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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/01/17 18:23:10」(JST)

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Amifostine is a cytoprotective adjuvant used in cancer chemotherapy and radiotherapy involving DNA-binding chemotherapeutic agents. It is marketed by MedImmune under the trade name Ethyol.

Indications[edit]

Amifostine is used therapeutically to reduce the incidence of neutropenia-related fever and infection induced by DNA-binding chemotherapeutic agents including alkylating agents (e.g. cyclophosphamide) and platinum-containing agents (e.g. cisplatin). It is also used to decrease the cumulative nephrotoxicity associated with platinum-containing agents. Amifostine is also indicated to reduce the incidence of xerostomia in patients undergoing radiotherapy for head and neck cancer.

Amifostine was originally indicated to reduce the cumulative renal toxicity from cisplatin in non-small cell lung cancer. However, while nephroprotection was observed, the probability that amifostine could protect tumors could not be excluded. Additional data have shown that amifostine-mediated tumor protection, in any clincal scenario, is unlikely.

Pharmacokinetics[edit]

WR-1065, 2-((aminopropyl)amino)ethanethiol, the active metabolite of amifostine

Amifostine is an organic thiophosphate prodrug which is hydrolysed in vivo by alkaline phosphatase to the active cytoprotective thiol metabolite, WR-1065. The selective protection of non-malignant tissues is believed to be due to higher alkaline phosphatase activity, higher pH, and vascular permeation of normal tissues.

Amifostine can be administered intravenously or subcutaneously after reconstitution with normal saline. Infusions lasting less than 15 minutes decrease the risk of adverse effects. The patient should be well-hydrated prior to administration.

Mechanism of action[edit]

Inside cells, amifostine detoxifies reactive metabolites of platinum and alkylating agents, as well as scavenges free radicals.^[1]^[2] Other possible effects include accelerated DNA repair,^[1] induction of cellular hypoxia,^[1] inhibition of apoptosis,^[2] alteration of gene expression^[2] and modification of enzyme activity.^[2]

Adverse effects[edit]

Common side effects of amifostine include hypocalcemia, diarrhea, nausea, vomiting, sneezing, somnolence, and hiccoughs. Serious side effects include: hypotension (found in 62% of patients), erythema multiforme, Stevens–Johnson syndrome and toxic epidermal necrolysis, immune hypersensitivity syndrome, erythroderma, anaphylaxis, and loss of consciousness (rare).

Contraindications[edit]

Contraindications to receiving amifostine include hypersensitivity to amifostine and aminothiol compounds like WR-1065. Ethyol contains mannitol.

References[edit]

^ ^a ^b ^c Kouvaris JR, Kouloulias VE, Vlahos LJ (June 2007). "Amifostine: the first selective-target and broad-spectrum radioprotector". Oncologist 12 (6): 738–47. doi:10.1634/theoncologist.12-6-738. PMID 17602063.
^ ^a ^b ^c ^d "Amifostine : BC Cancer Agency". British Columbia Cancer Agency. 2006-03-01. Retrieved 2011-01-01.

UpToDate Contents

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1. シスプラチン腎障害 cisplatin nephrotoxicity
2. 頭頸部癌の初期治療中の合併症のマネージメントおよび予防 management and prevention of complications during initial treatment of head and neck cancer
3. 化学療法誘発性末梢神経障害の予防および治療 prevention and treatment of chemotherapy induced peripheral neuropathy
4. 放射線誘発性線維症の臨床症状、予防、および治療 clinical manifestations prevention and treatment of radiation induced fibrosis
5. 放射線療法誘発性肺障害 radiation induced lung injury

English Journal

Melatonin can Ameliorate Radiation-Induced Oxidative Stress and Inflammation-Related Deterioration of Bone Quality in Rat Femur.

Çakir ZÜ1, Demirel C2, Kilciksiz SC3, Gürgül S4, Zincircioğlu SB5, Erdal N6.
Inflammation.Inflammation.2016 Jun;39(3):1134-40. doi: 10.1007/s10753-016-0347-x.
The aim of the present study was to evaluate the radioprotective effects of melatonin on the biomechanical properties of bone in comparison to amifostine (WR-2721). Forty Sprague Dawley rats were divided equally into 5 groups namely; control (C), irradiation (R; single dose of 50 Gy), irradiation�
PMID 27052631

The effect of amifostine on differentiation of the human megakaryoblastic Dami cell line.

