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Telavancin (Theravance) 总被引:2,自引:0,他引:2
Pace JL Judice JK 《Current opinion in investigational drugs (London, England : 2000)》2005,6(2):216-225
Theravance is developing telavancin, an injectable peptidoglycan inhibitor antibiotic for potential use in the treatment of Gram-positive bacterial infection. Phase III trials in complicated skin and skin structure infections commenced in September 2004. 相似文献
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《Drugs in R&D》2006,7(6):384-388
Telavancin [TD-6424, ARBELIC] is an injectable, bactericidal lipoglycopeptide antibacterial that is in clinical development with Theravance (formerly Advanced Medicine) in the US. Telavancin, which was discovered by Theravance through the application of multivalent drug design, has a broad spectrum of activity against Gram-positive pathogens. Telavancin is currently in phase III development for complicated skin and soft tissue infections (including those caused by methicilin-resistant Staphylococcus aureus [MRSA]), nosocomial pneumonia, as well as other Gram-positive pathogens. The antibacterial effects of telavancin are mediated through multiple mechanisms, including inhibition of cell wall (peptidoglycan) synthesis. The drug also produces changes in bacterial cell membrane permeability. The multiple mechanisms of action may be responsible for the low frequency of spontaneous resistance to telavancin. Theravance and Astellas Pharma entered into a licensing agreement for telavancin in November 2005. The two companies will collaborate for the development and commercialisation of the antibacterial agent worldwide, except Japan. Under the terms of the agreement, Astellas will make a 65 million US dollars up-front payment and royalties on global sales to Theravance; in addition, Theravance is eligible to receive 156 million US dollars in clinical and regulatory milestones payments, including 136 million US dollars for completing enrollment, filling and approval of ongoing phase III programmes, and 20 million US dollars if phase III data indicate telavancin's superiority over vancomycin for the treatment of MRSA. Theravance will continue to explore partnering opportunities in the Japanese market. Telavancin was granted fast-track status by the US FDA in March 2005 for the treatment of complicated skin and skin structure infections (cSSSIs), as well as hospital-acquired pneumonia (nosocomial pneumonia). The compound is currently in phase III trials for these indications in the US. Theravance has also conducted two randomised, double-blind phase II trials (FAST and FAST 2) of telavancin in patients with cSSSIs caused by Gram-positive bacteria, in which telavancin (7 or 10 mg/kg) was compared with standard vancomycin therapy. Results showed that while telavancin was comparable to standard therapy overall, telavancin was associated with superior MRSA eradication rates. 相似文献
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PURPOSE: The pharmacology, activity, pharmacokinetics, pharmacodynamics, clinical efficacy, safety, dosage, and place in therapy of telavancin are reviewed. SUMMARY: Telavancin is a lipoglycopeptide antimicrobial agent under development for use in the treatment of multidrug-resistant gram-positive infections. Telavancin, like vancomycin, inhibits cell-wall biosynthesis by binding to late-stage cell-wall precursors. However, unlike vancomycin, telavancin also depolarizes the bacterial cell membrane and disrupts its functional integrity. Telavancin has concentration-dependent bactericidal activity and is active against gram-positive aerobic and anaerobic organisms. It is highly protein bound (93%) and has a volume of distribution of 115 mL/kg and a half-life of approximately eight hours. Telavancin is eliminated renally, and a dosage reduction is required in renally impaired patients. Animal models suggest that telavancin may be effective in the treatment of soft-tissue infections, bacteremia, endocarditis, meningitis, and pneumonia caused by gram-positive pathogens. Telavancin was not inferior to standard treatment for complicated skin and soft-tissue infections in two Phase II clinical trials and two Phase III clinical trials. A new drug application has been submitted for this indication, and Phase III trials to evaluate use in hospital-acquired-pneumonia, including infections caused by methicillin-resistant Staphylococcus aureus (MRSA), are planned. Adverse effects include metallic taste, nausea, vomiting, headache, foamy urine, Q-Tc-interval prolongation, hypokalemia, and serum creatinine increases. In trials evaluating telavancin for skin and soft-tissue infections, the dosage was 10 mg/kg i.v. once daily. CONCLUSION: Telavancin is a promising new agent for gram-positive infections and may offer an alternative to vancomycin for MRSA-associated infections. 相似文献
