英文药名：TARCEVA Tablet(Erlotinib Hydrochloride) 中文药名：盐酸厄洛替尼片 生产厂家：中外制药 タルセバ錠25mg/タルセバ錠100mg/タルセバ錠150mg 治疗类别名称 抗肿瘤药 表皮生长因子受体（EGFR）酪氨酸激酶抑制剂 商標名 TARCEVA 一般名 エルロチニブ塩酸塩 (Erlotinib Hydrochloride)(JAN) 化学名 N-（3-Ethynylphenyl）-6,7-bis（2-methoxyethoxy）quinazoline-4-amine monohydrochloride 構造式 分子式 C22H23N3O4・HCl 分子量 429.90 性　状 白用细黄色粉末或块状粉末。极微溶于水和乙醇（99.5），略溶于甲醇，并在乙腈和环己烷几乎不溶。 熔点 约231〜232℃ 条件批准 ○不能切除的胰腺癌 这种药物的给药，胰腺癌诊断，熟悉化疗，以便仅在原始药房谁是医生，医疗机构和管理药剂师可充分控制也有关此代理人的风险进行，和类似物，有必要在生产销售不采取行动的事情。 适应病症 ○与患有癌症化疗后不能手术切除的进展反复，渐进的，非小细胞肺癌 ○与EGFR基因突变阳性，癌症化疗未处理的非小细胞肺癌的不可切除复发和进展 ○不能切除的胰腺癌 禁忌症 对本品及成份过敏者禁用。 不良反应 最常见的不良反应是皮疹和腹泻，3/4度皮疹和腹泻的发生率分别为9%和6%，皮疹的中位出现时间是8天，腹泻中位出现时间为12天。 发生率大于10%的不良反应有：皮疹、腹泻、食欲减低、疲劳、呼吸困难、咳嗽、恶心、感染、呕吐、口腔炎、瘙痒、皮肤干燥、结膜炎、角膜结膜炎、腹痛。  用法与用量 1. 非小细胞肺癌 成人：每天一次，每次为150mg。此外，根据该状态的患者用药。 2. 不能切除的胰腺癌 与吉西他滨组合，每天一次，每次为100mg，此外，根据该状态的患者用药。 药效药理 1. 抗肿瘤作用 在体外系统中，厄洛替尼抑制人结肠癌细胞系DIFI和头颈部癌细胞系HN5的生长[在DIFI细胞系的IC 50：100％抑制在100nM的，HN5：250NM]。 人的头部和颈部癌细胞系HN5，外阴癌细胞系A431，在胰腺癌细胞系HPAC和非小细胞肺癌细胞系（H460a，A549）人类恶性肿瘤使用，埃罗替尼抑制肿瘤生长移植的裸鼠系统20表现。此外，胰腺癌细胞系HPAC人类恶性肿瘤移植裸鼠系统中使用的组合使用吉西他滨厄洛替尼，观察到增强的肿瘤生长抑制效果。 2. 作用机序 埃罗替尼选择性抑制表皮生长因子受体酪氨酸激酶（EGFR-TK）。IC 50是2nm至纯化全长EGFR-TK，是1纳米到重组表皮生长因子受体的胞内结构域的酪氨酸激酶。另一方面，其它酪氨酸激酶对C-？Src和是v-abl抑制活性为1/1000或更小全长EGFR-TK的，在人胰岛素受体和I型胰岛素样生长因子受体激酶的细胞内结构域下面对细胞内EGFR-TK抑制活性1/10000。此外，19的G1期阻滞和厄洛替尼的细胞周期的细胞凋亡诱发作用已被证实）。 通过抑制表皮生长因子受体酪氨酸磷酸化的厄洛替尼推测为抑制抑制的基础上的肿瘤生长和凋亡的细胞增殖的诱导。 包装规格 片剂 25毫克   14片（粒PTP14×1） 100毫克  14片（粒PTP14×1） 150毫克  14片（粒PTP14×1） 制造厂商 中外制药有限公司 完整处方附件： 1）：http://www.info.pmda.go.jp/go/pack/4291016F1020_1_14/ 2）：http://www.info.pmda.go.jp/go/pack/4291016F3023_1_07/4291016F3023_1_07?view=body TARCEVA Tablet 25mg 100mg 150mg(Erlotinib Hydrochloride) TARCEVA Tablet 25mg（タルセバ錠25mg） Brand name : TARCEVA Tablet 25mg 　Active ingredient: Erlotinib hydrochloride 　Dosage form: white to yellowish white tablet (φ: approx. 6.5mm, thickness: approx. 3.3mm) 　Print on wrapping: タルセバ25 TARCEVA Tablet 100mg（タルセバ錠100mg） Brand name : TARCEVA Tablet 100mg 　Active ingredient: Erlotinib hydrochloride 　Dosage form: white to yellowish white tablet (φ: approx. 8.9mm, thickness: approx. 4.9mm) 　Print on wrapping: タルセバ100 TARCEVA Tablet 150mg（タルセバ錠150mg） Brand name : TARCEVA Tablet 150mg 　Active ingredient: Erlotinib hydrochloride 　Dosage form: white to yellowish white tablet (φ: approx. 10.5mm, thickness: approx. 5.4mm) 　Print on wrapping: タルセバ150 Effects of this medicine This medicine inhibits the growth of non-small cell lung cancer and pancreatic cancer by suppressing selectively the function of EGFR, a protein necessary for cancer growth. It is usually used to treat non-small cell lung cancer which is unresectable, recurrent and progressive, and got worse after cancer chemotherapy, to treat chemotherapy-naive non-small cell lung cancer with EGFR mutation which is unresectable, recurrent and progressive, and to treat pancreatic cancer not amenable to curative resection. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you are a patient with interstitial lung disease (interstitial pneumonia, pneumonitis, irradiation pneumonitis, organized pneumonia, pulmonary fibrosis, acute respiratory distress syndrome, pulmonary infiltration, alveolitis, etc.), lung infection, gastrointestinal ulcer, or diverticulum of large intestine. If you ever had any of those diseases mentioned above. If you are a patient with hepatic disorder. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •For treatment of non-small cell lung cancer: In general, for adults, take 150mg of erlotinib once a day, either over 1 hour before meal or over 2 hours after meal. The dose may be decreased according to your symptoms. 