Wang HT1,2,3, Yang B1, Hu B2,4, Chi XH5, Luo LL2, Yang HQ1, Lang XL2, Geng J2, Qiao CX2, Li Y2, Wu XX3, Zhu HL1, Lv M2, Lu XC1.
Cancer medicine.Cancer Med.2016 May 26. doi: 10.1002/cam4.759. [Epub ahead of print]
Amifostine is a cytoprotective drug that was initially used to control and treat nuclear radiation injury and is currently used to provide organ protection in cancer patients receiving chemotherapy. Clinical studies have also found that amifostine has some efficacy in the treatment of cytopenia caus
PMID 27228575

Improvement of the in vitro safety profile and cytoprotective efficacy of amifostine against chemotherapy by PEGylation strategy.

Yang X1, Ding Y2, Ji T2, Zhao X2, Wang H2, Zhao X2, Zhao R2, Wei J3, Qi S4, Nie G5.
Biochemical pharmacology.Biochem Pharmacol.2016 May 15;108:11-21. doi: 10.1016/j.bcp.2016.02.014. Epub 2016 Mar 2.
Amifostine, an organic thiophosphate prodrug, has been clinically utilized for selective protection of normal tissues with high expression of alkaline phosphatase from oxidative damage elicited by chemotherapy or radiotherapy. However, the patients receiving amifostine suffer from severe dose-depend
PMID 26944193

Japanese Journal

Amifostine Modulates Radio-induced Apoptosis of Peripheral Blood Lymphocytes in Head and Neck Cancer Patients

SAAVEDRA Maite M.,HENRIQUEZ-HERNANDEZ Luis Alberto,LARA Pedro C.,PINAR Beatriz,RODRIGUEZ-GALLEGO Carlos,LLORET Marta
Journal of radiation research 51(5), 603-607, 2010-09-16
… One of the strategies aimed at decreasing radiation toxicity is the use of radioprotective agents, such as amifostine. … The aim of the present study was to explore the effects of amifostine on the radiation-induced apoptosis of peripheral blood lymphocytes from patients suffering head and neck cancer. … Peripheral blood lymphocytes were isolated before and after the treatment with amifostine. …
NAID 10026644550

Effect of Preliminary Amifostine Administration in Irradiation of Parotid Glands

YACHI Yoshifumi,NASU Masanori,YOSUE Takashi
Oral science international : official journal of the Japanese Stomatological Society 5(2), 104-111, 2008-11-01
NAID 10027107198

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リンク元	「アミホスチン」「アミフォスチン」

「アミホスチン」

Amifostine
Systematic (IUPAC) name
	2-(3-aminopropylamino)ethylsulfanyl; phosphonic acid
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	C (US)
Legal status	℞-only (US)
Routes	Intravenous
Pharmacokinetic data
Bioavailability	complete
Half-life	8 minutes
Identifiers
CAS number	20537-88-6
ATC code	V03AF05
PubChem	CID 2141
DrugBank	DB01143
ChemSpider	2056
UNII	M487QF2F4V
KEGG	C06819
ChEBI	CHEBI:2636
ChEMBL	CHEMBL1006
Chemical data
Formula	C5H15N2O3PS
Mol. mass	214.224 g/mol
	SMILES O=P(O)(O)SCCNCCCN;
	InChI InChI=1S/C5H15N2O3PS/c6-2-1-3-7-4-5-12-11(8,9)10/h7H,1-6H2,(H2,8,9,10) ; Key:JKOQGQFVAUAYPM-UHFFFAOYSA-N ;
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英: amifostine
同: アミフォスチン
商: ETHYOL

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アミホスチン : 約 2,740 件
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放射線治療の副作用を抑える放射線防護剤

「アミフォスチン」

　　[★] アミホスチン、amifostine

[theoncologist-1] Kouvaris JR, Kouloulias VE, Vlahos LJ (June 2007). "Amifostine: the first selective-target and broad-spectrum radioprotector". Oncologist 12 (6): 738–47. doi:10.1634/theoncologist.12-6-738. PMID 17602063.

[bccancer-2] "Amifostine : BC Cancer Agency". British Columbia Cancer Agency. 2006-03-01. Retrieved 2011-01-01.

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amifostine