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Details

Stereochemistry ACHIRAL
Molecular Formula C19H36O5
Molecular Weight 344.4861
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BEMPEDOIC ACID

SMILES

CC(C)(CCCCCC(O)CCCCCC(C)(C)C(O)=O)C(O)=O

InChI

InChIKey=HYHMLYSLQUKXKP-UHFFFAOYSA-N
InChI=1S/C19H36O5/c1-18(2,16(21)22)13-9-5-7-11-15(20)12-8-6-10-14-19(3,4)17(23)24/h15,20H,5-14H2,1-4H3,(H,21,22)(H,23,24)

HIDE SMILES / InChI
Bempedoic acid (also known as ETC-1002) is a novel investigational drug being developed for the treatment of dyslipidemia, hypercholesterolemia and other cardio-metabolic risk factors. The hypolipidemic, anti-atherosclerotic, anti-obesity, and glucose-lowering properties of ETC-1002, characterized in preclinical disease models, are believed to be due to dual inhibition of sterol and fatty acid synthesis and enhanced mitochondrial long-chain fatty acid β-oxidation. Investigations into the mechanism of action revealed that bempedoic acid-free acid activates AMP-activated protein kinase in a Ca(2+)/calmodulin-dependent kinase β-independent and liver kinase β-1-dependent manner, without detectable changes in adenylate energy charge. In the liver, bempedoic acid is also converted to a coenzyme A (CoA) derivative (ETC-1002-CoA )which directly inhibits ATP citrate lyase (ACL), a key enzyme that supplies a substrate for cholesterol and fatty acid synthesis in the liver. Inhibition of ACL by ETC-1002-CoA results in reduced cholesterol synthesis and upregulation of LDL receptor activity in the liver. This promotes the removal of LDL-C from the blood.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P53396
Gene ID: 47.0
Gene Symbol: ACLY
Target Organism: Homo sapiens (Human)
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
20.6 μg/mL
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BEMPEDOIC ACID plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
289 μg × h/mL
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BEMPEDOIC ACID plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
21 h
180 mg 1 times / day steady-state, oral
dose: 180 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
BEMPEDOIC ACID plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Disc. AE: Muscle spasms, Pain in extremity...
Other AEs: Upper respiratory tract infection, Muscle spasms...
AEs leading to
discontinuation/dose reduction:
Muscle spasms (0.5%)
Pain in extremity (0.3%)
Diarrhea (0.4%)
Other AEs:
Upper respiratory tract infection (4.5%)
Muscle spasms (3.6%)
Hyperuricemia (3.5%)
Back pain (3.3%)
Abdominal pain (3.1%)
Bronchitis (3%)
Pain in extremity (3%)
Anemia (2.8%)
Elevated liver enzymes (2.1%)
Sources:
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Disc. AE: Muscle spasms, Myalgia...
Other AEs: Blood uric acid increased, Headache...
AEs leading to
discontinuation/dose reduction:
Muscle spasms (0.55%)
Myalgia (0.55%)
Pain in extremity (0.55%)
Other AEs:
Blood uric acid increased (grade 1-2, 7.7%)
Headache (grade 1-2, 4.4%)
Urinary tract infection (grade 1-2, 2.8%)
Liver function test increased (grade 1-2, 3.9%)
Nausea (grade 1-2, 2.8%)
Sinusitis (grade 1-2, 2.8%)
Nasopharyngitis (grade 1-2, 2.2%)
Glomerular filtration rate decreased (grade 1-2, 2.2%)
Diabetes mellitus (grade 1-2, 1.1%)
Muscle spasms (grade 1-2, 3.3%)
Myalgia (grade 1-2, 1.7%)
Transaminases increased (grade 1-2, 3.9%)
Muscular weakness (grade 1-2, 0.6%)
Pain in extremity (grade 1-2, 0.6%)
Sources:
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Disc. AE: Myalgia...
Other AEs: Arthralgia, Hypertension...
AEs leading to
discontinuation/dose reduction:
Myalgia (3.4%)
Other AEs:
Arthralgia (grade 1-2, 6%)
Hypertension (grade 1-2, 4.3%)
Fatigue (grade 1-2, 3.4%)
Urinary tract infection (grade 1-2, 3.4%)
Back pain (grade 1-2, 3%)
Dizziness (grade 1-2, 3%)
Bronchitis (grade 1-2, 2.6%)
Blood creatine phosphokinase increased (grade 1-2, 2.1%)
Dyspepsia (grade 1-2, 2.1%)
Pain in extremity (grade 1-2, 5.6%)
Myalgia (grade 1-2, 4.7%)
Muscle spasms (grade 1-2, 4.3%)
Muscular weakness (grade 1-2, 0.4%)
Gout (grade 1-2, 1.7%)
Transaminases increased (grade 1-2, 1.7%)
Sources:
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, adults
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 2009
Sources:
Other AEs: Tendon rupture, Gout...
Other AEs:
Tendon rupture (0.5%)
Gout (1.5%)
Benign prostatic hyperplasia (1.3%)
Atrial fibrillation (1.7%)
Sources:
220 mg 1 times / day multiple, oral
Highest studied dose
Dose: 220 mg, 1 times / day
Route: oral
Route: multiple
Dose: 220 mg, 1 times / day
Sources:
healthy
240 mg 1 times / day steady, oral
Highest studied dose
Dose: 240 mg, 1 times / day
Route: oral
Route: steady
Dose: 240 mg, 1 times / day
Sources:
unhealthy
n = 36
Health Status: unhealthy
Condition: hypercholesterolemia
Population Size: 36
Sources:
250 mg 1 times / day single, oral
Highest studied dose
Dose: 250 mg, 1 times / day
Route: oral
Route: single
Dose: 250 mg, 1 times / day
Sources:
healthy
n = 9
AEs

