA
88.61
氢键供体(HBD)数目
2
氢键受体(HBA)数目
8
可旋转键数目(RBC)
8
重原子数目
34
分子复杂度/Complexity
702
定义原子立体中心数目
1
SMILES
N(C1C=CC(F)=C(Cl)C=1)C1=NC=NC2=CC(=C(C=C12)NC(=O)/C=C/CN(C)C)O[C@@H]1COCC1
InChi Key
ULXXDDBFHOBEHA-CWDCEQMOSA-N
InChi Code
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
化学名
(E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide
别名
BIBW2992; Afatinib free base; BIBW 2992; BIBW 2992; Afatinib; trade name: Gilotrif, Tomtovok and Tovok
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: ~97 mg/mL (~199.6 mM)
Water: <1 mg/mL
Ethanol: ~15 mg/mL (~30.9 mM)
溶解度 (体内实验)
配方 1 中的溶解度: ≥ 2.5 mg/mL (5.14 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: ≥ 2.5 mg/mL (5.14 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (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 900 μL 玉米油中并混合均匀。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (5.14 mM) (饱和度未知) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
*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 4 中的溶解度: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10 mg/mL

配方 5 中的溶解度: 5 mg/mL (10.29 mM) in 0.5% Methylcellulose/saline water (这些助溶剂从左到右依次添加,逐一添加), 悬浊液; 超声助溶。
*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。

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 2.0579 mL 10.2893 mL 20.5787 mL
5 mM 0.4116 mL 2.0579 mL 4.1157 mL
10 mM 0.2058 mL 1.0289 mL 2.0579 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

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
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。

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
g/mol

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。
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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)
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。
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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。

(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
Sotorasib Activity in Subjects With Advanced Solid Tumors With KRAS p.G12C Mutation (CodeBreak 101)
CTID: NCT04185883
Phase: Phase 1    Status: Recruiting
Date: 2024-11-29
Dual Inhibition of EGFR With Afatinib and Cetuximab in the Treatment of Advanced Squamous Cell Cancers of the Head and Neck
CTID: NCT02979977
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-26
Afatinib in Patients with Fanconi Anemia (FA) and Advanced Head and Neck Squamous Cell Carcinoma (HNSCC)
CTID: NCT06648096
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-20
Afatinib With CT and RT for EGFR-Mutant NSCLC
CTID: NCT01553942
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-20
Pemigatinib + Afatinib in Advanced Refractory Solid Tumors
CTID: NCT06302621
Phase: Phase 1    Status: Recruiting
Date: 2024-11-18
View More

Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
CTID: NCT02465060
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-11-18


Trastuzumab Deruxtecan(T-DXd) and Afatinib Combination in HER2-low Advanced Gastric Cancer
CTID: NCT06085755
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-11-06
The Study Observes Afatinib as First-line Treatment in Patients With Epidermal Growth Factor Receptor (EGFR) Mutation-positive Advanced Non-small Cell Lung Cancer
CTID: NCT04206787
Phase:    Status: Completed
Date: 2024-11-05
LUX-Head&Neck 3: Afatinib (BIBW2992) Versus Methotrexate for the Treatment of Recurrent and/or Metastatic Head and Neck Squamous Cell Cancer After Platinum Based Chemotherapy
CTID: NCT01856478
Phase: Phase 3    Status: Active, not recruiting
Date: 2024-10-31
Target Therapy With GEMOX in Recectable Gallbladder Carcinoma Patients Monitored by ctDNA
CTID: NCT04183712
Phase: Phase 2    Status: Recruiting
Date: 2024-10-16
Study Evaluating Zenocutuzumab in Patients with or Without Molecularly Defined Cancers
CTID: NCT05588609
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-10-03
Phase 1/2 Study of MRTX849 in Patients With Cancer Having a KRAS G12C Mutation KRYSTAL-1
CTID: NCT03785249
Phase: Phase 1/Phase 2    Status: Recruiting
Date: 2024-09-20
Real-World Effectiveness of Afatinib (Gilotrif) Following Immunotherapy in the Treatment of Metastatic, Squamous Cell Carcinoma of the Lung: A Multi-Site Retrospective Chart Review Study in the U.S.
CTID: NCT04750824
Phase:    Status: Completed
Date: 2024-09-19
A Study to Learn About the Effectiveness of Cancer Medicines in Patients With Metastatic Non-small Cell Lung Cancer in Norway.
