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当前位置:药品说明书与价格首页 >> 药品专题 >> 拉帕替尼(lapatinib) >> 拉帕替尼泊片, 索拉非尼|Tykerb(Iapatinib Tablets)

拉帕替尼泊片, 索拉非尼|Tykerb(Iapatinib Tablets)

2012-04-22 22:59:48  作者:新特药房  来源:中国新特药网天津分站  浏览次数:360  文字大小:【】【】【
简介: 英文药名: Tykerb(Iapatinib Tablets) 中文药名: 拉帕替尼泊片, 索拉非尼 品牌药生产厂家: Glaxo Smith Kline 药物名称 【中文名称】: 拉帕替尼泊 【商品名】:TYKERB 泰克泊,泰克博 【通用名】:二甲 ...

英文药名: Tykerb(Iapatinib Tablets)

中文药名: 拉帕替尼泊片, 索拉非尼

品牌药生产厂家: Glaxo Smith Kline

药物名称

【中文名称】: 拉帕替尼泊
【商品名】:TYKERB 泰克泊,泰克博
【通用名】:二甲苯磺酸拉帕替尼片
【英文名】:lapatinib ditosylate monohydrate
【性状】:拉帕替尼泊(lapatinib)是一种口服的小分子表皮生长因子(EGFR:ErbB-1,ErbB-2)酪氨酸激酶抑制剂。黄色片剂,水中溶解度为0.007 mg/mL,0.1N HCl盐酸中溶解度为0.001 mg/mL at 25°C.
介绍

乳腺癌在全球范围内是女性发病率最高的恶性肿瘤,近年来在中国发病率也呈现逐年上升的趋势。近20年来,通过手术、化疗、放疗、激素治疗等综合治疗方式,早期乳腺癌的复发和死亡率显著降低,然而晚期乳腺癌的治疗特别是伴有脑转移的和耐药患者群的治疗仍是临床上有待攻克的难点。专家对于拉帕替尼预防及治疗乳腺癌脑转移的最新研究结果进行了深入的解读。
约三分之一的ErbB2(Her2)阳性转移性乳腺癌妇女在疾病进程中可能出现脑转移,最新的研究结果表明,拉帕替尼与卡培他滨联合可缩小ErbB2(Her2)阳性乳腺癌脑转移瘤的体积。随着女性晚期乳腺癌的生存期的延长,虽然经过各种治疗,脑转移的发生率会逐渐增大。目前,很少有药物在治疗脑转移、特别是ErbB2(Her2)阳性的乳腺癌脑转移中表现出活性,因此,这些数据是相当令人鼓舞的。与会专家认为,拉帕替尼作为ErbB2抑制剂,其小分子、双靶向的特点为脑转移患者带来治疗的新希望。拉帕替尼治疗脑转移,降低脑转移发生率的作用在一些临床实验中已得到验证。
拉帕替尼泊Lapatinib可使晚期转移性癌患者的病情稳定。
拉帕替尼泊lapatinib可使晚期转移性癌患者的病情稳定研究人员报告,双重egfr激酶抑制剂lapatinib可诱导约半数参加i期研究的晚期难治性实体瘤患者出现部分反应或疾病稳定。药物相对无毒性。
拉帕替尼泊Lapatinib可使晚期转移性癌患者的病情稳定。
拉帕替尼泊lapatinib可使晚期转移性癌患者的病情稳定研究人员报告,双重egfr激酶抑制剂lapatinib可诱导约半数参加i期研究的晚期难治性实体瘤患者出现部分反应或疾病稳定。药物相对无毒性。
适应症   

