Karboplatin
(Preusmjereno sa stranice Carboplatin)
Karboplatin, ili cis-Diamin(1,1-ciklobutandikarboksilato)platina(II) (prodajna imena Paraplatin i Paraplatin-AQ) je hemoterapijski lek koji se koristi protiv pojedinih formi kancera (uglavnom karcinoma jajnika, pluća, glave i vrata kao i endometrijuma, jednjaka, bešike, dojki; tumora centralnog nervnog sistema; osteogenog sarkoma, i kao priprema za trasplant matičnih ćelija i koštane srži).[5] Uveden je u upotrebu tokom kasnih 1980-tih i stekao je popularnost u kliničkim tretmanima zbgo znadno umanjenih nuspojava u odnosu na njegovo roditeljsko jedinjenje cisplatin. Cisplatin i karboplatin pripadaju grupi antineoplastičnih agenasa baziranih na platini. Oni formiraju interakcije sa DNK čime ometaju popravku DNK.[6][7][8][9][10]
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| Klinički podaci | |||
|---|---|---|---|
| Robne marke | Paraplatin, Paraplatin-AQ | ||
| AHFS/Drugs.com | Monografija | ||
| Identifikatori | |||
| CAS broj | 41575-94-4 | ||
| ATC kod | L01XA02 | ||
| PubChem[1][2] | 38904 | ||
| DrugBank | DB00958 | ||
| ChemSpider[3] | 436073 | ||
| ChEBI | CHEBI:31355 
| ||
| ChEMBL[4] | CHEMBL288376
| ||
| Hemijski podaci | |||
| Formula | C6H12N2O4Pt | ||
| Mol. masa | 371,254 | ||
| SMILES | eMolekuli & PubHem | ||
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| Farmakokinetički podaci | |||
| Poluvreme eliminacije | 1,1 - 2 h | ||
| Izlučivanje | Renalno | ||
| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
| Način primene | Intravenozno | ||
Karboplatin je organsko jedinjenje, koje sadrži 6 atoma ugljenika i ima molekulsku masu od 371,254 Da.
Osobine uredi
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 6 |
| Broj donora vodonika | 2 |
| Broj rotacionih veza | 0 |
| Particioni koeficijent[11] (ALogP) | 0,1 |
| Rastvorljivost[12] (logS, log(mol/L)) | 1,6 |
| Polarna površina[13] (PSA, Å2) | 122,6 |
Reference uredi
- ↑ 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.
- ↑ Wheate NJ, Walker S, Craig GE, Oun R (September 2010). „The status of platinum anticancer drugs in the clinic and in clinical trials”. Dalton Transactions 39 (35): 8113–27. DOI:10.1039/C0DT00292E. PMID 20593091.
- ↑ Natarajan G, Malathi R, Holler E: Increased DNA-binding activity of cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts: activation theory revisited. Biochem Pharmacol. 1999 Nov 15;58(10):1625-9. PMID 10535754
- ↑ Knox RJ, Friedlos F, Lydall DA, Roberts JJ: Mechanism of cytotoxicity of anticancer platinum drugs: evidence that cis-diamminedichloroplatinum(II) and cis-diammine-(1,1-cyclobutanedicarboxylato)platinum(II) differ only in the kinetics of their interaction with DNA. Cancer Res. 1986 Apr;46(4 Pt 2):1972-9. PMID 3512077
- ↑ Canetta R, Rozencweig M, Carter SK: Carboplatin: the clinical spectrum to date. Cancer Treat Rev. 1985 Sep;12 Suppl A:125-36. PMID 3002623
- ↑ 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.
- ↑ 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
- 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.
