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before the Christian era; used following dates before the supposed year Christ was born; "in 200 BC" (同)B.C., before Christ

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/11 04:46:00」(JST)

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Carmustine or BCNU (bis-chloroethylnitrosourea) is a mustard gas-related β-chloro-nitrosourea compound used as an alkylating agent in chemotherapy. As a dialkylating agent, BCNU is able to form interstrand crosslinks in DNA, which prevents DNA replication and DNA transcription.

It has the appearance of an orange-yellow solid.

Carmustine for injection is marketed under the name BiCNU by Bristol-Myers Squibb. In India, carmustine is marketed under the name Carustine by Curacell Biotech.

Uses [edit]

It is used in the treatment of several types of brain cancer (including glioma, glioblastoma multiforme, medulloblastoma and astrocytoma), multiple myeloma and lymphoma (Hodgkin's and non-Hodgkin). BCNU is sometimes used in conjunction with alkyl guanine transferase (AGT) inhibitors, such as O⁶-benzylguanine. The AGT-inhibitors increase the efficacy of BCNU by inhibiting the Direct Reversal pathway of DNA repair, which will prevent formation of the interstrand crosslink between the N¹ of guanine and the N³ of cytosine.

It is also used as part of chemotherapeutic protocol to prepare for hematological stem cell transplantation, to reduce the white blood cells in the recipient (patient). This use under this protocol, usually with Fludarabine and Melphalan, was coined by oncologist at MD Anderson Cancer Center.

Side effects [edit]

Bone marrow may take 6 weeks to recover function following treatment with carmustine. Weekly monitoring of platelet and white blood cell counts are recommended as a basis for patient-specific adjustments to dosage regimens. Bone marrow and pulmonary toxicities are a function of lifetime cumulative dose. Pulmonary toxicity characterized by pulmonary infiltrates and/or fibrosis (scarring of the lungs). Cases of fatal pulmonary toxicity have been reported. Delayed onset pulmonary fibrosis and myelosuppression may occur. Thrombocytopenia usually occurs about 4 weeks post administration. Leukopenia occurs approximately 5–6 weeks after administration. Cumulative myelosuppression, manifested by more depressed indices may occur. Anemia also occurs, but is less frequent and less severe than thrombocytopenia or leukopenia. The occurrence of acute leukemia and bone marrow dysplasias have been reported in patients following long-term nitrosourea therapy.

Nausea and vomiting after IV administration are noted frequently. This usually occurs within 2 hours of administration. This is usually dose related. Prior administration of antiemetics is effective in diminishing and sometimes preventing these effects.

A reversible type of hepatic toxicity, manifested by increased transaminase, alkaline phosphatase and bilirubin levels, has been reported in a small percentage of patients. Renal abnormalities consisting of progressive azotemia, decrease in kidney size and renal failure have been reported in patients who received large cumulative doses after prolonged therapy. Kidney damage has also been reported occasionally in patients receiving lower total doses.

Implants [edit]

In the treatment of brain tumours, the U.S. Food and Drug Administration (FDA) approved biodegradable discs, Gliadel, infused with carmustine can be used.^[2] They are implanted under the skull during a surgery called a craniotomy.^[3]

References [edit]

^ "Carmustine - Compound Summary". PubChem Compound. USA: National Center for Biotechnology Information. 25 March 2005. Identification. Retrieved 11 April 2012.
^ Ewend MG, Brem S, Gilbert M, et al. (June 2007). "Treatment of single brain metastasis with resection, intracavity carmustine polymer wafers, and radiation therapy is safe and provides excellent local control". Clin. Cancer Res. 13 (12): 3637–41. doi:10.1158/1078-0432.CCR-06-2095. PMID 17575228.
^ http://www.cancerbackup.org.uk/Treatments/Chemotherapy/Individualdrugs/Gliadelimplants

External links [edit]

MedlinePlus DrugInfo medmaster-a682060
BiCNU (package insert; U.S.)

UpToDate Contents

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1. 悪性神経膠腫に対する補助化学療法 adjuvant chemotherapy for malignant gliomas
2. 再発悪性神経膠腫の管理 management of recurrent malignant gliomas
3. 悪性神経膠腫に対する実験的治療アプローチ experimental treatment approaches for malignant gliomas
4. 間質性肺疾患における肺生検結果の解釈 interpretation of lung biopsy results in interstitial lung disease
5. ニトロソウレア誘発性肺障害 nitrosourea induced pulmonary injury

English Journal

AN in vitro evaluation of a carmustine-loaded Nano-co-Plex for potential magnetic-targeted intranasal delivery to the brain.

Akilo OD1, Choonara YE1, Strydom AM2, du Toit LC1, Kumar P1, Modi G3, Pillay V4.
International journal of pharmaceutics.Int J Pharm.2016 Mar 16;500(1-2):196-209. doi: 10.1016/j.ijpharm.2016.01.043. Epub 2016 Jan 19.
Targeted delivery of carmustine (BCNU), an efficient brain tumor therapeutic, has been challenged with bioavailability issues due to the Blood Brain Barrier (BBB). The currently effective delivery approach is by implants at the site of the tumor, but this is highly invasive. The intranasal route, wh
PMID 26806465

Anti-tumor activities of luteolin and silibinin in glioblastoma cells: overexpression of miR-7-1-3p augmented luteolin and silibinin to inhibit autophagy and induce apoptosis in glioblastoma in vivo.

