Telmisartan

Summary

Telmisartan (CHEMBL1017) is an approved small-molecule antihypertensive agent (ATC C09CA07) targeting AGTR1; indicated across 22 conditions including hypertensive disorder and cardiovascular disorder; with CIViC clinical evidence for 1 variant-indication association (e.g. ATP7B Expression in ovarian cancer).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C09CA07
• Targets: 1 (AGTR1)
• Indications: 22 conditions
• Clinical trials: 206
• Precision-oncology evidence (CIViC): 1 variant–indication association
• Chemistry: 514.6 Da · C33H30N4O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1017
Name	Telmisartan
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	65999
ChEBI	CHEBI:9434
ATC	C09CA07
Molecular formula	C33H30N4O2
Molecular weight	514.6
InChIKey	RMMXLENWKUUMAY-UHFFFAOYSA-N

SMILES: CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C

IUPAC name: 2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid

ChEBI definition: A member of the class of benzimidazoles used widely in the treatment of hypertension.

Pharmacological roles (ChEBI): antihypertensive agent, angiotensin receptor antagonist, EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor.

Other ChEBI roles (chemical / environmental): xenobiotic, environmental contaminant.

Also known as: BIBR 277 SE, BIBR-277, BIBR-277 SE, Bibr-277se, C09CA07, Kinzalmono, Micardis, Pritor, Semintra, Telmisartan, Telmisartan actavis, Telmisartan component of kinzalkomb

Patent coverage: 7,414 distinct patent families (27,457 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 27,172 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
AGTR1	AT1 receptor	Antagonist	8.4	0.4%	P30556

Broader ChEMBL bioactivity targets: 40 (assay-derived). Sample: Lysine-specific demethylase 4E, Ubiquitin carboxyl-terminal hydrolase 2, Solute carrier organic anion transporter family member 1B1, Solute carrier organic anion transporter family member 1B3, Multidrug and toxin extrusion protein 1, ATP-binding cassette sub-family C member 4, Angiotensin-converting enzyme, 5-hydroxytryptamine receptor 2B, Alpha-2A adrenergic receptor, Cholecystokinin receptor type A.

Bioactivity

ChEMBL activities: 54 potent at pChembl ≥ 5 of 82 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P25095	9.64	Ki	0.23	nM	CHEMBL_ACT_12463672
P25095	9.64	Ki	0.23	nM	CHEMBL_ACT_2981091
AGTR2	9.48	IC50	0.33	nM	CHEMBL_ACT_8017391
AGTR1	9.31	IC50	0.49	nM	CHEMBL_ACT_12661340
AGTR1	9.31	IC50	0.49	nM	CHEMBL_ACT_6274128
AGTR1	9	IC50	1	nM	CHEMBL_ACT_10956561
AGTR1	9	IC50	1	nM	CHEMBL_ACT_13483302
AGTR1	9	AC50	1	nM	CHEMBL_ACT_25177109
AGTR1	9	IC50	1	nM	CHEMBL_ACT_8017360
AGTR1	8.7	IC50	2	nM	CHEMBL_ACT_13903245
AGTR1	8.7	IC50	2	nM	CHEMBL_ACT_19030356
P29089	8.52	IC50	3	nM	CHEMBL_ACT_175439
AGTR1	8.52	IC50	3	nM	CHEMBL_ACT_3099920
AGTR1	8.27	IC50	5.4	nM	CHEMBL_ACT_25751205
CYP2J2	7	Ki	100	nM	CHEMBL_ACT_15449375
AGTR1	6.82	IC50	150	nM	CHEMBL_ACT_10956585
CYP2J2	6.72	Ki	190	nM	CHEMBL_ACT_15449373
CYP2J2	6.38	IC50	420	nM	CHEMBL_ACT_15461601
CYP2J2	6.27	IC50	540	nM	CHEMBL_ACT_15449379
CYP2J2	6.27	IC50	540	nM	CHEMBL_ACT_15449381
PPARG	6.16	EC50	700	nM	CHEMBL_ACT_16823111
SLCO1B3	6.02	Ki	960	nM	CHEMBL_ACT_13798651
SLCO1B1	5.99	Ki	1030	nM	CHEMBL_ACT_13800650
PPARG	5.97	Ki	1080	nM	CHEMBL_ACT_25084873
SLCO1B3	5.9	IC50	1259	nM	CHEMBL_ACT_13798585
NPSR1	5.9	Potency	1259	nM	CHEMBL_ACT_4905144
PPARG	5.82	EC50	1520	nM	CHEMBL_ACT_12660133
PPARG	5.82	EC50	1520	nM	CHEMBL_ACT_6274755
SLCO1B1	5.73	IC50	1862	nM	CHEMBL_ACT_13800584
PPARG	5.7	EC50	2020	nM	CHEMBL_ACT_13903244

