Telmisartan

Biological Activity

Telmisartan (Micardis) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. In addition to blocking the Renin-Angiotensin System (RAS), telmisartan acts as a selective modulator of Peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. Telmisartan has binding affinity 3000 times greater for AT1 than AT2 receptors. Telmisartan also has the longest half life (24 hrs) of all angiotensin II type 1 receptor antagonists.

Chemical Information

Molecular Weight	514.62
Formula	C33H30N4O2
CAS Number	144701-48-4
Form	Solid
Solubility (25°C)	DMSO 10 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Bianca N Loureno, et al. Efficacy of telmisartan for the treatment of persistent renal proteinuria in dogs: A double-masked, randomized clinical trial

[2] Xuan Jin, et al. Efficacy and safety of co-administered telmisartan/amlodipine and rosuvastatin in subjects with hypertension and dyslipidemia

[3] Rodolfo Pedro Rothlin, et al. Telmisartan as tentative angiotensin receptor blocker therapeutic for COVID-19

[4] Jiagen Wen, et al. The influence of telmisartan on metformin pharmacokinetics and pharmacodynamics

[5] Yan Wang, et al. Telmisartan Improves Insulin Resistance: A Meta-Analysis