Page last updated: 2024-11-12

etc-1002

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid: inhibits ATP citrate lyase (ACL); has anti-atherosclerotic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bempedoic acid : An alpha,omega-dicarboxylic acid that is pentadecanedioic acid which is substituted by methyl groups groups at positions 2 and 14, and by a hydroxy group at position 8. It is a drug used for the treatment of high LDL cholesterol, which is sometimes referred to as 'bad cholesterol'. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID10472693
CHEMBL ID3545313
CHEBI ID149601
SCHEMBL ID185768
MeSH IDM0585022

Synonyms (58)

Synonym
CHEBI:149601 ,
esp 55016
bempedoic acid
etc 1002
acide bempedoique
etc1002
etc-1002
nexletol
acidum bempedoicum
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid
738606-46-7
esp-55016
acido bempedoico
bempedoate
1ej6z6q368 ,
esp55016
pentadecanedioic acid, 8-hydroxy-2,2,14,14-tetramethyl-
bempedoic acid [usan:inn]
nilemdo
unii-1ej6z6q368
nexlizet component bempedoic acid
bempedoic acid [who-dd]
bempedoic acid [inn]
bempedoic acid [usan]
bempedoic acid [jan]
bempedoic acid [orange book]
bempedoic acid component of nexlizet
S7953
SCHEMBL185768
HYHMLYSLQUKXKP-UHFFFAOYSA-N
CS-3952
bempedoic acid (usan/inn)
D10691
nexletol (tn)
gtpl8321
HY-12357
AC-29040
c19h36o5
CHEMBL3545313
EX-A1243
AKOS027439916
mfcd18800820
bempedoic acid(etc-1002;esp-55016)
DB11936
BCP16083
bempedoic acid|esp-55016
AS-49804
Q27075007
etc-1002;esp-55016
bempedoic-acid
AMY31933
CCG-267969
8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid;etc-1002
A905695
N10681
SY244715
DTXSID401027952
c10ax15

Research Excerpts

Toxicity

ETC-1002 significantly lowered LDL-C levels up to 27% across a broad range of baseline triglycerides and was generally safe and well tolerated. The ETC- 1002 and placebo groups did not demonstrate clinically meaningful differences in adverse events or other safety assessments.

