更新于：2024-11-01

PBPs x CYP2C9

更新于：2024-11-01

基本信息

关联

项与 PBPs x CYP2C9 相关的药物

Ampicillin/Probenecid

氨苄西林/丙磺舒

靶点

CYP2C9 x PBPs

作用机制

CYP2C9抑制剂 [+1]

在研机构

陕西香菊医药有限责任公司

原研机构

陕西香菊医药有限责任公司

在研适应症

感染

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

中国

首次获批日期1998-01-01

100 项与 PBPs x CYP2C9 相关的临床结果

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100 项与 PBPs x CYP2C9 相关的转化医学

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0 项与 PBPs x CYP2C9 相关的专利（医药）

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项与 PBPs x CYP2C9 相关的文献（医药）

2010-06-15·American Journal of Health-System Pharmacy4区 · 医学

Ceftobiprole: A novel, broad-spectrum cephalosporin with activity against methicillin-resistantStaphylococcus aureus

4区 · 医学

Review

作者: Dauner, Daniel G. ; Taketa, Donna C. ; Nelson, Robert E.

PURPOSEThe pharmacology, antimicrobial activity, pharmacokinetics, pharmacodynamics, clinical efficacy, safety, and place in therapy of ceftobiprole are reviewed.SUMMARYCeftobiprole, a novel, broad-spectrum, parenteral cephalosporin, inhibits the cell-wall synthesis of penicillin-binding proteins (PBPs) PBP2a and PBP2x, responsible for the resistance in staphylococci and pneumococci, respectively. Ceftobiprole has good activity against gram-positive aerobes and anaerobes, and its activity against gram-negative aerobes and anaerobes is species dependent. Ceftobiprole is relatively inactive against Acinetobacter species. Its ability to bind relevant PBPs of resistant gram-positive and gram-negative bacteria indicates its potential use in the treatment of hospital-acquired pneumonia and complicated skin and skin-structure infections (cSSSIs). Ceftobiprole is primarily excreted unchanged by the kidneys and exhibits linear pharmacokinetics. The half-life of the drug is approximately 3-4 hours. It exhibits minimal plasma protein binding (16%). Ceftobiprole does not inhibit the cytochrome P-450 isoenzyme system, so the possibility of drug-drug interactions is low. The drug has not been approved for use in the United States but has been approved in Canada and elsewhere. Ceftobiprole is currently undergoing Phase III clinical trials and has demonstrated activity against methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and Pseudomonas aeruginosa. Completed Phase III trials used i.v. dosages of 500 mg every 8-12 hours. The most commonly observed adverse effects of ceftobiprole included headache and gastrointestinal upset.CONCLUSIONCeftobiprole is a novel, broad-spectrum, parenteral cephalosporin undergoing Phase III clinical trials. Its broad spectrum of activity makes it a candidate for monotherapy of cSSSIs and pneumonias that have required combination therapy in the past.

2005-01-01·Journal of Environmental Pathology, Toxicology and Oncology4区 · 医学

Inhibitory Effect(s) of Polymeric Black Tea Polyphenols on the Formation of B(a)P-Derived DNA Adducts in Mouse Skin

4区 · 医学

Article

作者: Girish B Maru ; Rajesh Krishnan

The biological activities and chemopreventive properties of green tea polyphenols have been demonstrated, while similar information regarding newly formed major polymeric polyphenols in black tea are not available. Cancer chemoprevention may be achieved by the inhibition of any stage of carcinogenesis. In the present study, we investigated the anti-initiating effects of five polymeric black tea polyphenol (PBP) fractions, by determining their effects on the formation of [3H]-B(a)P-derived DNA adducts as well as the activity of cytochrome P-450 isozymes CYP 1A1 and 1A2 in vitro employing rat liver microsomes. PBP 1-3 inhibited both the microsome catalyzed [3H]-B(a)P-derived DNA adduct formation as well as the activity of CYP 1A1 and 1A2 as assessed by the decreased formation of resorufin from the respective substrates. Further investigation revealed that topical pretreatment(s) of mice with PBP 1-5 (200 mug/day x 4) resulted in a significant decrease in the levels of single topical B(a)P (1 mg/mouse) - induced DNA adducts in epidermal DNA determined by employing 32P-post labeling analysis. Overall, our results suggest that black tea-derived PBPs have one of the chemopreventive properties shown by monomeric green tea polyphenols.