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DRUG CLASS:

Cholesterol absorption inhibitor

28d
New trial
29d
Pharmacist Interventions in Cholesterol Management of Very High Risk Patients (clinicaltrials.gov)
P=N/A, N=150, Not yet recruiting, Wake Forest University Health Sciences
New trial
2ms
A Study Evaluating the Safety, Tolerability, and Efficacy of Aramchol Meglumine in Primary Sclerosing Cholangitis (clinicaltrials.gov)
P2, N=24, Suspended, Galmed Pharmaceuticals Ltd | Trial completion date: Dec 2026 --> Dec 2027 | Not yet recruiting --> Suspended | Trial primary completion date: Sep 2025 --> Sep 2026
Trial completion date • Trial suspension • Trial primary completion date
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Aramchol (aramchol meglumine)
2ms
New trial
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APOA1 (Apolipoprotein A-I) • CRP (C-reactive protein)
3ms
Ezetimibe Utilization Early After Acute Myocardial Infarction, "EzAMI Trial" (clinicaltrials.gov)
P=N/A, N=500, Recruiting, Cairo University | Trial completion date: Apr 2024 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2025
Trial completion date • Trial primary completion date
3ms
Ezetimibe protects against Gentamycin-induced ototoxicity in rats by antioxidants, anti-inflammatory mechanisms, and BDNF upregulation. (PubMed, Immunopharmacol Immunotoxicol)
Correlations were significantly negative between BDNF and MDA, NO, TNF-α, COX 2, and caspase-3 immunoreaction and significantly positive with CAT, HO-1, and PCNA immunoreaction. EZE can safeguard inner ear tissues from GM via antioxidant, anti-inflammatory, and antiapoptotic mechanisms, as well as upregulation of BDNF mechanisms.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • CASP3 (Caspase 3) • PCNA (Proliferating cell nuclear antigen) • BDNF (Brain Derived Neurotrophic Factor) • CAT (Catalase)
3ms
Open-Label Study to Evaluate the Safety, Tolerability, and PK of Aramchol in Subjects With Hepatic Impairment (clinicaltrials.gov)
P1, N=57, Completed, Galmed Research and Development, Ltd. | Enrolling by invitation --> Completed
Trial completion
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Aramchol (aramchol meglumine)
4ms
New P1 trial
4ms
New P1 trial
|
Aramchol (aramchol meglumine)
4ms
A Study Evaluating the Safety, Tolerability, and Efficacy of Aramchol Meglumine in Primary Sclerosing Cholangitis (clinicaltrials.gov)
P2, N=24, Not yet recruiting, Galmed Research and Development, Ltd. | Initiation date: Jun 2024 --> Jun 2025
Trial initiation date
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Aramchol (aramchol meglumine)
5ms
Study to Evaluate the Management Status of Dyslipidemia Following Administration of Statin and Ezetimibe Complex Treatment Patient (clinicaltrials.gov)
P=N/A, N=18000, Active, not recruiting, Daewoong Pharmaceutical Co. LTD. | Recruiting --> Active, not recruiting | Trial completion date: Dec 2023 --> Dec 2024 | Trial primary completion date: Jun 2023 --> Dec 2023
Enrollment closed • Trial completion date • Trial primary completion date • Real-world evidence • Real-world
7ms
New P4 trial
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Repatha (evolocumab) • Praluent (alirocumab)
7ms
A Study to Evaluate the Efficacy and Safety of Fixed-Dose Combination of Pitavastatin/Ezetimib (clinicaltrials.gov)
P=N/A, N=8606, Recruiting, Boryung Pharmaceutical Co., Ltd | Not yet recruiting --> Recruiting
Enrollment open • Real-world evidence • Real-world
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pitavastatin
7ms
Rosuzet-IVUS: Usual Dose Rosuvastatin Plus Ezetimibe Versus High-dose Rosuvastatin on Coronary Atherosclerotic Plaque (clinicaltrials.gov)
P4, N=280, Active, not recruiting, Samsung Medical Center | Recruiting --> Active, not recruiting | Trial completion date: Dec 2024 --> Jan 2027 | Trial primary completion date: Dec 2023 --> Jan 2027
Enrollment closed • Trial completion date • Trial primary completion date
7ms
To Study the Effect of Vytorin on Intracellular Lipid and Inflammation in Obese Subjects (clinicaltrials.gov)
P=N/A, N=20, Completed, University at Buffalo | Unknown status --> Completed | Phase classification: P3 --> PN/A
Trial completion • Phase classification
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CD68 (CD68 Molecule)
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simvastatin • ezetimibe/simvastatin
7ms
Drug Concentrations in Breast Milk and Prediction of Blood Levels of the Breastfed Infants (clinicaltrials.gov)
P=N/A, N=39, Completed, The Hospital for Sick Children | Recruiting --> Completed | N=304 --> 39
Trial completion • Enrollment change
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methotrexate • Xatmep (methotrexate oral solution)
8ms
Ezetimibe inhibits the migration and invasion of triple-negative breast cancer cells by targeting TGFβ2 and EMT. (PubMed, FEBS Open Bio)
Overexpression of TGFβ2 reversed the inhibitory effect of ezetimibe on the migration and invasion of breast cancer cells. Taken together, our results suggest that ezetimibe might be a potential candidate for the treatment of breast cancer metastasis.
