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Overview of CAS 139481-59-7

Client Email Product
4CH-015556
PharmaCompass
4CH-015556
Also known as: 139481-59-7, Blopress, Ratacand, 1-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylic acid, Cv-11974, Candesartan [ban]
Molecular Formula
C24H20N6O3
Molecular Weight
440.463  g/mol
InChI Key
HTQMVQVXFRQIKW-UHFFFAOYSA-N
FDA UNII
S8Q36MD2XX

Candesartan is an angiotensin-receptor blocker (ARB) that may be used alone or with other agents to treat hypertension. It is available as a prodrug in the form of [Candesartan cilexetil](https://www.drugbank.ca/drugs/DB00796).
Candesartan is an Angiotensin 2 Receptor Blocker. The mechanism of action of candesartan is as an Angiotensin 2 Receptor Antagonist.
1 2D Structure

4CH-015556

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid
2.1.2 InChI
InChI=1S/C24H20N6O3/c1-2-33-24-25-20-9-5-8-19(23(31)32)21(20)30(24)14-15-10-12-16(13-11-15)17-6-3-4-7-18(17)22-26-28-29-27-22/h3-13H,2,14H2,1H3,(H,31,32)(H,26,27,28,29)
2.1.3 InChI Key
HTQMVQVXFRQIKW-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O
2.2 Other Identifiers
2.2.1 UNII
S8Q36MD2XX
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. 139481-59-7

2. Blopress

3. Ratacand

4. 1-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylic Acid

5. Cv-11974

6. Candesartan [ban]

7. Cv 11974

8. [3h]candesartan

9. Unii-s8q36md2xx

10. 2-ethoxy-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic Acid

11. Candesartan (usan/inn)

12. Candesartan [usan:inn]

13. Cv11974

14. Ks-5003

15. Chembl1016

16. 2-ethoxy-1-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylic Acid

17. 2-ethoxy-3-[[4-[2-(1h-tetrazol-5-yl)phenyl]phenyl]methyl]-3h-benzoimidazole-4-carboxylic Acid

18. Chebi:3347

19. C24h20n6o3

20. Ncgc00167474-01

21. Ak-57139

22. Dsstox_cid_2725

23. 2-ethoxy-7-carboxy-1-(2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methylbenzimidazole

24. Dsstox_rid_75453

25. Dsstox_gsid_22725

26. 1h-benzimidazole-7-carboxylic Acid, 2-ethoxy-1-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-

27. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]-1h-benzimidazole-7-carboxylic Acid

28. 2-ethoxy-1-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-1h-benzimidazole-7-carboxylic Acid

29. 2-ethoxy-3-[2'-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic Acid

30. 2-(ethyloxy)-1-{[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl}-1h-benzimidazole-7-carboxylic Acid

31. 2-ethoxy-1-({2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl)-1h-benzimidazole-7-carboxylic Acid

32. 2-ethoxy-3-[[4-[2-(1h-tetrazol-5-yl)phenyl]phenyl] Methyl]-3h-benzoimidazole-4-carboxylic Acid

33. Cas-139481-59-7

34. Sr-05000001447

35. Cilexitil

36. Candesartan [usan:inn:ban]

37. Hsdb 7520

38. 2-ethoxy-3-[[4-[2-(1h-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic Acid

39. 2-ethoxy-3-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-4-benzimidazolecarboxylic Acid

40. Blopress (tn)

41. Ratacand (tn)

42. 2-ethoxy-1-([2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl]methyl)-1h-benzimidazole-7-carboxylic Acid

43. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl]methyl]-1h-benzimidazole-7-carboxylic Acid

44. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-benzimidazole-7-carboxylic Acid

45. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]-1h-benzimidazole-7-carboxylic Acid (candesartan)

