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Samuel E Wilson, Donald R Graham, Whedy Wang, Jon B Bruss, Bibiana Castaneda-Ruiz
INTRODUCTION: Concurrent Staphylococcus aureus bacteremia (SAB) worsens outcomes and increases mortality in patients with complicated skin and skin structure infections (cSSSI), hospital-acquired bacterial pneumonia, and ventilator-associated bacterial pneumonia (HABP/VABP). These challenges highlight the need for alternative treatments. Telavancin (TLV), a bactericidal lipoglycopeptide with high in vitro potency, effectively treats patients with cSSSI and HABP/VABP caused by Gram-positive pathogens, particularly S...
September 2017: Infectious Diseases and Therapy
Biswadeep Das, Chayna Sarkar, Debasmita Das, Amit Gupta, Arnav Kalra, Shubham Sahni
Telavancin (TD-6424), a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). The US Food and Drug Administration (USFDA) had approved telavancin in 2009 for the treatment of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria, including MRSA (S. aureus, Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus anginosus group, or Enterococcus faecalis)...
March 2017: Therapeutic Advances in Infectious Disease
Lan Jiang, David T Beattie, John R Jacobsen, Samuel Kintz, Glenmar P Obedencio, Daisuke Saito, Ioanna Stergiades, Ross G Vickery, Daniel D Long
Gastrointestinal dysfunction as a consequence of the use of opioid analgesics is of significant clinical concern. First generation drugs to treat these opioid-induced side-effects were limited by their negative impact on opioid receptor agonist-induced analgesia. Second generation therapies target a localized, peripherally-restricted, non-CNS penetrant drug distribution of opioid receptor antagonists. Herein we describe the discovery of the N-substituted-endo-3-(8-aza-bicyclo[3.2.1]oct-3-yl)-phenol and -phenyl carboxamide series of μ-opioid receptor antagonists...
July 1, 2017: Bioorganic & Medicinal Chemistry Letters
Jennifer I Smart, Gordon Ralph Corey, Martin E Stryjewski, Whedy Wang, Steven L Barriere
INTRODUCTION: The broth microdilution method (BMD) for testing telavancin minimum inhibitory concentrations (MICs) was revised (rBMD) in 2014 to improve the accuracy, precision, and reproducibility of the testing method. The aim of this study was to determine the effect of the revised method on telavancin MIC values for Staphylococcus aureus (S. aureus) clinical isolates obtained from hospital-acquired pneumonia (HAP) patients. METHODS: Isolates from patients who participated in the phase 3 Assessment of Telavancin for Treatment of HAP Studies were retested using the rBMD method...
December 2016: Infectious Diseases and Therapy
Juwon Yim, Jordan R Smith, Katie E Barber, Jessica A Hallesy, Michael J Rybak
INTRODUCTION: In clinical trials comparing telavancin (TLV) with vancomycin for treatment of hospital-acquired pneumonia, TLV demonstrated lower clinical cure rates than vancomycin in patients who had mixed gram-positive and -negative infections and were concomitantly treated with either aztreonam (ATM) or piperacillin/tazobactam (PTZ). Here, we investigated therapeutic interactions between TLV and ATM or PTZ in an in vitro pharmacokinetic/pharmacodynamic (PK/PD) model under simulated reduced renal function conditions...
September 2016: Infectious Diseases and Therapy
Patrick Sand, Traci Aladeen, Paul Kirkegaard, Dennis LaChance, Christine Slover
BACKGROUND: VIBATIV is a once-daily, injectable lipoglycopeptide antibiotic approved in the U.S. for the treatment of hospital-acquired and ventilator-associated bacterial pneumonia (HABP/VABP) caused by susceptible isolates of Staphylococcus aureus when alternative treatments are not suitable. In addition, VIBATIV is approved in the U.S. for the treatment of adult patients with complicated skin & skin structure infections (cSSSI) caused by susceptible isolates of Gram-positive bacteria, including Staphylococcus aureus, both methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) strains...
