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更新于：2026-10-23
Cefpiramide Sodium
头孢匹胺钠
更新于：2026-10-23
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (1989-01-31), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C25H24N8NaO7S2 |
InChIKeyQJEAXQCIQHYEIT-ALLHVENQSA-N |
CAS号74849-93-7 |
关联
1
项与 头孢匹胺钠 相关的临床试验NCT05622578
Phenotyping of Chronic Pain in Diffused Systemic Scleroderma: Characteristics and Perturbations of Mechanisms of Pain, Impact on the Quality of Life and Correlations of Fatigue, Sleeping Disorders and Mood or Anxiety Disorders
100 项与 头孢匹胺钠 相关的临床结果
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100 项与 头孢匹胺钠 相关的转化医学
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100 项与 头孢匹胺钠 相关的专利（医药）
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286
项与 头孢匹胺钠 相关的文献（医药）2026-07-09ACS Medicinal Chemistry Letters
Cefpiramide Restricts
Mycobacterium tuberculosis
Growth by Binding to the DNA-Binding Domain of an Essential Response Regulator, MtrA
Article
作者: Saxena, Shalini ; Voina, Vidya Chitta ; Rangaraj, Siranjeevi ; Mohareer, Krishnaveni ; Banerjee, Sharmistha
The rise in drug-resistant Mycobacterium tuberculosis (M.tb) necessitates new therapeutic strategies. Hypothesizing that a single compound targeting multiple M.tb proteins would make resistance less likely to evolve, we focused on identifying a single compound targeting multiple M.tb OmpR family two-component response regulators (RRs). We screened ∼8000 FDA-approved DrugBank compounds using computational tools (active-site prediction, receptor-ligand docking, and molecular dynamics simulations) to identify one compound acting on M.tb RRs: MtrA, PrrA, MprA, RegX3, and PhoP. Cefpiramide showed strong docking scores and favorable interactions with all five RRs. Experimental validations confirmed that cefpiramide binds MtrA and RegX3 with K b values of 109.69 ± 27.99 nM-1 and 113.49 ± 36.63 nM-1, respectively. Further, the disruption of transcription repressor function of MtrA is possibly by disruption of its DNA binding property, as mutant analysis indicated that cefpiramide targets the DNA-binding domain of MtrA. Cefpiramide inhibited M.tb H37Rv growth (MIC50 = 4 ± 2.38 μg/mL), warranting further investigation as a component of combinatorial tuberculosis therapy.
2025-09-01PHARMACEUTICAL RESEARCH
Fraction-based Linear Extrapolation (FLEX) Method for Predicting Human Pharmacokinetic Clearance: Advanced Allometric Scaling Method and Machine Learning Approach
Article
作者: Kageyama, Michiharu ; Yoshimura, Saki ; Umemori, Yuki ; Handa, Koichi
PURPOSE:
Accurate prediction of human clearance (CL) is essential in early drug development. Single Species Scaling (SSS) using rat pharmacokinetic (PK) data, particularly with unbound plasma fraction (fu,plasma), is widely used. However, its accuracy declines for compounds with extremely low fu,plasma, and no systematic method has addressed this limitation.
METHODS:
We developed a new approach, called Fraction-based Linear EXtrapolation SSS (FLEX-SSS fu Rat), which switches between SSS fu Rat and SSS Rat formulas based on an optimized fu threshold. The threshold and scaling coefficients were derived using a training set of 200 compounds. Additionally, a random forest (RF) machine learning model was built using molecular descriptors. Both models were validated using an external dataset of 62 compounds.
RESULTS:
All five predictive models showed comparable performance; among them, the consensus model combining FLEX-SSS fu Rat and RF yielded the best result: 40.3% within 2-fold error, only 16.1% above 5-fold, and GMFE of 2.7.
CONCLUSION:
This study is the first to systematically validate SSS fu Rat using an independent dataset. The integration of threshold-based allometry and machine learning enabled more accurate human CL prediction, supporting informed decisions in first-in-human dose selection.
2025-02-13JOURNAL OF PHYSICAL CHEMISTRY B
In Silico Discovery of SARS-CoV-2 Main Protease Inhibitors Using Docking, Molecular Dynamics, and Fragment Molecular Orbital Calculations
Article
作者: Mika Okamoto ; Kenji Matsumoto ; Toshiyuki Hamada ; Masanori Baba ; Takeshi Ishikawa ; Masayuki Sudoh ; Hinako Koze
The 3C-like protease of severe acute respiratory syndrome coronavirus 2, known as the main protease (Mpro), is an attractive drug target for the treatment of coronavirus disease 2019. This study reports the discovery of novel Mpro inhibitors using several in silico techniques, including docking, molecular dynamics (MD), and fragment molecular orbital (FMO) calculations. We performed docking calculations on 5950 compounds with bioactivity, and 12 compounds were selected. An enzymatic assay was conducted, revealing that BP-1-102 exhibits significant Mpro inhibitory activity with an IC50 of 11.1 μM. The identification of seed compounds from the experiments on a few compounds demonstrates the effectiveness of our docking calculations. Furthermore, the detailed analyses using MD and FMO calculations suggested an interaction mechanism in which the hydroxyl group of BP-1-102 forms a hydrogen bond with E166 of Mpro. The Mpro inhibitory activity of SH-4-54, a derivative without the aforementioned hydroxyl group, was investigated and observed to be significantly reduced, with an IC50 of 81.5 μM. This result strongly supports the suggested interaction mechanism.
100 项与 头孢匹胺钠 相关的药物交易
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研发状态
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 烧伤 | 中国 | 2004-07-23 | |
| 喉炎 | 中国 | 2004-07-23 | |
| 咽炎 | 中国 | 2004-07-23 | |
| 脓毒症 | 中国 | 1999-12-30 | |
| 细菌感染 | 美国 | 1989-01-31 |
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