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Telavancin, a once-daily dosing lipoglycopeptide derived from vancomycin, has a broad-spectrum microbiologic activity against gram-positive bacteria, including vancomycin-resistant staphylococci. Telavancin displays a dual mode of action and a rapid bactericidal killing. The in vitro activity of telavancin is superior to vancomycin and comparable with, or greater than, linezolid, daptomycin and other novel lipoglycopeptides. Telavancin is effective against gram-positive pathogens in animal models of soft tissue infections and deep-seated infections including endocarditis, pneumonia and bacteremia. Clinical experience with telavancin in Phase II and III studies for complicated skin and skin structure infections have demonstrated similar efficacy and tolerability compared with standard anti-staphylococcal beta-lactams and vancomycin. Telavancin is in Phase III studies for nosocomial pneumonia. Telavancin seems to be promising as a novel agent for empiric therapy or as an alternative agent in serious infections caused by clinically important resistant gram-positive pathogens such as methicillin-resistant Staphylococcus aureus, vancomycin intermediate-susceptible S. aureus, vancomycin-resistant S. aureus and vancomycin-resistant enterococci. 相似文献
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《Expert opinion on investigational drugs》2013,22(3):347-357
Telavancin, a once-daily dosing lipoglycopeptide derived from vancomycin, has a broad-spectrum microbiologic activity against Gram-positive bacteria, including vancomycin-resistant staphylococci. Telavancin displays a dual mode of action and a rapid bactericidal killing. The in vitro activity of telavancin is superior to vancomycin and comparable with, or greater than, linezolid, daptomycin and other novel lipoglycopeptides. Telavancin is effective against Gram-positive pathogens in animal models of soft tissue infections and deep-seated infections including endocarditis, pneumonia and bacteremia. Clinical experience with telavancin in Phase II and III studies for complicated skin and skin structure infections have demonstrated similar efficacy and tolerability compared with standard anti-staphylococcal β-lactams and vancomycin. Telavancin is in Phase III studies for nosocomial pneumonia. Telavancin seems to be promising as a novel agent for empiric therapy or as an alternative agent in serious infections caused by clinically important resistant Gram-positive pathogens such as methicillin-resistant Staphylococcus aureus, vancomycin intermediate-susceptible S. aureus, vancomycin-resistant S. aureus and vancomycin-resistant enterococci. 相似文献
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Background and Objective:
Intravenous (IV) infusions of telavancin for injection are generally administered in-hospital, but in some circumstances they may be administered in an outpatient environment. In that setting, antibiotics may be premixed and frozen. This study determined the chemical stability of nonpreserved telavancin in various commonly used reconstitution diluents stored in IV bags (polyvinyl chloride [PVC] and PVC-free) at -20°C (-4°F) without light.Methods:
Telavancin (750 mg/vial) was reconstituted with 5% dextrose injection USP (D5W) or 0.9% sodium chloride injection USP (NS) to obtain drug solutions at approximately 15 mg/mL. Infusion solutions of telavancin at diluted concentrations of 0.6 mg/mL and 8.0 mg/mL covering the range utilized in clinical practice were prepared in both PVC and PVC-free IV bags using D5W or NS solutions. The infusion solutions were stored under frozen conditions (-20°C ± 5°C [-4°F ± 41°F]) and the chemical stability was evaluated for up to 32 days. Telavancin concentration, purity, and degradant levels were determined using a stability-indicating high-performance liquid chromatography (HPLC) method.Results:
Telavancin IV infusion solutions in D5W or NS at 0.6 mg/mL and 8 mg/mL and stored at -20°C (-4°F) met the chemical stability criteria when tested on days 0, 7, 14, and 32. The assayed telavancin concentration at each time point was within 97% to 103% of the initial mean assay value. The total degradants quantified by the HPLC stability-indicating method did not show any significant change over the 32-day study period.Conclusion:
Telavancin IV infusion solutions (in D5W or NS) in both PVC and PVC-free IV bags were stable for at least 32 days when stored at -20°C (-4°F) without light. These results provide prolonged frozen stability data further to that previously established for 7 days under refrigerated conditions (2°C-8°C [36°F -46°F]), and for 12 hours at room temperature when diluted into IV bags containing D5W, NS, or lactated Ringer’s solution. 相似文献7.