Chakrabarti M1, Ray SK2.
Apoptosis : an international journal on programmed cell death.Apoptosis.2016 Mar;21(3):312-28. doi: 10.1007/s10495-015-1198-x.
Glioblastoma is the deadliest brain tumor in humans. High systemic toxicity of conventional chemotherapies prompted the search for natural compounds for controlling glioblastoma. The natural flavonoids luteolin (LUT) and silibinin (SIL) have anti-tumor activities. LUT inhibits autophagy, cell prolif
PMID 26573275

Brain targeted delivery of carmustine using solid lipid nanoparticles modified with tamoxifen and lactoferrin for antitumor proliferation.

Kuo YC1, Cheng SJ2.
International journal of pharmaceutics.Int J Pharm.2016 Feb 29;499(1-2):10-9. doi: 10.1016/j.ijpharm.2015.12.054. Epub 2015 Dec 22.
Solid lipid nanoparticles (SLNs) conjugated with tamoxifen (TX) and lactoferrin (Lf) were applied to carry anticancer carmustine (BCNU) across the blood-brain barrier (BBB) for enhanced antiproliferation against glioblastoma multiforme (GBM). BCNU-loaded SLNs with modified TX and Lf (TX-Lf-BCNU-SLNs
PMID 26721730

Japanese Journal

Double-edged Sword in the Placement of Carmustine (BCNU) Wafers along the Eloquent Area: A Case Report

, , ,
NMC Case Report Journal 2(1), 40-45, 2015
Although direct Gliadel® wafer implantation into the resection cavity has been shown to significantly improve survival in patients with high-grade gliomas, several complications have been associated w …
NAID 130005056826

Temozolomide (TMZ)を中心とした悪性神経膠腫化学療法の世界の現状

若林俊彦
Neuro-Oncologyの進歩 21(3), 45-50, 2014
… However, its clinical outcomes depend on the O6-methylguanine-DNA methyltransferase (MGMT) status, and MGMT modification is one of the key factors to obtain greater clinical benefits in the future.TMZ and other antitumor drugs, especially anti VEGF antibody (Avascin®) and/or BCNU wafer (Gliadel®) combination therapy have been aggressively tried for the treatment of gliomas. …
NAID 130005002163

グリオーマに対する化学療法:—最新のエビデンスを中心に—

佐々木光
脳神経外科ジャーナル 23(7), 547-558, 2014
… BCNU徐放剤とベバシズマブ (BEV) について, これまでの知見と薬剤の特徴について概説し, また退形成性乏突起膠腫と高齢者膠芽腫における最新のエビデンスを紹介する. … BCNU徐放剤の留置により, 再発ならびに初発悪性神経膠腫患者の生存期間が延長した. … BCNU徐放剤やBEVを有効活用するうえでは, 治療効果や副作用を含め各薬剤の特徴を十分に理解することが重要である. …
NAID 130004842124

Related Pictures

★リンクテーブル★

リンク元	「カルムスチン」「carmustine」
関連記事	「BC」

「カルムスチン」

Carmustine
	IUPAC name 1,3-Bis(2-chloroethyl)-1-nitrosourea
	Other names N,N’-Bis(2-chloroethyl)-N-nitroso-urea[citation needed]
Identifiers
CAS number	154-93-8
PubChem	2578
ChemSpider	2480
UNII	U68WG3173Y
EC number	205-838-2
UN number	2811
DrugBank	DB00262
KEGG	D00254
MeSH	Carmustine
ChEBI	CHEBI:3423
ChEMBL	CHEMBL513
RTECS number	YS2625000
ATC code	L01AD01
Jmol-3D images	Image 1; Image 2
	SMILES ClCC[nH]:c(:[o]):n(CCCl):n:[o] ClCCNC(=O)N(CCCl)N=O ;
	InChI InChI=1S/C5H9Cl2N3O2/c6-1-3-8-5(11)10(9-12)4-2-7/h1-4H2,(H,8,11) ; Key: DLGOEMSEDOSKAD-UHFFFAOYSA-N ;
Properties
Molecular formula	C5H9Cl2N3O2
Molar mass	214.05 g mol−1
Appearance	Orange crystals
Odor	Odourless
Melting point	30 °C, 303 K, 86 °F
log P	1.375
Acidity (pKa)	10.194
Basicity (pKb)	3.803
Pharmacology
Bioavailability	5–28%
Routes of; administration	Intravenous; Intralesional;
Metabolism	Hepatic
Elimination; half-life	15–30 min
Protein binding	80%
Excretion	Renal; Respiratory;
Legal status	; ℞ Prescription only
Pregnancy; category	D(US)
Hazards
GHS pictograms
GHS signal word	DANGER
GHS hazard statements	H300, H350, H360
GHS precautionary statements	P301+310, P308+313
EU classification	T+
R-phrases	R45, R46, R60, R61, R28
S-phrases	S22, S36/37/39, S45
LD50	20 mg kg−1 (oral, rat)
Related compounds
Related ureas	Dimethylurea
Related compounds	Noxytiolin; 1,1,3,3-Tetramethylguanidine; Metformin; Allantoic acid; Buformin;
	(verify) (what is: /?); Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
	Infobox references