CTID: NCT05834348
Phase:    Status: Completed
Date: 2024-09-04
A Phase II Evaluation of Afatinib in Patients With Persistent or Recurrent HER2-positive Uterine Serous Carcinoma
CTID: NCT02491099
Phase: Phase 2    Status: Recruiting
Date: 2024-08-20
Study of Afatinib in Advanced Cutaneous Squamous Cell Carcinoma
CTID: NCT05070403
Phase: Phase 2    Status: Recruiting
Date: 2024-08-02
Low-dose Radiotherapy Plus Tislelizumab in Combination With Afatinib for Neoadjuvant Treatment of Surgically Resectable Head and Neck Squamous Carcinoma
CTID: NCT06494189
Phase: Phase 1    Status: Recruiting
Date: 2024-07-10
Phase 2 Trial of Afatinib Plus Prednisone for Advanced Squamous NSCLC
CTID: NCT04497584
Phase: Phase 2    Status: Recruiting
Date: 2024-07-09
Pilot Trial for Treatment of Recurrent Glioblastoma
CTID: NCT05432518
PhaseEarly Phase 1    Status: Recruiting
Date: 2024-06-03
Observational Study of Afatinib 30 mg Daily
CTID: NCT04909073
Phase:    Status: Recruiting
Date: 2024-05-17
Study of EGFR TKI in Patients With Advanced NSCLC Harbouring EGFR Mutations
CTID: NCT06062823
Phase: Phase 2    Status: Recruiting
Date: 2024-05-17
Testing Afatinib as Potentially Targeted Treatment in Cancers With EGFR Genetic Changes (MATCH - Subprotocol A)
CTID: NCT06385483
Phase: Phase 2    Status: Active, not recruiting
Date: 2024-05-06
Afatinib in Advanced NRG1-Rearranged Malignancies
CTID: NCT04410653
Phase: Phase 2    Status: Completed
Date: 2024-04-05
An Open Label Trial of Afatinib (Giotrif) in Treatment-naive (1st Line) or Chemotherapy Pre-treated Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) Harboring EGFR Mutation(s)
CTID: NCT01853826
Phase: Phase 3    Status: Completed
Date: 2024-03-26
Safety Study of Afatinib and Postoperative Radiation Therapy to Treat Head and Neck Cancer
CTID: NCT01783587
Phase: Phase 1    Status: Completed
Date: 2024-03-06
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
CTID: NCT03878524
Phase: Phase 1    Status: Terminated
Date: 2024-03-04
Treatment With BIBW 2992, Irreversible Inhibitor of EGFR and HER-2 in Non-small Cell Lung Cancer
CTID: NCT01542437
Phase: Phase 2    Status: Completed
Date: 2024-02-06
Cambridge Brain Mets Trial 1
CTID: NCT02768337
Phase: Phase 1/Phase 2    Status: Terminated
Date: 2024-01-31
The Drug Rediscovery Protocol (DRUP Trial)
CTID: NCT02925234
Phase: Phase 2    Status: Recruiting
Date: 2024-01-24
Neoadjuvant Chemotherapy, Tislelizumab With Afatinib for HNSCC
CTID: NCT05516589
Phase: Phase 2    Status: Recruiting
Date: 2023-12-29
Neoadjuvant Tislelizumab With Afatinib for Resectable Head and Neck Squamous Cell Carcinoma
CTID: NCT05517330
Phase: Phase 2    Status: Recruiting
Date: 2023-12-29
Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations
CTID: NCT02795156
Phase: Phase 2    Status: Completed
Date: 2023-12-05
Deciphering Afatinib Response and Resistance With INtratumour Heterogeneity
CTID: NCT02183883
Phase: Phase 2    Status: Completed
Date: 2023-11-29
Biomarker-based Study in R/M SCCHN
CTID: NCT03088059
Phase: Phase 2    Status: Active, not recruiting
Date: 2023-11-03
Non-interventional Study for Real-world Data of Afatinib Treatment in First-line Setting and of Subsequent Therapies for Patients With Advanced Epidermal Growth Factor Receptor (EGFR) Mutation-positive Lung Adenocarcinoma
CTID: NCT04795245
Phase:    Status: Completed
Date: 2023-10-31
Afatinib and Cetuximab in Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertion Positive Non-small-cell Lung Cancer
CTID: NCT03727724
Phase: Phase 2    Status: Completed
Date: 2023-10-18
A Study of Afatinib in Patients With Advanced Cancer With Changes in the HER Gene
