您的位置: 印度药房网 > 医药大数据 > 乳腺癌 >
拉帕替尼

印度拉帕替尼

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:59:07

【药品简介】 拉帕替尼是一种口服的小分子表皮生长因子酪氨酸激酶抑制剂。主要用于联合卡培他滨治疗ErbB-2过度表达的,既往接受过包括蒽环类,紫杉醇,曲妥珠单抗(赫赛汀)治疗的晚期或转移性乳腺癌.服用时需注意不良反应。

【适应症状】 拉帕替尼,乳腺癌:拉帕替尼用于联合卡培他滨治疗ErbB-2过度表达的,既往接受过包括蒽环类,紫杉醇,曲妥珠单抗(赫赛汀)治疗的晚期或转移性乳腺癌;或与来曲唑联用治疗绝境女性HER2过表达的激素受体阳性乳腺癌。(在使用赫赛汀时疾病急需进展的,适合开始拉帕替尼联合卡培他滨治疗)

【 药品别名 】 拉帕替尼 LAPATINIB TYKERB

印度拉帕替尼(拉帕替尼 LAPATINIB TYKERB)价格,正品图片,治疗乳腺癌药物, 购买拉帕替尼请到印度药房官方网站进行购买 【印度药房大全目录】

播放/暂停

印度全球药房排名

【印度拉帕替尼说明书,怎么吃?】

【药品特色】    HER2阳性乳腺癌的绝经后女性,联合来曲唑成为一线口服用药方案。

作用机制:

拉帕替尼是小分子4-苯胺基喹唑啉类受体酪氨酸激酶抑制剂,抑制表皮生长因子受体(ErbB1)和人表皮因子受体2(ErbB2)
 
常见副作用:

乏力、恶心、呕吐、腹泻、便秘、皮肤干燥、脱发、头痛等
拉帕替尼
  
给药方法:

每天一次,空腹口服(饭前1小时或饭后1小时)。定时定量服药,不建议将一天的剂量分散为多次服用。注:与卡培他滨联用的,卡培他滨应该每天两次,与食物同时服用,或饭后30分钟内服用。
 
注意事项:

在临床试验及上市后调查中发现有部分服药患者出现严重肝损,并且有死亡案例,如果有肝脏疾病,请务必告知医生。
 
参考用法:

1. 有转移的乳腺癌,HER2阳性(经紫杉醇、环蒽类或赫赛汀治疗):口服, 1250 mg,每天一次(与卡培他滨联用),直至疾病进展或不可接受的副作用。

2. 有转移的乳腺癌,HER2阳性,需要激素疗法:口服, 1500 mg,每天一次(与来曲唑联用),直至疾病进展。

3. HER2阳性乳腺癌,脑转移,一线治疗(FDA未批准为标签的疗法):口服,1250 mg,每天一次(与卡培他滨联用),直至疾病进展或不可接受的副作用。

4. HER2阳性乳腺癌,用赫赛汀中出现了疾病进展(FDA未批准为标签的疗法):1000 mg,每天一次(与卡培他滨联用)


USES OF TYKERB TABLET
Breast cancer

TYKERB TABLET SIDE EFFECTS
Common
Nausea
Headache
Back pain
Breathing difficulty
Rash
Joint pain
Pain in extremity
Insomnia (difficulty in sleeping)
Vomiting
Weakness
Abdominal pain
Indigestion
Loss of appetite
Fatigue
Diarrhea
Cough
Mucosal inflammation
Constipation
Hot flashes
Stomatitis (Inflammation of the mouth)
Weight gain
Increased bilirubin in the blood
Liver damage

HOW TO USE TYKERB TABLET
Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Tykerb 250 mg Tablet is to be taken empty stomach.

HOW TYKERB TABLET WORKS
Tykerb 250 mg Tablet is an anti-cancer medication. This works against the HER2 (human epidermal growth factor receptor protein) receptors and EGFRs (epidermal growth factor receptor) which is responsible for the over-proliferation of cells. This is how it inhibits the growth of cancerous cells causing downstream signaling pathways.