AEs

AESignificanceDosePopulation
Pain in extremity 0.3%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Diarrhea 0.4%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Muscle spasms 0.5%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Elevated liver enzymes 2.1%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Anemia 2.8%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Bronchitis 3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Pain in extremity 3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Abdominal pain 3.1%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Back pain 3.3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Hyperuricemia 3.5%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Muscle spasms 3.6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Upper respiratory tract infection 4.5%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, 65.4 years
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: 65.4 years
Sex: M+F
Population Size: 2009
Sources:
Muscle spasms 0.55%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Myalgia 0.55%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Pain in extremity 0.55%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Muscular weakness grade 1-2, 0.6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Pain in extremity grade 1-2, 0.6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Diabetes mellitus grade 1-2, 1.1%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Myalgia grade 1-2, 1.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Glomerular filtration rate decreased grade 1-2, 2.2%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Nasopharyngitis grade 1-2, 2.2%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Nausea grade 1-2, 2.8%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Sinusitis grade 1-2, 2.8%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Urinary tract infection grade 1-2, 2.8%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Muscle spasms grade 1-2, 3.3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Liver function test increased grade 1-2, 3.9%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Transaminases increased grade 1-2, 3.9%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Headache grade 1-2, 4.4%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Blood uric acid increased grade 1-2, 7.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
ezetimibe(10 mg/day; oral; 4 weeks)
Sources:
unhealthy, adults
n = 181
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 181
Sources:
Myalgia 3.4%
Disc. AE
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Muscular weakness grade 1-2, 0.4%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Gout grade 1-2, 1.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Transaminases increased grade 1-2, 1.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Blood creatine phosphokinase increased grade 1-2, 2.1%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Dyspepsia grade 1-2, 2.1%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Bronchitis grade 1-2, 2.6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Back pain grade 1-2, 3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Dizziness grade 1-2, 3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Fatigue grade 1-2, 3.4%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Urinary tract infection grade 1-2, 3.4%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Hypertension grade 1-2, 4.3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Muscle spasms grade 1-2, 4.3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Myalgia grade 1-2, 4.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Pain in extremity grade 1-2, 5.6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Arthralgia grade 1-2, 6%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Sources:
unhealthy, adults
n = 234
Health Status: unhealthy
Condition: hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 234
Sources:
Tendon rupture 0.5%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, adults
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 2009
Sources:
Benign prostatic hyperplasia 1.3%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, adults
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 2009
Sources:
Gout 1.5%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, adults
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 2009
Sources:
Atrial fibrillation 1.7%
180 mg 1 times / day steady, oral
Recommended
Dose: 180 mg, 1 times / day
Route: oral
Route: steady
Dose: 180 mg, 1 times / day
Co-administed with::
Statin
Other Lipid Lowering Therapies
Sources:
unhealthy, adults
n = 2009
Health Status: unhealthy
Condition: atherosclerotic cardiovascular disease & heterozygous familial hypercholesterolemia
Age Group: adults
Sex: M+F
Population Size: 2009
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
PubMed

