Azilsartan

Azilsartan medoxomil
(IUPAC) ime
	(5-metil-2-okso-1,3-dioksol-4-il)metil 2-etoksi-1-([2'-(5-okso-4,5-dihidro-1,2,4-oksadiazol-3-il)bifenil-4-il]metil)-1H-benzimidazol-7-karboksilat
Klinički podaci
Robne marke	Edarbi
AHFS/Drugs.com	Potrošačka informacije o leku
MedlinePlus	a611028
Identifikatori
CAS broj	147403-03-0
ATC kod	C09CA09
PubChem	9825285
ChemSpider	9413866
UNII	F9NUX55P23
ChEBI	CHEBI:68845
Hemijski podaci
Formula	C25H20N4O5
Mol. masa	456,46 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C30H24N4O8/c1-3-38-28-31-23-10-6-9-22(27(35)39-16-24-17(2)40-30(37)41-24)25(23)34(28)15-18-11-13-19(14-12-18)20-7-4-5-8-21(20)26-32-29(36)42-33-26/h4-14H,3,15-16H2,1-2H3,(H,32,33,36) ; Key: QJFSABGVXDWMIW-UHFFFAOYSA-N
Farmakoinformacioni podaci
Licenca	US FDA:link
Trudnoća	?
Pravni status	℞-only (SAD)
Način primene	Oralno

Azilsartan je antagonist angiotenzinskog II receptora koji se koristi za tretman hipertenzije. Ovaj lek je razvilo preduzeće Takeda.

On je u prodaji pod imenom Edarbi kao prolek azilsartan medoksomil (TAK-491). FDA je 25. februara 2011. odobrila azilsartan medoksomil za tretman visokog krvnog pritiska kod odraslih osoba.^[4] Sledeće godine je odobren u Kanadi za lečenje blage do umerene hipertenzije.^[5]

Osobine

Osobina	Vrednost
Broj akceptora vodonika	10
Broj donora vodonika	1
Broj rotacionih veza	10
Particioni koeficijent^[6] (ALogP)	5,3
Rastvorljivost^[7] (logS, log(mol/L))	-7,5
Polarna površina^[8] (PSA, Å²)	139,6

Reference

↑ 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. edit
↑ 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. edit
↑ "FDA approves Edarbi to treat high blood pressure" (Press release). U.S. Food and Drug Administration (FDA). 2011-02-23. Retrieved 2011-02-01.
↑ Notice of Decision for EDARBI
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] 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. edit

[2] 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.

[3] 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. edit

[4] "FDA approves Edarbi to treat high blood pressure" (Press release). U.S. Food and Drug Administration (FDA). 2011-02-23. Retrieved 2011-02-01.

[5] Notice of Decision for EDARBI

[6] 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.

[7] 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.

[8] 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.

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