Journal
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TGFB1 (Transforming Growth Factor Beta 1) • TGFB2 (Transforming Growth Factor Beta 2)
8ms
A Clinical Trial to Evaluate the Tolerability and Pharmacokinetics of CKD-348(6) (clinicaltrials.gov)
P1, N=63, Completed, Chong Kun Dang Pharmaceutical | Not yet recruiting --> Completed
Trial completion
8ms
ARTCAP: Aggressive Risk-Prevention Therapies for Coronary Atherosclerotic Plaque (ART-CAP) (clinicaltrials.gov)
P4, N=200, Recruiting, University of Louisville | Not yet recruiting --> Recruiting
Enrollment open
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icosapent ethyl
8ms
New trial • Real-world evidence • Real-world
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pitavastatin
9ms
LDL-ALERT: Randomized Controlled Trial of Alert-Based Computerized Decision Support for Optimizing Low-Density Lipoprotein Management (clinicaltrials.gov)
P=N/A, N=400, Active, not recruiting, Brigham and Women's Hospital | Trial completion date: Dec 2023 --> Sep 2024
Trial completion date
9ms
New P4 trial
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icosapent ethyl
9ms
Ezetimibe treatment reduces oxidized low-density lipoprotein in biliary cirrhotic rats. (PubMed, J Chin Med Assoc)
Ezetimibe reduced plasma and intrahepatic ox-LDL levels in the cirrhotic rats. Furthermore, it ameliorated intrahepatic fat accumulation and oxidative stress. However, ezetimibe did not alleviate hepatic fibrosis or inflammation in the biliary cirrhotic rats.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha)
10ms
A Clinical Trial to Evaluate the Tolerability and Pharmacokinetics of CKD-348 (clinicaltrials.gov)
P1, N=70, Completed, Chong Kun Dang Pharmaceutical | Not yet recruiting --> Completed
Trial completion
10ms
A Clinical Trial to Evaluate the Tolerability and Pharmacokinetics of CKD-348(2) (clinicaltrials.gov)
P1, N=62, Completed, Chong Kun Dang Pharmaceutical | Recruiting --> Completed
Trial completion
10ms
A Clinical Trial to Evaluate the Tolerability and Pharmacokinetics of CKD-348(5) (clinicaltrials.gov)
P1, N=65, Completed, Chong Kun Dang Pharmaceutical | Not yet recruiting --> Completed | N=30 --> 65
Trial completion • Enrollment change
11ms
Trial completion date • Trial primary completion date
11ms
Ezetimibe ameliorates cisplatin-induced nephrotoxicity: A novel therapeutic approach via modulating AMPK/Nrf2/TXNIP signaling. (PubMed, FASEB J)
Cisplatin (Cis) is among the most powerful antineoplastic medications, nevertheless, its serious side effects; particularly nephrotoxicity designates a major concern. Collectively, Eze exerts significant renal protection against Cis-induced nephrotoxicity via antioxidant, anti-inflammatory and anti-apoptotic pathways that are probably mediated, at least partly, via activating AMPK/Nrf2/HO-1 pathway and conquering both TXNIP/NLRP3 inflammasome and TXNIP/ASK1 signaling pathways. To confirm the protective effect of Eze via AMPK-activation, an AMPK-inhibitor, dorsomorphin (Dors), when co-administered with Eze abolished its protective effect.
Journal
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HMOX1 (Heme Oxygenase 1) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • IL18 (Interleukin 18) • TXN (Thioredoxin) • NLRP3 (NLR Family Pyrin Domain Containing 3) • TXNIP (Thioredoxin Interacting Protein)
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cisplatin • dorsomorphin (Compound C)
12ms
Enhancing Ezetimibe Anticancer Activity Through Development of Drug Nano-Micelles Formulations: A Promising Strategy Supported by Molecular Docking. (PubMed, Int J Nanomedicine)
Cell cycle analysis revealed that both ezetimibe and F5-treated T47D cells exhibited an increase in the subG1 phase, indicating reduced DNA content and cell death. These findings suggest that F5 could serve as a proficient drug delivery system in augmenting the cytotoxic activity of ezetimibe against breast cancer.
