Telmisartan
[CAS# 144701-48-4]

Identification

• Classification: API >> Circulatory system medication >> Antihypertensive drug
• Name: Telmisartan
• Synonyms: 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid
• Molecular Formula: C₃₃H₃₀N₄O₂
• Molecular Weight: 514.62
• CAS Registry Number: 144701-48-4
• EC Number: 620-494-7
• SMILES: CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C

Properties

• Water solubility: insoluble
• Density: 1.2±0.1 g/cm³, Calc.^*
• Index of Refraction: 1.667, Calc.^*
• Boiling Point: 771.9±70.0 °C (760 mmHg), Calc.^*
• Flash Point: 420.6±35.7 °C, Calc.^*

^* Calculated using Advanced Chemistry Development (ACD/Labs) Software.

Safety Data

• Hazard Symbols: GHS08;GHS09 Warning
• Risk Statements: H361-H411
• Safety Statements: P203-P273-P280-P318-P391-P405-P501

Hazard Classification

Hazard	Class	Category Code	Hazard Statement
Chronic hazardous to the aquatic environment	Aquatic Chronic	2	H411
Reproductive toxicity	Repr.	2	H361
Chronic hazardous to the aquatic environment	Aquatic Chronic	4	H413
Specific target organ toxicity - repeated exposure	STOT RE	2	H373
Eye irritation	Eye Irrit.	2	H319
Acute toxicity	Acute Tox.	4	H302

Discovery and Applications

Telmisartan, a member of the angiotensin II receptor blocker (ARB) class of medications. Discovered in the late 1990s, Telmisartan represented a significant advancement in pharmacotherapy for hypertension. Its discovery was a result of targeted drug design efforts focusing on blocking the angiotensin II receptor, a key component of the renin-angiotensin-aldosterone system involved in blood pressure regulation. Telmisartan's unique pharmacological profile, characterized by high affinity and long duration of action, contributed to its recognition as a promising antihypertensive agent.

Telmisartan is widely used for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. By selectively blocking the angiotensin II receptor, Telmisartan inhibits the vasoconstrictive and aldosterone-releasing effects of angiotensin II, leading to vasodilation and reduction in blood pressure. Beyond its blood pressure-lowering effects, Telmisartan offers cardiovascular protection in patients with hypertension and other cardiovascular risk factors. Studies have shown that Telmisartan may reduce the risk of cardiovascular events such as heart attack, stroke, and heart failure by improving vascular function, reducing arterial stiffness. Telmisartan is indicated for the management of diabetic nephropathy, a common complication of diabetes characterized by progressive kidney damage and loss of renal function. By inhibiting the detrimental effects of angiotensin II on the kidneys, Telmisartan helps slow the progression of diabetic nephropathy and preserve renal function in diabetic patients. Telmisartan is utilized in the management of heart failure with reduced ejection fraction, a condition characterized by impaired cardiac function and inadequate pumping of blood by the heart. As an ARB, Telmisartan improves cardiac function, reduces left ventricular hypertrophy, and prevents adverse cardiac remodeling. Telmisartan has shown promise in stroke prevention, particularly in patients with a history of cardiovascular events or high cardiovascular risk. Clinical trials have demonstrated that Telmisartan may reduce the risk of recurrent stroke and other vascular events in these patients, highlighting its potential role in secondary prevention strategies. Telmisartan exerts beneficial effects on metabolic parameters such as insulin sensitivity, lipid profile, and adipokine levels, making it a valuable therapeutic option for patients with metabolic syndrome, a cluster of risk factors for cardiovascular dise

References

2024-07-09. Management of Device Detected Subclinical Atrial Fibrillation
DOI: 10.1007/s12170-024-00748-3

2010-08. Acute effects of renin-angiotensin system blockade on arterial function in hypertensive patients
DOI: 10.1038/sj.jhh.1002211

2007-04-17. Regulation of prostate cancer cell growth and PSA expression by angiotensin II receptor blocker with peroxisome proliferator‐activated receptor gamma ligand like action
DOI: 10.1002/pros.20571