Miltefosine

Miltefosine 속성

Miltefosine C화학적 특성, 용도, 생산

개요

Miltefosin, representing the prototype of a new phospholipid structure, was introduced for the palliative treatment of skin metastases in patients with breast cancer. It is highly active against the human leukemia tumor cells xenograft in nude mice, leading to growth inhibition and regression of large established tumors. Its mode of antitumor activity is not mediated by the host immune system but by its pharmacological effects at the level of the cancer cell membrane, distinctly different from that of the classical cytostatic drugs which interact with cell proliferation at the level of DNA replication. Protein kinase C inhibition has been suggested as a possible mechanism.

용도

A phospholipid drug with antineoplastic and antiprotozoal/antifungal properties, also acts as an Akt inhibitor, and under investigation as a potential therapy against HIV infection.

정의

ChEBI: A phospholipid that is the hexadecyl monoester of phosphocholine.

Antimicrobial activity

Concentrations of 1–5 μm inhibit the promastigotes and amastigotes of Leishmania spp. and the epimastigotes and amastigotes of T. cruzi. Inhibitory concentrations against T. brucei spp. and E. histolytica are closer to 50 μm. Acanthamoeba spp. are variably susceptible, depending on the experimental conditions.

원료

There are no reports of clinical resistance in Leishmania so far. Experimental resistance has been induced in vitro against the promastigote stage of Leishmania and two plasma membrane proteins, LdMT and Ld Ros3, are necessary for miltefosine uptake. There is evidence that reduced sensitivity of promastigotes is passed on to intracellular amastigotes.

Pharmaceutical Applications

An alkylphospholipid, originally investigated as an anticancer compound, formulated for oral administration.

Pharmacokinetics

In rodent models the drug is almost completely absorbed after oral administration. About 90% is bound to plasma proteins. It is widely distributed in the body; studies in rats showed highest uptake in kidney, liver and spleen. In rats and dogs bioavailability was 82% and 94%, with maximum values reached after 4–48 h.
In adult human trials repeated oral dosing with 100 mg per day achieved a peak plasma concentration of 70 mg/L after 8–24 h (day 23). The half-life is 6–8 days.

Clinical Use

Visceral leishmaniasis
Cutaneous leishmaniasis

부작용

Mild to moderate gastrointestinal side effects are reported in 40–60% of patients. Moderate to severe nephrotoxicity was seen in 2% and 1% of patients, respectively; increases in creatinine levels were reversible. Miltefosine is contraindicated in pregnancy, based on findings of teratogenicity in rats. It causes hemolysis and cannot be given intravenously.

Miltefosine 준비 용품 및 원자재

원자재

준비 용품

Miltefosine 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Beijing Mesochem Technology Co.,Ltd	+8613651027935	rachel@mesochem.com	China	191	58
Hebei Chuanghai Biotechnology Co,.LTD	+86-13131129325	sales1@chuanghaibio.com	China	5893	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	997	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	973	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	444	58
Capot Chemical Co.,Ltd.	+86-（0）57185586718 +86-13336195806	sales@capot.com	China	29791	60
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21634	55
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32957	60
career henan chemical co	+86-0371-86658258 +8613203830695	sales@coreychem.com	China	29884	58
SHANDONG ZHI SHANG CHEMICAL CO.LTD	+86 18953170293	sales@sdzschem.com	China	2930	58

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