CTID: NCT02506517
Phase: Phase 2    Status: Completed
Date: 2023-08-01
Afatinib After Chemoradiation and Surgery in Treating Patients With Stage III-IV Squamous Cell Carcinoma of the Head and Neck at High-Risk of Recurrence
CTID: NCT01824823
Phase: Phase 2    Status: Terminated
Date: 2023-06-28
AFAMOSI: Efficacy and Safety of Afatinib Followed by Osimertinib Compared to Osimertinib in Patients With EGFRmutated/T790M Mutation Negative Nonsquamous NSCLC
CTID: NCT04413201
Phase: Phase 4    Status: Active, not recruiting
Date: 2023-06-02
Palbociclib Combined With Afatinib for Advanced Squamous Carcinoma of Esophagus or Gastroesophageal Junction
CTID: NCT05865132
Phase: Phase 2    Status: Recruiting
Date: 2023-05-18
Dry Pleurodesis With Talcum and Afatinib is Used to Treat Patients With Non-Small Cell Lung Carcinoma
CTID: NCT03827070
Phase: Phase 1    Status: Active, not recruiting
Date: 2023-04-25
To Evaluate the Efficacy and Safety of Afatinib for Advanced ALTRK-negative ESCC
CTID: NCT05818982
Phase: Phase 2    Status: Recruiting
Date: 2023-04-19
Primary Tumor Resection With EGFR TKI for Stage IV NSCLC
CTID: NCT05215548
Phase: Phase 2    Status: Recruiting
Date: 2023-04-04
Phase II Study of Afatinib Plus Bevacizumab in the Treatment Epidermal Growth Factor Receptor (EGFR) Exon G719X, S768I, and L861Q Mutation Metastatic Non-Small Cell Lung Cancer
CTID: NCT05267288
Phase: Phase 2    Status: Recruiting
Date: 2023-03-29
Afatinib, Paclitaxel, 2nd Line, Advanced Gastric Cancer
CTID: NCT02501603
Phase: Phase 2    Status: Completed
Date: 2023-01-27
Neoadjuvant Afatinib Therapy for Potentially Resectable Stage III EGFR Mutation-Positive Lung Adenocarcinoma
CTID: NCT04201756
Phase: Phase 2    Status: Completed
Date: 2022-12-23
Phase II Umbrella Study Directed by Next Generation Sequencing
CTID: NCT03574402
Phase: Phase 2    Status: Recruiting
Date: 2022-12-06
Afatinib (GILOTRIF®) in Patients Suffering From Tumors Harboring Neuregulin 1 (NRG1) Gene Alterations (Specifically NRG1 Gene Fusion-positive Advanced Solid Tumors)
CTID: NCT05107193
Phase:    Status: No longer available
Date: 2022-11-08
Study to Evaluate the Efficacy of Afatinib in Skull Base Chordoma
CTID: NCT05519917
Phase: Phase 2    Status: Not yet recruiting
Date: 2022-09-30
Afatinib in NSCLC With HER2 Mutation
CTID: NCT02369484
Phase: Phase 2    Status: Completed
Date: 2022-08-24
Combination of Cetuximab With Afatinib for Patient With EGFR Mutated Lung Cancer
CTID: NCT02716311
Phase: Phase 2    Status: Completed
Date: 2022-08-11
BIBW 2992 (Afatinib) for the Treatment of Patients With HER2-positive, Hormone-refractory Prostate Cancer
CTID: NCT01320280
Phase: Phase 2    Status: Terminated
Date: 2022-07-01
Afatinib on CNS Metastases and LMD in EGFR Mutation Positive NSCLC
CTID: NCT03711422
Phase: Phase 1    Status: Terminated
Date: 2022-06-14
Evaluate the Impact of Afatinib on Quality of Life and Symptom Burden of Greek Subjects With Advanced NSCLC in Routine Patient Care Settings
CTID: NCT02440854
Phase:    Status: Completed
Date: 2022-04-27
Afatinib and Pembrolizumab for Head and Neck Squamous Cell Carcinoma (ALPHA Study)
CTID: NCT03695510
Phase: Phase 2    Status: Completed
Date: 2022-04-21
Afatinib in Locally Advanced and Metastatic Chordoma
CTID: NCT03083678
Phase: Phase 2    Status: Unknown status
Date: 2022-04-20
Afatinib and Necitumumab in Patients With EGFR Mutation Positive Advanced or Metastatic Non-small Cell Lung Cancer
CTID: NCT03054038
Phase: Phase 1    Status: Terminated
Date: 2022-04-14
BIBW 2992 Plus Simvastatin vs. BIBW 2992 in Previously Treated Patients With Advanced Non-adenocarcinomatous NSCLC
CTID: NCT01156545