46. 2-ethoxy-3-[[4-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic Acid

47. Celexetil

48. Amias (tn)

49. Candesartan (atacand)

50. Candesartan - Atacand

51. Ac1l1dwt

52. Tcv-116 (prodrug)

53. D0a0ql

54. D0d5sq

55. Schembl3938

56. S8q36md2xx

57. Gtpl587

58. Mls003915631

59. Mls004774041

60. Bidd:gt0350

61. Gtpl6907

62. Dtxsid0022725

63. Ctk8e8165

64. Htqmvqvxfrqikw-uhfffaoysa-n

65. Molport-003-845-570

66. Molport-005-943-739

67. Bcpp000302

68. Hms2089m22

69. Hms3651c13

70. Pharmakon1600-01502288

71. Act02607

72. Ebd40593

73. Hy-b0205

74. Ks-000001ux

75. Zinc3782818

76. Tox21_112478

77. Ac-203

78. An-839

79. Bdbm50240609

80. Cc0016

81. Mfcd00864463

82. Nsc759858

83. S1578

84. Akos015888154

85. Akos025117340

86. Tox21_112478_1

87. Ab07470

88. Am84369

89. Api0001828

90. At-3243

91. Bcp9000479

92. Ccg-213059

93. Cs-2146

94. Db13919

95. Nsc-759858

96. Rtr-005177

97. Ncgc00167474-02

98. Ncgc00167474-04

99. Bc205774

100. Br-57139

101. Candesartan ( For Candesartan Cilexetil )

102. Kb-48662

103. Ls-32740

104. Sc-15284

105. Smr002203608

106. Smr003500711

107. Ab0011997

108. Ax8018243

109. St2414902

110. Tl8000897

111. 4ch-015556

112. Bg01730494

113. Candesartan[candesartancilexetilintermediates]

114. Ft-0083585

115. Ft-0602912

116. Atacand, Blopress, Amias, Ratacand,candesartan

117. C07468

118. D00522

119. J10263

120. S-2839

121. Ab01275447-01

122. Ab01275447_02

123. Ab01275447_03

124. 481c597

125. A807545

126. A808309

127. L000156

128. I01-0374

129. J-007281

130. Sr-05000001447-1

131. Sr-05000001447-2

132. Sr-05000001447-5

133. 2-ethoxy-1-[[2'-(1 H-tetrazol-5-yl)biphenyl-4-yl]methyl]-benzimidazole-7-carboxylic Acid

134. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]-benzimidazole-7-carboxylic Acid

135. 2-ethoxy-1-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic Acid

136. 2-ethoxy-1-{[2'-(1h-tetrazol-5-yl)biphenyl-4ethyl]}-1h-benzimidazole-7-carboxylic Acid

137. 2-ethoxy-1-{[2'-(1h-tetrazol-5-yl)biphenyl-4ethyl}-1h-benzimidazole-7-carboxylic Acid

138. 2-ethoxy-3-[2'-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzimidazole-4-carboxylic Acid

139. 1-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylic Ac

140. 1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylic Acid

141. 1-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1h-benzo[d]imidazole-7-carboxylic Acid

142. 2-ethoxy-1-({4-[2-(1h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1h-1,3-benzodiazole-7-carboxylic Acid

143. 2-ethoxy-1-({4-[2-(2h-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1h-1,3-benzodiazole-7-carboxylic Acid

144. 2-ethoxy-1-<<2'-(1h-tetrazol-5-yl)biphenyl-4-yl>methyl>-1h-benzimidazole-7-carboxylic Acid

145. 2-ethoxy-1-<<2'-(1h-tetrazol-5-yl)biphenyl-4-yl>methyl>-1h-benzimidazole-7-carboxylic Acid;

146. 2-ethoxy-1-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-benzimidazole-7-carboxylic Acid

147. 2-ethoxy-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic Acid

148. 2-ethoxy-3-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic Acid(cv-11974)

149. 2-ethoxy-3-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3h-benzoimidazole-4-carboxylic Acid

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 440.463 g/mol
Molecular Formula C24H20N6O3
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count7
Exact Mass440.16 g/mol
Monoisotopic Mass440.16 g/mol
Topological Polar Surface Area119 A^2
Heavy Atom Count33
Formal Charge0
Complexity660
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Therapeutic Uses

