Journal of Tuberculosis and Lung Disease ›› 2025, Vol. 6 ›› Issue (5): 495-515.doi: 10.19983/j.issn.2096-8493.20252004
• Guideline·Standard·Consensus • Previous Articles Next Articles
Multidisciplinary Diagnosis and Treatment Branch of Chinese Antituberculosis Association , National Clinical Research Center for Infectious Disease/Shenzhen Third People’s Hospital, Beijing Chao-Yang Hospital , Capital Medical University , Guangdong Lung Cancer Institute
Received:2025-07-01
Online:2025-10-20
Published:2025-10-15
Supported by:CLC Number:
Multidisciplinary Diagnosis and Treatment Branch of Chinese Antituberculosis Association , National Clinical Research Center for Infectious Disease/Shenzhen Third People’s Hospital, Beijing Chao-Yang Hospital , Capital Medical University , Guangdong Lung Cancer Institute . Expert consensus on the diagnosis and treatment of coexistent pulmonary tuberculosis and lung cancer[J]. Journal of Tuberculosis and Lung Disease , 2025, 6(5): 495-515. doi: 10.19983/j.issn.2096-8493.20252004
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| 药品 | 药物代谢酶 | 与利福平相互作用 | 建议 |
|---|---|---|---|
| 紫杉醇类(含紫杉醇、紫杉醇脂质体、白蛋白紫杉醇、紫杉醇胶束) | CYP3A4/2C8 | 利福平诱导CYP3A4,加速紫杉醇类药物代谢,降低血药浓度,药品说明书建议谨慎合用 | A |
| 多西他赛 | CYP3A4/2C8 | 利福平诱导CYP3A4,导致多西他赛清除率增加,血药浓度下降。药品说明书建议谨慎合用 | A |
| 顺铂/卡铂 | 非CYP代谢 | 铂类药物通过DNA交联发挥作用,不依赖CYP酶代谢。药品说明书建议使用利福平无需调整剂量 | C |
| 培美曲塞 | 非CYP代谢 | 培美曲塞主要经肾排泄,利福平不影响其清除率。药品说明书建议无需调整剂量 | C |
| 吉西他滨 | 非CYP代谢 | 吉西他滨通过胞嘧啶脱氨酶代谢,利福平不影响该酶活性。药品说明书建议无需调整剂量 | C |
| 依托泊苷 | CYP3A4 | 利福平可能诱导CYP3A4,加速依托泊苷代谢,增加骨髓抑制风险。药品说明书建议谨慎合用 | A |
| 伊立替康 | CYP3A4 | 利福平诱导CYP3A4,增加伊立替康活性代谢产物SN-38生成,可能加重腹泻毒性。药品说明书建议谨慎合用 | A |
| 长春瑞滨 | CYP3A4 | 利福平诱导CYP3A4,可能降低长春瑞滨血药浓度。药品说明书建议谨慎合用 | A |
| 替莫唑胺 | 非酶水解 | 替莫唑胺在酸性条件下水解为活性产物,利福平不影响其分解过程。药品说明书建议无需调整剂量 | C |
| 芦比替定 | CYP3A4 | 芦比替定主要经CYP3A4代谢,利福平诱导酶活性可能降低其疗效。药品说明书建议尽量避免使用 | A |
