“Momelotinib”的意思、由来-开放百科全书

As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions.^[3]

As of 2016, momelotinib is being investigated for primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis (post-PV/ET MF),^[4] as well as a treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin).^[5]

Discovery

The drug was originally discovered by Australian drug discovery company Cytopia, then developed by YM BioSciences Inc. (since acquired by Gilead Sciences as of 2013).

References

1. ^{{cite web|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 107|url=http://www.prescrire.org/Docu/DOCSDCI/WHO_INN_ProposedList107.pdf|publisher=World Health Organization|accessdate=16 July 2016|page=189}}
2. ^{{cite journal | last1 = Pardanani | first1 = A | last2 = Lasho | first2 = T | last3 = Smith | first3 = G | last4 = Burns | first4 = CJ | last5 = Fantino | first5 = E | last6 = Tefferi | first6 = A | title = CYT387, a Selective JAK1/JAK2 Inhibitor: in vitro Assessment of Kinase Selectivity and Preclinical Studies Using Cell Lines and Primary Cells from Polycythemia vera Patients | journal = Leukemia | date = August 2009 | volume = 23 | issue = 8 | pages = 1441–5 | doi = 10.1038/leu.2009.50 | pmid = 19295546 | url = http://www.nature.com/leu/journal/v23/n8/pdf/leu200950a.pdf | accessdate = 16 July 2016}}
3. ^{{cite journal | last1 = Pardanani | first1 = A | last2 = Vannucchi | first2 = AM | last3 = Passamonti | first3 = F | last4 = Cervantes | first4 = F | last5 = Barbui | first5 = T | last6 = Tefferi | first6 = A | title = JAK Inhibitor Therapy for Myelofibrosis: Critical Assessment of Value and Limitations | journal = Leukemia | date = February 2011 | volume = 25 | issue = 2 | pages = 218–25 | doi = 10.1038/leu.2010.269 | pmid = 21079613 | url = http://www.nature.com/leu/journal/v25/n2/pdf/leu2010269a.pdf | accessdate = 16 July 2016}}
4. ^{{cite web | title = Momelotinib in Transfusion-Dependent Adults with Primary Myelofibrosis (PMF) or Post-polycythemia Vera or Post-essential Thrombocythemia Myelofibrosis (Post-PV/ET MF) | url = https://clinicaltrials.gov/ct2/show/NCT02515630?term=momelotinib&rank=7 | publisher = ClinicalTrials.gov | accessdate = 16 July 2016}}
5. ^{{cite web | title = Momelotinib Combined with Capecitabine and Oxaliplatin in Adults with Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma | url = https://clinicaltrials.gov/ct2/show/NCT02244489?term=momelotinib&rank=8 | publisher = ClinicalTrials.gov | accessdate = 16 July 2016}}

