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词条 Pentostatin
释义

  1. Mechanism

  2. Uses

  3. References

{{Drugbox
| Watchedfields = changed
| verifiedrevid = 464198455
| 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
| image = Pentostatin structure.svg
| width = 200
| image2 = Pentostatin ball-and-stick.png
| width2 = 200
| tradename = Nipent
| Drugs.com = {{drugs.com|monograph|pentostatin}}
| MedlinePlus = a692004
| pregnancy_US = D
| legal_CA = Rx-only
| legal_UK = POM
| legal_US = Rx-only
| routes_of_administration = Intravenous
| bioavailability = n/a
| protein_bound = 4%
| metabolism = Hepatic, minor
| elimination_half-life = 2.6 to 16 hours, mean 5.7 hours
| IUPHAR_ligand = 4805
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 53910-25-1
| ATC_prefix = L01
| ATC_suffix = XX08
| PubChem = 439693
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00552
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 388759
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 395575MZO7
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00155
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 1580
| C=11 | H=16 | N=4 | O=4
| molecular_weight = 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
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = FPVKHBSQESCIEP-JQCXWYLXSA-N
}}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

1. ^{{cite journal |vauthors=Kay NE, Geyer SM, Call TG, etal |title=Combination chemoimmunotherapy with pentostatin, cyclophosphamide, and rituximab shows significant clinical activity with low accompanying toxicity in previously untreated B chronic lymphocytic leukemia |journal=Blood |volume=109 |issue=2 |pages=405–11 |date=January 2007 |pmid=17008537 |pmc=1785105 |doi=10.1182/blood-2006-07-033274 |url=http://www.bloodjournal.org/cgi/pmidlookup?view=long&pmid=17008537}}
2. ^{{cite journal |vauthors=Sauter C, Lamanna N, Weiss MA |title=Pentostatin in chronic lymphocytic leukemia |journal=Expert Opin Drug Metab Toxicol |volume=4 |issue=9 |pages=1217–22 |date=September 2008 |pmid=18721115 |doi=10.1517/17425255.4.9.1217 }}
3. ^{{cite journal |vauthors=Cannon T, Mobarek D, Wegge J, Tabbara IA |title=Hairy cell leukemia: current concepts |journal=Cancer Invest. |volume=26 |issue=8 |pages=860–5 |date=October 2008 |pmid=18798068 |doi=10.1080/07357900801965034 }}
4. ^{{cite journal |vauthors=Bolaños-Meade J, Jacobsohn DA, Margolis J, Ogden A, Wientjes MG, Byrd JC, Lucas DM, Anders V, Phelps M, Grever MR, Vogelsang GB |title=Pentostatin in steroid-refractory acute graft-versus-host disease |journal=J Clin Oncol |volume=23 |issue=12 |pages=2661–8 |date=April 2005 |pmid=15837980 |doi=10.1200/JCO.2005.06.130}}
{{Chemotherapeutic agents}}{{antineoplastic-drug-stub}}

3 : Nucleosides|Purine antagonists|Adenosine deaminase inhibitors

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