Research graph
References from Oral PCSK9 inhibitors: closing the gap between potency and practicality. Local targets link to admitted publications; unresolved targets remain external evidence.
Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170 000 participants in 26 randomised trials
10.1016/s0140-6736(10)61350-5 · 2010 · External reference
2026 ACC/AHA/AACVPR/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of dyslipidemia: a report of the American College of Cardiology/American Heart Association Joint Committee on Clinical Practice Guidelines
10.1016/j.jacc.2025.11.016 · 2026 · External reference
Prevalence of statin intolerance: a meta-analysis
10.1093/eurheartj/ehac015 · 2022 · External reference
Early ezetimibe initiation after myocardial infarction protects against later cardiovascular outcomes in the SWEDEHEART Registry
10.1016/j.jacc.2025.02.007 · 2025 · External reference
Achievement of LDL-C <55 mg/dl among US adults: findings from the cvMOBIUS2 registry
10.1016/j.ahj.2024.06.012 · 2025 · External reference
PCSK9 monoclonal antibodies for the primary and secondary prevention of cardiovascular disease
2020 · External reference
Evolocumab and clinical outcomes in patients with cardiovascular disease
10.1056/nejmoa1615664 · 2017 · External reference
Alirocumab and cardiovascular outcomes after acute coronary syndrome
10.1056/nejmoa1801174 · 2018 · External reference
PCSK9: a key modulator of cardiovascular health
10.1161/circresaha.114.301621 · 2014 · External reference
A 52-week placebo-controlled trial of evolocumab in hyperlipidemia
10.1056/nejmoa1316222 · 2014 · External reference
Efficacy and safety of alirocumab in reducing lipids and cardiovascular events
10.1056/nejmoa1501031 · 2015 · External reference
Evolocumab in patients without a previous myocardial infarction or stroke
10.1056/nejmoa2514428 · 2026 · External reference
Efficacy and Safety of lerodalcibep in patients with or at high risk of cardiovascular disease: a randomized clinical trial
10.1001/jamacardio.2024.1659 · 2024 · External reference
Pooled patient-level analysis of inclisiran trials in patients with familial hypercholesterolemia or atherosclerosis
10.1016/j.jacc.2020.12.058 · 2021 · External reference
Prescriber uptake and use of novel lipid-lowering therapies
10.1161/jaha.125.040768 · 2025 · External reference
Contemporary national patterns of eligibility and use of novel lipid-lowering therapies in the United States
10.1161/jaha.122.026075 · 2022 · External reference
Trends in PCSK9 inhibitor prescriptions before and after the price reduction in patients with atherosclerotic cardiovascular disease
10.3390/jcm10173828 · 2021 · External reference
Use of lipid-lowering therapies over 2 years in GOULD, a registry of patients with atherosclerotic cardiovascular disease in the US
10.1001/jamacardio.2021.1810 · 2021 · External reference
Overcoming barriers to adherence through innovative injectable medications: a systematic review of therapeutic options for cardiovascular disease, reported adherence, and perspectives on their use
10.1002/bcp.70286 · 2026 · External reference
Patients’ perceptions on the facilitators and barriers using injectable therapies in dyslipidaemia: an empirical qualitative descriptive international study
10.1111/jan.15739 · 2023 · External reference
A placebo-controlled trial of the oral PCSK9 inhibitor enlicitide
10.1056/nejmoa2511002 · 2026 · External reference
Phase 2b randomized trial of the oral PCSK9 inhibitor MK-0616
10.1016/j.jacc.2023.02.018 · 2023 · External reference
Efficacy and safety of oral PCSK9 inhibitor enlicitide in adults with heterozygous familial hypercholesterolemia