| 芦康沙妥珠单抗 | TROP2抗体部分不依赖CYP代谢,细胞毒性部分(KL610023,拓扑异构酶Ⅰ抑制剂)由CYP3A4代谢 | 尚缺乏患者体内相互作用研究,但理论上利福平可能会削弱芦康沙妥珠单抗的疗效,建议谨慎合用 | B |
| 德曲妥珠单抗 | HER2抗体部分不依赖CYP代谢,细胞毒性部分(DXd,拓扑异构酶Ⅰ抑制剂)主要由CYP3A4代谢 | 尚缺乏患者体内相互作用研究,但理论上利福平可能会削弱德曲妥珠单抗的疗效,建议谨慎合用 | B |
| 药品 | 作用靶点 | 药物代谢酶 | 与利福平相互作用及底物AUC变化 | 建议 | ||
|---|---|---|---|---|---|---|
| 奥希替尼 | EGFR | CYP3A4 | 说明书提示利福平诱导CYP3A4会显著降低其血药浓度。使奥希替尼的稳态AUC下降78%[ | A | ||
| 阿美替尼 | EGFR | CYP3A4 | 说明书提示阿美替尼与利福平联用会导致暴露量显著降低(AUC降低约90%)。药品说明书建议谨慎合用 | A | ||
| 伏美替尼 | EGFR | CYP3A4 | 伏美替尼与强诱导剂或抑制剂联合使用时需谨慎。药品说明书建议谨慎合用 | B | ||
| 贝福替尼 | EGFR | CYP3A4 | 与强诱导剂合并使用可能会导致本品血药浓度降低。药品说明书建议谨慎合用 | B | ||
| 阿法替尼 | EGFR、HER2 | P-gp | 利福平为P-gp诱导剂。上市后研究表明:利福平连续7d,可将阿法替尼的血浆暴露量降低33.8%(AUC)和21.6%(药峰浓度)[ | B | ||
| 达可替尼 | EGFR | CYP2D6、CYP3A4 | 说明书提示利福平作为强CYP3A4诱导剂,合用会导致AUC降低80%,导致治疗失败。药品说明书禁止联用 | A | ||
| 吉非替尼 | EGFR | CYP3A4 | 与CYP3A4强诱导剂利福平合用,吉非替尼的平均AUC比单服时降低83%[ | A | ||
| 厄洛替尼 | EGFR | CYP3A4、CYP1A2 | 说明书提示与CYP3A4强诱导剂利福平合用,导致厄洛替尼的平均AUC降低69%[ | A | ||
| 埃克替尼 | EGFR | CYP2C19、CYP3A4 | 与利福平合用,导致暴露量显著降低。药品说明书建议注意避免潜在的药物相互作用 | A | ||
| 利厄替尼 | EGFR | CYP3A4 | 与利福平合用,导致暴露量显著降低。药品说明书建议避免合用 | A | ||
| 瑞厄替尼 | EGFR | CYP3A4 | 利福平加速代谢,显著减少药物暴露量[ | A | ||
| 瑞齐替尼 | EGFR | CYP3A4、CYP2B6 CYP2C8、CYP2C9 CYP2C19、CYP2D6 | 利福平诱导代谢酶,导致血药浓度下降。药品说明书建议避免合用 | A | ||
| 阿来替尼 | ALK | CYP3A4 | 利福平合并用药对阿来替尼的总暴露量的影响较小[ | B | ||
| 布格替尼 | ALK | CYP2C8、CYP3A4 | 说明书提示利福平合并使用,可使布格替尼的AUC降低80%[ | A | ||
| 洛拉替尼 | ALK | CYP3A4 | 说明书提示本品禁用于正在服用强效CYP3A诱导剂的患者。利福平使洛拉替尼AUC平均值下降85%[ | A | ||
| 恩沙替尼 | ALK | CYP3A4 | 与强诱导剂联合使用可能会导致本品血药浓度降低。慎用利福平。药品说明书建议谨慎合用 | B | ||
| 伊鲁阿克 | ALK | CYP3A4 | 伊鲁阿克尚未完成与CYP3A4抑制剂和诱导剂联用的药物-药物相互作用研究。与利福平合用可能会导致伊鲁阿克血药浓度的降低 | A | ||
| 塞瑞替尼 | ALK | CYP3A4、P-gp | 与强效诱导剂利福平联用可显著降低本品的血浆浓度。药品说明书建议避免合用 | B | ||
| 克唑替尼 | ALK、ROS1、MET | CYP3A4 | 说明书提示利福平合并服用时,克唑替尼的稳态AUC0-Tau降低84%[ | A | ||
| 依奉阿克 | ALK、ROS1、MET | CYP3A4 | 利福平显著降低依奉阿克药物浓度。药品说明书建议避免合用 | A | ||
