Product Name

Telmisartan

CAS Number

144701-48-4

LGM Pharma is an API distributor. LGM Pharma can supply CGMP and/or DMF products, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, pharmacies, or any pharmaceutical companies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:
Telmisartan
CAS Number:
144701-48-4
Indication:
Used alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart failure (only in patients who cannot tolerate ACE inhibitors).
Mode of Action:

Telmisartan interferes with the binding of angiotensin II to the angiotensin II AT_-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. Studies also suggest that telmisartan is a partial agonist of PPAR_, which is an established target for antidiabetic drugs. This suggests that telmisartan can improve carbohydrate and lipid metabolism, as well as control insulin resistance without causing the side effects that are associated with full PPAR_ activators.

Pharmacodynamics:

Telmisartan is an orally active nonpeptide angiotensin II antagonist that acts on the AT1 receptor subtype. It has the highest affinity for the AT1 receptor among commercially available ARBS and has minimal affinity for the AT2 receptor. New studies suggest that telmisartan may also have PPAR_ agonistic properties that could potentially confer beneficial metabolic effects, as PPAR_ is a nuclear receptor that regulates specific gene transcription, and whose target genes are involved in the regulation of glucose and lipid metabolism, as well as anti-inflammatory responses. 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.

Metabolism:

Minimally metabolized by conjugation to form a pharmacologically inactive acylglucuronide; the glucuronide of the parent compound is the only metabolite that has been identified in human plasma and urine. The cytochrome P450 isoenzymes are not involved in the metabolism of telmisartan.

Toxicity:

Intravenous LD50 in rats is 150-200 mg/kg in males and 200 to 250 mg/kg in females. Acute oral toxicity is low: no deaths and no changes occurred in rats or dogs at 2000 mg/kg, the highest dose tested. Limited data are available with regard to overdosage in humans. The most likely manifestations of overdosage with telmisartan would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation.

IUPAC:
2-(4-{[4-methyl-6-(1-methyl-1H-1, 3-benzodiazol-2-yl)-2-propyl-1H-1, 3-benzodiazol-1-yl]methyl}phenyl)benzoic acid
ATC:
C09CA07
PubChem:
65999
DrugBank:
DB00966 (APRD01247)
Formula:
C32H32O13S
Molecular Mass:
514.6169
Synonyms:
BIBR 277 BIBR 277SE
SMILES:
CCCC1=NC2=C(C=C(C=C2C)C2=NC3=CC=CC=C3N2C)N1CC1=CC=C(C=C1)C1=CC=CC=C1C(O)=O
AHFS Code:
24:32.1
InChi:
RMMXLENWKUUMAY-UHFFFAOYSA-N
General Reference:
General Reference:

  1. Sharpe M, Jarvis B, Goa KL: Telmisartan: a review of its use in hypertension. Drugs. 2001;61(10):1501-29. Pubmed
  2. Smith DH: Treatment of hypertension with an angiotensin II-receptor antagonist compared with an angiotensin-converting enzyme inhibitor: a review of clinical studies of telmisartan and enalapril. Clin Ther. 2002 Oct;24(10):1484-501. Pubmed
  3. Kumar AS, Ghosh S, Mehta GN: Efficient and improved synthesis of Telmisartan. Beilstein J Org Chem. 2010 Mar 11;6:25. Pubmed
  4. Galzerano D, Capogrosso C, Di Michele S, Galzerano A, Paparello P, Lama D, Gaudio C: New standards in hypertension and cardiovascular risk management: focus on telmisartan. Vasc Health Risk Manag. 2010 Mar 24;6:113-33. Pubmed

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210. 

Ask us about this product

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants
  • Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any submission type based on specific customer requirements

Find an API Product

Search
Generic filters