ExcerptReferenceRelevance
" The ETC-1002 and placebo groups did not demonstrate clinically meaningful differences in adverse events or other safety assessments."( Efficacy and safety of a novel dual modulator of adenosine triphosphate-citrate lyase and adenosine monophosphate-activated protein kinase in patients with hypercholesterolemia: results of a multicenter, randomized, double-blind, placebo-controlled, paral
Ballantyne, CM; Bays, HE; Davidson, MH; Dicarlo, LA; Macdougall, DE; Margulies, J; Newton, RS; Rosenberg, NL, 2013
)
0.9
"ETC-1002 significantly lowered LDL-C levels up to 27% across a broad range of baseline triglycerides and was generally safe and well tolerated."( Efficacy and safety of a novel dual modulator of adenosine triphosphate-citrate lyase and adenosine monophosphate-activated protein kinase in patients with hypercholesterolemia: results of a multicenter, randomized, double-blind, placebo-controlled, paral
Ballantyne, CM; Bays, HE; Davidson, MH; Dicarlo, LA; Macdougall, DE; Margulies, J; Newton, RS; Rosenberg, NL, 2013
)
1.83
" Bempedoic acid was well tolerated; rates of treatment-emergent adverse events, muscle-related adverse events, and discontinuations were similar in the bempedoic acid and placebo treatment groups."( Efficacy and safety of bempedoic acid added to ezetimibe in statin-intolerant patients with hypercholesterolemia: A randomized, placebo-controlled study.
Ballantyne, CM; Banach, M; Hanselman, JC; Leiter, LA; Lepor, NE; Mancini, GBJ; Zhao, X, 2018
)
0.48
"Due to the myopathic adverse events of statins, safer alternatives are being studied."( Safety and efficacy of ETC-1002 in hypercholesterolaemic patients: a meta-analysis of randomised controlled trials.
Gan, X; He, C; Huang, R; Luo, S; Wang, X,
)
0.44
"ETC-1002 is a safe and effective lipid-lowering agent and may be a suitable alternative in statin-intolerant pa-tients."( Safety and efficacy of ETC-1002 in hypercholesterolaemic patients: a meta-analysis of randomised controlled trials.
Gan, X; He, C; Huang, R; Luo, S; Wang, X,
)
1.88
" The incidence of adverse events (1167 of 1487 patients [78."( Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol.
Ballantyne, CM; Bays, HE; Bloedon, LT; Catapano, AL; Lalwani, ND; Ray, KK; Robinson, PL; Sterling, LR, 2019
)
0.51
"In this 52-week trial, bempedoic acid added to maximally tolerated statin therapy did not lead to a higher incidence of overall adverse events than placebo and led to significantly lower LDL cholesterol levels."( Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol.
Ballantyne, CM; Bays, HE; Bloedon, LT; Catapano, AL; Lalwani, ND; Ray, KK; Robinson, PL; Sterling, LR, 2019
)
0.51
" Bempedoic acid was safe and well tolerated."( Efficacy and Safety of Bempedoic Acid in Patients With Hypercholesterolemia and Statin Intolerance.
Banach, M; Bloedon, LT; Gaudet, D; Kelly, S; Laufs, U; Mancini, GBJ; Sterling, LR; Stroes, ESG, 2019
)
0.51
" BA-treated subjects reported a higher rate of treatment discontinuation caused by adverse effects, of gout flare, and of increase in uric acid compared with controls."( Efficacy and Safety of Bempedoic Acid in Patients With Hypercholesterolemia: Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Ambrosino, P; Calcaterra, I; Di Minno, A; Di Minno, MND; Forte, F; Iannuzzo, G; Lupoli, R; Poggio, P; Spadarella, G, 2020
)
0.56
" The primary outcomes were major adverse cardiac events, and percent change in LDL-C."( Efficacy and safety of bempedoic acid for prevention of cardiovascular events and diabetes: a systematic review and meta-analysis.
Chong, W; Fang, F; Tan, H; Wang, P; Wang, X; Zha, X; Zhang, Y; Zhou, L, 2020
)
0.56
"An ongoing need exists for safe and effective lipid-lowering therapies (LLTs) for patients unable to achieve desired lipid levels with current treatment options."( Bempedoic acid safety analysis: Pooled data from four phase 3 clinical trials.
Ballantyne, CM; Banach, M; Bays, HE; Bloedon, LT; Catapano, AL; Duell, PB; Gotto, AM; Laufs, U; Leiter, LA; Mancini, GBJ; Ray, KK; Sasiela, WJ; Ye, Z,
)
