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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/03/25 17:22:36」(JST)
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Pentostatin
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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
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Clinical data |
Trade names |
Nipent |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a692004 |
Pregnancy
category |
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Routes of
administration |
Intravenous |
Legal status |
Legal status |
- CA: ℞-only
- UK: POM (Prescription only)
- US: ℞-only
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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 Y |
ATC code |
L01XX08 (WHO) |
PubChem |
CID 439693 |
IUPHAR/BPS |
4805 |
DrugBank |
DB00552 Y |
ChemSpider |
388759 Y |
UNII |
395575MZO7 Y |
KEGG |
D00155 Y |
ChEMBL |
CHEMBL1580 Y |
Chemical data |
Formula |
C11H16N4O4 |
Molar mass |
268.269 g/mol |
SMILES
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n1c3c(n(c1)[C@@H]2O[C@@H]([C@@H](O)C2)CO)N\C=N/C[C@H]3O
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InChI
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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 Y
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Key:FPVKHBSQESCIEP-JQCXWYLXSA-N Y
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(verify) |
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.
UpToDate Contents
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English Journal
- High-Dose Sirolimus and Immune-Selective Pentostatin plus Cyclophosphamide Conditioning Yields Stable Mixed Chimerism and Insufficient Graft-versus-Tumor Responses.
- Mossoba ME1, Halverson DC1, Kurlander R2, Schuver BB1, Carpenter A1, Hansen B1, Steinberg SM3, Ali SA1, Tageja N1, Hakim FT1, Gea-Banacloche J1, Sportes C4, Hardy NM5, Hickstein DD1, Pavletic SZ1, Khuu H6, Sabatini M6, Stroncek D6, Levine BL7, June CH7, Mariotti J8, Rixe O9, Fojo AT10, Bishop MR11, Gress RE1, Fowler DH12.
- Clinical cancer research : an official journal of the American Association for Cancer Research.Clin Cancer Res.2015 Oct 1;21(19):4312-20. doi: 10.1158/1078-0432.CCR-15-0340. Epub 2015 Jun 12.
- PURPOSE: We hypothesized that lymphoid-selective host conditioning and subsequent adoptive transfer of sirolimus-resistant allogeneic T cells (T-Rapa), when combined with high-dose sirolimus drug therapy in vivo, would safely achieve antitumor effects while avoiding GVHD.EXPERIMENTAL DESIGN: Patient
- PMID 26071480
- An unusual indication for splenectomy in hairy cell leukaemia: a report of three cases with persistent splenomegaly after chemoimmunotherapy.
- Sarid N1, Ahmad HN2, Wotherspoon A3, Dearden CE3, Else M4, Catovsky D4.
- British journal of haematology.Br J Haematol.2015 Sep 25. doi: 10.1111/bjh.13767. [Epub ahead of print]
- We describe three cases of relapsed hairy cell leukaemia (HCL) treated with pentostatin plus rituximab. All three achieved bone marrow complete remission but had persistent splenomegaly and hypersplenism. Because of the clinical uncertainty of its significance, they were all splenectomized. The sple
- PMID 26403440
- Potential breakthroughs with investigational drugs for hairy cell leukemia.
- Robak T1, Wolska A, Robak P.
- Expert opinion on investigational drugs.Expert Opin Investig Drugs.2015 Sep 2:1-13. [Epub ahead of print]
- INTRODUCTION: Hairy cell leukemia (HCL) is a rare subtype of B-cell chronic lymphoid leukemia. It is characterized by progressive pancytopenia, splenomegaly and infiltrations of the bone marrow, liver and spleen. Over the last few years, several new immunological drugs, particularly immunotoxins, BR
- PMID 26329588
Related Links
- NIPENT , Vial U.S. Physician Prescribing Information See related articles SEARCH PRODUCTS Submit Need help paying for Pfizer medicines? Patient Assistance Programs Pfizer RxPathways ® may be able to help. Pfizer ...
- Nipent Description Nipent (pentostatin for injection) is supplied as a sterile, apyrogenic, lyophilized powder in single-dose vials for intravenous administration. Each vial contains 10 mg of pentostatin and 50 mg of ...
- Nipent can cause harmful side effects on your kidneys, liver, lungs, or central nervous system. Call your doctor at once if you have symptoms such as: swelling, rapid weight gain, little or no urinating, pink or red urine, severe shortness of breath, wheezing, chest pain, cough, vision problems, numbness , tingling, or burning pain.
Related Pictures
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- 英
- pentostatin
- 商
- コホリン, Nipent
- 関
- Aspergillus nidulans