10.1001/jama.2025.20620 · 2026 · External reference
MK-0616: an oral PCSK9 inhibitor for hypercholesterolemia treatment
10.1080/13543784.2023.2267972 · 2023 · External reference
An overview of the clinical pharmacology of enlicitide decanoate: a first-in-class oral PCSK9 inhibitor
2026 · External reference
Pharmacokinetics and pharmacokinetic-pharmacodynamic correlations of therapeutic peptides
10.1007/s40262-013-0079-0 · 2013 · External reference
Discovery process of enlicitide, a highly engineered macrocyclic peptide therapeutic, through issue-driven fragment-based synthetic assembly and SAR
10.1021/acs.jmedchem.6c00463 · 2026 · External reference
Metabolism of peptide drugs and strategies to improve their metabolic stability
10.2174/1389200219666180628171531 · 2018 · External reference
Phase 1 update: the novel oral PCSK9 inhibitor enlicitide does not affect the pharmacokinetics of narrow therapeutic index concomitant medications
10.1016/j.jacc.2026.02.664 · 2026 · External reference
Phase 1 evaluation of pharmacokinetic drug-drug interactions between enlicitide and multiple concomitant medications
2026 · External reference
Oral PCSK9 Inhibitor Enlicitide Versus Oral Nonstatin Therapies
10.1016/j.jacc.2026.03.036 · 2026 · External reference
Laroprovstat, the first oral small-molecule PCSK9 inhibitor for the treatment of hypercholesterolemia: results from a randomized, single-blind, placebo-controlled phase 1 trial in treatment-naive patients
10.1161/circulationaha.125.075973 · 2026 · External reference
An oral PCSK9 inhibitor for treatment of hypercholesterolemia
10.1016/j.jacc.2025.03.499 · 2025 · External reference
Pharmacokinetics, disposition, and biotransformation of laroprovstat in humans: in vivo and in vitro evaluations
10.1002/jcph.70162 · 2026 · External reference
PCSK9 inhibition with orally administered NNC0385-0434 in hypercholesterolaemia: a randomised, double-blind, placebo-controlled and active-controlled phase 2 trial
10.1016/s2213-8587(23)00325-x · 2024 · External reference
Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial
10.1016/j.cmet.2022.03.006 · 2022 · External reference
New frontiers in the treatment of hypercholesterolaemia: oral inhibition of PCSK9
10.1093/eurheartjsupp/suag035 · 2026 · External reference
Ezetimibe added to statin therapy after acute coronary syndromes
10.1056/nejmoa1410489 · 2015 · External reference
Bempedoic acid and cardiovascular outcomes in statin-intolerant patients
10.1056/nejmoa2215024 · 2023 · External reference
Phase 3 study results for oral PCSK9 inhibition with enlicitide
10.1016/j.medj.2026.101097 · 2026 · External reference
Association of prior authorization and out-of-pocket costs with patient access to PCSK9 inhibitor therapy
10.1001/jamacardio.2017.3451 · 2017 · External reference
Cost-effectiveness of PCSK9 inhibitor therapy in patients with heterozygous familial hypercholesterolemia or atherosclerotic cardiovascular disease
10.1001/jama.2016.11004 · 2016 · External reference
Updated cost-effectiveness analysis of evolocumab in patients with very high-risk atherosclerotic cardiovascular disease
10.1001/jamacardio.2019.1647 · 2019 · External reference
Cost-effectiveness of alirocumab in patients with acute coronary syndromes
10.1016/j.jacc.2020.03.029 · 2020 · External reference
Prior authorization requirements for proprotein convertase subtilisin/kexin type 9 inhibitors across US private and public payers
10.1161/circoutcomes.117.003939 · 2018 · External reference
Have the major cardiovascular outcomes trials impacted payer approval rates for PCSK9 inhibitors?