0.13
" Assessments included treatment-emergent adverse events (TEAEs) and clinical laboratory tests."( Bempedoic acid safety analysis: Pooled data from four phase 3 clinical trials.
Ballantyne, CM; Banach, M; Bays, HE; Bloedon, LT; Catapano, AL; Duell, PB; Gotto, AM; Laufs, U; Leiter, LA; Mancini, GBJ; Ray, KK; Sasiela, WJ; Ye, Z,
)
0.13
"Bempedoic acid is generally safe and well tolerated among patients with hypercholesterolemia who require additional LLT."( Bempedoic acid safety analysis: Pooled data from four phase 3 clinical trials.
Ballantyne, CM; Banach, M; Bays, HE; Bloedon, LT; Catapano, AL; Duell, PB; Gotto, AM; Laufs, U; Leiter, LA; Mancini, GBJ; Ray, KK; Sasiela, WJ; Ye, Z,
)
0.13
" Odds ratio (OR) of the incidence of adverse events (AEs) were calculated to evaluate the safety of bempedoic acid."( Efficacy and safety of bempedoic acid alone or combining with other lipid-lowering therapies in hypercholesterolemic patients: a meta-analysis of randomized controlled trials.
Deng, Z; Jiang, S; Jin, Y; Liu, P; Luo, X; Ma, X; Qiu, C; Shi, Z; Shu, Y; Tan, L; Tang, B; Xiao, Z; Zhao, X, 2020
)
0.56
"Primary efficacy outcomes were major adverse cardiovascular events (MACE), all-cause mortality, CV mortality and non-fatal myocardial infarction (MI)."( Clinical efficacy and safety outcomes of bempedoic acid for LDL-C lowering therapy in patients at high cardiovascular risk: a systematic review and meta-analysis.
Brockmeyer, M; Chernyak, N; Icks, A; Karathanos, A; Kelm, M; Krieger, T; Lin, Y; Parco, C; Schulze, V; Wolff, G, 2022
)
0.72
" Safety and tolerability were assessed by laboratory values and adverse events."( Efficacy and safety of bempedoic acid in patients not receiving statins in phase 3 clinical trials.
Ballantyne, CM; Banach, M; Bays, H; Bloedon, LT; Catapano, AL; Duell, PB; Goldberg, AC; Gotto, AM; Laufs, U; Leiter, LA; MacDougall, D; Mancini, GBJ; Ray, KK; Zhang, Y,
)
0.13
" Safety assessments included treatment-emergent adverse events, adverse events of special interest, and clinical laboratory abnormalities."( Long-Term Safety and Efficacy of Bempedoic Acid in Patients With Atherosclerotic Cardiovascular Disease and/or Heterozygous Familial Hypercholesterolemia (from the CLEAR Harmony Open-Label Extension Study).
Ballantyne, CM; Banach, M; Bays, HE; Catapano, AL; Laufs, U; Lei, L; Ray, KK; Robinson, P; Stroes, ESG, 2022
)
0.72
" Bempedoic acid was generally safe and well tolerated up to a dose of 220 mg/day across the study populations described herein."( Phase 1, Single- and Multiple-Ascending-Dose, Food-Effect, and East Asian Subject Studies to Assess the Pharmacokinetics, Safety, and Tolerability of Bempedoic Acid, a Selective Inhibitor of Adenosine Triphosphate Citrate Lyase.
Amore, BM; Emery, MG; Hanselman, JC; MacDougall, DE, 2023
)
0.91
" The primary outcome was major adverse cardiovascular events (MACE), and secondary outcomes were all-cause mortality, serum lipid profile, and adverse events between bempedoic acid and comparators."( Efficacy and safety of bempedoic acid lipid-lowering therapy: a systematic review and meta-analysis of randomized controlled trials.
Bagepally, BS; Cherian, JJ; Das, S; Eerike, M; Venkatraman, S, 2023
)
0.91
" Major adverse cardiovascular events (MACE) were the primary efficacy endpoint."( Safety and efficacy of bempedoic acid: a systematic review and meta-analysis of randomised controlled trials.
Bertaina, M; Biondi Zoccai, G; Borzillo, I; Brizzi, MF; Bruno, F; D'Ascenzo, F; De Ferrari, GM; De Filippo, O; Giacobbe, F; Iannaccone, M; Leone, A; Monticone, S; Muscoli, S; Nebiolo, M; Pagliassotto, I; Ravetti, E; Solano, A, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Because pharmacodynamic interaction between statins and bempedoic acid is complex, a dose-response model was developed to predict LDL-C pharmacodynamics following administration of statins combined with bempedoic acid."( Pharmacodynamic effect of bempedoic acid and statin combinations: predictions from a dose-response model.
