vinblastine sulfate | 865-21-4

• 物质功能分类: 原料药 - 抗肿瘤药 - 天然来源类抗肿瘤药
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 长春花生物碱
• 英文名称: vinblastine sulfate
• 英文别名: vinblastine sulfuric acid salt；Vinblastine sulphate；methyl (1S,9R,10S,11R,12R,19R)-11-acetyloxy-12-ethyl-4-[(13S,15S,17S)-17-ethyl-17-hydroxy-13-methoxycarbonyl-11-aza-1-azoniatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-10-hydroxy-5-methoxy-8-methyl-8-aza-16-azoniapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carboxylate;sulfate
• CAS: 865-21-4；143-67-9
• 化学式: C₄₆H₅₈N₄O₉*H₂O₄S
• 分子量: 909.067
• InChiKey: KDQAABAKXDWYSZ-JKDPCDLQSA-N

物化性质

• 熔点：
  267 °C (dec.)(lit.)
• 比旋光度：
  -21.7 º (c=2, CH3OH 21 ºC)
• 溶解度：
  在水中的溶解度10 mg/mL
• 物理描述：
  Vinblastine sulfate appears as an anticancer drug. White to slightly yellow crystalline powder. (NTP, 1992)

计算性质

• 辛醇/水分配系数(LogP)：
  3.34
• 重原子数：
  64
• 可旋转键数：
  10
• 环数：
  9.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  237
• 氢给体数：
  5
• 氢受体数：
  16

ADMET

毒理性

• 致癌物分类

国际癌症研究机构致癌剂：硫酸长春碱

IARC Carcinogenic Agent:Vinblastine sulfate

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构（IARC）致癌物分类：第3组：对其对人类的致癌性无法分类

IARC Carcinogenic Classes:Group 3: Not classifiable as to its carcinogenicity to humans

来源:International Agency for Research on Cancer (IARC)

毒理性

• 致癌物分类

国际癌症研究机构专著：第26卷：(1981年)一些抗癌和免疫抑制剂

IARC Monographs:Volume 26: (1981) Some Antineoplastic and Immunosuppressive Agents

来源:International Agency for Research on Cancer (IARC)

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间的用药概述：大多数资料认为，在母体抗肿瘤药物治疗期间，母乳喂养是禁忌的。由于长春碱类药物的半衰期较长，因此在长春碱治疗结束后恢复母乳喂养可能是不切实际的。化疗可能会不利地影响母乳的正常微生物组和化学成分。在孕期接受化疗的女性更可能难以哺乳她们的婴儿。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：一名在孕中期被诊断为霍奇金淋巴瘤的女性在孕晚期接受了3轮化疗，并在产后4周恢复化疗。在重新开始化疗后的16周内，收集了她在化疗前后15至30分钟的乳汁样本。治疗方案包括每2周一次，2小时内给予多柔比星40毫克，博来霉素16单位，长春碱9.6毫克和达卡巴嗪600毫克。将该患者的乳汁微生物群和代谢概况与8名未接受化疗的健康女性进行了比较。患者的乳汁微生物群与健康女性明显不同，其中不动杆菌属、黄色单胞菌科和窄食单胞菌属增加，而双歧杆菌属和真杆菌属减少。在接受治疗的女性乳汁中的许多化学成分也发现了显著差异，尤其是DHA和肌醇的减少。 通过对在一个中心在孕中期或孕晚期接受癌症化疗的74名女性进行电话随访研究，以确定她们产后是否成功进行母乳喂养。只有34%的女性能够完全母乳喂养她们的婴儿，而66%的女性报告遇到了母乳喂养困难。这与其他22位在孕期被诊断但未接受化疗的母亲91%的母乳喂养成功率形成了对比。其他具有统计学意义的相关性包括：1. 有哺乳困难的母亲平均接受了5.5个周期的化疗，而没有困难的母亲平均接受了3.8个周期；2. 有哺乳困难的母亲平均在孕早期3.4周就开始了她们的第一个化疗周期。在接受了含有长春新碱方案的6名女性中，有5名遇到了哺乳困难。

◉ Summary of Use during Lactation:Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy. It is probably impractical to resume breastfeeding after vinblastine therapy because of the drug's long half-life. Chemotherapy may adversely affect the normal microbiome and chemical makeup of breastmilk. Women who receive chemotherapy during pregnancy are more likely to have difficulty nursing their infant. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:A woman diagnosed with Hodgkin's lymphoma during the second trimester of pregnancy received 3 rounds of chemotherapy during the third trimester of pregnancy and resumed chemotherapy 4 weeks postpartum. Milk samples were collected 15 to 30 minutes before and after chemotherapy for 16 weeks after restarting. The regimen consisted of doxorubicin 40 mg, bleomycin 16 units, vinblastine 9.6 mg and dacarbazine 600 mg, all given over a 2-hour period every 2 weeks. The microbial population and metabolic profile of her milk were compared to those of 8 healthy women who were not receiving chemotherapy. The breastmilk microbial population in the patient was markedly different from that of the healthy women, with increases in Acinetobacter sp., Xanthomonadacae and Stenotrophomonas sp. and decreases in Bifidobacterium sp. and Eubacterium sp. Marked differences were also found among numerous chemical components in the breastmilk of the treated woman, most notably DHA and inositol were decreased. A telephone follow-up study was conducted on 74 women who received cancer chemotherapy at one center du