Lymecycline | 992-21-2

• 物质功能分类: 原料药 - 抗生素类药物 - 四环素类药
• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 四环素类
• 英文名称: Lymecycline
• 英文别名: (2S)-6-[[[(4S,4aS,5aS,6S,12aR)-4-(dimethylamino)-1,6,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4,4a,5,5a-tetrahydrotetracene-2-carbonyl]amino]methylamino]-2-aminohexanoic acid
• CAS: 992-21-2
• 化学式: C₂₉H₃₈N₄O₁₀
• 分子量: 602.6
• InChiKey: PZTCVADFMACKLU-UEPZRUIBSA-N

物化性质

• 熔点：
  192.5°C
• 沸点：
  648.97°C (rough estimate)
• 密度：
  1.53
• 溶解度：
  极易溶于水，微溶于乙醇（96%），几乎不溶于二氯甲烷。

计算性质

• 辛醇/水分配系数(LogP)：
  -4.4
• 重原子数：
  43
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  243
• 氢给体数：
  9
• 氢受体数：
  13

ADMET

毒理性

• 毒性总结

大鼠口服赖氨环素的LD50为3200毫克/千克。[L13913] 赖氨环素过量情况罕见。在发生过量时，应立即进行洗胃。提供支持性治疗并维持体液平衡。[L13883]

The oral LD50 of lymecycline in rats is 3200 mg/kg.[L13913] Overdoses with lymecycline are rare. In the case of an overdose, gastric lavage should be performed immediately. Provide supportive treatment and maintain fluid balance.[L13883]

来源:DrugBank

吸收、分配和排泄

• 吸收

林美环素口服给药后吸收率为77-88%，相对生物利用度为70%。林美环素的Cmax为2.1 mg/L，大约在给药后3小时达到。AUC为21.9 ± 4.3 mg·h/L。

Lymecycline is 77-88% absorbed after oral administration with a relative bioavailability of 70%.[A203258] The Cmax of lymecycline is 2.1 mg/L and is achieved about 3 hours after administration.[A1424] The AUC is 21.9 ± 4.3 mg·h/L.[A1424]

来源:DrugBank

吸收、分配和排泄

• 消除途径

Lymecycline is 25% eliminated in the urine.[A1424] Based on being a member of the tetracycline drug class, fecal elimination is likely another route of elimination.[A203366] 林美环素在尿液中排除了25%。[A1424]由于林美环素属于四环素类药物，因此粪便排出可能是另一种排除途径。[A203366]

Lymecycline is 25% eliminated in the urine.[A1424] Based on being a member of the tetracycline drug class, fecal elimination is likely another route of elimination.[A203366]

来源:DrugBank

吸收、分配和排泄

• 分布容积

林可霉素是亲脂性的，能够轻易穿过细胞膜，并通过细菌孔蛋白通道被动扩散。[A1424,A19429] 作为第二代四环素，它在胆汁中的浓度是血浆浓度的10到25倍。[A1424,A203366] 通常，四环素类药物的分布体积范围在1.3-1.7升/千克或100-130升。[A1424]

Lymecycline is lipophilic and easily crosses the cell membrane and passively diffuses through bacterial porin channels.[A1424,A19429] As a second-generation tetracycline, the concentration in the bile ranges from 10 to 25 times higher than plasma concentration.[A1424,A203366] In general, the volume of distribution of tetracyclines ranges from 1.3–1.7 L/kg or 100–130 L.[A1424]

来源:DrugBank

吸收、分配和排泄

• 清除

莱姆环素部分通过肾脏清除，与其他四环素类抗生素相似。[A203366]

Lymecycline is partially cleared by the kidneys, like other tetracyclines.[A203366]

来源:DrugBank

文献信息

• [EN] COMBINATION OF ZIDOVUDINE WITH A TETRACYCLINE ANTIBIOTIC<br/>[FR] COMBINAISON DE ZIDOVUDINE ET D'UN ANTIBIOTIQUE TÉTRACYCLINE
  申请人：HELPERBY THERAPEUTICS LTD

  公开号：WO2021074598A1

  公开（公告）日：2021-04-22

  The present invention relates to a combination comprising zidovudine or a pharmaceutically acceptable derivative thereof and a tetracycline antibiotic or a pharmaceutically acceptable derivative or prodrug thereof, for use in treating a microbial infection, particularly a bacterial infection such as a urinary tract infection.