ALPHA-2B干扰素

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: ALPHA-2B干扰素
• 中文别名: 干扰素alfa-2b；干扰素 alfa-2b; alpha-2b 干扰素
• 英文名称: sodium;diiodomethanesulfonate;N-propyl-N-[2-(2,4,6-trichlorophenoxy)ethyl]imidazole-1-carboxamide
• 化学式: C16H17Cl3I2N3NaO5S
• 分子量: 746.5
• InChiKey: MIXCUJKCXRNYFM-UHFFFAOYSA-M

计算性质

• 辛醇/水分配系数(LogP)：
  2.29
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  113
• 氢给体数：
  0
• 氢受体数：
  6

ADMET

毒理性

• 药物性肝损伤

干扰素阿尔法-2b

Compound:interferon alfa-2b

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注解：最令人关注的药物性肝损伤

DILI Annotation:Most-DILI-Concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

严重等级：8

Severity Grade:8

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：警告和预防措施

Label Section:Warnings and precautions

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 用于研究药物诱导肝损伤的FDA批准药物标签，药物发现今日，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按在人类中发展药物诱导肝损伤风险排名的最大参考药物清单。药物发现今日2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

吸收、分配和排泄

为了产生系统性效果，干扰素α通过胃肠道外途径给药，因为该药物容易受到胃肠道中的蛋白水解酶的降解。干扰素α通过肌内注射或皮下注射吸收良好；肌内或皮下注射后吸收的剂量分数明显超过80%。静脉注射干扰素α后，峰值血清浓度通常在15-60分钟内出现，并且显著高于肌内或皮下给药后达到的浓度。然而，与快速静脉注射或快速（例如，40分钟或更少）静脉输注产生的浓度相比，肌内或皮下给药后的血清干扰素α浓度通常能维持更长的时间。

For systemic effects, interferon alfa is administered parenterally because the drug is susceptible to degradation by proteolytic enzymes in the GI tract. Interferon alfa is well absorbed following IM or subcutaneous injection; the apparent fraction of the dose absorbed after IM or subcutaneous injection exceeds 80%. Peak serum interferon alfa concentrations following IV administration of the drug generally occur within 15-60 minutes and are substantially greater than those attained after IM or subcutaneous administration. However, serum interferon alfa concentrations following IM or subcutaneous administration generally are maintained for longer periods of time than those produced by rapid IV injection or rapid (e.g., 40 minutes or less) IV infusion.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

静脉给药后，血清干扰素A浓度在30分钟输注结束时达到峰值（135-273 IU/mL），然后下降速度比肌肉或皮下给药后的下降速度略快，输注后4小时检测不到。

After intravenous administration, serum INTRON A concentrations peaked (135-273 IU/mL) by the end of the 30-minute infusion, then declined at a slightly more rapid rate than after intramuscular or subcutaneous drug administration, becoming undetectable 4 hours after the infusion.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

INTRON A的药代动力学在12名健康男性志愿者中进行研究，他们在交叉设计下接受了单次剂量为5百万IU/平方米的INTRON A，通过肌肉注射、皮下注射和30分钟静脉输注给药。通过肌肉注射和皮下注射获得的平均血清INTRON A浓度相似。通过这些途径获得的最大血清浓度大约为18至116 IU/mL，在给药后3至12小时出现。注射后16小时血清浓度无法检测到。

The pharmacokinetics of INTRON A were studied in 12 healthy male volunteers following single doses of 5 million IU/sq m administered intramuscularly, subcutaneously, and as a 30-minute intravenous infusion in a crossover design. The mean serum INTRON A concentrations following intramuscular and subcutaneous injections were comparable. The maximum serum concentrations obtained via these routes were approximately 18 to 116 IU/mL and occurred 3 to 12 hours after administration. Serum concentrations were undetectable by 16 hours after the injections.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

动物干扰素组织分布的数据有限，提示自然发生的混合人源或动物源干扰素在静脉给药后广泛且迅速地分布到体内各组织中，其中在脾脏、肾脏、肝脏和肺部的浓度最高。

Limited data on the tissue distribution of interferon in animals suggest that mixtures of naturally occurring human or animal interferons are widely and rapidly distributed into body tissues after parenteral administration, with the highest concentrations occurring in spleen, kidney, liver, and lung.

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• RETROVIRAL VECTORS WITH ENHANCED EFFICIENCY OF TRANSGENE EXPRESSION AND SAFETY
  申请人：HAHM Sung Ho

  公开号：US20060019396A1

  公开（公告）日：2006-01-26

  The present application discloses a MoMSV/MoMLV hybrid-based retroviral vector, wherein gag and pol genes are completely removed.

  本申请公开了一种基于 MoMSV/MoMLV 杂交的逆转录病毒载体，其中 gag 和 pol 基因被完全去除。