Angiotensin II Type 1 Receptor Blockers; Antihypertensive Agents

National Library of Medicine's Medical Subject Headings. Candesartan. Online file (MeSH, 2014). Available from, as of September 2, 2014: http://www.nlm.nih.gov/mesh/2014/mesh_browser/MBrowser.html


Atacand is indicated for the treatment of hypertension in adults and children 1 to < 17 years of age. It may be used alone or in combination with other antihypertensive agents. /Included in US product labeling/

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Atacand is indicated for the treatment of heart failure (NYHA class II-IV) in adults with left ventricular systolic dysfunction (ejection fraction = 40%) to reduce cardiovascular death and to reduce heart failure hospitalizations. Atacand also has an added effect on these outcomes when used with an ACE inhibitor. /Included in US product labeling/

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Both angiotensin II receptor antagonists and ACE inhibitors have been shown to slow the rate of progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy, and use of a drug from either class is recommended in such patients. /NOT included in US product label/

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2059


Hypertension in middle-aged or elderly women is often accompanied with various symptoms, which may be related to climacteric. The symptoms of post-menopausal women are suggested to be derived in part from instability of the sympathetic nerve system due to a low estrogen state. An angiotensin-receptor blocker, candesartan cilexetil (candesartan), is known to suppress sympathetic nerve activity by inhibiting the renin-angiotensin system in the brain, suggesting that it may be effective for ameliorating these symptoms. The aim of this study was to elucidate whether candesartan improves menopausal symptoms in hypertensive women. A total of 69 female patients, aged 40 years or older, who had hypertension and various menopausal-like symptoms, were recruited from 39 centers to participate in this study. Patients were prescribed candesartan 4 to 8 mg/day (average dose 7.2 mg/day), alone or in addition to current antihypertensive medications. We interviewed patients in regard to their menopausal symptoms and scored them using the Simplified Menopausal Index (SMI). During the 12-month observation period, significant decreases were seen in both blood pressure (157+/-21/85+/-11 to 141+/-18/77+/-12 mmHg, p<0.001) and SMI (29+/-18 to 18+/-7, p<0.001), although the heart rate did not change. The percentage of decrease in SMI was correlated with that in systolic blood pressure (r=0.43, p<0.001). ...

Ikeda H et al; Hypertens Res 29 (12): 1007-12 (2006)


EXPL THER Gastric cancer with peritoneal dissemination has poor clinical prognosis because of the presence of rich stromal fibrosis and acquired drug resistance. Recently, Angiotensin II type I receptor blockers such as candesartan have attracted attention for their potential anti-fibrotic activity. We examined whether candesartan could attenuate tumor proliferation and fibrosis through the interaction between gastric cancer cell line (MKN45) cells and human peritoneal mesothelial cells. Candesartan significantly reduced TGF-beta1 expression and epithelial-to-mesenchymal transition-like change, while tumor proliferation and stromal fibrosis were impaired. Targeting the Angiotensin II signaling pathway may therefore be an efficient strategy for treatment of tumor proliferation and fibrosis.[Okazaki M et al; Cancer Lett. 2014 Sep 16. pii: S0304-3835(14)00531-X. doi: 10.1016/j.canlet.2014.09.019.

Epub ahead of print]