| 安奈克替尼 | ALK、ROS1、c-Met | CYP3A4 | 与CYP3A4强诱导剂合用会导致血药浓度降低。药品说明书建议避免合用 | A | ||
| 达拉非尼+ 曲美替尼 | BRAFV600 MEK1/2 | CYP2C8、CYP3A4 | 说明书提示本身是CYP3A4诱导剂,利福平增强CYP3A4活性,显著降低达拉非尼浓度,AUC下降34%;药品说明书建议避免合用。曲美替尼与利福平无明显相互作用;药品说明书建议可以合用 | 达拉菲尼B; 曲美替尼C | ||
| 恩曲替尼 | NTRK、ROS1 | CYP3A4 | 说明书提示与强诱导剂利福平合用,可使恩曲替尼的全身暴露量下降77%[ | A | ||
| 拉罗替尼 | NTRK | CYP3A4 | 说明书提示利福平诱导CYP3A4会显著降低其血药浓度(AUC降低81%)。药品说明书建议避免合用 | A | ||
| 瑞普替尼 | ROS1、NTRK | CYP3A4/5 | 强效诱导剂利福平显著降低其血药浓度。药品说明书建议避免合用 | A | ||
| 他雷替尼 | ROS1、NTRK | CYP3A4、CYP2D6、 CYP2C8 | 说明书提示与强诱导剂利福平合用,AUCinf降低86%。药品说明书建议避免合用 | A | ||
| 谷美替尼 | MET | CYP3A4 | CYP3A4为谷美替尼的主要代谢酶,但其对其代谢贡献有限(<5%),提示CYP抑制剂或诱导剂不太可能与临床剂量的谷美替尼发生相互作用。药品说明书建议无需调整剂量 | C | ||
| 伯瑞替尼 | MET | CYP3A4、CYP2C9 | 伯瑞替尼可通过多种代谢酶代谢,但主要通过CYP3A4代谢。说明书提示与强诱导剂利福平合用,可使伯瑞替尼的AUC下降65%。药品说明书建议避免合用 | A | ||
| 特泊替尼 | MET | CYP3A4、P-gp | 强效P-gp诱导剂可能会降低特泊替尼的暴露量。强效CYP诱导剂也可能会降低特泊替尼的暴露量。药品说明书建议避免合用 | A | ||
| 赛沃替尼 | MET | CYP1A2、CYP3A4、 CYP3A5 | 说明书提示与利福平合用会使赛沃替尼AUC降低61%[ | A | ||
| 卡马替尼 | MET | CYP3A4 | 利福平诱导CYP3A4会显著降低其血药浓度。药品说明书建议避免合用或增加剂量 | A | ||
| 氟泽雷塞 | KRAS G12C | 谷胱甘肽S-转移酶 | 氟泽雷赛的主要代谢途径为谷胱甘肽S-转移酶介导的半胱氨酸结合,其对CYP3A4既有潜在抑制作用,也有潜在诱导作用。药品说明书建议可以合用 | C | ||
| 格索雷塞 | KRAS G12C | CYP3A4、CYP2C8 | 利福平显著降低药物暴露量。药品说明书建议避免合用 | A | ||
| 塞普替尼 | RET | CYP3A4 | 说明书提示利福平强效诱导CYP3A4会降低其血药浓度,AUC下降87%。药品说明书建议避免合用 | A | ||
| 普拉替尼 | RET | CYP3A4、CYP2D6、 CYP1A2 | 说明书提示强效CYP3A抑制剂避免与强效CYP3A抑制剂联合用药,AUC下降68%。药品说明书建议避免合用 | A | ||
| 埃万妥单抗 | EGFR、MET | 网状内皮系统降解 | 尚未开展药物相互作用研究 | B | ||
| 贝伐珠单抗 | VEGF-A | 蛋白水解分解代谢 | 与利福平无药代动力学相互作用。药品说明书建议可以合用 | C | ||
| 重组人血管 内皮抑素 | VEGFR2、MMP、 lntegrin等 | 通过蛋白水解代谢 | 与利福平合用未见报道。说明书中无具体提及。根据生物药品特征,其对CYP3A4酶的影响不大,故与利福平合用风险小 | C | ||
| 依沃西单抗 | VEGF-A、PD-1 | 网状内皮系统降解 | 与利福平合用未见相互作用报道。药品说明书建议可以合用 | C | ||
| 安罗替尼 | VEGFR1-3、FGFR、 PDGFR等 | CYP1A2、 CYP3A4/5 | CYP3A4/5诱导剂(利福平、利福布汀、利福喷丁等)可能加速安罗替尼的代谢,降低安罗替尼的血浆浓度。药品说明书建议避免合用 | A | ||
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