10.1161/circoutcomes.119.006019 · 2020 · External reference
Individualized low-density lipoprotein cholesterol reduction with alirocumab titration strategy in heterozygous familial hypercholesterolemia: results from an open-label extension of the ODYSSEY LONG TERM trial
10.1016/j.jacl.2018.11.007 · 2019 · External reference
Long-term evolocumab in patients with established atherosclerotic cardiovascular disease
10.1161/circulationaha.122.061620 · 2022 · External reference
Oral PCSK9 inhibitors
10.1016/j.jacc.2025.03.518 · 2025 · External reference
Effect of statin therapy on plasma proprotein convertase subtilisin kexin 9 (PCSK9) concentrations: a systematic review and meta-analysis of clinical trials
10.1111/dom.12536 · 2015 · External reference
Efficacy of alirocumab according to background statin type and dose: pooled analysis of 8 ODYSSEY Phase 3 clinical trials
10.1038/srep45788 · 2017 · External reference
Cost-effectiveness of PCSK9 inhibitor therapy in patients with heterozygous familial hypercholesterolemia or atherosclerotic cardiovascular disease
10.1001/jama.2016.11004 · ExternalCitation · doi-reference
Efficacy and safety of oral PCSK9 inhibitor enlicitide in adults with heterozygous familial hypercholesterolemia
10.1001/jama.2025.20620 · ExternalCitation · doi-reference
Association of prior authorization and out-of-pocket costs with patient access to PCSK9 inhibitor therapy
10.1001/jamacardio.2017.3451 · ExternalCitation · doi-reference
Updated cost-effectiveness analysis of evolocumab in patients with very high-risk atherosclerotic cardiovascular disease
10.1001/jamacardio.2019.1647 · ExternalCitation · doi-reference
Use of lipid-lowering therapies over 2 years in GOULD, a registry of patients with atherosclerotic cardiovascular disease in the US
10.1001/jamacardio.2021.1810 · ExternalCitation · doi-reference
Efficacy and Safety of lerodalcibep in patients with or at high risk of cardiovascular disease: a randomized clinical trial
10.1001/jamacardio.2024.1659 · ExternalCitation · doi-reference
Overcoming barriers to adherence through innovative injectable medications: a systematic review of therapeutic options for cardiovascular disease, reported adherence, and perspectives on their use
10.1002/bcp.70286 · ExternalCitation · doi-reference
Pharmacokinetics, disposition, and biotransformation of laroprovstat in humans: in vivo and in vitro evaluations
10.1002/jcph.70162 · ExternalCitation · doi-reference
Pharmacokinetics and pharmacokinetic-pharmacodynamic correlations of therapeutic peptides
10.1007/s40262-013-0079-0 · ExternalCitation · doi-reference
Achievement of LDL-C <55 mg/dl among US adults: findings from the cvMOBIUS2 registry
10.1016/j.ahj.2024.06.012 · ExternalCitation · doi-reference
Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial
10.1016/j.cmet.2022.03.006 · ExternalCitation · doi-reference
Cost-effectiveness of alirocumab in patients with acute coronary syndromes
10.1016/j.jacc.2020.03.029 · ExternalCitation · doi-reference
Pooled patient-level analysis of inclisiran trials in patients with familial hypercholesterolemia or atherosclerosis
10.1016/j.jacc.2020.12.058 · ExternalCitation · doi-reference
Phase 2b randomized trial of the oral PCSK9 inhibitor MK-0616
10.1016/j.jacc.2023.02.018 · ExternalCitation · doi-reference
Early ezetimibe initiation after myocardial infarction protects against later cardiovascular outcomes in the SWEDEHEART Registry
10.1016/j.jacc.2025.02.007 · ExternalCitation · doi-reference
An oral PCSK9 inhibitor for treatment of hypercholesterolemia
10.1016/j.jacc.2025.03.499 · ExternalCitation · doi-reference
Oral PCSK9 inhibitors
10.1016/j.jacc.2025.03.518 · ExternalCitation · doi-reference
2026 ACC/AHA/AACVPR/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of dyslipidemia: a report of the American College of Cardiology/American Heart Association Joint Committee on Clinical Practice Guidelines
10.1016/j.jacc.2025.11.016 · ExternalCitation · doi-reference
Phase 1 update: the novel oral PCSK9 inhibitor enlicitide does not affect the pharmacokinetics of narrow therapeutic index concomitant medications
10.1016/j.jacc.2026.02.664 · ExternalCitation · doi-reference
Oral PCSK9 Inhibitor Enlicitide Versus Oral Nonstatin Therapies
10.1016/j.jacc.2026.03.036 · ExternalCitation · doi-reference
Individualized low-density lipoprotein cholesterol reduction with alirocumab titration strategy in heterozygous familial hypercholesterolemia: results from an open-label extension of the ODYSSEY LONG TERM trial
