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Research and Development of Delamanid (Deltyba<sup>®</sup>) for the treatment of Multi-drug Resistant Mycobacterium Tuberculosis
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- Sasaki Hirofumi
- Otsuka Pharmaceutical Co., Ltd., Medicinal Chemistry Research Laboratories, Pharmaceutical Business Division
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- Tsubouchi Hidetsugu
- Otsuka Pharmaceutical Co., Ltd., Compliance & Ethics Department, Osaka Head Office
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- Hashizume Hiroyuki
- Otsuka Pharmaceutical Co., Ltd., Product Management Group, Pharmaceutical Marketing Headquarters, Pharmaceutical Business Division
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- Kawasaki Masanori
- Otsuka Pharmaceutical Co., Ltd., TB Projects, Pharmaceutical Business Division
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- Matsumoto Makoto
- Otsuka Pharmaceutical Co., Ltd., Pharmaceutical Business Division
Bibliographic Information
- Other Title
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- 多剤耐性肺結核治療薬Delamanid（Deltyba<sup>®</sup>）の研究開発
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Description
<p>Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis. In recent years, the spread of multi-drug resistant Mtb (MDR-TB) and extensively drug-resistant Mtb (XDR-TB) strains have greatly complicated treatment and reduces successful treatment outcomes. Furthermore, the co-infection of TB and HIV has become a critical issue. In spite of this situation, one of the first anti-TB medications developed in the last 40 years with a novel structure and mechanism of action has the potential to alter the current treatment landscape. Otsuka was interested in the nitroimidazooxazole structure having anti-TB activities as the lead compound, and we expanded mainly a side chain moiety of the second position. We optimized these derivatives by the measurement of in vitro antitubercular activities and the in vivo examination in TB-infected mice. As a result, we found many derivatives having potent in vitro and in vivo activities without mutagenicity, and finally discovered delamanid for the treatment of multi-drug resistant pulmonary tuberculosis.</p>
Journal
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- MEDCHEM NEWS
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MEDCHEM NEWS 26 (3), 125-131, 2016-08-01
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390282681108828032
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- NII Article ID
- 130006731090
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- ISSN
- 24328626
- 24328618
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- Text Lang
- ja
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- Data Source
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- JaLC
- CiNii Articles
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- Abstract License Flag
- Disallowed
