Telmisartan
Angiotensin 2 Receptor Blocker — CARDIOVASCULAR SYSTEM
Also known as: micardis, pritor, tolura
Data last refreshed: (DrugCentral release 2024-11-01)
Key facts
Telmisartan is an ofp drug in the Angiotensin 2 Receptor Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1998. Its mechanism of action is classified as Angiotensin 2 Receptor Antagonists. DrugCentral lists 9 molecular targets, including Agtr1, AGTR2 and AGTR1. Recorded indications include Cerebrovascular accident, Disorder due to type 2 diabetes mellitus, History of myocardial infarction due to atherothrombotic coronary artery disease and Hypertensive disorder.
- Approval status: ofp (first approved 1998 by the FDA).
- Drug class: Angiotensin 2 Receptor Blocker.
- Mechanism of action: Angiotensin 2 Receptor Antagonists.
- Molecular targets: Agtr1, AGTR2, AGTR1 and Agtr1b (9 listed in DrugCentral).
- Indications: Cerebrovascular accident, Disorder due to type 2 diabetes mellitus, History of myocardial infarction due to atherothrombotic coronary artery disease, Hypertensive disorder and Myocardial Infarction Prevention.
- ATC code: C09CA07 (Angiotensin II receptor blockers (ARBs), plain).
- Molecular formula: C33H30N4O2; molecular weight 514.63 g/mol.
Indications & contraindications
Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).
Indications (5)
- Cerebrovascular accident
- Disorder due to type 2 diabetes mellitus
- History of myocardial infarction due to atherothrombotic coronary artery disease
- Hypertensive disorder
- Myocardial Infarction Prevention
Off-label uses (5)
- Atrial fibrillation
- Chronic heart failure
- Diabetic renal disease
- Diastolic heart failure
- Nondiabetic Proteinuric Nephropathy
Contraindications (35)
- Acute pancreatitis
- Anuria
- Azotemia
- Cholestasis
- Chronic idiopathic constipation
- Dehydration
- Diabetes mellitus
- Disease of liver
- Gout
- Hepatic coma
- Hepatic failure
- Hypercalcemia
- Hypercholesterolemia
- Hyperkalemia
- Hyperparathyroidism
- Hyperuricemia
- Hypochloremic alkalosis
- Hypokalemia
- Hypomagnesemia
- Hyponatremia
- Hypovolemia
- Kidney disease
- Low blood pressure
- Neonatal hyperbilirubinemia
- Obstruction of bile duct
- Pregnancy, function
- Renal artery stenosis
- Second trimester pregnancy
- Secondary angle-closure glaucoma
- Severe Aortic Valve Stenosis
- + 5 more
Mechanism & targets
| Mechanism of action (MoA) | Angiotensin 2 Receptor Antagonists |
|---|---|
| Established pharmacologic class | Angiotensin 2 Receptor Blocker |
Molecular targets (9)
| Target | Gene | Action | Activity |
|---|---|---|---|
| Type-1A angiotensin II receptor | Agtr1 | unknown | Ki 9.64 |
| Type-2 angiotensin II receptor | AGTR2 | unknown | IC50 9.48 |
| Type-1 angiotensin II receptor | AGTR1 | antagonist | IC50 9.31 |
| Type-1B angiotensin II receptor | Agtr1b | unknown | IC50 8.52 |
| Peroxisome proliferator-activated receptor gamma | PPARG | unknown | EC50 5.82 |
| Glycine receptor subunit alpha-1 | GLRA1 | unknown | EC50 5.49 |
| Angiotensin-converting enzyme | ACE | unknown | Ki 5.22 |
| ATP-binding cassette sub-family G member 2 | ABCG2 | unknown | IC50 4.77 |
| Multidrug and toxin extrusion protein 1 | SLC47A1 | unknown | IC50 4.75 |
Regulatory approvals (2)
| Date | Agency | Marketed as | Applicant | Orphan |
|---|---|---|---|---|
| 1998-11-12 | EMA | — | KRKA, D.D., NOVO MESTO | |
| 1998-11-10 | FDA | — | BOEHRINGER INGELHEIM |
ATC classification
| ATC code | Therapeutic hierarchy |
|---|---|
C09CA07 | CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN › Angiotensin II receptor blockers (ARBs), plain |
C09DA07 | CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS › Angiotensin II receptor blockers (ARBs) and diuretics |
C09DB04 | CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS › Angiotensin II receptor blockers (ARBs) and calcium channel blockers |
C09DX08 | CARDIOVASCULAR SYSTEM › AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM › ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), COMBINATIONS › Angiotensin II receptor blockers (ARBs), other combinations |
C10BX20 | CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, COMBINATIONS › Lipid modifying agents in combination with other drugs |
C10BX24 | CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, COMBINATIONS › Lipid modifying agents in combination with other drugs |
Reported adverse-event signals
Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.
| MedDRA term | LLR |
|---|---|
| Blood pressure increased | 516.5 |
| Amaurosis fugax | 433.8 |
| Head discomfort | 412.5 |
| Haemorrhagic stroke | 400.6 |
| Altered state of consciousness | 368.6 |
| Carotid artery thrombosis | 356.8 |
| Neurologic neglect syndrome | 350.9 |
| Ocular discomfort | 347.8 |
| Urinary tract disorder | 346.1 |
| Affect lability | 312.9 |
| Adjustment disorder | 307.2 |
| Arterial occlusive disease | 296.3 |
Chemical structure
| Molecular formula | C33H30N4O2 |
|---|---|
| Molecular weight | 514.63 g/mol |
| CAS number | 144701-48-4 |
| InChIKey | RMMXLENWKUUMAY-UHFFFAOYSA-N |
| PubChem CID | 65999 |
Frequently asked questions
Answers are generated from the structured data on this page, not written by hand.
What is Telmisartan used for?
DrugCentral lists the following indications for Telmisartan: Cerebrovascular accident, Disorder due to type 2 diabetes mellitus, History of myocardial infarction due to atherothrombotic coronary artery disease, Hypertensive disorder and Myocardial Infarction Prevention.
How does Telmisartan work?
Telmisartan is classified as Angiotensin 2 Receptor Antagonists; its molecular targets in DrugCentral include Agtr1, AGTR2, AGTR1 (antagonist) and Agtr1b.
When was Telmisartan first approved?
Telmisartan was first approved by the FDA in 1998.
What drug class does Telmisartan belong to?
Telmisartan is in the Angiotensin 2 Receptor Blocker class.
What is the chemical formula of Telmisartan?
Telmisartan has the molecular formula C33H30N4O2 and a molecular weight of 514.63 g/mol.
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Sources
- DrugCentral drug card 2583 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
- ChEMBL CHEMBL1017 — compound record and bioactivity
- PubChem CID 65999 — chemical identifiers
- DrugBank DB00966 — drug record
- FDA UNII U5SYW473RQ — substance identity
- DailyMed: FDA labels for Telmisartan — current prescribing information (label search)
- UniProt P50052 (AGTR2) — target protein
- UniProt P30556 (AGTR1) — target protein
- UniProt P37231 (PPARG) — target protein
- UniProt P23415 (GLRA1) — target protein
- UniProt P12821 (ACE) — target protein
- UniProt Q9UNQ0 (ABCG2) — target protein
- FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
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