장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킬 수 있음
특정 표적장기 독성 - 반복 노출
구분 2
경고
P260, P314, P501
H400
수생생물에 매우 유독함
수생 환경유해성 물질 - 급성
구분 1
경고
P273, P391, P501
H410
장기적 영향에 의해 수생생물에 매우 유독함
수생 환경유해성 물질 - 만성
구분 1
경고
P273, P391, P501
예방조치문구:
P260
분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P270
이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P273
환경으로 배출하지 마시오.
P301+P310
삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.
P314
불편함을 느끼면 의학적인 조치·조언을 구하시오.
P321
(…) 처치를 하시오.
P330
입을 씻어내시오.
P391
누출물을 모으시오.
P405
밀봉하여 저장하시오.
P501
...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
2
0
TMC-207 C화학적 특성, 용도, 생산
개요
In December 2012, the US FDA approved bedaquiline as part of combination
therapy for the treatment of multi-drug resistant tuberculosis (MDRTB).
Bedaquiline is the first drug approved for MDR-TB and is the first
approval from a new class of antituberculosis agents in the past 40 years.
Due to the high unmetmedical need for treating MDR-TB, the FDA granted
bedaquiline accelerated approval based on Phase II results, providing patients access to the drug while additional clinical studies are carried out. Bedaquiline (also known as TMC207 and R207910) is a diarylquinoline
that was discovered from a high-throughput, whole-cell screening
strategy with Mycobacterium smegmatis used as a surrogate for
M. tuberculosis. Bedaquiline is a single enantiomer of an initial screening
hit. Bedaquiline has potent and selective activity against mycobacteria, and
is active against both drug-sensitive and drug-resistant M. tuberculosis. The mechanism of action of bedaquiline is unique amongst anti-TB drugs and
involves inhibition of mycobacterial ATP synthase; it is not active against
human ATP synthase. Bedaquiline has in vivo activity in numerous preclinical models of TB infection, alone and in combination with other anti-TB agents, and has bactericidal activity in established TB infection models. Bedaquiline is synthesized in five steps from 3-phenylpropionic acid
and para-bromoaniline. Following amide formation, treatment with POCl3
and DMF under Vilsmeier–Hack conditions gave a 2-chloroquinoline product.
Treatment with sodium methoxide, followed by condensation with
3-(dimethylamino)-1-(naphthalen-1-yl)propan-1-one, and separation of isomers
gave bedaquiline.
용도
(αS,βR)-Bedaquiline is a diarylquinoline derivative that acts as a mycobacterial inhibitor. Bedaquiline shows promise as potential drug in the treatment of tuberculosis.