Drug Information

General Information
Drug ID
DR00248
Drug Name
Telmisartan
Synonyms
2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid; 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid; 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic acid; 4'-((4-mehtyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimmidazolyl)methyl)-2-biphenylcarboxylic acid; 4'-[(1,4'-dimethyl-2'propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid; 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid; 4'-[(1,7'-dimethyl-2'-propyl-1H,3'H-2,5'-bibenzimidazol-3'-yl)methyl]biphenyl-2-carboxylic acid; Abbott brand of telmisartan; BIBR 277; BIBR 277SE; BIBR-277; BIBR-277-SE; BIBR-277SE; Bay 68-9291; Boehringer Ingelheim brand of telmisartan; Glaxo Wellcome brand of telmisartan; GlaxoSmithKline brand of telmisartan; Kinzal; Kinzalmono; Micardis; Micardis (TN); Micardis, Targit, Temax, BIBR277, Telmisartan; Pritor; Telmisartan (JAN/USAN/INN); Telmisartan [USAN:INN]; YM-086
Drug Type
Small molecular drug
Indication High blood pressure [ICD11:BA00] Approved [1]
Therapeutic Class
Antihypertensive Agents
Structure
3D MOL 2D MOL
Formula
C33H30N4O2
Canonical SMILES
CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C
InChI
InChI=1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
InChIKey
RMMXLENWKUUMAY-UHFFFAOYSA-N
CAS Number
CAS 144701-48-4
Pharmaceutical Properties Molecular Weight 514.6 Topological Polar Surface Area 72.9
Heavy Atom Count 39 Rotatable Bond Count 7
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 4
XLogP
6.9
PubChem CID
65999
PubChem SID
103271997 ,103974749 ,104253350 ,104335216 ,11372057 ,11374980 ,11485867 ,11489792 ,11490904 ,11493075 ,11528632 ,117546129 ,117867825 ,12014783 ,14860450 ,26612858 ,26680963 ,26719833 ,26749005 ,26749006 ,43122721 ,46386620 ,46505370 ,46530547 ,47350860 ,47796474 ,48416595 ,49648460 ,49830991 ,50107502 ,56312042 ,56313977 ,57315885 ,6866718 ,7847693 ,79018553 ,7980737 ,81041072 ,81092854 ,8190092 ,85209733 ,85789678 ,87225392 ,92124871 ,92308092 ,92308546 ,92309313 ,92712346 ,93166523 ,9912
ChEBI ID
ChEBI:9434
TTD Drug ID
D0N6RF
DT(s) Transporting This Drug OATP1A2 Transporter Info Organic anion transporting polypeptide 1A2 Substrate [2]
OATP1B3 Transporter Info Organic anion transporting polypeptide 1B3 Substrate [2]
OATP2B1 Transporter Info Organic anion transporting polypeptide 2B1 Substrate [3]
Drug-Transporter Activity Data
Drug-Transporter Activity Data OATP1B3 Transporter Info Km =0.81 microM Human embryonic kidney cells (HEK293)-OATP1B3 [2]
OATP1B3 Transporter Info Km =3.4 microM Human embryonic kidney cells (HEK293)-OATP1B3 [3]
OATP2B1 Transporter Info Km =1.09 microM Human embryonic kidney cells (HEK293)-OATP2B1 [3]
References
1 Telmisartan was approved by FDA. The official website of the U.S. Food and Drug Administration. (2019)
2 Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos. 2006 Jul;34(7):1109-15.
3 Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. Drug Metab Dispos. 2008 Apr;36(4):796-805.

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