| 词条 | Forodesine |
| 释义 |
| INN = | type = | IUPAC_name = 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-1,5-dihydropyrrolo[2,3-e]pyrimidin-4-one | image = Immucillin H.svg | width = | alt = | image2 = | width2 = | alt2 = | imageL = | widthL = | altL = | imageR = | widthR = | altR = | caption = | pronounce = | tradename = Mundesine and Fodosine | Drugs.com = | MedlinePlus = | licence_CA = | licence_EU = | DailyMedID = | licence_US = | pregnancy_AU = | pregnancy_AU_comment = | pregnancy_US = | pregnancy_US_comment = | pregnancy_category= | dependency_liability = | addiction_liability = | routes_of_administration = oral | legal_AU = | legal_AU_comment = | legal_BR = | legal_BR_comment = | legal_CA = | legal_CA_comment = | legal_DE = | legal_DE_comment = | legal_NZ = | legal_NZ_comment = | legal_UK = | legal_UK_comment = | legal_US = | legal_US_comment = | legal_UN = | legal_UN_comment = | legal_status = | bioavailability = | protein_bound = | metabolism = | metabolites = | onset = | elimination_half-life = | duration_of_action = | excretion = | CAS_number = 209799-67-7 | CAS_supplemental = | class = | ATCvet = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 444499 | PubChemSubstance = | IUPHAR_ligand = | DrugBank = | ChemSpiderID = 392417 | UNII = 426X066ELK | KEGG = D06596 | ChEBI = | ChEMBL = 218291 | NIAID_ChemDB = | synonyms = | chemical_formula = | C=11 | H=14 | Ag= | Al= | As= | Au= | B= | Bi= | Br= | Ca= | Cl= | Co= | F= | Fe= | Gd= | I= | K= | Li= | Mg= | Mn= | N=4 | Na= | O=4 | P= | Pt= | S= | Sb= | Se= | Sr= | Tc= | Zn= | charge= | molecular_weight = | SMILES = C1=C(C2=C(N1)C(=O)NC=N2)[C@H]3[C@@H]([C@@H]([C@H](N3)CO)O)O | Jmol = | StdInChI = 1S/C11H14N4O4/c16-2-5-9(17)10(18)7(15-5)4-1-12-8-6(4)13-3-14-11(8)19/h1,3,5,7,9-10,12,15-18H,2H2,(H,13,14,19)/t5-,7+,9-,10+/m1/s1 | StdInChI2 = 1/C11H14N4O4/c16-2-5-9(17)10(18)7(15-5)4-1-12-8-6(4)13-3-14-11(8)19/h1,3,5,7,9-10,12,15-18H,2H2,(H,13,14,19)/t5-,7+,9-,10+/m1/s1 | StdInChIKey = IWKXDMQDITUYRK-KUBHLMPHBW | density = | density_notes = | melting_point = | melting_high = | melting_notes = | boiling_point = | boiling_notes = | solubility = | sol_units = | specific_rotation = }} Forodesine (INN; also known as Immucillin H; trade names Mundesine and Fodosine) is a transition-state analog inhibitor of purine nucleoside phosphorylase[1] studied for the treatment of patients with T-cell acute lymphoblastic leukemia (T-ALL) and for treatment of B-cell acute lymphocytic leukemia (B-ALL). Forodesine was originally discovered by Vern Schramm's laboratory at the Albert Einstein College of Medicine in New York and Industrial Research Limited in New Zealand. Forodesine is being developed by BioCryst Pharmaceuticals. {{As of|2008}}, it is currently in phase II clinical trials.[2]{{update inline|date=March 2015}}. In 2006, BioCryst entered into a licensing agreement with Mundipharma International Holdings Limited to develop and commercialize forodesine in markets across Europe, Asia, and Australasia for use in oncology.[3] In April 2017, forodesine was approved in Japan for the treatment of relapsed/refractory peripheral T-cell lymphoma.[4] References1. ^{{cite journal |vauthors=Kicska GA, Long L, Hörig H |title=Immucillin H, a powerful transition-state analog inhibitor of purine nucleoside phosphorylase, selectively inhibits human T lymphocytes |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=98 |issue=8 |pages=4593–8 |date=April 2001 |pmid=11287638 |pmc=31879 |doi=10.1073/pnas.071050798 |url=|display-authors=etal|bibcode=2001PNAS...98.4593K }} 2. ^{{cite web |url=http://www.clinicaltrials.gov/ct2/results?term=Forodesine&flds=Xabce |title=Complete list of clinical trials for forodesine (BCX-1777) (ClinicalTrials.gov) |format= |work= |accessdate=2008-07-22}} 3. ^{{Cite press release | url = http://investor.shareholder.com/biocryst/releasedetail.cfm?releaseid=225663 | title = Biocryst Initiates Pivotal Fodosine Phase IIb Clinical Trial In Patients With Relapsed/Refractory T-Lymphoblastic Leukemia/Lymphoma | date = January 16, 2007}} 4. ^{{Cite press release | url = http://investor.shareholder.com/biocryst/releasedetail.cfm?ReleaseID=1019740| title = BioCryst Announces Mundipharma Receives Approval for Mundesine® in Japan| date = April 3, 2017}} See also
External links
2 : Experimental cancer drugs|Pyrimidones |
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