《Expert opinion on pharmacotherapy》2013,14(17):2737-2750
Introduction: Hospital-acquired pneumonia is a common infection, associated with substantial mortality. Despite the increasing prevalence of nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus (MRSA), approved treatment options for this pathogen are limited. Areas covered: This article reviews the pharmacokinetics, dosing, preclinical studies and clinical efficacy, and safety of telavancin, with a particular focus on results from trials in nosocomial pneumonia. PubMed and Congress websites were searched for relevant articles published between 2003 and 2010. Expert opinion: Telavancin is a lipoglycopeptide antibiotic with rapid, bactericidal activity against MRSA, and may provide another option for the treatment of nosocomial pneumonia, owing to Gram-positive pathogens. 相似文献
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Rubinstein E Corey GR Stryjewski ME Kanafani ZA 《Expert opinion on pharmacotherapy》2011,12(17):2737-2750
INTRODUCTION: Hospital-acquired pneumonia is a common infection, associated with substantial mortality. Despite the increasing prevalence of nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus (MRSA), approved treatment options for this pathogen are limited. AREAS COVERED: This article reviews the pharmacokinetics, dosing, preclinical studies and clinical efficacy, and safety of telavancin, with a particular focus on results from trials in nosocomial pneumonia. PubMed and Congress websites were searched for relevant articles published between 2003 and 2010. EXPERT OPINION: Telavancin is a lipoglycopeptide antibiotic with rapid, bactericidal activity against MRSA, and may provide another option for the treatment of nosocomial pneumonia, owing to Gram-positive pathogens. 相似文献
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2012年12月14日,FDA批准ponatinib hydrochloride(商品名为Iclusig)在美国上市,该药由Ariad制药公司开发,该药为片剂,用于慢性髓细胞白血病(CML)和费城染色体阳性急性淋巴细胞白血病(Ph+ALL)的治疗。Ponatinib hydrochloride的中文名称:3-(咪唑并[1,2-b]哒嗪-3-基乙炔基)-4-甲基-N-{4-[(4-甲基哌嗪-1-基)甲基]- 相似文献
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Racemic salbutamol (racemic albuterol) ameliorates symptoms of asthma by activating beta-adrenoceptors on nerve, smooth muscle and inflammatory cells within the airways. Racemic salbutamol comprises equal proportions of 2 isomers: (S)-salbutamol and (R)-salbutamol, with the latter being exclusively responsible for activation of beta-adrenoceptors. Accordingly, within racemic salbutamol it is (R)-salbutamol that efficiently relieves obstruction of asthmatic airways and affords highly effective protection from bronchoconstrictor stimuli, including allergens. During regular use of racemic salbutamol, there is a progressive decline of protective efficacy and a corresponding intensification of airway responsiveness. This decline is largely absent during regular use of (R)-salbutamol. Consequently, bronchodilator responses to sub-maximal doses of (R)-salbutamol exceed responses to the equivalent dose of (R)-salbutamol given as the racemate. For example, in asthmatics with baseline FEVs 相似文献
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盐酸鲁拉西酮(lurasidone hydrochloride,商品名为 Latuda)是由日本住友制药公司开发的具有双重作用的新型抗精神病药物。它对 5-HT2A 受体和多巴胺 D2 受体均具有高度亲和力。对精神病人的阳性和阴性症状均具有显著疗效。该药于2010年10月28日经美国食品药品管理局(FDA)批准在美国上市。 盐酸鲁拉西酮的中文化学名称:(3aR, 4S , 7R, 7aS ) -2-[ (1R, 2R ) -2-[ 4-(1, 2-苯并异噻唑-3-基)哌嗪-1-基甲基] 环己基甲基]六氢-1H-4, 7-甲基异吲哚-1, 3-二酮盐酸盐;英文化学名称:(3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl] cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione hydrochloride;分子式:C28H36N4O2S; 相对分子量:492.26;CAS 登记号:367514-88-3。 相似文献
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