Target pathways

Aggregated over 1 target gene(s): AGTR1.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	1	AGTR1
Membrane Trafficking	1	AGTR1
Signaling by GPCR	1	AGTR1
Class A/1 (Rhodopsin-like receptors)	1	AGTR1
Peptide ligand-binding receptors	1	AGTR1
GPCR downstream signalling	1	AGTR1
G alpha (q) signalling events	1	AGTR1
GPCR ligand binding	1	AGTR1
Vesicle-mediated transport	1	AGTR1
Cargo recognition for clathrin-mediated endocytosis	1	AGTR1
Clathrin-mediated endocytosis	1	AGTR1

Dominant GO biological processes

GO term	Targets
regulation of cell growth	1
kidney development	1
renin-angiotensin regulation of aldosterone production	1
maintenance of blood vessel diameter homeostasis by renin-angiotensin	1
regulation of systemic arterial blood pressure by renin-angiotensin	1
inflammatory response	1
G protein-coupled receptor signaling pathway	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
positive regulation of cytosolic calcium ion concentration	1
Rho protein signal transduction	1
positive regulation of macrophage derived foam cell differentiation	1
regulation of vasoconstriction	1
calcium-mediated signaling	1
low-density lipoprotein particle remodeling	1
regulation of renal sodium excretion	1

Indications & clinical

Indications

22 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
hypertensive disorder	4	MONDO:0005044	EFO:0000537
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
diabetes mellitus	4	MONDO:0005015	EFO:0000400
myocardial infarction	4	MONDO:0005068	EFO:0000612
stroke disorder	4	MONDO:0005098	EFO:0000712
heart disorder	3	MONDO:0005267	EFO:0003777
diabetic kidney disease	3	MONDO:0005016	EFO:0000401
polycystic kidney disease	3	MONDO:0020642	EFO:0008620
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
essential hypertension	3	MONDO:0001134	MONDO:0001134
type 2 diabetes mellitus	3	MONDO:0005148	MONDO:0005148
kidney disorder	3	MONDO:0005240	EFO:0003086
chronic kidney disease	3	MONDO:0005300	MONDO:0024327
HIV infectious disease	2	MONDO:0005109	EFO:0000764
neuralgia	2	MONDO:0021667	EFO:0005762
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
obstructive sleep apnea syndrome	0	MONDO:0007147	EFO:0003918

5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 206.

