Clinical application progress of the new Oxazolidinone antibiotic Contezolid

doi:10.3877/cma.j.issn.2096-1537.2025.01.016

Abstract

Abstract:

Oxazolidinones are a novel class of fully synthetic antibiotics that have shown activity against multi-drug resistant Gram-positive bacteria and Mycobacterium tuberculosis. Contezolid is a novel Oxazolidinone with potent activity against Methicillin-sensitive Staphylococcusaureus （MSSA），Methicillinresistant Staphylococcus aureus （MRSA），Streptococci and Enterococci. Compared to Linezolid，Contezolid is associated with a lower risk of causing thrombocytopenia. This paper reviews the chemical properties，usage and dosage of the approved indications，pharmacological activity，antibacterial activity，safety，and clinical application and research progress，providing a reference for its clinical rational application and future research.

Key words: Contezolid, Oxazolidinones, Antibacterials

Yunsong Yu, Baiyi Chen, Minggui Wang, Yingchun Xu, Suodi Zhai, Haibo Qiu, Yi Shi. Clinical application progress of the new Oxazolidinone antibiotic Contezolid[J]. Chinese Journal of Critical Care & Intensive Care Medicine(Electronic Edition), 2025, 11(01): 78-90.

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References 62

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抗菌药物	MRSAMIC₉₀	CD34⁺抑制IC₅₀	MAO-A抑制IC₅₀	MPSIC₅₀	MTBSI
LZD	1	6.3～7.9	4.1～4.9	4.8	5
TZD	0.5	0.2	1.8	0.2	0.7
CZD	0.5	15.7	12.3	10.6	11

抗菌药物	MRSAMIC₉₀	CD34⁺抑制IC₅₀	MAO-A抑制IC₅₀	MPSIC₅₀	MTBSI
LZD	1	6.3～7.9	4.1～4.9	4.8	5
TZD	0.5	0.2	1.8	0.2	0.7
CZD	0.5	15.7	12.3	10.6	11

年龄	体质量	给药剂量
6 ～ 11 岁	20 kg ～＜35 kg	400 mg，q12 h
6 ～ 17 岁	35 kg ～＜50 kg	600 mg，q12 h
12 ～ 17 岁	≥ 50 kg	800 mg，q12 h

年龄	体质量	给药剂量
6 ～ 11 岁	20 kg ～＜35 kg	400 mg，q12 h
6 ～ 17 岁	35 kg ～＜50 kg	600 mg，q12 h
12 ～ 17 岁	≥ 50 kg	800 mg，q12 h

参数	LZD^［24］600 mg q12 h	TZD^［25］200 mg qd	CZD^［3］800 mg q12 h
分子量	337.35	450.32	408.33
C_max（μg/ml）	21.0±5.8	2.2	26.4
C_min（μg/ml）	6.2±2.9	0.41±0.17^［26］	0.19
T_max（h）	1.0	3.5	2.5
AUC_{0 ～ t}（μg·h/ml）	138±42	25.6	85.8
Vd	0.65 L/kg	67 ～ 80 L	0.61 L/kg
t_1/2（h）	5.4	12	2.63
血浆蛋白结合率（%）	31	70 ～ 90	90
代谢	主要为吗啉环的氧化；细胞色素酶P450 在LZD 代谢中起次要作用^［27］	肝脏内通过多种磺基转移酶同工酶介导代谢为无活性的硫酸盐结合物	由黄素单加氧酶FMO5 和肝胞浆中的还原酶共同催化
清除	约30% 原型和50% 以代谢产物形式从尿排泄；约10% 以代谢产物形式从粪便排泄	粪便排泄约82%，尿液排泄约18%	原型经尿液和粪便排泄＜5%，主要以代谢物的形式随尿和粪便排泄
PK/PD 靶值	51^［28］	3^［29］	2.3^［22］
fAUC_{0 ～ 24 h} /MIC生物利用度（%）	100	90 以上	109

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