Fimasartan
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Also known as Fimasartan component of br1015Fimasartan component of br1019
Summary
Fimasartan (CHEMBL1951143) is a phase-3 clinical-stage small molecule (ATC C09CA10); indicated across 5 conditions including cardiovascular disorder and hypertensive disorder.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: C09CA10
- Indications: 5 conditions
- Clinical trials: 52
- Chemistry: 501.6 Da · C27H31N7OS
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1951143 |
| Name | Fimasartan |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 9870652 |
| ATC | C09CA10 |
| Molecular formula | C27H31N7OS |
| Molecular weight | 501.6 |
| InChIKey | AMEROGPZOLAFBN-UHFFFAOYSA-N |
SMILES: CCCCC1=NC(=C(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CC(=S)N(C)C)C
IUPAC name: 2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide
Also known as: Fimasartan, Fimasartan component of br1015, Fimasartan component of br1019, FIMASARTAN
Parent form; salt/anhydrous children: CHEMBL1951146
Patent coverage: 229 distinct patent families (580 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 532 (92%) 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
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Type-1 angiotensin II receptor, Type-1 angiotensin II receptor.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P34976 | 9.38 | IC50 | 0.42 | nM | CHEMBL_ACT_8034602 |
| AGTR1 | 8.35 | IC50 | 4.5 | nM | CHEMBL_ACT_18764734 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
5 indications (0 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 |
|---|---|---|---|
| cardiovascular disorder | 3 | MONDO:0004995 | EFO:0000319 |
| hypertensive disorder | 3 | MONDO:0005044 | EFO:0000537 |
| essential hypertension | 3 | MONDO:0001134 | MONDO:0001134 |
| kidney disorder | 1 | MONDO:0005240 | EFO:0003086 |
| hyperlipidemia | 1 | MONDO:0021187 | MONDO:0021187 |
Clinical trials
Total trials: 52.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 23 |
| PHASE3 | 13 |
| PHASE4 | 8 |
| PHASE2 | 5 |
| Not specified | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01384747 | PHASE4 | TERMINATED | Effect of Fimasartan for Modification of Atheroma Vulnerability in DEFERred Coronary Disease (FIMA-DEFER) |
| NCT01589380 | PHASE4 | UNKNOWN | A Randomized Trial of Angiotensin Receptor bLocker,Fimasartan, in Aortic Stenosis (ALFA Trial) |
| NCT01691118 | PHASE4 | COMPLETED | A Trial of Fimasartan for Early Diastolic Heart Failure |
| NCT01736488 | PHASE4 | COMPLETED | Clinical Study to Evaluate the Antihypertensive Efficacy and Changes of Neurohormonal Markers of Fimasartan and Atenolol With Exaggerated Blood Pressure Response During Exercise in Essential Hypertensive Patients |
| NCT02403349 | PHASE4 | UNKNOWN | Comparison of Peripheral and Cerebral Arterial Flow in Acute Ischemic Stroke: Fimasartan vs. Valsartan vs. Atenolol |
| NCT02495324 | PHASE4 | COMPLETED | Fimasartan Achieving SBP Target (FAST) Study |
| NCT02958631 | PHASE4 | UNKNOWN | Comparison of Blood Pressure Lowering Effect Between Fimasartan and Losartan |
| NCT05173025 | PHASE4 | UNKNOWN | Effect of Fimasartan on Extended RAS and Vascular Functions in Patients With Type 2 Diabetes and Hypertension |
| NCT00922480 | PHASE3 | COMPLETED | Clinical Study to Evaluate the Antihypertensive Efficacy and Safety of Fimasartan in Hypertension Patients |
| NCT01135212 | PHASE3 | COMPLETED | The Clinical Study to Evaluate the Efficacy and Safety of Fimasartan in Patients With Mild to Moderate Essential Hypertension |
| NCT01258673 | PHASE3 | COMPLETED | A Clinical Study to Evaluate Efficacy and Safety of Fimasartan/Hydrochlorothiazide Combination-therapy |
| NCT01672476 | PHASE3 | COMPLETED | A Multicenter, Phase 3 Study to Evaluate the Antihypertensive Efficacy and Safety of Fimasartan(BR-A-657∙K) 30mg Compared to Placebo in Patients With Mild to Moderate Essential Hypertension |
| NCT02152306 | PHASE3 | COMPLETED | Fimasartan/Amlodipine Combination Phase III |
| NCT02166814 | PHASE3 | COMPLETED | A Randomized, Double-blind, Multicenter, Phase III Study to Evaluate the Efficacy and Safety of Combination of Fimasartan/Rosuvastatin in Comparison to Each Component Administered Alone in Patients With Essential Hypertension and Dyslipidemia |
| NCT02248961 | PHASE3 | COMPLETED | Efficacy and Safety Evaluating Study to Compare Kanarb (Fimasartan) and Cozaar® (Losartan) in Adult Patients With Grade I-II Arterial Hypertension |