10.1016/j.jacl.2018.11.007 · ExternalCitation · doi-reference
Phase 3 study results for oral PCSK9 inhibition with enlicitide
10.1016/j.medj.2026.101097 · ExternalCitation · doi-reference
Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170 000 participants in 26 randomised trials
10.1016/s0140-6736(10)61350-5 · ExternalCitation · doi-reference
PCSK9 inhibition with orally administered NNC0385-0434 in hypercholesterolaemia: a randomised, double-blind, placebo-controlled and active-controlled phase 2 trial
10.1016/s2213-8587(23)00325-x · ExternalCitation · doi-reference
Discovery process of enlicitide, a highly engineered macrocyclic peptide therapeutic, through issue-driven fragment-based synthetic assembly and SAR
10.1021/acs.jmedchem.6c00463 · ExternalCitation · doi-reference
Efficacy of alirocumab according to background statin type and dose: pooled analysis of 8 ODYSSEY Phase 3 clinical trials
10.1038/srep45788 · ExternalCitation · doi-reference
A 52-week placebo-controlled trial of evolocumab in hyperlipidemia
10.1056/nejmoa1316222 · ExternalCitation · doi-reference
Ezetimibe added to statin therapy after acute coronary syndromes
10.1056/nejmoa1410489 · ExternalCitation · doi-reference
Efficacy and safety of alirocumab in reducing lipids and cardiovascular events
10.1056/nejmoa1501031 · ExternalCitation · doi-reference
Evolocumab and clinical outcomes in patients with cardiovascular disease
10.1056/nejmoa1615664 · ExternalCitation · doi-reference
Alirocumab and cardiovascular outcomes after acute coronary syndrome
10.1056/nejmoa1801174 · ExternalCitation · doi-reference
Bempedoic acid and cardiovascular outcomes in statin-intolerant patients
10.1056/nejmoa2215024 · ExternalCitation · doi-reference
A placebo-controlled trial of the oral PCSK9 inhibitor enlicitide
10.1056/nejmoa2511002 · ExternalCitation · doi-reference
Evolocumab in patients without a previous myocardial infarction or stroke
10.1056/nejmoa2514428 · ExternalCitation · doi-reference
MK-0616: an oral PCSK9 inhibitor for hypercholesterolemia treatment
10.1080/13543784.2023.2267972 · ExternalCitation · doi-reference
Prevalence of statin intolerance: a meta-analysis
10.1093/eurheartj/ehac015 · ExternalCitation · doi-reference
New frontiers in the treatment of hypercholesterolaemia: oral inhibition of PCSK9
10.1093/eurheartjsupp/suag035 · ExternalCitation · doi-reference
Effect of statin therapy on plasma proprotein convertase subtilisin kexin 9 (PCSK9) concentrations: a systematic review and meta-analysis of clinical trials
10.1111/dom.12536 · ExternalCitation · doi-reference
Patients’ perceptions on the facilitators and barriers using injectable therapies in dyslipidaemia: an empirical qualitative descriptive international study
10.1111/jan.15739 · ExternalCitation · doi-reference
Prior authorization requirements for proprotein convertase subtilisin/kexin type 9 inhibitors across US private and public payers
10.1161/circoutcomes.117.003939 · ExternalCitation · doi-reference
Have the major cardiovascular outcomes trials impacted payer approval rates for PCSK9 inhibitors?
10.1161/circoutcomes.119.006019 · ExternalCitation · doi-reference
PCSK9: a key modulator of cardiovascular health
10.1161/circresaha.114.301621 · ExternalCitation · doi-reference
Long-term evolocumab in patients with established atherosclerotic cardiovascular disease
10.1161/circulationaha.122.061620 · ExternalCitation · doi-reference
Laroprovstat, the first oral small-molecule PCSK9 inhibitor for the treatment of hypercholesterolemia: results from a randomized, single-blind, placebo-controlled phase 1 trial in treatment-naive patients
10.1161/circulationaha.125.075973 · ExternalCitation · doi-reference
Contemporary national patterns of eligibility and use of novel lipid-lowering therapies in the United States
10.1161/jaha.122.026075 · ExternalCitation · doi-reference
Prescriber uptake and use of novel lipid-lowering therapies
10.1161/jaha.125.040768 · ExternalCitation · doi-reference
Metabolism of peptide drugs and strategies to improve their metabolic stability
10.2174/1389200219666180628171531 · ExternalCitation · doi-reference
Trends in PCSK9 inhibitor prescriptions before and after the price reduction in patients with atherosclerotic cardiovascular disease
10.3390/jcm10173828 · ExternalCitation · doi-reference