Phase: Phase 2    Status: Completed
Date: 2022-04-06
Safety Study of Afatinib for Brain Cancer
CTID: NCT02423525
Phase: Phase 1    Status: Completed
Date: 2022-03-10
Efficacy and Safety of Precision Therapy in Refractory Tumor
CTID: NCT03239015
Phase: Phase 2    Status: Unknown status
Date: 2022-03-04
Research of Biomarkers of Activity and Efficacy of BIBW2992 in Untreated Non-metastatic HNSCC Patients
CTID: NCT01415674
Phase: Phase 2    Status: Completed
Date: 2022-02-02
JMT101 Combined With Afatinib in Patients With Advanced Esophageal Squamous Cell Carcinoma After Standard Therapy
CTID: NCT05164848
Phase: Phase 1    Status: Unknown status
Date: 2021-12-21
Safety, Tolerability and Efficacy of Vaginal Suppositories for Treatment of the Endometriosis
CTID: NCT03481842
Phase: Phase 1/Phase 2    Status: Withdrawn
Date: 2021-10-29
Afatinib in Lung Cancer With EGFR Mutation From Circulating Tumor DNA
CTID: NCT02629523
Phase: Phase 2    Status: Completed
Date: 2021-08-03
Afatinib Plus Toripalimab in Previously Treated ESCC With EGFR Overexpression or EGFR Amplification
CTID: NCT04880811
Phase: Phase 2    Status: Unknown status
Date: 2021-07-13
Evaluation of Afatinib in Maintenance Therapy in Squamous Cell Carcinoma of the Head and Neck
CTID: NCT01427478
Phase: Phase 3    Status: Completed
Date: 2021-06-01
Trial of Afatinib in Pediatric Tumours
CTID: NCT02372006
Phase: Phase 1/Phase 2    Status: Completed
Date: 2021-03-04
Testing Afatinib in Combination With Pembrolizumab in Patients With Squamous Cell Carcinoma of the Lung
CTID: NCT03157089
Phase: Phase 2    Status: Completed
Date: 2021-02-23
Afatinib Osimertinib Sequencing NIS
CTID: NCT03370770
Phase:    Status: Completed
Date: 2020-12-24
-------
The effects of the proton pump inhibitor esomeprazole on the bioavailability of afatinib (Giotrif®) in patients with non-small cell lung cancer (NSCLC) 'the BIO-GIO study'
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2017-07-05
Precision 2: an open explorative phase II, open label study of afatinib in the treatment of advanced cancer carrying an EGFR, a HER2 or a HER3 mutation.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2017-06-21
Phase II open label single arm exploratory trial of oral afatinib monotherapy following platinum failure for patients with advanced/metastatic urothelial tract carcinoma with ERBB receptor deregulation.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2016-04-29
Phase II trial of Afatinib as induction treatment in patients with stage IIIA or stage IIIB N2 requiring neoadjuvant treatment for pN2 non squamous non small cell lung cancer (NSCLC) with EGFR-activating mutations.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2016-04-26
Phase II study evaluating the combination of cetuximab with afatinib as first-line treatment for patients with EGFR mutated Non Small Cell Lung Cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-11-20
A randomised, double blind phase I/II trial to investigate efficacy, immunogenicity and safety of intradermally administered BI 1361849 (CV9202) plus afatinib versus placebo plus afatinib as first-line treatment for patients with stage IV adenocarcinoma of the lung harbouring common EGFR mutations.
CTID: null
Phase: Phase 1, Phase 2    Status: Prematurely Ended, Completed
Date: 2015-11-19
Maintaining ERBB blockade in EGFR-mutated lung cancer (MARBLE) - A randomized, open-label, phase II study of maintaining pan-ERBB blockade following platinum-based induction chemotherapy in patients with EGFR mutated, metastatic non-small-cell lung cancer progressing after treatment with afatinib as first EGFR-targeting agent.
