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Description: Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. Generally, angiotensin II receptor blockers (ARBs) such as telmisartan bind to the angiotensin II type 1 (AT1) receptors with high affinity, causing inhibition of the action of angiotensin II on vascular smooth muscle, ultimately leading to a reduction in arterial blood pressure. Recent studies suggest that telmisartan may also have PPAR-gamma agonistic properties that could potentially confer beneficial metabolic effects.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. New studies suggest that telmisartan may also have PPARγ agonistic properties that could potentially confer beneficial metabolic effects. This observation is currently being explored in clinical trials. 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. Telmisartan works by blocking the vasoconstrictor and aldosterone secretory effects of angiotensin II.
Mechanism of Action: Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT1-receptor by binding reversibly and selectively to the receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance. Telmisartan does not inhibit the angiotensin converting enzyme, other hormone receptors, or ion channels.
Indication: For the treatment of hypertension.
Half Life: Bi-exponential decay kinetics with a terminal elimination half-life of approximately 24 hours.
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Individual Studies
  • Drug target sets for approved compounds

    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…

  • Studies of new selective PPAR-gamma modulators

    Mus musculus Mus musculus | RNA Expression   RNA Expression

    Expression pattern of adipocytes after telmisartan, pioglitazone or irbesartan treatment

    Authors: Witt Henning, Schupp Michael, Clemenz Markus et al.

    Organization: Max Planck Institute for Molecular Genet…

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Thought leaders and organizations working on research involving Telmisartan.

  • Roland E Schmieder
  • Salim Yusuf
  • Helmut Schumacher
  • Peggy Gao
  • Peter Sleight
  • Boehringer Ingelheim Pharmaceuticals
  • Bayer
  • University of Erlangen-Nürnberg
  • Ludwig-Maximilians - University of Munich
  • Second University of Naples
  • Charité-Universitätsmedizin Berlin
  • Tokyo Medical University
  • Third Military Medical University
  • Ludwig Maximilians University
  • Ludwig Maximilians University Munchen

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