PubMed

TitleDatePubMed
Cloning and expression of a human ATP-citrate lyase cDNA.
1992 Mar 1
Patents

Sample Use Guides

ETC-1002 (BEMPEDOIC ACID) 180 mg tablets taken orally, once per day.
Route of Administration: Oral
Consistent with ETC-1002-induced AMPK activation observed in rat liver, HepG2 cells treated with ETC-1002 (100 uM) revealed a sustained and concentration-dependent increase in AMPK (T172) and ACC (S79) phosphorylation comparable to the AMPK-activating effect of metformin (1,000 μM). To further characterize the mechanism leading to AMPK activation by ETC-1002, HepG2 cells were pretreated with STO-609, an AMPK kinase Ca2+/calmodulin-dependent kinase β (CaMKKβ)-specific inhibitor. STO-609 did not significantly reduce AMPK or ACC phosphorylation in ETC-1002- or metformin-treated cells, indicating that AMPK activation is not dependent on intracellular Ca2+ signaling. Intriguingly, while the ATP analog and AMPK inhibitor, compound C, significantly reduced AMPK and ACC phosphorylation by metformin, it did not inhibit ETC-1002-dependent AMPK activation. To determine whether ETC-1002-dependent AMPK activation is associated with reductions in AEC, intracellular ATP, ADP, and AMP concentrations were measured in HepG2 cells treated with vehicle, rotenone (10 μM), or ETC-1002 (100 μM). Treatment with rotenone (complex I inhibitor) resulted in increased AMP and ADP levels and in reduced ATP levels and AEC compared with vehicle treatment, while ETC-1002 had no effect. These data suggest that the activation of the AMPK pathway by ETC-1002 may be independent of reductions in energy production.
Name Type Language
BEMPEDOIC ACID
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
PENTADECANEDIOIC ACID, 8-HYDROXY-2,2,14,14-TETRAMETHYL-
Common Name English
BEMPEDOIC ACID [ORANGE BOOK]
Common Name English
8-Hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
Systematic Name English
NEXLIZET COMPONENT BEMPEDOIC ACID
Brand Name English
ETC1002
Code English
NEXLETOL
Brand Name English
ETC-1002
Code English
ESP-55016
Code English
BEMPEDOIC ACID [USAN]
Common Name English
Bempedoic acid [WHO-DD]
Common Name English
BEMPEDOIC ACID [JAN]
Common Name English
BEMPEDOIC ACID COMPONENT OF NEXLIZET
Brand Name English
bempedoic acid [INN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 812621
Created by admin on Fri Dec 15 19:39:04 GMT 2023 , Edited by admin on Fri Dec 15 19:39:04 GMT 2023
Code System Code Type Description
FDA UNII
1EJ6Z6Q368
Created by admin on Fri Dec 15 19:39:04 GMT 2023 , Edited by admin on Fri Dec 15 19:39:04 GMT 2023
PRIMARY
PUBCHEM
10472693
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PRIMARY
EPA CompTox
DTXSID401027952
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PRIMARY
ChEMBL
CHEMBL3545313
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PRIMARY
DAILYMED
1EJ6Z6Q368
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PRIMARY
SMS_ID
100000169469
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PRIMARY
EVMPD
SUB183128
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PRIMARY
CHEBI
149601
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PRIMARY
USAN
B-131
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PRIMARY
NCI_THESAURUS
C166494
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PRIMARY
DRUG BANK
DB11936
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PRIMARY
LACTMED
Bempedoic Acid
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PRIMARY
DRUG CENTRAL
5382
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PRIMARY
CAS
738606-46-7
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PRIMARY
INN
9891
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PRIMARY
RXCUI
2282403
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PRIMARY
WIKIPEDIA
Bempedoic acid
Created by admin on Fri Dec 15 19:39:04 GMT 2023 , Edited by admin on Fri Dec 15 19:39:04 GMT 2023
PRIMARY