EXPL THER Several authors have investigated the antitumor activity of angiotensin II type 1 receptor (AT1R) antagonists, which are widely used as antihypertensive drugs. In this study, we evaluated the efficacy of the AT1R antagonist candesartan against bladder cancer. For the study in vitro, human bladder cancer cells (KU-19-19) were cultured with and without angiotensin II (A II) and candesartan, and cell viability and vascular endothelial growth factor (VEGF) secretion were analyzed. Also for the study in vivo, a tumor xenograft model was prepared in nude mice using KU-19-19 cells. Mice were administered candesartan daily by oral gavage, and paclitaxel via intravenous infusion. Microvessel density, VEGF expression, and apoptosis were investigated. Candesartan did not induce direct toxicity in KU-19-19 cells, but VEGF was significantly lower in candesartan-treated cells than in the A II-treated control cells. In mice, candesartan, paclitaxel and candesartan-paclitaxel significantly suppressed tumor growth to 46.0%, 35.8% and 17.3%, respectively, of the tumor volume in the control group, showing that combined treatment significantly inhibited tumor growth compared to the candesartan group. Microvessel density and VEGF were significantly decreased in the candesartan and candesartan-paclitaxel groups compared to the control group. The apoptotic index was significantly increased in the paclitaxel and candesartan-paclitaxel groups compared to the control and candesartan groups. In our experimental model, candesartan prevented bladder cancer growth by inhibiting angiogenesis. Furthermore, combined treatment with candesartan and paclitaxel enhanced paclitaxel-induced cytotoxicity. These results suggest that the AT1R antagonist candesartan may be a candidate for innovative therapy for bladder cancer.

Kosugi M et al; Hum Cell 20 (1): 1-9 (2007)


4.2 Drug Warning

/BOXED WARNING/ WARNING: FETAL TOXICITY. When pregnancy is detected, discontinue Atacand as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Use of drugs that act on the renin-angiotensin system during the second and third trimesters of pregnancy reduces fetal renal function and increases fetal and neonatal morbidity and death. Resulting oligohydramnios can be associated with fetal lung hypoplasia and skeletal deformations. Potential neonatal adverse effects include skull hypoplasia, anuria, hypotension, renal failure, and death. When pregnancy is detected, discontinue Atacand as soon as possible. These adverse outcomes are usually associated with use of these drugs in the second and third trimester of pregnancy. Most epidemiologic studies examining fetal abnormalities after exposure to antihypertensive use in the first trimester have not distinguished drugs affecting the renin-angiotensin system from other antihypertensive agents. Appropriate management of maternal hypertension during pregnancy is important to optimize outcomes for both mother and fetus.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Neonates with a history of in utero exposure to Atacand: If oliguria or hypotension occurs, direct attention toward support of blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


FDA Pregnancy Risk Category: D /POSITIVE EVIDENCE OF RISK. Studies in humans, or investigational or post-marketing data, have demonstrated fetal risk. Nevertheless, potential benefits from the use of the drug may outweigh the potential risk. For example, the drug may be acceptable if needed in a life-threatening situation or serious disease for which safer drugs cannot be used or are ineffective./

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


It is not known whether candesartan is excreted in human milk, but candesartan has been shown to be present in rat milk. Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue Atacand, taking into account the importance of the drug to the mother.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Symptomatic hypotension may occur. Patients at particular risk include those with volume or salt depletion secondary to salt restriction, prolonged diuretic therapy, heart failure, or dialysis. In patients with heart failure, a temporary reduction in the dosage of candesartan cilexetil and/or of a diuretic may be needed; blood pressure should be monitored during dosage escalation and periodically thereafter.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2059


Adverse effects occurring in 1% or more of patients receiving candesartan cilexetil include back pain, dizziness, upper respiratory tract infection, pharyngitis, and rhinitis. The incidence of adverse effects was not affected by age, gender, or race.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Sensitivity reactions, including various anaphylactoid reactions and/or angioedema, have been reported with use of angiotensin II receptor antagonists, including candesartan. Candesartan is not recommended in patients with a history of angioedema associated with or unrelated to ACE or angiotensin II receptor antagonist therapy.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Because the renin-angiotensin-aldosterone (RAA) system appears to contribute substantially to maintenance of glomerular filtration in patients with congestive heart failure in whom renal perfusion is severely compromised, renal function may deteriorate markedly (e.g., oliguria, progressive azotemia, renal failure, death) in these patients during therapy with an angiotensin-converting enzyme (ACE) inhibitor or an angiotensin II receptor antagonist (e.g., candesartan cilexetil). Increases in serum creatinine requiring discontinuance of the drug may occur in patients with congestive heart failure receiving candesartan. Serum creatinine should be monitored during dosage escalation and periodically thereafter. Renal artery stenosis, preexisting renal impairment, and concomitant diuretic therapy also are risk factors for renal impairment during therapy with drugs that inhibit the RAA system. Although reports received to date have involved patients treated with ACE inhibitors, this adverse effect also would be expected to occur when drugs with similar pharmacologic activity (e.g., angiotensin II receptor antagonists) are used in a similar manner.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Children < 1 year of age must not receive Atacand for hypertension. Drugs that act directly on the renin-angiotensin system (RAS) can have effects on the development of immature kidneys.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