Phase distribution

Phase	Trials
PHASE3	51
PHASE4	50
PHASE1	49
Not specified	34
PHASE2	16
PHASE2/PHASE3	2
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06041529	PHASE4	ACTIVE_NOT_RECRUITING	Study to Evaluate the Efficacy and Safety of TEL/AML/CTD in Elderly Patients With Essential Hypertension
NCT06431477	PHASE4	RECRUITING	Efficacy and Safety of Telmisartan Compared With Losartan
NCT07547878	PHASE4	NOT_YET_RECRUITING	Rapid and Simultaneous Initiation of Four Guideline-Directed CKD Therapies (RAPID-CKD)
NCT00034840	PHASE4	COMPLETED	Telmisartan vs. Valsartan in Patients With Mild to Moderate Hypertension Following a Missed Dose
NCT00153023	PHASE4	COMPLETED	1 Year Trial Telmisartan 80 mg Versus Valsartan 160 mg in Hypertensive Type 2 Diabetic Patients With Overt Nephropathy
NCT00153062	PHASE4	COMPLETED	PRoFESS - Prevention Regimen For Effectively Avoiding Second Strokes
NCT00153101	PHASE4	COMPLETED	Effectiveness and Safety of Ramipril Alone Compared With Telmisartan Alone and in Combination With Ramipril in Patients at High Risk for Cardiovascular Events. Patients Intolerant to Ramipril Were Entered in TRANSCEND, Telmisartan Compared to Placebo.
NCT00168857	PHASE4	COMPLETED	A Prospective, Randomised, Double-blind, Double-dummy, Forced-titration, Multicentre, Parallel Group, One Year Treatment Trial to Compare Telmisartan (MICARDIS) 80 mg Versus Losartan (COZAAR) 100 mg, in Hypertensive Type 2 Diabetic Patients With Overt Nephropathy (AMADEO Study)
NCT00240422	PHASE4	COMPLETED	Trial to Compare the Effects of Either Telmisartan (40-80 mg PO Once Daily) or Ramipril (5-10 mg PO Once Daily) on Renal Endothelial Dysfunction in Hypertensive Patients With Type 2 Diabetes
NCT00240448	PHASE4	COMPLETED	A Randomized, Double-blind, Placebo Controlled Comparison of Telmisartan Hydrochlorothiazide (HCT) and Valsartan HCT in Hypertension (HTN) Stage I/II Patients
NCT00242814	PHASE4	COMPLETED	Phase IV, 9 Weeks Comparison Between MICARDIS 80 mg and Amlodipine 10 mg on Biological PPAR Gamma Activities
NCT00274105	PHASE4	TERMINATED	SAFE-CRP: Structural Alterations and Function of Endothelium in Cardiovascular Risk Patients
NCT00274144	PHASE4	COMPLETED	Inflammation and Coronary Artery Disease: Role of AT1-Receptor Antagonism
NCT00274599	PHASE4	COMPLETED	PROBE Investigation of the Safety & Efficacy of Telmisartan (Micardis®) vs Ramipril (Altace®) Using ABPM in HTN
NCT00274612	PHASE4	COMPLETED	Prospective Randomised Investigation of the Safety and Efficacy of Micardis® vs Ramipril Using ABPM
NCT00274638	PHASE4	COMPLETED	PROBE Parallel 6-week Treatment Comparing Telmisartan/Hydrochlorothiazide (HCT) (40/12.5 or 80/12.5) With Losartan/HCT (50/12.5) Using Ambulatory Blood Pressure Monitoring (ABPM)
NCT00295542	PHASE4	COMPLETED	Ambulatory Blood Pressure Monitoring in the Prediction of Cardiovascular Events and Effects of Chronotherapy
NCT00407862	PHASE4	COMPLETED	Telmisartan and Losartan in Hypertensive IGT
NCT00421863	PHASE4	COMPLETED	Italian Study on the Cardiovascular Effects of Systolic Blood Pressure Control - CARDIOSIS Study
NCT00490958	PHASE4	COMPLETED	Telmisartan in Haemodialysis Patients With Chronic Heart Failure
NCT00538486	PHASE4	COMPLETED	A Randomized, Double-Blind, Active Control Trial Comparing Effects of Telmisartan, Candesartan and Amlodipine, Alone or Plus Metformin, on Non-Diabetic, Obese Hypertensive Patients
NCT00559286	PHASE4	TERMINATED	Effect of the Known Antihypertensive Drug Telmisartan on Red Blood Cells and Circulation in the Smallest Blood Vessels
NCT00599885	PHASE4	COMPLETED	Comparison of Effects of Telmisartan and Valsartan on Neointima Volume in Diabetes
NCT00702936	PHASE4	UNKNOWN	Telmisartan Versus Ramipril After Acute Coronary Syndrome
NCT00750113	PHASE4	COMPLETED	Study Evaluating the Efficacy of Nifedipine GITS - Telmisartan Combination in Blood Pressure Control.
NCT00865020	PHASE4	COMPLETED	Efficacy and Safety of Aliskiren 300 mg Compared to Telmisartan 80 mg After 1 Week of Treatment Withdrawal
NCT00926289	PHASE4	COMPLETED	Telmisartan 80mg Plus Hydrochlorothiazide 25mg First Line in Moderate or Severe Hypertension
NCT00926341	PHASE4	COMPLETED	The Effects of Peroxisome Proliferators Activated Receptor-Gamma (PPAR-γ) Agonists on Certain Biochemical and Inflammatory Markers in Metabolic Syndrome
NCT00981526	PHASE4	COMPLETED	Telmisartan as an Adjunctive Treatment for Metabolic Problems in Patients With Schizophrenia
NCT01011660	PHASE4	UNKNOWN	Effects of Angiotensin II Receptor Blocker Compared With Diuretics in High-risk Hypertensive Patients
NCT01180205	PHASE4	UNKNOWN	Telmisartan, Amlodipine and Flow Mediated Dilation
NCT01435161	PHASE4	COMPLETED	Nifedipine vs Telmisartan on Prevention of Atrial Fibrillation (AF) Recurrence in Hypertensive Patients With AF
NCT01541267	PHASE4	COMPLETED	The Effect of Various Types of the Renin-angiotensin-aldosterone System Blockade on Proteinuria
NCT01683084	PHASE4	COMPLETED	Study of the Effectiveness of Telmisartan in Slowing the Progression of Abdominal Aortic Aneurysms
NCT01819220	PHASE4	COMPLETED	Randomized, Open Labeled Clinical Trial to Compare the Effectiveness of Amlodipine/Valsartan vs Hydrochlorothiazide/Telmisartan on Glucose Tolerance in Patients With Hypertension With Metabolic Syndrome
NCT01830530	PHASE4	COMPLETED	HIGH Altitude CArdiovascular REsearch in the ANDES
NCT02057328	PHASE4	UNKNOWN	Comparative Study of the Effects of Telmisartan and Nebivolol
NCT02079805	PHASE4	COMPLETED	A Study to Explore the Effects of Azilsartan Compared to Telmisartan on Insulin Resistance of Patients With Essential Hypertension on Type 2 Diabetes Mellitus by HOMA-R
NCT02172586	PHASE4	COMPLETED	Telmisartan With or Without Hydrochlorothiazide (HCTZ) Compared With Losartan With or Without HCTZ in Mild to Moderate Hypertensive Patients
NCT02177461	PHASE4	COMPLETED	Telmisartan Compared With Enalapril in Elderly Patients With Blood Hypertension