December 2015: Current Therapeutic Research, Clinical and Experimental
P Rogliani, M G Matera, M Cazzola
The critical role of the combination therapy of an inhaled corticosteroid (ICS) and a long-acting β-adrenoceptor agonist (LABA) in the treatment of patients suffering from asthma and also severe chronic obstructive pulmonary disease (COPD) patients with frequent exacerbations explains why there is a strong interest within the pharmaceutical industry in developing a once-daily ICS/LABA fixed-dose combination (FDC), in an attempt to simplify the treatment and, consequently, increase adherence to the prescribed therapy, and also to overcome the loss of patent protection...
August 2015: Drugs of Today
A Torres, E Rubinstein, G R Corey, M E Stryjewski, S L Barriere
OBJECTIVES: Telavancin is approved in Europe for the treatment of nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus when other alternatives are not suitable. The approved European prescribing information contraindicates the use of telavancin in patients with severe renal impairment (creatinine clearance <30 mL/min, including patients on haemodialysis) and pre-existing acute renal failure owing to the higher observed mortality in these patients. Data from the ATTAIN studies were reanalysed, excluding patients with these contraindicating conditions at baseline...
April 2014: Journal of Antimicrobial Chemotherapy
Michael P Ero, Nathaniel R Harvey, Jack L Harbert, James W Janc, Kay H Chin, Steven L Barriere
Telavancin is approved in the United States, Canada, and Europe (At the time of submission, the telavancin European marketing authorization for nosocomial pneumonia was suspended until Theravance provides evidence of a new European Medicines Agency approved supplier) as an antibiotic to treat certain Gram-positive bacterial skin infections. Telavancin has been shown to prolong plasmatic prothrombin (PT) and activated partial thromboplastin (aPTT) clotting times in clinical diagnostic lab-based assays. In this study, we evaluated the potential for telavancin to prolong whole blood PT/International Normalized Ratio (INR) and aPTT tests on point-of-care (POC) instruments...
2014: Journal of Thrombosis and Thrombolysis
Daniel D Long, Bryan Frieman, Sharath S Hegde, Craig M Hill, Lan Jiang, Samuel Kintz, Daniel G Marquess, Hans Purkey, Jeng-Pyng Shaw, Tod Steinfeld, Michael S Wilson, Kevin Wrench
Lowering of intra-ocular pressure is the primary pharmacologic approach for the treatment of glaucoma and a number of distinct mechanisms of action have been clinically validated. Targeting of multiple mechanisms in combination therapies has proven effective both clinically and commercially although potential improvements with regards to efficacy, tolerability and dosing frequency remain. Application of Theravance's multivalent approach to drug discovery towards linked dual-pharmacology prostaglandin F receptor (FP) agonist/carbonic anhydrase (CA)-II inhibitor compounds is described...
February 15, 2013: Bioorganic & Medicinal Chemistry Letters
Daniel D Long, Scott R Armstrong, David T Beattie, Seok-Ki Choi, Paul R Fatheree, Roland A L Gendron, Daniel Genov, Adam A Goldblum, Patrick P Humphrey, Lan Jiang, Daniel G Marquess, Jeng-Pyng Shaw, Jacqueline A M Smith, S Derek Turner, Ross G Vickery
Utilization of Theravance's multivalent approach to drug discovery towards 5-HT(4) receptor agonists with a focus on identification of neutral (non-charged at physiological pH) secondary binding groups is described. Optimization of a quinolone-tropane primary binding group with a chiral 2-propanol linker to a range of neutral secondary binding group motifs, for binding affinity and functional potency at the 5-HT(4) receptor, selectivity over the 5-HT(3) receptor, oral pharmacokinetics, and in vivo efficacy in models of GI motility, afforded velusetrag (TD-5108)...
October 1, 2012: Bioorganic & Medicinal Chemistry Letters
John Paul Seale
The European Respiratory Society Congress, held in Barcelona, included topics covering new therapeutic developments in the field of respiratory health and disease. This conference report highlights selected presentations on therapies targeting inflammatory cells, with a focus on therapeutic agents for asthma and COPD. This report also includes a discussion of novel therapeutic agents for pulmonary hypertension. Investigational drugs discussed include OC-000459 (Oxagen), SCH-527123 (Merck & Co), AZD-9668 (AstraZeneca), benralizumab (MedImmune/Kyowa Hakko Kirin/BioWa), PF-3429281 (Pfizer), vilanterol (GlaxoSmithKline/Theravance), LAS-100977 (Almirall Prodesfarma), selexipag (Nippon Shinyaku/Actelion) and GW-0742 (GlaxoSmithKline)...