TYKERB TABLET RELATED WARNINGS
warnings
Alcohol
Interaction with alcohol is unknown. Please consult your doctor.

warnings
Pregnancy
WEIGH RISKS VS BENEFITS
Tykerb 250 mg Tablet is unsafe to use during pregnancy.
There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk, for example in life-threatening situations. Please consult your doctor.

warnings
Lactation
UNSAFE
Tykerb 250 mg Tablet is unsafe to use during lactation. Data suggests that the drug may cause toxicity to the baby, or the mother is suffering from a condition in which breastfeeding is not advisable.

warnings
Driving
Tykerb 250 mg Tablet may cause side effects which could affect your ability to drive.

warnings
Kidney
Tykerb 250 mg Tablet should be used with caution in patients with severe kidney disease. Dose adjustment of Tykerb 250 mg Tablet may be needed. Please consult your doctor.
Limited information is available on the use of Tykerb 250 mg Tablet in these patients. No dose adjustment is recommended in patients with mild to moderate kidney disease.

warnings
Liver
CAUTION
Tykerb 250 mg Tablet should be used with caution in patients with liver disease. Dose adjustment of Tykerb 250 mg Tablet may be needed. Please consult your doctor.
Limited information is available on the use of this medicine in patients with the severe liver disease.

Lapatinib

生物活性

产品描述

Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor

靶点活性

C-Raf-1,>10μM

c-Src,3.5μM

EGFR,10.8nM

HER2/ErbB2,367nM

实验溶液

15% Captisol: 30 mg/mL

体外活性

培养HN5 细胞群2周(不加 Lapatinib )左右后,再加30 μM Lapatinib 短暂处理,细胞生长完全被抑制。浓度>3.3 μM时,抑制率达50%;浓度为0.37 μM时,抑制率达20%。另一种细胞A-431(EGFR过量表达)与HN5反应类似。在抑制 EGFR过量表达的细胞生长方面,Lapatinib与 OSI-774 相似。除ErbB-4外, Lapatinib 对EGFR 和 ErbB-2的选择性比其他测试激酶高300多倍,如c-Src, MEK和ERK。Lapatinib抑制EGFR 和ErbB-2受体自磷酸化的作用存在剂量依赖性,对BT474 和HN5 细胞的IC50 分别为 0.17 和0.08 μM。作用于EGFR-和ErbB-2-过量表达的肿瘤细胞时,Lapatinib的抑制作用比作用于上述纯化酶的效力低10倍左右。Lapatinib 抑制 EGFR- 和ErbB-2过量表达的细胞生长,而EGFR选择性抑制剂OSI-774和 Iressa则会优先抑制 EGFR过量表达的细胞生长。Lapatinib对肿瘤细胞的作用比正常成纤维细胞效果高约100倍。ErbB-2转染后的乳腺上皮细胞HB4a c5.2对 Lapatinib的敏感度比未转染的亲本细胞高40倍左右。

体内活性

实验对象:肿瘤携带小鼠。给药剂量:30和 100 mg/kg ,2次/天,口服。实验结果:以剂量依赖的方式抑制肿瘤生长。100 mg/kg Lapatinib可完全抑制肿瘤生长。按这种剂量处理,在21天内,有<10%肿瘤损失。Lapatinib可有效抑制人类移植瘤BT474 和HN5 的生长。

激酶实验

In vitro kinase assays: The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.

细胞实验

Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.(Only for Reference)

细胞系: HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells

动物实验

动物模型:CD-1 nude femice implanted s.c. with HN5 cells, and C.B-17 SCID femice implanted s.c. with BT474 cells

化学信息

分子量

581.06

分子式

C29H26ClFN4O4S

CAS

231277-92-2

溶解度

DMSO: 93 mg/mL (160.1 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 1.721 ml 8.605 ml 17.21 ml
5 mM 0.344 ml 1.721 ml 3.442 ml
10 mM 0.172 ml 0.86 ml 1.721 ml
50 mM 0.034 ml 0.172 ml 0.344 ml

参考文献
 
1. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94
2. Chefrour M et al. Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants. Fundam Clin Pharmacol. 2012 Aug;26(4):530-7.
3. Wainberg ZA, et al. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res. 2010 Mar 1;16(5):1509-19.
4. Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418.
注:本站拉帕替尼(拉帕替尼 LAPATINIB TYKERB)药品说明,价格,正品图片均来自于官方,拉帕替尼如何服用请尊医嘱。如需药品请到正规印度药房进行购买
上一篇:Everolimus 下一篇:没有了
拉帕替尼相关药品
帕博西尼
帕博西尼

帕博西尼与来曲唑治疗绝经后妇女的雌激素受体(ER)阳性,人表皮生长因子受体2(HER2)阴性晚期乳腺癌,作为初始内分泌为基础的治疗...

