Levofolinic酸钙（Levofolinic酸的衍生物）-为新一代抗胃癌、结肠癌、胰腺癌新药
治疗类别名称
叶酸制剂的活性形式
商標名
ISOVORIN INJECTION
一般名
レボホリナートカルシウム（Levofolinate Calcium）
化学名
Monocalcium N-（4-｛［（6S）-2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxopteridin-6-yl］methylamino｝benzoyl）-L-glutamate
構造式

分子式
C20H21CaN7O7
分子量
511.50
融点
約264℃（分解）
旋光度
［α］20D：－15～－19゜
（脱水物に換算したもの0.250g，0.2mol/Lトリス緩衝液pH8.1，25mL，100mm）
性状
本产品为浅黄白色至浅黄褐色结晶性粉末，无臭，味。此产品是微溶于水，几乎不溶于甲醇或乙醇（99.5）。
适应病症
1. Rebohorinato氟尿嘧啶治疗
氟尿嘧啶对胃癌（不能手术或复发）与大肠癌的抗肿瘤作用增强
2. Rebohorinato氟尿嘧啶持续输注联合治疗
氟尿嘧啶结肠直肠癌和不能切除的胰腺癌的抗肿瘤效果增强
用法用量
1. Rebohorinato氟尿嘧啶治疗
成人一次250毫克体表面积/平方米以上一个周期2小时注射一次输注静脉作为Rebohorinato的。静脉内注射到一次作为氟尿嘧啶1小时从Rebohorinato在不到3分钟600毫克体表面积/平方米的起始缓慢滴注静脉注射后。每星期经过反复六次，两个星期的休息。
2. Rebohorinato氟尿嘧啶联合静脉滴注治疗大肠癌
(1) 成人一次100毫克体表面积/平方米以上一个周期2小时注射一次输注静脉作为Rebohorinato的。为400mg/m2的氟尿嘧啶与静脉注射，600毫克/平方米以上（体表面积）22小时，连续静脉内注射如氟尿嘧啶Rebohorinato输注静脉注射端（体表面积）之后。这是连续两天进行，每2周重复。
(2) 成人一次250毫克体表面积/平方米以上一个周期2小时注射一次输注静脉作为Rebohorinato的。如氟尿嘧啶后立即Rebohorinato2600mg/平方米（体表面积）的输注静脉注射端在持续静脉历时24小时注射。经过反复六次每星期，两个星期的休息。
(3) 成人一次200毫克体表面积/平方米以上一个周期2小时注射一次输注静脉作为Rebohorinato的。为400mg/m2的氟尿嘧啶与静脉注射，2400〜3000毫克/平方米（体表面积）Rebohorinato输注静脉注射端（体表面积）后，立即将在持续静脉历时46小时，氟尿嘧啶注入。这是每两周重复。
3. Rebohorinato氟尿嘧啶联合静脉滴注治疗不能切除的胰腺癌
对成年人一次200毫克体表面积/平方米以上一个周期2小时注射一次输注静脉作为Rebohorinato的。为400mg/m2的氟尿嘧啶Rebohorinato的（体表面积）用静脉注射，2400mg/平方米（体表面积）的输注静脉注射结束后立即在持续静脉历时46小时，氟尿嘧啶注入。这是每两周重复。
药效药理
1.抗肿瘤效果增强作用
(1)体外试验
人类结肠癌细胞（COLO201），对人胃癌细胞（TMK-1，KATOIII，MKN28）用20μM浓度的Rebohorinato体外试验，氟尿嘧啶的抗肿瘤作用的增强已被观察到。
(2)体内试验
用于与人结肠癌0-4细胞和人胃癌的H-111细胞移植的裸鼠，表明在组合Rebohorinato（200毫克/千克）和氟尿嘧啶（90毫克/千克）的肿瘤细胞的生长抑制效果。
2. 作用机序
Rebohorinato是，提升氟尿嘧啶通过生化调制的抗肿瘤作用。抑制：（TS胸苷酸合成酶）与和，通过抑制该TS活性相结合，抑制和DNA合成胸苷酸合成氟尿嘧啶是氟脱氧尿苷酸是一种活性代谢物（FdUMP），胸苷酸合成酶到。 Rebohorinato在细胞减少，一个5,10-亚甲基四氢叶酸（5,10-CH 2 THF）中。 5,10-CH THF为FdUMP，形式TS和紧三元复合物（三元复合物），通过延迟TS的解离，从而提高氟尿嘧啶的抗肿瘤效果。
包装规格
静脉滴注
25毫克：10瓶

100毫克：5瓶

制造和销售
辉瑞公司日本
提示：以上中文资料仅供参考，使用以原文为准：http://www.info.pmda.go.jp/go/pack/3929407D1063_1_09/

Levofolinate calcium(Levofolinate calcium)
ISOVORIN INJECTION 25mg（アイソボリン点滴静注用25mg） 
Brand name : ISOVORIN INJECTION 25mg
　Active ingredient: Levofolinate calcium
　Dosage form: injection
　Print on wrapping:
ISOVORIN INJECTION 100mg（アイソボリン点滴静注用100mg） 
Brand name : ISOVORIN INJECTION 100mg
　Active ingredient: Levofolinate calcium
　Dosage form: injection
　Print on wrapping: 
Effects of this medicine
This medicine boosts the effectiveness of antitumor effect with concomitant use of fluorouracil.
Usually, used for the purpose of enhancing the effect of fluorouracil for the treatment of gastric cancer (which is inoperable or recurrent), colorectal cancer and 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 have: fever, generalized dullness, diarrhea, varicella (chickenpox) or other infectious disease, ascites, pleural effusion, heart disease or its history, poor general condition, discontinuation of receiving the combination preparation of tegafur, gimeracil and oteracil potassium (TS-1) within 7 days, liver disease, renal disease, liver metastasis, gastrointestinal ulcer or hemorrhage, ongoing treatment by radiation.
•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>>
•In general, for adults, this medicine is administered by intravenous drip infusion at one time over the period of 2 hours.
•The administration intervals depend on concomitant drugs and symptoms/condition. Contact your doctor about the specific dosing schedule.
Precautions while taking this medicine
•If you have decreased bone-marrow function, infection or bleeding may tend to occur. However, it is difficult to find out these symptoms so that you should receive clinical examination (blood test, liver/renal function test, etc) regularly (frequently during early treatment period, in particular) to find any symptoms early.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include diarrhea, loss of appetite, nausea/vomiting, stomatitis, fever, rash, taste abnormality, abdominal pain, epigastric pain, thirst, constipation, gum inflammation, cheilitis, melena, angular cheilitis, tongue inflammation, heartburn and abdominal bloating. 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.
•persistent muddy or watery stool [severe diarrhea]
•chill, fever, bleeding tendency [bone-marrow depression]
•severe abdominal pain, diarrhea [serious enteritis]
•breathing difficulty, generalized hot flashes, urticaria [shock, anaphylaxis]
•dullness, loss of appetite, yellowing of the skin or whites of the eyes [liver dysfunction, jaundice]
•decreased urine output, swelling of limbs, dullness [acute renal failure]
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.
Pfizer Pharmaceuticals Inc.Injection
Revised: 12/2013
The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.