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Pentostatin (or deoxycoformycin, trade name Nipent, manufactured by SuperGen) is an anticancer chemotherapeutic drug.^[1]

Mechanism

It is classified as a purine analog, which is a type of antimetabolite.

It mimics the nucleoside adenosine and thus inhibits the enzyme adenosine deaminase, interfering with the cell's ability to process DNA.^[2]

Cancer cells generally divide more often than healthy cells; DNA is highly involved in cell division (mitosis) and drugs which target DNA-related processes are therefore more toxic to cancer cells than healthy cells.

Uses

Pentostatin is used to treat hairy cell leukemia.^[3] It is given by intravenous infusion once every two weeks for three to six months.

Additionally, pentostatin has been used to treat steroid-refractory acute and chronic graft-versus-host disease.^[4]

Pentostatin is also used in chronic lymphocytic leukemia (CLL) patients who have relapsed.

References

^ Kay NE, Geyer SM, Call TG, et al. (January 2007). "Combination chemoimmunotherapy with pentostatin, cyclophosphamide, and rituximab shows significant clinical activity with low accompanying toxicity in previously untreated B chronic lymphocytic leukemia". Blood 109 (2): 405–11. doi:10.1182/blood-2006-07-033274. PMC: 1785105. PMID 17008537.
^ Sauter C, Lamanna N, Weiss MA (September 2008). "Pentostatin in chronic lymphocytic leukemia". Expert Opin Drug Metab Toxicol 4 (9): 1217–22. doi:10.1517/17425255.4.9.1217. PMID 18721115.
^ Cannon T, Mobarek D, Wegge J, Tabbara IA (October 2008). "Hairy cell leukemia: current concepts". Cancer Invest. 26 (8): 860–5. doi:10.1080/07357900801965034. PMID 18798068.
^ Bolaños-Meade J, Jacobsohn DA, Margolis J, Ogden A, Wientjes MG, Byrd JC, Lucas DM, Anders V, Phelps M, Grever MR, Vogelsang GB (April 2005). "Pentostatin in steroid-refractory acute graft-versus-host disease". J Clin Onc 23 (12): 2661–8. doi:10.1200/JCO.2005.06.130. PMID 15837980.

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UpToDate Contents

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1. 有毛細胞白血病の治療 treatment of hairy cell leukemia
2. T細胞性前リンパ性白血病の治療 treatment of t cell prolymphocytic leukemia
3. 急性移植片対宿主病の治療 treatment of acute graft versus host disease
4. 化学療法関連腎毒性および腎不全患者における用量調整 chemotherapy related nephrotoxicity and dose modification in patients with renal insufficiency
5. 症候性または進行した慢性リンパ性白血病に対する初期治療の選択 selection of initial therapy for symptomatic or advanced chronic lymphocytic leukemia

English Journal

A randomized phase II trial comparing chemoimmunotherapy with or without bevacizumab in previously untreated patients with chronic lymphocytic leukemia.

Kay NE1, Strati P1, LaPlant BR1, Leis JF2, Nikcevich D3, Call TG1, Pettinger AM1, Lesnick CE1, Hanson CA1, Shanafelt TD1.
Oncotarget.Oncotarget.2016 Nov 16. doi: 10.18632/oncotarget.13412. [Epub ahead of print]
Bevacizumab is a monoclonal antibody targeting vascular endothelial growth factor (VEGF) with in vitro pro-apoptotic and antiangiogenic effects on chronic lymphocytic leukemia (CLL) cells. As monotherapy in patients with CLL, it has no clinical activity. Here we report the results of an open-label,
PMID 27861157

Cross-resistance and synergy with bendamustine in chronic lymphocytic leukemia.

Kost SE1, Bouchard ED2, LaBossière É1, Ye X3, Queau ML1, Liang WS4, Banerji V2, Gibson SB2, Katyal S2, Johnston JB5.
Leukemia research.Leuk Res.2016 Nov;50:63-71. doi: 10.1016/j.leukres.2016.09.016. Epub 2016 Sep 20.
Bendamustine (BEN) has structural similarities to an alkylating agent and a nucleoside analog, and effective against tumor cells that are resistant to standard therapy. In this study we compared the activities of BEN against that of the alkylating agent, chlorambucil (CLB), and the nucleoside analog
PMID 27683974

Ofatumumab monotherapy as a consolidation strategy in patients with previously untreated chronic lymphocytic leukaemia: a phase 2 trial.