1 tablet contains 100mg of erlotinib. Strictly follow the instructions. For treatment of pancreatic cancer not amenable to curative resection: It is used along with gemcitabin. In general, for adults, take 1 tablet (100mg of erlotinib) once a day, either over 1 hour before meal or over 2 hours after meal. The dose may be decreased according to your symptoms. Strictly follow the instructions. •Avoid taking the medicine from just 1 hour before the meal to 2 hours after meal. Otherwise, you may have more severe side effects. •If you miss a dose, take the missed dose on an empty stomach. If it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. However, you should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. You may have severe diarrhea, rash, or elevation of ALT(GPT)/AST(GOT). •Do not stop taking this medicine unless your doctor instructs you to do so. Precautions while taking this medicine •You may have serious side effects by taking the medicine. You need to be informed of precautions and so on until you fully understand them. •The medicine may cause side effects such as interstitial lung disease, rash, diarrhea, and corneal perforation/ulcer. If you have symptoms such as shortness of breath, breathing difficulty, cough, fever, rash, diarrhea, and ocular pain, or if you feel that those symptoms get worse, go and see a doctor immediately. •Avoid pregnancy if you have the possibility of it. •Avoid breastfeeding. •Grapefruit juice, hypericum perforatum-contained food and tobacco (smoking) affect the medicine. Avoid them while taking the medicine. Possible adverse reactions to this medicine The most commonly reported adverse reactions include rash, diarrhea, dry skin, pruritus and loss of appetite. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •shortness of breath, breathing difficulty, labored and frequent breathing, cough, dry cough, fever, weight loss, phlegm, loss of appetite, bluish lips and finger/toe nails  [interstitial lung disease (interstitial pneumonia, pneumonitis, irradiation pneumonitis, organized pneumonia, pulmonary fibrosis, acute respiratory distress syndrome, pulmonary infiltration, alveolitis, etc.)] •lassitude, loss of appetite, nausea, vomiting, itch, yellowness in the skin and/or the white of the eye, dark urine, flapping tremor in hands  [hepatitis, hepatic failure, hepatic function disorder] •muddy/watery stool, severe abdominal pain, nausea, sweating  [serious diarrhea] •decreased consciousness, swollen body/eyes, easy fatigability, decreased urinary volume, urinary retention, headache, lassitude, breathing difficulty  [acute renal failure] •acne-like rash, pain/warmth/redness/swelling around nails, dry skin, chapped skin, skin ulceration, itchiness  [severe dermopathy] •lassitude, loss of appetite, fever, high fever, joint pain, red spots with dropsical swelling in the center, red spots and breakable blisters (bullas) all over the body, rash and blister, inflamed eyelid/eye, conjunctival sore, severe stomatitis, lip/intraoral sore, pain in the genitalia  [mucocutaneous ocular syndrome (Stevens-Johnson syndrome), toxic epidermal necrolysis (TEN), erythema multiforme] •nausea, vomiting, stomachache, vomiting of blood, abdominal pain, severe abdominal pain, bloody/black stool  [perforation of the digestive tract, gastrointestinal ulcer, gastrointestinal bleeding] •sensitive to light, blurred vision, irritation in the eyes, ocular pain, teary eyes  [corneal perforation, corneal ulcer] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store at room temperature (1-30℃), away from direct sunlight and moisture. •Discard the remainder. Do not store them. Ask the pharmacist or healthcare facility how to discard them.