Vinorelbin
(Preusmjereno sa stranice Navelbine)
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| Klinički podaci | |||
|---|---|---|---|
| Robne marke | Navelbine, Navelbine Base | ||
| AHFS/Drugs.com | Monografija | ||
| Identifikatori | |||
| CAS broj | 71486-22-1 | ||
| ATC kod | L01CA04 | ||
| PubChem[1][2] | 5311497 | ||
| DrugBank | DB00361 | ||
| ChemSpider[3] | 4470974 | ||
| ChEBI | CHEBI:480999 
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| ChEMBL[4] | CHEMBL607994
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| Hemijski podaci | |||
| Formula | C45H54N4O8 | ||
| Mol. masa | 778,932 | ||
| SMILES | eMolekuli & PubHem | ||
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| Farmakokinetički podaci | |||
| Poluvreme eliminacije | 27,7-43,6 h | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
| Način primene | Intravenozno | ||
Vinorelbin (prodajno ime Navelbin) je antimitotički hemoterapijski lek, koji se koristi kao tretman za pojedine tipove kancera, uključujući rak dojke i makrocelularni karcinom pluća.
U kliničkoj praksi se ponekad koristi skraćenica "NVB" za vinorelbin, mada ona nije jedinstveni identifikator.
Vinorelbin je organsko jedinjenje, koje sadrži 45 atoma ugljenika i ima molekulsku masu od 778,932 Da.[5][6][7]
Farmakologija[uredi | uredi kod]
Antitumorno dejstvo se ostvaruje inhibicijom mitoze putem interakcije sa tubulinom.[8] Vinorelbin je bio prvi 5´NOR polusintetički vinka alkaloid. On se dobija polusintetičkim putem iz alkaloida ekstrahovanih iz biljke Catharanthus roseus. U prodaji pod nazivom Navelbin.
Osobine[uredi | uredi kod]
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 11 |
| Broj donora vodonika | 2 |
| Broj rotacionih veza | 10 |
| Particioni koeficijent[9] (ALogP) | 5,4 |
| Rastvorljivost[10] (logS, log(mol/L)) | -7,4 |
| Polarna površina[11] (PSA, Å2) | 133,9 |
Reference[uredi | uredi kod]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.
- ↑ Marty M, Fumoleau P, Adenis A, Rousseau Y, Merrouche Y, Robinet G, Senac I, Puozzo C: Oral vinorelbine pharmacokinetics and absolute bioavailability study in patients with solid tumors. Ann Oncol. 2001 Nov;12(11):1643-9. PMID 11822766
- ↑ Knox C, Law V, Jewison T, Liu P, Ly S, Frolkis A, Pon A, Banco K, Mak C, Neveu V, Djoumbou Y, Eisner R, Guo AC, Wishart DS (2011). „DrugBank 3.0: a comprehensive resource for omics research on drugs”. Nucleic Acids Res. 39 (Database issue): D1035-41. DOI:10.1093/nar/gkq1126. PMC 3013709. PMID 21059682.
- ↑ David S. Wishart, Craig Knox, An Chi Guo, Dean Cheng, Savita Shrivastava, Dan Tzur, Bijaya Gautam, and Murtaza Hassanali (2008). „DrugBank: a knowledgebase for drugs, drug actions and drug targets”. Nucleic Acids Res 36 (Database issue): D901-6. DOI:10.1093/nar/gkm958. PMC 2238889. PMID 18048412.
- ↑ Jordan, M.A.; Wilson, L. (2004). „Microtubules as a target for anticancer drugs.”. Nature Reviews. Cancer 4 (4): 253–65. DOI:10.1038/nrc1317. PMID 15057285.
- ↑ Ghose, A.K., Viswanadhan V.N., and Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A 102: 3762-3772. DOI:10.1021/jp980230o.
- ↑ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE. (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488-1493. DOI:10.1021/ci000392t. PMID 11749573.
- ↑ Ertl P., Rohde B., Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714-3717. DOI:10.1021/jm000942e. PMID 11020286.
Literatura[uredi | uredi kod]
- Hardman JG, Limbird LE, Gilman AG. (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10 izd.). New York: McGraw-Hill. DOI:10.1036/0071422803. ISBN 0-07-135469-7.
- Thomas L. Lemke, David A. Williams, ur. (2007). Foye's Principles of Medicinal Chemistry (6 izd.). Baltimore: Lippincott Willams & Wilkins. ISBN 0-7817-6879-9.