Amore, BM; Barrett, PHR; Catapano, AL; Chapel, S; Crass, RL; Emery, MG; Jadhav, SB; Kerschnitzki, M; Sasiela, WJ; Watts, GF, 2022
)
0.72
"6 µg/mL, area under the concentration-time curve over 24 hours of 289 µg·h/mL, and elimination half-life of 21."( Phase 1, Single- and Multiple-Ascending-Dose, Food-Effect, and East Asian Subject Studies to Assess the Pharmacokinetics, Safety, and Tolerability of Bempedoic Acid, a Selective Inhibitor of Adenosine Triphosphate Citrate Lyase.
Amore, BM; Emery, MG; Hanselman, JC; MacDougall, DE, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" These observed decreases in total and unbound oral clearance in subjects with decreased renal function are not explained by the increases in free fraction and might therefore also be attributable to changes in bioavailability or intrinsic clearance."( Pharmacokinetics of bempedoic acid in patients with renal impairment.
Amore, BM; Emery, MG; Ries, DK; Sasiela, WJ; Tresh, P, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" Atorvastatin and metabolites' steady-state levels were analyzed before first dosing with bempedoic acid and after 2 weeks of treatment."( Complementary low-density lipoprotein-cholesterol lowering and pharmacokinetics of adding bempedoic acid (ETC-1002) to high-dose atorvastatin background therapy in hypercholesterolemic patients: A randomized placebo-controlled trial.
Cramer, CT; Hanselman, JC; Lalwani, ND; MacDougall, DE; Sterling, LR,
)
0.34
" Bempedoic acid given at a dosage of 180 mg orally once daily produces a highly significant reduction in low-density lipoprotein cholesterol (LDL-C), non-high-density lipoprotein cholesterol, total cholesterol, apolipoprotein B and importantly also in high-sensitivity C-reactive protein."( Bempedoic acid: effect of ATP-citrate lyase inhibition on low-density lipoprotein cholesterol and other lipids.
Paton, DM, 2020
)
0.56
" Because pharmacodynamic interaction between statins and bempedoic acid is complex, a dose-response model was developed to predict LDL-C pharmacodynamics following administration of statins combined with bempedoic acid."( Pharmacodynamic effect of bempedoic acid and statin combinations: predictions from a dose-response model.
Amore, BM; Barrett, PHR; Catapano, AL; Chapel, S; Crass, RL; Emery, MG; Jadhav, SB; Kerschnitzki, M; Sasiela, WJ; Watts, GF, 2022
)
0.72
"Bempedoic acid and statin dosing and LDL-C data were pooled from 14 phase 1-3 clinical studies."( Pharmacodynamic effect of bempedoic acid and statin combinations: predictions from a dose-response model.
Amore, BM; Barrett, PHR; Catapano, AL; Chapel, S; Crass, RL; Emery, MG; Jadhav, SB; Kerschnitzki, M; Sasiela, WJ; Watts, GF, 2022
)
0.72
" Comparisons of bempedoic acid 180 mg/day pharmacokinetics after single and multiple dosing revealed no clinically meaningful differences between Japanese, Chinese, and Western subjects."( Phase 1, Single- and Multiple-Ascending-Dose, Food-Effect, and East Asian Subject Studies to Assess the Pharmacokinetics, Safety, and Tolerability of Bempedoic Acid, a Selective Inhibitor of Adenosine Triphosphate Citrate Lyase.
Amore, BM; Emery, MG; Hanselman, JC; MacDougall, DE, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antilipemic drugA substance used to treat hyperlipidemia (an excess of lipids in the blood).
EC 2.3.3.8 (ATP citrate synthase) inhibitorAn EC 2.3.3.* (acyltransferase converting acyl to alkyl group on transfer) inhibitor that interferes with the action of ATP citrate synthase (EC 2.3.3.8).
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
alpha,omega-dicarboxylic acid
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (175)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's30 (17.14)24.3611
2020's145 (82.86)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.66 (24.57)
Research Supply Index5.41 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index35.22 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials25 (12.69%)5.53%
Reviews74 (37.56%)6.00%
Case Studies2 (1.02%)4.05%
Observational1 (0.51%)0.25%
Other95 (48.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]