No substantial differences in safety and efficacy for the treatment of hypertension /in geriatric patients/ relative to younger adults, but increased sensitivity cannot be ruled out. Increased incidence of candesartan-associated adverse effects (e.g., abnormal renal function, hypotension, hyperkalemia) and consequent discontinuance of candesartan have been reported in patients with congestive heart failure who were 75 years of age or older when compared with younger patients.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Like angiotensin-converting enzyme (ACE) inhibitors, the possibility that hypertensive black patients may respond less to candesartan than non-black patients should be considered.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2059


Drugs that act directly on the renin-angiotensin system (e.g., ACE inhibitors, angiotensin II receptor antagonists) can cause fetal and neonatal morbidity and mortality when used in pregnancy during the second and third trimesters. ACE inhibitors also may increase the risk of major congenital malformations when administered during the first trimester of pregnancy. Candesartan should be discontinued as soon as possible when pregnancy is detected, unless continued use is considered life-saving. Nearly all women can be transferred successfully to alternative therapy for the remainder of their pregnancy. Cases of fetal and neonatal toxicity in infants born to women who received candesartan cilexetil during pregnancy have been reported during postmarketing experience with the drug.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2059


When hydrochlorothiazide is used in fixed combination with candesartan, the usual cautions, precautions, and contraindications associated with hydrochlorothiazide must be considered in addition to those associated with candesartan.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Hyperkalemia may occur in patients with congestive heart failure receiving candesartan, especially in those receiving concomitant therapy with an ACE inhibitor and/or a potassium-sparing diuretic (e.g., spironolactone). Serum potassium should be monitored during dosage escalation and periodically thereafter.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Valvular Stenosis: There is concern on theoretical grounds that patients with aortic stenosis might be at particular risk of decreased coronary perfusion when treated with vasodilators because they do not develop as much afterload reduction.

Health Canada; Product Monograph for Atacand (Candesartan Cilexetil), Drug Identification Number (DIN): 02239090, p5 (Revision date: April 7, 2014). Available from, as of October 10, 2014: http://webprod5.hc-sc.gc.ca/dpd-bdpp/start-debuter.do?lang=eng


Hypotension may occur in patients undergoing major surgery and anesthesia who are receiving angiotensin II receptor antagonists, including candesartan, presumably secondary to blockade of the renin-angiotensin system. Rarely, hypotension may be severe enough to require volume expansion and/or vasopressors.

American Society of Health-System Pharmacists 2014; Drug Information 2014. Bethesda, MD. 2014, p. 2060


Do not co-administer aliskiren with Atacand in patients with diabetes. Avoid use of aliskiren with Atacand in patients with renal impairment (GFR <60 mL/min).

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Attenuation of the antihypertensive effect may occur when simultaneously administering angiotensin receptor antagonists (ARBs) and Non-steroidal antiinflammatory drugs (NSAIDs); i.e. selective COX-2 inhibitors, acetylsalicylic acid and non-selective NSAIDs. As with angiotensin converting enzyme inhibitors (ACEIs), concomitant use of ARBs and NSAIDs may lead to an increased risk of worsening of renal function, including possible acute renal failure, and an increase in serum potassium, especially in patients with poor pre-existing renal function. The combination ARBs and NSAIDs should be administered with caution, especially in older patients and in volume depleted patients. Patients should be adequately hydrated and consideration should be given to monitoring renal function after initiation of concomitant therapy and periodically thereafter. /From table/

Health Canada; Product Monograph for Atacand (Candesartan Cilexetil), Drug Identification Number (DIN): 02239090, p18 (Revision date: April 7, 2014). Available from, as of October 10, 2014: http://webprod5.hc-sc.gc.ca/dpd-bdpp/start-debuter.do?lang=eng


5 Pharmacology and Biochemistry
5.1 Pharmacology

Candesartan is a synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity. Candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure.