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2015-06-29
Afatinib in pretreated patients with advanced NSCLC harbouring HER2 exon 20 mutations
CTID: null
Phase: Phase 2    Status: Completed
Date: 2015-05-18
Phase I/II open label, dose escalation trial to determine the MTD, safety, PK and efficacy of afatinib monotherapy in children aged ≥ 1 year to <18 years with recurrent/refractory neuroectodermal tumours, rhabdomyosarcoma and/or other solid tumours with known ErbB pathway deregulation regardless of tumour histology
CTID: null
Phase: Phase 1, Phase 2    Status: GB - no longer in EU/EEA, Temporarily Halted, Completed
Date: 2015-04-18
Phase I/II study with the combination of afatinib and selumetinib in advanced KRAS mutant positive and PIK3CA wildtype non-small cell lung cancer and colorectal cancer
CTID: null
Phase: Phase 1, Phase 2    Status: Ongoing
Date: 2015-01-14
An open label, single-arm phase IV study to assess the efficacy and safety of afatinib as second-line therapy for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harbouring an EGFR mutation (Del19 or L858R) who have failed first-line treatment with platinum-based chemotherapy
CTID: null
Phase: Phase 4    Status: Completed
Date: 2014-12-17
A randomized open-label Phase II study of letrozole plus afatinib (BIBW2992) versus letrozole alone in first-line treatment of advanced ER+, HER2- postmenopausal breast cancer with low ER expression
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-10-17
An open label trial of afatinib (Giotrif) in treatment-naive (1st line) or chemotherapy pre-treated patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR mutation(s)
CTID: null
Phase: Phase 3    Status: Ongoing, Completed
Date: 2013-06-25
Etude de phase II, randomisée, multicentrique, de l’Afatinib (BIBW2992) administré en pré-opératoire, chez des patients ayant un carcinome épidermoïde des voies aérodigestives supérieures non métastatique, en vue d'identifier des biomarqueurs prédictifs et/ou pharmacodynamiques de l'activité biologique et de l'efficacité
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-05-28
An Open Label Multi-Centre Preoperative Window of Opportunity Study of Afatinib in Stage Ia to IIb Non-Small Cell Lung Cancer
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2013-01-25
Gemcitabine in Combination with the Oral Irreversible ErbB Inhibitor Afatinib versus Gemcitabine Alone in Patients with Metastatic Pancreatic Cancer: an Explorative Randomized Phase II Trial
CTID: null
Phase: Phase 2    Status: Completed
Date: 2013-01-17
A Phase II, single-arm clinical trial of administration of cisplatin and 5-fluorouracil with afatinib as first-line therapy in patients with inoperable gastric or gastroesophageal junction cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-10-24
Neoadjuvant BIBW 2992 followed by surgery in squamous cell carcinoma of the head and neck: an EORTC NOCI-HNCG window study.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-06-07
A multicentric randomized phase II study evaluating dual targeting of the EGFR using the combination of cetuximab and afatinib versus cetuximab alone in patients with chemotherapy refractory wtKRAS metastatic colorectal cancer.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2012-05-29
LUX-Lung 8: A randomized, open-label Phase III trial of afatinib versus erlotinib in patients with advanced squamous cell carcinoma of the lung as second-line therapy following first-line platinum-based chemotherapy
CTID: null
Phase: Phase 3    Status: Completed
Date: 2012-02-22
Single-arm, open-label, multicentre phase II study evaluating the efficacy and safety of BIBW 2992 (Afatinib) in combination with vinorelbine for the treatment of patients with metastatic breast cancer with intermediate HER2 expression (HER2 2+ by immunohistochemistry, fluorescence in-situ hybridisation (FISH) negative) after failure of first-line therapy in the metastatic setting and having been pre-treated with anthracyclines
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2012-02-13
LUX-Lung 7: A randomised, open-label Phase IIb Trial of afatinib versus gefitinib as first-line treatment of patients with EGFR mutation positive advanced adenocarcinoma of the lung
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-12-29
Trial of afatinib (BIBW 2992) in suspected or confirmed mutant EGFR lung cancer patients unfit for chemotherapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-12-19
LUX-Head & Neck 1
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-10-25
Randomised phase II study of afatinib alone or in combination with vinorelbine versus investigator’s choice of treatment in patients with HER2-positive breast cancer with progressive brain metastases after trastuzumab or lapatinib based therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-09-14
A randomized, double-blind, placebo-controlled, phase III study to evaluate the efficacy of afatinib (BIBW 2992) in maintenance therapy after postoperative concurrent radiotherapy and chemotherapy for squamous-cell carcinoma of the head and neck : a GORTEC collaborative group study 2010-02
