Ramoplanin

Ramoplanin 속성

Ramoplanin C화학적 특성, 용도, 생산

개요

Ramoplanin (A 16686, A16686A, MDL 62198) is a novel oral nonabsorbable 17-amino-acid cyclic lipoglycodepsipeptide antibiotic from Biosearch Italy. Ramoplanin is an antibiotic complex, first identified in 1984, that was isolated from the fermentation broth of Actinoplanes sp. ATCC 33076. It is a mixture of three closely related compounds, ramoplanin A1–A3, which differ only in the acyl group attached to the Asn-1 N-terminus; ramoplanin A2 is the most abundant.

용도

Ramoplanin is a potent cyclic lipoglycodepsipeptide antibiotic that exhibits wide spectrum of antibiotic properties against gram-positive and gram-negative bacteria.

Antimicrobial activity

Ramoplanin displays activity against aerobic and anaerobic Grampositive bacteria by preventing cell wall peptidoglycan formation through binding to a key intermediate moiety, lipid II, and thereby disrupting bacterial cell wall synthesis. The primary use of ramoplanin is in the treatment of Clostridium difficile infections.

Mechanism of action

The mechanism of action of ramoplanin involves sequestration of peptidoglycan biosynthesis lipid intermediates, thus physically occluding these substrates from proper utilization by the latestage peptidoglycan biosynthesis enzymes MurG and the transglycosylases (TGases). Ramoplanin is structurally related to two cell wall-active lipodepsipeptide antibiotics, janiemycin and enduracidin, and is functionally related to members of the lantibiotic class of antimicrobial peptides (mersacidin, actagardine, nisin, and epidermin) and glycopeptide antibiotics. As a consequence of its unique mechanism of action, cross-resistance with existing glycopeptides and beta-lactam antibiotics has not been observed.

Pharmacokinetics

Ramoplanin is not absorbed from the intestinal tract. When ramoplanin (200 and 400 mg) was administered orally to two groups of healthy volunteers over a period of 10 days, no ramoplanin could be detected in plasma and urine. With the 200-mg dose, concentrations in stools varied between 467 and 1043 mg/g, and with the 400-mg dose, concentrations were between 765 and 2032 mg/g. Results from an in vitro gut model and hamster model revealed that ramoplanin may be more effective than vancomycin at killing spores and preventing spore recrudescence.

Toxicology

When administered orally in a double-blind randomized placebocontrolled study, no adverse reactions were observed in patients receiving two daily doses of ramoplanin (100 or 400 mg) in comparison with the placebo. Single and repeated topical application in ten healthy human volunteers revealed very low irritation rates and no sensitization after 21 days.

Ramoplanin 준비 용품 및 원자재

원자재

준비 용품

Ramoplanin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Fuxin Pharmaceutical	+86-021-021-50872116 +8613122107989	contact@fuxinpharm.com	China	10297	58
AFINE CHEMICALS LIMITED	0571-85134551 18958018566;	info@afinechem.com	China	15377	58
Finetech Industry Limited	+86-27-87465837 +8618971612321	info@finetechnology-ind.com	China	9634	58
BOC Sciences	+16314854226	inquiry@bocsci.com	United States	19743	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418684 +8618949823763	sales@tnjchem.com	China	25363	58
Chengdu Youngshe Chemical Co., Ltd.	+8618108235634	Cecilia@youngshechem.com	China	2345	58
Hebei Duling International Trade Co. LTD	+8618712993135	sales01@hbduling.cn	China	15734	58
Jiangsu shring Biopharma Co., Ltd.	+8613372282299	sales@shringchem.com	China	3545	58
Hebei Miaoyin Technology Co.,Ltd	+86-17367732028 +86-17367732028	kathy@hbyinsheng.com	China	3582	58

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