A Phase I, Single-Centre, Double-Blind, Placebo-Controlled, Escalating Single Oral Dose, Safety and Tolerability Clinical Trial With BTA9881 in Healthy Subjects

This is a placebo-controlled, double-blind, randomised, single dose escalation Phase I clinical trial to determine the safety and tolerability of BTA9881 administered orally to healthy subjects

开始日期2007-07-01

申办/合作机构

Biota Scientific Management Pty Ltd.

100 项与 BTA-9881 相关的临床结果

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100 项与 BTA-9881 相关的转化医学

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100 项与 BTA-9881 相关的专利（医药）

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项与 BTA-9881 相关的文献（医药）

2015-02-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

1,2,3,9b-Tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones as a new class of respiratory syncytial virus (RSV) fusion inhibitors. Part 2: Identification of BTA9881 as a preclinical candidate

4区 · 医学

Article

作者: Tucker, Simon P ; Draffan, Alistair G ; Lambert, John ; Morton, Craig J ; Fenner, Jennifer E ; Lin, Bo ; Anderson, Kelly H ; Bond, Silas ; Sanford, Vanessa ; Lim, Chin Yu ; Mayes, Penelope A ; Nearn, Roland H ; Luttick, Angela ; Mitchell, Jeffrey P

Respiratory syncytial virus (RSV) is a major cause of respiratory tract infections in infants, young children and adults. 1,2,3,9b-Tetrahydro-5H-imidazo[2,1-a]isoindol-5-ones with general structure 1 were previously identified as promising inhibitors of RSV targeting the fusion glycoprotein. In particular, the introduction of a nitrogen at the 8-position of the tricyclic core yielded lead compounds 2 and 3. Extensive exploration of the R(2) group established that certain heterocyclic amides conferred potent RSV A&B activity and a good balance of physicochemical and pharmacokinetic properties. The antiviral activity was found to reside in a single enantiomer and compound 33a, (9bS)-9b-(4-chlorophenyl)-1-(pyridin-3-ylcarbonyl)-1,2,3,9b-tetrahydro-5H-imidazo[1',2':1,2]pyrrolo[3,4-c]pyridin-5-one (known as BTA9881), was identified as a candidate for preclinical development.

2009-07-01·Current opinion in drug discovery & development

Prospects for the development of fusion inhibitors to treat human respiratory syncytial virus infection.

Review

作者: Roymans, Dirk ; Bonfanti, Jean-François

Human respiratory syncytial virus (hRSV) is a significant cause of respiratory illness in at-risk pediatric patients, immunocompromised adults and the elderly. No vaccine is currently available for the virus and treatment options are limited to the prophylactic treatment of at-risk infants with the mAb palivizumab (Synagis) and to therapeutic intervention with the nucleoside analog ribavirin (Rebetol). The clinical use of these agents is limited and a need exists for more effective treatment for the at-risk population. The merging of viral and cellular membranes is a crucial event in the hRSV life cycle that enables the virus to enter a host cell. The multistep fusion process is facilitated by the substantial refolding of a trimeric class I fusion protein (F protein), which is the main target of fusion inhibitors. Several small-molecule fusion inhibitors have been discovered, of which some have progressed significantly in the drug development process. BTA-9881 (Biota Holdings Ltd/MedImmune) and TMC-353121 (Johnson & Johnson) are the most advanced of this drug class. In addition, progress has been made in the development of next-generation antibodies such as motavizumab (Numax; MedImmune). This review will discuss the status and latest developments of compounds and antibodies that inhibit hRSV fusion.

2009-07-01·Cardiovascular & Hematological Agents in Medicinal Chemistry

Respiratory Syncytial Virus (RSV) Prevention and Treatment: Past, Present, and Future

Review

作者: Weisman, Leonard E

Respiratory syncytial virus (RSV) is a very important pathogen worldwide. It occurs and recurs naturally throughout life. Both short and long term morbidity, and mortality are particularly significant for infants, especially those infants with underlying conditions and risk factors. Current treatment strategies for these patients (e.g Ribavirin) are limited but several new interventions (e.g. RSV604, BTA9881, ALN-RSV01) are under investigation. Several preventive agents and strategies have been developed (e.g. RSV-IGIV, palivizumab) and others are in the pipeline (e.g. motavizumab) and under development (e,g, Medi-557). In this article, we review the RSV clinical condition with a focus on the highest risk populations. In addition we review prevention and treatment strategies of the past, present and future for these high-risk patients. This review should provide a single valuable source of information to clinicians and investigators.

100 项与 BTA-9881 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05226

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
呼吸道合胞体病毒感染	临床2期	-	阿斯利康制药有限公司	-
呼吸道合胞体病毒感染	临床2期	-	Aviragen Therapeutics	-
呼吸道合胞体病毒感染	临床2期	-	阿斯利康制药有限公司	-
呼吸道合胞体病毒感染	临床2期	-	Aviragen Therapeutics	-