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
ATP7B Expression	Ovarian Cancer	Sensitivity/Response	Telmisartan	CIViC D	EID12307

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

140 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
LOSARTAN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
OLMESARTAN MEDOXOMIL	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
RIFAMPIN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
SPARSENTAN	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
TEGASEROD	ChEMBL + PubChem	Phase 4 (approved)	AGTR1
ALFACALCIDOL	ChEMBL	Phase 4 (approved)	AGTR1
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	AGTR1
ANGIOTENSIN II	ChEMBL	Phase 4 (approved)	AGTR1
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
BALSALAZIDE	ChEMBL	Phase 4 (approved)	AGTR1
BENZBROMARONE	ChEMBL	Phase 4 (approved)	AGTR1
BUTOCONAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
CALCITRIOL	ChEMBL	Phase 4 (approved)	AGTR1
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	AGTR1
CARVEDILOL	ChEMBL	Phase 4 (approved)	AGTR1
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
DABIGATRAN ETEXILATE	ChEMBL	Phase 4 (approved)	AGTR1
DESOGESTREL	ChEMBL	Phase 4 (approved)	AGTR1
DISULFIRAM	ChEMBL	Phase 4 (approved)	AGTR1
DOFETILIDE	ChEMBL	Phase 4 (approved)	AGTR1
DONEPEZIL	ChEMBL	Phase 4 (approved)	AGTR1
EFAVIRENZ	ChEMBL	Phase 4 (approved)	AGTR1
EPALRESTAT	ChEMBL	Phase 4 (approved)	AGTR1
EPROSARTAN	ChEMBL	Phase 4 (approved)	AGTR1
FELODIPINE	ChEMBL	Phase 4 (approved)	AGTR1
FENTICONAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
GUAIFENESIN	ChEMBL	Phase 4 (approved)	AGTR1
HALOPERIDOL	ChEMBL	Phase 4 (approved)	AGTR1
IBANDRONIC ACID	ChEMBL	Phase 4 (approved)	AGTR1
INDOCYANINE GREEN ACID FORM	ChEMBL	Phase 4 (approved)	AGTR1
IRBESARTAN	ChEMBL	Phase 4 (approved)	AGTR1
IVACAFTOR	ChEMBL	Phase 4 (approved)	AGTR1
LEFLUNOMIDE	ChEMBL	Phase 4 (approved)	AGTR1
LOVASTATIN	ChEMBL	Phase 4 (approved)	AGTR1
MILTEFOSINE	ChEMBL	Phase 4 (approved)	AGTR1
NIFEDIPINE	ChEMBL	Phase 4 (approved)	AGTR1
NIMESULIDE	ChEMBL	Phase 4 (approved)	AGTR1
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	AGTR1
NORGESTIMATE	ChEMBL	Phase 4 (approved)	AGTR1
NOSCAPINE	ChEMBL	Phase 4 (approved)	AGTR1
OXYMETHOLONE	ChEMBL	Phase 4 (approved)	AGTR1
PIMOZIDE	ChEMBL	Phase 4 (approved)	AGTR1
PONATINIB	ChEMBL	Phase 4 (approved)	AGTR1
PRAZOSIN	ChEMBL	Phase 4 (approved)	AGTR1
PROPRANOLOL	ChEMBL	Phase 4 (approved)	AGTR1
PYRVINIUM	ChEMBL	Phase 4 (approved)	AGTR1
RIMONABANT	ChEMBL	Phase 4 (approved)	AGTR1
RITONAVIR	ChEMBL	Phase 4 (approved)	AGTR1
ROCURONIUM	ChEMBL	Phase 4 (approved)	AGTR1
ROSIGLITAZONE	ChEMBL	Phase 4 (approved)	AGTR1
SARALASIN	ChEMBL	Phase 4 (approved)	AGTR1
SELEXIPAG	ChEMBL	Phase 4 (approved)	AGTR1
SIMVASTATIN	ChEMBL	Phase 4 (approved)	AGTR1
SORAFENIB	ChEMBL	Phase 4 (approved)	AGTR1
SULCONAZOLE	ChEMBL	Phase 4 (approved)	AGTR1
SUNITINIB	ChEMBL	Phase 4 (approved)	AGTR1
TELOTRISTAT	ChEMBL	Phase 4 (approved)	AGTR1
TELOTRISTAT ETHYL	ChEMBL	Phase 4 (approved)	AGTR1
TIPRANAVIR	ChEMBL	Phase 4 (approved)	AGTR1