November 2010: IDrugs: the Investigational Drugs Journal
Peter Norman
A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore attached to a second, less functionalised moiety via a variable length spacer incorporating heteroatoms. Eight of the applications utilise a a 4-piperidinylester of biphenylcarbamic acid as the muscarinic pharmacophore and two utilise 2,2-diphenyl-2-(S)-pyrrolidin-3-ylacetamide...
September 2006: Expert Opinion on Therapeutic Patents
Asma Al-Shamahi, Konrad Kirkham, Livia Hookes
The 39th Annual Meeting of the Society for Neuroscience (SFN), held in Chicago, included topics covering new therapeutic developments in the field of neuroscience. This conference report highlights selected presentations on novel neuroprotective and antiparkinsonian agents, and compounds in development for the treatment of dementia, schizophrenia, depression, obesity and spinal muscular atrophy. Investigational drugs discussed include velusetrag and TD-8954 (both from Theravance Inc), SEP-228791 and SEP-226330 (both from Sepracor Inc), ADL-5510 (Adolor Corp), PF-217830 (Pfizer Inc), KB-099520 (Karo Bio AB), tesofensine (NeuroSearch A/S) and TRP6-01 (Theraptosis)...
December 2009: IDrugs: the Investigational Drugs Journal
Ben Turner, Lisa Murch
The Interscience Conference on Antimicrobial Agents and Chemotherapy held in San Francisco included topics covering new therapeutic developments for the treatment of infectious diseases. This conference report highlights selected presentations on a beta-cyclodextrin derivative for the treatment of Staphylococcus aureus infections, a type 3 secretion system inhibitor for the treatment of Pseudomonas aeruginosa infections, a small-molecule inhibitor of the fungal Hos2 HDAC, a TLR9 agonist used as an adjuvant, a CMV vaccine, a glycopeptide-cephalosporin heterodimer antibiotic, a topical quinolone for the treatment of complicated skin and skin structure infections, a broad-spectrum glycylcycline antibiotic and an HCV RNA replication inhibitor...
November 2009: IDrugs: the Investigational Drugs Journal
Lisa Charneski, Priti N Patel, Donna Sym
OBJECTIVE: To review the pharmacology, antimicrobial activity, pharmacokinetics, clinical applications, and safety of telavancin, a new lipoglycopeptide antibiotic. DATA SOURCES: Literature was obtained from MEDLINE (1966-April 2009) and International Pharmaceutical Abstracts (1971-April 2009) using the search terms telavancin and TD-6424, and also from Theravance, Inc., and Astellas Pharma US, Inc. STUDY SELECTION AND DATA EXTRACTION: Available English-language articles were reviewed, as well as information obtained from Theravance, Inc...
May 2009: Annals of Pharmacotherapy
(no author information available yet)
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...
2006: Drugs in R&D
John L Pace, J Kevin Judice
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.
February 2005: Current Opinion in Investigational Drugs
Josephine S Villa, Robert T Cass, Dane E Karr, Stacy M Adams, Jeng-Pyng Shaw, Donald E Schmidt
The movement towards a 96-well format has greatly increased productivity and throughput in bioanalytical laboratories. Improvements in automated sample preparation and analytical methods have further contributed to increased productivity. We have focused on sample collection and transfer to the bioanalyst and have found improvements to the current available methods. The problem of manual transfers and plasma clotting issues can be overcome with the use of microtainers. Specifically, for illustrative purposes, three proprietary Theravance compounds were tested for stability, non-specific binding, and electrospray ion suppression in microtainers...
2004: Rapid Communications in Mass Spectrometry: RCM
Alice A McCarthy
No abstract text is available yet for this article.
June 2003: Chemistry & Biology
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