5.2 MeSH Pharmacological Classification

Angiotensin II Type 1 Receptor Blockers

Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.


Antihypertensive Agents

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety

CANDESARTAN


5.3.2 FDA UNII

S8Q36MD2XX


5.3.3 Pharmacological Classes

Mechanisms of Action [MoA]

Angiotensin 2 Receptor Antagonists


Established Pharmacologic Class [EPC]

Angiotensin 2 Receptor Blocker


5.4 ATC Code

C - Cardiovascular system
C09 - Agents acting on the renin-angiotensin system
C09C - Angiotensin ii antagonists, plain
C09CA - Angiotensin ii antagonists, plain
C09CA06 - Candesartan


5.5 Absorption, Distribution and Excretion

The volume of distribution of candesartan is 0.13 L/kg. Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells. The protein binding is constant at candesartan plasma concentrations well above the range achieved with recommended doses. In rats, it has been demonstrated that candesartan crosses the blood-brain barrier poorly, if at all. It has also been demonstrated in rats that candesartan passes across the placental barrier and is distributed in the fetus.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Following administration of candesartan cilexetil, the absolute bioavailability of candesartan was estimated to be 15%. After tablet ingestion, the peak serum concentration (Cmax) is reached after 3 to 4 hours. Food with a high fat content does not affect the bioavailability of candesartan after candesartan cilexetil administration.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


Total plasma clearance of candesartan is 0.37 mL/min/kg, with a renal clearance of 0.19 mL/min/kg. When candesartan is administered orally, about 26% of the dose is excreted unchanged in urine. Following an oral dose of (14)C-labeled candesartan cilexetil, approximately 33% of radioactivity is recovered in urine and approximately 67% in feces. Following an intravenous dose of (14)C-labeled candesartan, approximately 59% of radioactivity is recovered in urine and approximately 36% in feces. Biliary excretion contributes to the elimination of candesartan.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


It is not known whether candesartan is excreted in human milk, but candesartan has been shown to be present in rat milk.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


5.6 Metabolism/Metabolites

Candesartan cilexetil is rapidly and completely bioactivated by ester hydrolysis during absorption from the gastrointestinal tract to candesartan, a selective AT1 subtype angiotensin II receptor antagonist. Candesartan is mainly excreted unchanged in urine and feces (via bile). It undergoes minor hepatic metabolism by O-deethylation to an inactive metabolite.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


5.7 Biological Half-Life

The elimination half-life of candesartan is approximately 9 hours.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


5.8 Mechanism of Action

Although these agents /angiotensin II receptor antagonists/ are similar to ACE inhibitors in that they decrease the effects of angiotensin II, rather than decreasing the formation of angiotensin II, drugs antagonize angiotensin II at the type I angiotensin receptor. This allows the drugs to inhibit the vasoconstrictive and aldosterone promoting effects of angiotensin II without interfering with bradykinin degradation, significantly reducing the adverse effects of cough and angioedema seen with ACE inhibitor therapy. ... /Angiotensin II receptor antagonists/

Goldfrank, L.R. (ed). Goldfrank's Toxicologic Emergencies. 7th Edition McGraw-Hill New York, New York 2002., p. 782


Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathways for angiotensin II synthesis. There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Candesartan has much greater affinity (>10,000-fold) for the ATI receptor than for the AT2 receptor. Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because candesartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Candesartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of candesartan on blood pressure.

NIH; DailyMed. Current Medication Information for Atacand (Candesartan Cilexetil) Tablet (Revised: April 2013). Available from, as of October 9, 2014: http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=a73e1339-9643-4eea-2cbe-e879c88fb50e


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