拉帕替尼泊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.
药理与药代动力学   

拉帕替尼泊是小分子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)。4种乳腺癌细胞株中BT474和 SKBr3对拉帕替尼敏感,半抑制浓度为25 和32 nmol/L,MDA-MB-468和T47D细胞株不敏感,半抑制浓度在微摩尔级别级别,对于膀胱癌的2种细胞株,RT112(ErbB1和ErbB2高度表达)和J82(ErbB1和ErbB2低度表达),增强顺铂的疗效。
在多种动物均能抑制表皮因子驱动的肿瘤生长。拉帕替尼对曲妥单抗耐药的肿瘤细胞株有效。
口服吸收不完全,而且个体差异较大,约4 h后达到最大浓度(Cmax),半衰期24 h,每日给药后6~7 d达到稳态。每天给药1 250 mg,Cmax为2.43 μg/ml(1.57~3.77 μg/ml),血浆浓度时间曲线下面积(AUC) 为 36.2 μg.h/ml(23.4~56 μg.h/ml)。分开服用较每日1次AUC增加一倍,与食物同服,AUC增加3~4倍。
拉帕替尼泊与白蛋白及α1酸糖蛋白结合率高(>99%),体外研究证实,拉帕替尼是乳腺癌抗癌蛋白转运及P-糖蛋白的底物。单剂量终末半衰期为14.2 h,多次给药后,有效半衰期延长至24 h,主要由在肝脏中被CYP3A4和 CYP3A5代谢,小部分由CYP2C19和CYP2C8完成。肾脏排泄极微,粪便中回收率约为口服剂量的27%。
临床研究   

为考察拉帕替尼与卡培他宾联合治疗乳腺癌的有效性及安全性的三期临床试验中,入选患者HER2过度表达,为晚期或转移的乳腺癌患者,蒽环类抗生素、紫杉烷类及曲妥单抗无效的患者。患者随机给与拉帕替尼1,250 mg,每日1次,且在第1~14天每天给予2,500 mg/m2,21 d一循环。终末点为肿瘤进展时间,399名患者参加了试验,平均年龄为53岁,14%患者年龄超过65岁,91%为白种人,97%为四期乳腺癌,48%的患者雌激素受体阳性或孕酮阳性,95%为ErbB2 IHC 3阳性IHC 2阳性(荧光素原位杂交法确认),95%患者经过蒽环类抗生素、紫杉烷类及曲妥单抗治疗。4个月后拉帕替尼与卡培他宾联合治疗组与单用卡培他宾的肿瘤进展时间分别为27.1和18.6周。 67名转移实体瘤患者,拉帕替尼治疗8周,发现对曲妥单抗耐药的患者有效,能延长患者肿瘤进展时间。临床试验中,拉帕替尼剂量每日1,800 mg,患者耐受性良好,对各种实体肿瘤有效,包括乳腺癌及头颈部癌症。在于5-氟尿嘧啶、亚叶酸钙及依立替康合用治疗肿瘤的试验中,25名患者口服拉帕替尼,同时给与静脉注射上述三种药物,与传统化疗相比药物剂量降低40%,19名可评价患者中,4名有部分反应,9名疾病处于稳定状态。在对恶性唾液腺瘤的研究中,拉帕替尼能延长患者肿瘤稳定期6个月以上,且患者耐受性好。
致癌、致突变及生殖毒性   

以中国仓鼠为对象的试验中,未见致癌作用,也未发现导致染色体变异,但具有遗传毒性。大剂量下也未见大鼠的交配能力和生育能力有任何影响。有1例报道,孕妇在妊娠前3月服用拉帕替尼,足月妊娠后产下健康儿。  
拉帕替尼与卡培他宾合用治疗乳腺癌,效果较好,且对蒽环类抗生素、紫杉烷类及曲妥单抗耐药的患者有效,毒副作用轻微,对于晚期或转移性乳腺癌患者又多了一个治疗药物。
药物相互作用   

在体外拉帕替尼在治疗浓度可抑制CYP3A4和CYP2C8,并且主要由CYP3A4代谢,抑制此酶活性的药物能显著提高拉帕替尼的血药浓度。酮康唑,每次0.2 g,2次/d,7 d后可提高拉帕替尼AUC 3~7倍,半衰期延长1.7倍。健康志愿者口服CYP3A4诱导剂,每次100 mg,每日2次,3 d后改为每次200 mg,每日2次共用17 d,拉帕替尼AUC降低72%。拉帕替尼是P-糖蛋白的转运地物,抑制糖蛋白的药物可能增加该药的血药浓度。
用法用量   