Strati P1, Lanasa M2, Call TG1, Leis JF3, Brander DM2, LaPlant BR1, Pettinger AM1, Ding W1, Parikh SA1, Hanson CA1, Chanan-Khan AA4, Bowen DA1, Conte M1, Kay NE1, Shanafelt TD5.
The Lancet. Haematology.Lancet Haematol.2016 Sep;3(9):e407-14. doi: 10.1016/S2352-3026(16)30064-3. Epub 2016 Aug 1.
BACKGROUND: Although several consolidation strategies to prolong treatment-free survival (TFS) in chronic lymphocytic leukaemia have been investigated, most have proven either ineffective or toxic. Ofatumumab is a human type I anti-CD20 antibody approved by the US Food and Drug Administration as mai
PMID 27570087

Japanese Journal

治療抵抗性のT細胞性前リンパ球性白血病に対する同種骨髄移植例

臨床血液 = The Japanese Journal of Clinical Hematology 46(7), 527-531, 2005-07-30
NAID 10016601622

炎症歯周組織における内因性アデノシンの抗炎症作用の解析 : 歯肉線維芽細胞におけるアデノシンレセプター活性化の制御機構

炎症・再生 : 日本炎症・再生医学会雑誌 = Inflammation and regeneration 25(3), 181-185, 2005-05-25
NAID 10026499072

Deoxycoformycin-Containing Combination Chemotherapy for Adult T-Cell Leukemia-Lymphoma : Japan Clinical Oncology Group Study (JCOG9109)

International journal of hematology 77(2), 164-170, 2003-02-01
NAID 50000755649

Related Pictures

Growth curves for B16-BL6 and LLC cells in the presence of adenosine | Download 치료적 맞춤운동 연구소 :: adenosine A(1) receptor와 관련된 침의 진통 (PDF) Preclinical Assessment of the Treatment of Second-Stage African Trypanosomiasis Clinico-pathological profile of Hairy cell leukemia: Critical insights gained at a Newer Purine Analogues for the Treatment of Hairy-Cell Leukemia | NEJM Systemic Diseases and Conjunctivitis | Ento Key

★リンクテーブル★

拡張検索	「2'-deoxycoformycin」「2-deoxycoformycin」

「2'-deoxycoformycin」

Pentostatin
Systematic (IUPAC) name
	(R)-3-((2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol
Clinical data
Trade names	Nipent
AHFS/Drugs.com	monograph
MedlinePlus	a692004
Pregnancy; category	US: D (Evidence of risk); ;
Routes of; administration	Intravenous
Legal status
Legal status	CA: ℞-only; UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Bioavailability	n/a
Protein binding	4%
Metabolism	Hepatic, minor
Biological half-life	2.6 to 16 hours, mean 5.7 hours
Identifiers
CAS Number	53910-25-1
ATC code	L01XX08 (WHO)
PubChem	CID 439693
IUPHAR/BPS	4805
DrugBank	DB00552
ChemSpider	388759
UNII	395575MZO7
KEGG	D00155
ChEMBL	CHEMBL1580
Chemical data
Formula	C11H16N4O4
Molar mass	268.269 g/mol
	SMILES n1c3c(n(c1)[C@@H]2O[C@@H]([C@@H](O)C2)CO)N\C=N/C[C@H]3O ;
	InChI InChI=1S/C11H16N4O4/c16-3-8-6(17)1-9(19-8)15-5-14-10-7(18)2-12-4-13-11(10)15/h4-9,16-18H,1-3H2,(H,12,13)/t6-,7+,8+,9+/m0/s1 ; Key:FPVKHBSQESCIEP-JQCXWYLXSA-N ;
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　　[★] 2'-デオキシコホルマイシン

「2-deoxycoformycin」

　　[★]

同: dCF
関: pentostatin

[pmid17008537-1] Kay NE, Geyer SM, Call TG, et al. (January 2007). "Combination chemoimmunotherapy with pentostatin, cyclophosphamide, and rituximab shows significant clinical activity with low accompanying toxicity in previously untreated B chronic lymphocytic leukemia". Blood 109 (2): 405–11. doi:10.1182/blood-2006-07-033274. PMC: 1785105. PMID 17008537.

[pmid18721115-2] Sauter C, Lamanna N, Weiss MA (September 2008). "Pentostatin in chronic lymphocytic leukemia". Expert Opin Drug Metab Toxicol 4 (9): 1217–22. doi:10.1517/17425255.4.9.1217. PMID 18721115.

[pmid18798068-3] Cannon T, Mobarek D, Wegge J, Tabbara IA (October 2008). "Hairy cell leukemia: current concepts". Cancer Invest. 26 (8): 860–5. doi:10.1080/07357900801965034. PMID 18798068.

[PMID15837980-4] Bolaños-Meade J, Jacobsohn DA, Margolis J, Ogden A, Wientjes MG, Byrd JC, Lucas DM, Anders V, Phelps M, Grever MR, Vogelsang GB (April 2005). "Pentostatin in steroid-refractory acute graft-versus-host disease". J Clin Onc 23 (12): 2661–8. doi:10.1200/JCO.2005.06.130. PMID 15837980.

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案内

deoxycoformycin