词条	Momelotinib
释义	Discovery References External links {{Chembox \| ImageFile = Momelotinib.svg \| ImageSize = 255 \| IUPACName = N-(cyanomethyl)-4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzamide \| OtherNames = CYT-387, CYT-11387, GS-0387 \| Section1 = {{Chembox Identifiers \| IUPHAR_ligand = 7791 \| CASNo = 1056634-68-4 \| UNII_Ref = {{fdacite\|correct\|FDA}} \| UNII = 6O01GMS00P \| PubChem = 25062766 \| KEGG = D10315 \| ChemSpiderID = 24676202 \| SMILES = c1cc(ccc1c2ccnc(n2)Nc3ccc(cc3)N4CCOCC4)C(=O)NCC#N \| StdInChI = 1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28) \| StdInChIKey = ZVHNDZWQTBEVRY-UHFFFAOYSA-N \| Section2 = {{Chembox Properties \| C = 23 \| H = 22 \| N = 6 \| O = 2 \| Appearance = \| Density = \| MeltingPt = \| BoilingPt = \| Solubility = \| Section3 = {{Chembox Hazards \| MainHazards = \| FlashPt = \| AutoignitionPt = }}Momelotinib (INN,^[1] formerly GS-0387, CYT-387) is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC₅₀ values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC₅₀ = 0.16 μM).^[2] As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions.^[3] As of 2016, momelotinib is being investigated for primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis (post-PV/ET MF),^[4] as well as a treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin).^[5] Discovery The drug was originally discovered by Australian drug discovery company Cytopia, then developed by YM BioSciences Inc. (since acquired by Gilead Sciences as of 2013). References 1. ^{{cite web\|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed International Nonproprietary Names: List 107\|url=http://www.prescrire.org/Docu/DOCSDCI/WHO_INN_ProposedList107.pdf\|publisher=World Health Organization\|accessdate=16 July 2016\|page=189}} 2. ^{{cite journal \| last1 = Pardanani \| first1 = A \| last2 = Lasho \| first2 = T \| last3 = Smith \| first3 = G \| last4 = Burns \| first4 = CJ \| last5 = Fantino \| first5 = E \| last6 = Tefferi \| first6 = A \| title = CYT387, a Selective JAK1/JAK2 Inhibitor: in vitro Assessment of Kinase Selectivity and Preclinical Studies Using Cell Lines and Primary Cells from Polycythemia vera Patients \| journal = Leukemia \| date = August 2009 \| volume = 23 \| issue = 8 \| pages = 1441–5 \| doi = 10.1038/leu.2009.50 \| pmid = 19295546 \| url = http://www.nature.com/leu/journal/v23/n8/pdf/leu200950a.pdf \| accessdate = 16 July 2016}} 3. ^{{cite journal \| last1 = Pardanani \| first1 = A \| last2 = Vannucchi \| first2 = AM \| last3 = Passamonti \| first3 = F \| last4 = Cervantes \| first4 = F \| last5 = Barbui \| first5 = T \| last6 = Tefferi \| first6 = A \| title = JAK Inhibitor Therapy for Myelofibrosis: Critical Assessment of Value and Limitations \| journal = Leukemia \| date = February 2011 \| volume = 25 \| issue = 2 \| pages = 218–25 \| doi = 10.1038/leu.2010.269 \| pmid = 21079613 \| url = http://www.nature.com/leu/journal/v25/n2/pdf/leu2010269a.pdf \| accessdate = 16 July 2016}} 4. ^{{cite web \| title = Momelotinib in Transfusion-Dependent Adults with Primary Myelofibrosis (PMF) or Post-polycythemia Vera or Post-essential Thrombocythemia Myelofibrosis (Post-PV/ET MF) \| url = https://clinicaltrials.gov/ct2/show/NCT02515630?term=momelotinib&rank=7 \| publisher = ClinicalTrials.gov \| accessdate = 16 July 2016}} 5. ^{{cite web \| title = Momelotinib Combined with Capecitabine and Oxaliplatin in Adults with Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma \| url = https://clinicaltrials.gov/ct2/show/NCT02244489?term=momelotinib&rank=8 \| publisher = ClinicalTrials.gov \| accessdate = 16 July 2016}} External links [https://web.archive.org/web/20100506060243/http://www.ymbiosciences.com/patients/cyt387.php www.ymbiosciences.com] {{Extracellular chemotherapeutic agents}}{{Cytokine receptor modulators}}{{antineoplastic-drug-stub}} 7 : Benzamides\|Morpholines\|Nitriles\|Non-receptor_tyrosine_kinase_inhibitors\|Protein_kinase_inhibitors\|Pyrimidines\|Experimental cancer drugs
随便看	Cry, the Beloved Country Cry to Heaven Crytotis parva Cry Wolf (2005 film) Crângași Crângași metro station Crèche Crème anglaise Crème Brulée Crème Brûlée Crème caramel Crème de cacao Crème de cassis Crème de menthe Crème de Noyaux Crème de violette Crème fraîche Crème liqueur Crèvecoeur Crèvecoeur en Auge Crèvecœur-en-Auge Crécy Crécy-en-Ponthieu Crédit Agricole Crédit Agricole Corporate and Investment Bank

Discovery

References

External links