推荐剂量为1,250 mg,每日1次,第1~21天服用,与卡培他宾2,000 mg/d,第1~14天分2次服联用。拉帕替尼,应每日服用1次,不推荐分次服用。饭前1 h或饭后2 h后服用。如漏服1剂,第2天不需剂量加倍。妊娠级别D,孕妇禁用。是否通过乳汁分泌尚不清楚,哺乳期妇女应停止授乳。老年人用药与年轻患者未发现有明显差异。未对肾脏严重损害及透析患者做过临床试验,中重度肝损害的患者应酌减剂量。
任何疑问,请遵医嘱!
不良反应   

临床试验中观察到的大于10%的不良反应主要为胃肠道反应,包括恶心、腹泻、口腔炎和消化不良等,皮肤干燥、皮疹,其他有背痛、呼吸困难及失眠等。与卡培他宾合用,不良反应有恶心、腹泻及呕吐,掌跖肌触觉不良等。个别患者可出现左心室射血分数下降,间质性肺炎。
其最常见之副作用为肠胃消化道系统方面的副作用,即是恶心、呕吐、腹泻等症状,其他还有皮肤方面的红肿、搔痒、疼痛,以及疲倦等。另外还有极少见但是严重的副作用,包括心脏方面以及肺部方面。
当病患出现二级(New York Heart Association,NYHA class 2)以上的心脏左心室搏出分率(Left Ventricle Ejection Fraction,LVEF)下降时,必须停止使用,以避免产生心脏衰竭。当LVEF回复至正常值或病患无症状后两个礼拜便可以以较低剂量重新用药。与anthracycline类的化疗药品相比,拉帕替尼的心脏毒性为可逆的,不像anthracycline的不可逆性并有一生最多使用量,拉帕替尼并没有一生最多使用量。
由于拉帕替尼是以肝脏CYP酵素系统代谢的药物,在使用其他具有诱导或是抑制CYP酵素的药物时,必须要注意剂量的调整。孕妇一般不应该使用拉帕替尼,因为其怀孕毒性分类为D,因此如果没有绝对的需要或是对母体有极大的利益,否则不建议孕妇或育怀孕者使用。

包装规格:250mg *70 片

Brand Name: Tykerb 250mg

Contents: Lapatinib 250mg

Tykerb Information
Tykerb is a chemotherapeutical agent based on Lapatinib. It is available under the form of 250 mg film coated tablets, which also contain the inactive ingredients sodium starch glycolate, magnesium stearate, povidone and microcrystalline cellulose.

Tykerb Indications
Tykerb is usually employed in the treatment of HER2-positive breast cancer, in combination with Capecitabine (another chemotherapeutic agent), however this treatment is only applied in cases where the cancer did not respond to regular therapy. This medicine acts upon the cancer cells by hindering and even stopping their replication and growth.

There may be other uses for this medicine which are not listed in this information leaflet. If you are not suffering from breast cancer and you have received a prescription for this chemotherapeutic agent it is best that you consult with your health care professional in order to obtain more information on why you should start taking Tykerb.

Tykerb Warnings
You should not be prescribed a treatment with Tykerb before regular therapy courses have been attempted and no positive results have been obtained. Tykerb may not be prescribed or administered to pregnant patients. An effective contraceptive method should be employed for the entire duration of the therapy to prevent accidental pregnancy.

Tykerb should be used with caution in the case of patients suffering from heart or liver disorders as well as in the case of patients that have a medical record of Long QT syndrome. If you are suffering from any of the above medical conditions you should contact your personal health care professional for further details regarding the risks and benefits of the therapy.