CTID: null
Phase: Phase 3    Status: Completed
Date: 2011-08-11
LUX-Head & Neck 2
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2011-07-27
An open label, phase II trial of afatinib with or without vinorelbine for
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-07-21
Single-arm, open-label, monocentric Phase II study evaluating the efficacy and safety of BIBW 2992 (Afatinib) for the treatment of patients with HER2-positive, hormone-refractory prostate cancer after failure of treatment with docetaxel or ineligible for treatment with docetaxel
CTID: null
Phase: Phase 2    Status: Prematurely Ended
Date: 2011-06-20
LUX-Breast 2;An open label, phase II trial of BIBW 2992 (afatinib) in patients with metastatic HER2-overexpressing breast cancer failing HER2-targeted treatment in the neoadjuvant and/or adjuvant treatment setting
CTID: null
Phase: Phase 2    Status: Completed
Date: 2011-02-18
LUX-Breast 1; An open label, randomised phase III trial of BIBW 2992 and vinorelbine versus trastuzumab and vinorelbine in patients with metastatic HER2-overexpressing breast cancer failing one prior trastuzumab treatment
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2010-05-17
An open label, partially randomised Phase II trial to investigate the efficacy and safety of BIBW 2992 in patients with metastatic colorectal cancer who never received prior anti-EGFR treatment
CTID: null
Phase: Phase 2    Status: Completed
Date: 2010-05-13
Phase III randomized trial of BIBW 2992 plus weekly paclitaxel versus
CTID: null
Phase: Phase 3    Status: Completed
Date: 2010-03-02
A phase Ib open label clinical trial of continuous once daily oral treatment using BIBW 2992 plus cetuximab (Erbitux®) in patients with non-small cell lung cancer with progression following prior erlotinib (Tarceva®) or gefitinib (Iressa®)
CTID: null
Phase: Phase 1, Phase 2    Status: Completed
Date: 2010-02-09
LUX-Lung 3; A randomised, open-label, phase III study of BIBW 2992 versus chemotherapy as first-line treatment for patients with stage IIIB or IV adenocarcinoma of the lung harbouring an EGFR activating mutation
CTID: null
Phase: Phase 3    Status: Prematurely Ended, Completed
Date: 2009-09-28
A randomized, open-label Phase II study of BIBW 2992 versus cetuximab (Erbitux®) in patients with metastatic or recurrent Head and Neck Squamous Cell Carcinoma (HNSCC) after failure of platinum-containing therapy with a cross-over period for progressing patients.
CTID: null
Phase: Phase 2    Status: Completed
Date: 2009-05-07
Phase II open label trial to assess the efficacy and the impact on QTcF of continuous oral BIBW 2992 at a daily dose of 50 mg in patients with relapsed or refractory solid tumours including patients with brain metastases and those with glioblastoma not amenable to other therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2009-03-16
A Phase II single-arm trial of BIBW 2992(Tovok) in EGFR FISH positive non-small cell lung cancer patients
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-11-20
A Phase II single-arm trial of BIBW 2992 in demographically and genotypically selected non-small cell lung cancer patients
CTID: null
Phase: Phase 2    Status: Completed
Date: 2008-06-13
Phase IIb/III randomized, double-blind trial of BIBW 2992 plus best
CTID: null
Phase: Phase 2, Phase 3    Status: Completed
Date: 2008-05-13
Phase II trial of BIBW 2992 in patients with HER2-positive metastatic breast cancer after failure of trastuzumab therapy
CTID: null
Phase: Phase 2    Status: Completed
Date: 2007-10-31
A multicenter, randomized, open label phase II trial evaluating the efficacy and safety of mFOLFOX7 plus weekly alternating sequential oral administration of BIBF 1120 250 mg twice daily and BIBW 2992 50 mg once daily (BB) versus mFOLFOX7 alone as first-line therapy in patients with metastatic colorectal cancer.
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2007-01-22
A phase II study of BIBW 2992 added to letrozole in patients with estrogen receptor positive hormone refractory metastatic breast cancer progressing on letrozole
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-12-07
An open label phase II trial to assess the efficacy and safety of a once daily oral dose of 50 mg BIBW 2992 in two cohorts of patients with HER2-negative metastatic breast cancer after failure of no more than two chemotherapy regimen
CTID: null
Phase: Phase 2    Status: Completed, Prematurely Ended
Date: 2006-10-31
A multi-centre 3-arm randomized phase II trial of BIBF 1120 versus BIBW 2992 versus sequential administration of BIBF 1120 and BIBW 2992 in patients with hormone-resistant prostate cancer
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-02-16
Dual blockage with Afatinib and Trastuzumab as neooadjuvant treatment for patients with lo-cally advanced or operable breast cancer receiving taxane-anthracycline containing chemo-therapy (DAFNE study).