Olaparib
Olaparib

1)复发卵巢癌的维持治疗: ①对于上皮性复发性卵巢癌成人患者的维持治疗 ②对铂类敏感或部分敏感的输卵管或原发性腹膜癌的化...

赫赛汀
赫赛汀

Hertraz适用于治疗HER2过表达的转移性乳腺癌和转移性胃癌。 1、Hertraz作为单一药物治疗已接受过1个或多个化疗方案的转移性乳腺癌。...

Everolimus
Everolimus

1) 雌激素受体阳性,her2阴性乳腺癌 依维莫司联合依西美坦,用于雌激素受体阳性,HER2阴性的绝经后妇女,并且用来曲唑或阿那曲...

拉帕替尼
拉帕替尼

乳腺癌:拉帕替尼用于联合卡培他滨治疗ErbB-2过度表达的,既往接受过包括蒽环类,紫杉醇,曲妥珠单抗(赫赛汀)治疗的晚期或转移性乳...

拉帕替尼资讯
帕博西尼用于乳腺癌效果
帕博西尼用于乳腺癌效果

帕博西尼可以选择性抑制细胞周期蛋白依赖性激酶4和6(CDK4/6),阻隔肿瘤细胞增殖。与来曲唑联合使用,对比于单独使用来曲唑或...

帕博西尼与乳腺癌晚期
帕博西尼与乳腺癌晚期

乳腺癌是危害女性身体健康的首要杀手,晚期乳腺癌的局势更为严重。CDK属于丝/苏氨酸蛋白激酶家族,是进行细胞周期控制的核心激...

容易患乳腺癌的陋习
容易患乳腺癌的陋习

乳腺癌是威胁我国妇女健康的重要恶性肿瘤之一。根据世界癌症组织国际癌症研究机构在全球184个国家和地区的癌症报告,中国女性...

乳腺癌患者术后可以通过这些方式恢复身体
乳腺癌患者术后可以通过这些方式恢复身

乳腺癌是目前治疗恶性肿瘤最好的癌症之一,接受常规治疗的绝大多数患者能够长期存活。许多病人在得到良好的康复护理后也可以...

关于拉帕替尼用于治疗胃癌的研究
关于拉帕替尼用于治疗胃癌的研究

化疗是晚期胃癌的主要治疗方法,但胃癌细胞对化疗药物不敏感,耐药是导致高死亡率的主要原因。上皮间质转化(EMT)在胃癌的进展...

使用印度拉帕替尼的注意事项
使用印度拉帕替尼的注意事项

印度拉帕替尼自然指的就是印度生产的拉帕替尼了,也是仿制版拉帕替尼。该药在乳腺癌的治疗上出力不少,效果明显颇受患者信赖...

拉帕替尼耐药
拉帕替尼耐药

人表皮生长因子受体2(HER2)受体酪氨酸激酶(RTK),癌基因是HER2成瘾肿瘤的一个有吸引力的治疗靶点。...

拉帕替尼的联用效果
拉帕替尼的联用效果

在一项双盲、安慰剂对照、多中心研究中,评价了拉帕替尼联合来曲唑的疗效和安全性...

拉帕替尼治疗的成果
拉帕替尼治疗的成果

近年来,随着医学技术的不断发展,乳腺癌的诊断和治疗取得了很大的进步...

拉帕替尼是很好的选择
拉帕替尼是很好的选择

晚期乳腺癌的治疗仍分为激素受体阳性乳腺癌、HER2阳性乳腺癌和三阴性乳腺癌。...

拉帕替尼视频
泰立沙(Tykerb)拉帕替尼(Lapatinib)作用机理
泰立沙(Tykerb)拉帕替尼(Lapatinib)作用

在多细胞生物的机体内,生长和发育在细胞水平...

赫赛汀能治好乳腺癌吗?
赫赛汀能治好乳腺癌吗?

赫赛汀是目前是用的时间最久,证据也最为充分...

乳腺癌术后皮下积液怎么办
乳腺癌术后皮下积液怎么办

乳腺癌术后出现皮下积液,因为手术把整个乳腺都切掉,所以仅剩外边的一层皮肤。...

 如何面对乳腺癌?
如何面对乳腺癌?

乳腺癌并不等于死亡,可以带瘤生存,所以不要多多紧张、焦虑、绝望甚至盲目投医...

药房目录大全

Pharmacy Catalogue