Tykerb Intake Guidelines
You should only take Tykerb exactly as prescribed by your supervising health care specialist. He or she will provide with a set of detailed intake guidelines. Typically, you should take this drug once per day, orally, within one hour of a meal. You should avoid grapefruit or grapefruit juice based products for the duration of the therapy, as they may increase the amount of medicine in your blood and alter the effects of your treatment.

Take Tykerb for the full duration of the therapy. You may not stop taking this medicine without your supervising physician’s consent – you may only discontinue the therapy when your health state has improved significantly or when dangerous levels of toxicity are recorded.

Periodic testing of your heart and liver functions as well as other types of monitoring will be required for the duration of your Tykerb therapy, in order to determine the effects of the treatment and to detect any possible side effects.

Tykerb Dosage
The regular Tykerb dosage is of 1.250 mg daily – the equivalent of 5 tablets. You may take the tablets one at a time, however you should take the full dose at the same time every day. In certain situations, your supervising health care specialist may direct you to use a different Tykerb dosage or a different intake schedule. In such cases you should follow your prescriber’s directions, disregarding the above information. If you have trouble remembering or understanding the dosage information, you should seek the advice of your personal health care professional.

Tykerb Overdose
In order to prevent an overdose with Tykerb, you are strongly advised to only take the daily recommended dosage for the recommended period of time. Never take larger quantities of this medicine per day, and stop taking this drug when your supervising health care professional advises you to do so. An overdose with this product may have severe, if not lethal consequences. Most cases of Tykerb overdose are characterized by vomiting and diarrhea.

Tykerb Missed Dose
You are advised to pay special attention to your medication schedule in order to avoid accidentally missing any of your Tykerb intakes. Setting up a strict intake schedule and taking the tablets at around the same time each day will help reduce the risk of forgetting to take your daily dose.

In the event that you happen to miss one of your Tykerb intakes you should take it as soon as you remember; however, if it is almost time for the next dose, skip taking the missed dose completely and resume your normal intake plan. You should never ingest a larger dose of this medicine in an attempt to make up for a missed dose.

Tykerb Side Effects
Tykerb may cause a number of side effects, most of which are generally transient and mild. Such adverse reactions are manifested through nausea and vomiting, mouth sores, upset stomach, skin dryness, mild rashes or sleeping disorders. Diarrhea is also commonly encountered, but only rarely becomes severe.

In some rare cases more severe side effects may occur. These need to be brought to the attention of the supervising health care specialist immediately: allergic reactions, shortness of breath, dizziness, fainting, jaundice, dark urine, arrhythmia or tachycardia, tiredness, swelling of the feet or ankles.

It is possible for side effects that are not listed here to occur as well. It is best that you inform your health care provider of any unexpected / bothersome signs or symptoms you may experience during your Tykerb treatment.

下面拉帕替尼泊片在日本上市处方资料

グラクソ・スミスクライン(GSK)は19日、抗悪性腫瘍剤「タイケルブ錠250mg」(一般名:ラパチニブトシル酸塩水和物)を新発売した。

タイケルブ錠250mgは、GSKが開発した新規分子標的治療薬。EGFRとHER2の受容体チロシンキナーゼのシグナル伝達を阻害することで、癌細胞の増殖を抑制する。アントラサイクリン系・タキサン系化学療法剤、抗HER2陽性抗体「ハーセプチン」の治療後に悪化したHER2陽性の転移性乳癌患者に対し、カペシタビンとの併用療法で使用できる。

海外第III相試験では、ハーセプチン既治療のHER2陽性転移性乳癌患者に対し、カペシタビン単独群に比べ、タイケルブ+カペシタビンの併用療法で有意な無増悪生存期間の延長が認められている。

国内では4月から日本化薬と共同販促を開始し,海外では既に世界74カ国・地域で承認されている。

用法・用量は、カペシタビンとの併用で、成人には、ラパチニブとして1250mgを1日1回、食事の1時間前か、食後1時間以降に経口投与する。

 薬価は、250mg錠1錠


责任编辑:admin


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