| NCT02466490 | PHASE3 | COMPLETED | Efficacy and Safety of Fimasartan Alone or Combined With HCTZ in Mexican Patients With Essential Hypertension |
| NCT03156842 | PHASE3 | COMPLETED | Combination of Fimasartan/Amlodipine/Rosuvastatin in Patients With Essential Hypertension and Dyslipidemia |
| NCT03338426 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of Combination Treatment of Fimasartan/Atorvastatin in Patients With Essential Hypertension and Dyslipidemia |
| NCT03991442 | PHASE3 | COMPLETED | BR1010 in Patients With Essential Hypertension Patients Who do Not Adequately Respond to Fimasartan/Amlodipine Combination |
| NCT05878561 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of BR1015 Combination Therapy |
| NCT05930028 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy and Safety of BR1017A and BR1017B Combination Therapy in Essential Hypertension Patients With Primary Hypercholesterolemia |
| NCT00923611 | PHASE2 | COMPLETED | Antihypertensive Efficacy and Tolerability and Determine the Adequate Antihypertensive Dosage of Fimasartan in Mild to Moderate Essential Hypertension Patients |
| NCT00937651 | PHASE2 | COMPLETED | Efficacy, Safety and Pharmacodynamic/Pharmacokinetic Study of Fimasartan (BR-A-657•K) |
| NCT01518998 | PHASE2 | COMPLETED | A Randomized, Double-Blind, Placebo-Controlled, 3x3 Factorial Design, Phase II Study to Evaluate the Antihypertensive Efficacy and Safety of Combination of Fimasartan and Amlodipine in Patients With Essential Hypertension |
| NCT01878201 | PHASE2 | COMPLETED | A Valsartan 80 Mg-Referenced, Therapeutic Exploratory Clinical Study to Evaluate the Antihypertensive Efficacy of Fimasartan 30 mg During 24 Hours in Patients With Mild to Moderate Essential Hypertension |
| NCT02222480 | PHASE2 | COMPLETED | A Clinical Trial to Evaluate Efficacy, Tolerability, and Pharmacokinetic-Pharmacodynamic Relationship of Fimasartan/Hydrochlorothiazide |
| NCT00923533 | PHASE1 | COMPLETED | A Study to Evaluate the Safety and Pharmacokinetics After Oral Concurrent Administration of Fimasartan and Hydrochlorothiazide in Healthy Male Volunteers |
| NCT00937534 | PHASE1 | COMPLETED | Study to Compare and Assess the Safety and Pharmacokinetic Characteristics After Oral Administration of Fimasartan (BR-A-657∙K) in Healthy Elderly and Young Male Volunteers |
| NCT00938132 | PHASE1 | COMPLETED | A Clinical Trial to Evaluate the Effect of Fimarsartan on Pharmacodynamics, Pharmacokinetics, and the Safety of Warfarin in Healthy Male Volunteers |
| NCT00938197 | PHASE1 | COMPLETED | A Study to Evaluate the Pharmacokinetic Drug Interaction After Oral Concurrent Administration of Fimasartan and Amlodipine in Healthy Male Volunteers |
| NCT00938262 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Ketoconazole and Rifampicin on the Pharmacokinetics of Fimasartan in Healthy Male Volunteers |
| NCT00991705 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Atorvastatin on the Pharmacokinetics of Fimasartan in Healthy Male Volunteers |
| NCT00991783 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Fimasartan on Pharmacokinetics, and the Safety of Digoxin in Healthy Male Volunteers |
| NCT01007409 | PHASE1 | COMPLETED | A Study to Assess Food Effect on the Pharmacokinetics of Fimasartan in Healthy Male Volunteers |
| NCT01146938 | PHASE1 | COMPLETED | A Clinical Trial to Compare and Evaluate the Pharmacokinetic Characteristics and the Safety of Fimasartan in Hepatic Impairment Patients and Healthy Volunteers |
| NCT01148368 | PHASE1 | COMPLETED | A Clinical Trial to Compare and Evaluate the Pharmacokinetic Characteristics and the Safety of Fimasartan in Renal Impairment Patients and Healthy Volunteers |
| NCT01671020 | PHASE1 | COMPLETED | Clinical Trials for Single Oral Dose of 60mg Fimasartan and Single IV Infusion of 30mg Fimasartan to Evaluate the Absolute Bioavailability of Kanarb® Tablet (Fimasartan) in Healthy Subjects |
| NCT01921946 | PHASE1 | COMPLETED | To Evaluate the Pharmacokinetic Interactions and Safety Between Fimasartan and Rosuvastatin |
| NCT02205151 | PHASE1 | COMPLETED | To Compare the Pharmacokinetics of Fimasartan/Amlodipine Combination Tablet and Coadministration of Fimasartan and Amlodipine as Individual Tablets |
| NCT02205190 | PHASE1 | COMPLETED | to Compare the Pharmacokinetics and Safety of Fimasartan/Rosuvastatin Combination Tablet and Coadministration of Fimasartan and Rosuvastatin |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).