CTID: null
Phase: Phase 2    Status: Completed
Date:
First-line afatinib for elderly patients
CTID: jRCTs031180136
Phase:    Status: Complete
Date: 2019-02-19
Afatinib translational study in patients with EGFR mutation-positive non-squamous non-small cell lung cancer acquired resistance to osimertinib
CTID: jRCTs071180013
Phase:    Status: Not Recruiting
Date: 2019-01-24
Trial of the alternative therapy with osimeritinib and afatinib for NSCLC with EGFR mutation (Alt trial) (WJOG10818L)
CTID: jRCTs051180009
Phase:    Status: Complete
Date: 2018-11-26
Afa+Bev for EGFR mutant NSCLC
CTID: jRCTs061180006
Phase:    Status: Complete
Date: 2018-11-19
A phase I study; Afatinib in Combination of Osimertinib in patients with Relapsed Non-Small Cell Lung Cancer after failure of prior Osimertinib
CTID: jRCTs051180008
Phase:    Status: Complete
Date: 2018-11-08
Prospective study to investigate the resistant mechanism to afatinib treatment in EGFR mutation-positive non-small cell lung cancer
CTID: UMIN000031845
Phase:    Status: Complete: follow-up complete
Date: 2018-03-22
A phase I study Afatinib in Combination of Osimertinib in patients with Relapsed Non-Small Cell Lung Cancer after failure of prior Osimertinib
CTID: UMIN000031501
Phase:    Status: Complete: follow-up complete
Date: 2018-03-09
Multicenter, prospective interventional study to evaluate therapeutic effect of Afatinib in patients with advanced non-small cell lung cancer, EGFR mutation positive and brain metastasis
CTID: UMIN000031117
Phase:    Status: Complete: follow-up complete
Date: 2018-02-03
Afatinib plus Bevacizumab Combination after osimertinib failure for aDvanced EGFR-mutant non-small cell lung cancer: a multicenter prospective single arm phase II study (ABCD-study)
CTID: UMIN000030545
Phase: Phase II    Status: Recruiting
Date: 2018-01-01
Phase II study of afatinib for non-small cell lung cancer acquired resistance to osimertinib (North Japan Lung Cancer Study Group 1801)
CTID: UMIN000030399
Phase: Phase II    Status: Recruiting
Date: 2017-12-15
Afatinib alone or with bevacizumab as first-line therapy in patients with advanced non-squamous non-small-cell lung cancer harbouring active EGFR mutations : an open-label, randomized, multicenter, phase II study
CTID: UMIN000027432
Phase: Phase II    Status: Complete: follow-up complete
Date: 2017-06-18
A prospective, phase II trial of low-dose afatinib monotherapy for patients with EGFR, mutation-positive, non-small cell lung cancer(TORG1632).
CTID: UMIN000027338
Phase:    Status: Complete: follow-up complete
Date: 2017-05-15
A biomarker analysis of Afatinib treatment in patients with relapse of EGFR-T790M mutation-positive advanced lung adenocarcinoma after 3rd generation EGFR-TKI treatment.
CTID: UMIN000025126
Phase:    Status: Recruiting
Date: 2016-12-03
Resistant mechanisms to afatinib in non-small cell lung cancer with EGFR mutations
CTID: UMIN000024476
Phase:    Status: Recruiting
Date: 2016-10-19
Phase II study of low-dose afatinib for elderly patients with non-small cell lung cancer harboring EGFR mutation (based on TDM)
CTID: UMIN000022252
Phase: Phase II    Status: Recruiting
Date: 2016-05-10
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生物数据图片
  • Afatinib (BIBW2992)

  • Afatinib (BIBW2992)
  • Afatinib (BIBW2992)

    Afatinib covalently binds to cysteine number 797 of the epidermal growth factor receptor (EGFR) via a Michael addition (IC50 = 0.5 nM).Schubert-Zsilavecz, M, Wurglics, M,Neue Arzneimittel Frühjahr 2013.(in German)

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