Journal
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IL1B (Interleukin 1, beta)
12ms
Ezetimibe inhibits triple-negative breast cancer proliferation and promotes cell cycle arrest by targeting the PDGFR/AKT pathway. (PubMed, Heliyon)
Furthermore, the AKT inhibitor MK2206 enhanced the inhibitory effect of Ezetimibe on the cell cycle and proliferation ability of TNBC cells overexpressing PDGFRβ. In xenograft tumor models, we also found that Ezetimibe inhibited TNBC growth, an effect that can be blocked by overexpression of PDGFR or activation of AKT. In summary, we have demonstrated that EZ inhibits the PDGFR/AKT pathway, thereby halting TNBC cycle progression and tumor growth.
Journal
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PDGFRB (Platelet Derived Growth Factor Receptor Beta)
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MK-2206
12ms
Rosuzet-IVUS: Usual Dose Rosuvastatin Plus Ezetimibe Versus High-dose Rosuvastatin on Coronary Atherosclerotic Plaque (clinicaltrials.gov)
P4, N=280, Recruiting, Samsung Medical Center | Trial primary completion date: Dec 2022 --> Dec 2023
Trial primary completion date
1year
New P1 trial
1year
New P2 trial
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Aramchol (aramchol meglumine)
1year
URI alleviates tyrosine kinase inhibitors-induced ferroptosis by reprogramming lipid metabolism in p53 wild-type liver cancers. (PubMed, Nat Commun)
The combination of SCD1 inhibitor aramchol and deuterated sorafenib derivative donafenib displays promising anti-tumor effects in p53-wild type HCC patient-derived organoids and xenografted tumors. This combination therapy has potential clinical benefits for the patients with advanced HCC who have wild-type p53 and high levels of URI/SCD1.
Journal
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SCD (Stearoyl-CoA Desaturase) • TRIM28 (Tripartite Motif Containing 28)
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TP53 wild-type
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sorafenib • Zepsun (donafenib) • Aramchol (aramchol meglumine)
over1year
PCL-based nanoparticles for doxorubicin-ezetimibe co-delivery: A combination therapy for prostate cancer using a drug repurposing strategy. (PubMed, Bioimpacts)
The designed nanocarriers could serve as an ideal candidate for combination therapy of cancer. The results corroborated each other and presented successful EZ and DOX formulations containing PCEC NPs and their efficiency in treating prostate cancer.
Journal • Combination therapy
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doxorubicin hydrochloride
2years
CircRIC8B regulates the lipid metabolism of chronic lymphocytic leukemia through miR199b-5p/LPL axis. (PubMed, Exp Hematol Oncol)
In this study, the expressional and metabolic patterns of circRNAs in CLL was illustrated for the 1st time. Our findings revealed that circRIC8B regulates the lipid metabolism abnormalities in and development of CLL through the miR-199b-5p/LPL axis. CircRIC8B may serve as a promising prognostic marker and therapeutic target, which enhances the sensitivity to ezetimibe in CLL.
Journal
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MIR199B (MicroRNA 199b) • LPL (Lipoprotein Lipase) • MIR99B (MicroRNA 99b)
almost3years
Aramchol in patients with nonalcoholic steatohepatitis: a randomized, double-blind, placebo-controlled phase 2b trial. (PubMed, Nat Med)
Early termination due to adverse events (AEs) was <5%, and Aramchol 600 and 400 mg were safe, well tolerated and without imbalance in serious or severe AEs between arms. Although the primary end point of a reduction in liver fat did not meet the prespecified significance level with Aramchol 600 mg, the observed safety and changes in liver histology and enzymes provide a rationale for SCD1 modulation as a promising therapy for NASH and fibrosis and are being evaluated in an ongoing phase 3 program.
Clinical • P2b data • Journal
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SCD (Stearoyl-CoA Desaturase)
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Aramchol (aramchol meglumine)
3years
Cholesterol-lowering Intervention Decreases mTOR Complex 2 Signaling and Enhances Antitumor Immunity. (PubMed, Clin Cancer Res)
Lowering serum cholesterol decreased signaling through mTORC2 and enhance antitumor CD8+ T cell memory. We provide a rationale for large-scale clinical testing of cholesterol lowering strategies for prostate cancer chemoprevention.
Journal
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CD8 (cluster of differentiation 8)
3years
Oxidized low-density lipoprotein links hypercholesterolemia and bladder cancer aggressiveness by promoting cancer stemness. (PubMed, Cancer Res)
Inhibition of intestinal cholesterol absorption by Ezetimibe reversed diet-induced hypercholesterolemia and cancer stemness...Lowering serum ox-LDL or targeting the CD36/JAK2/STAT3 axis might serve as a potential therapeutic strategy for UBCs with hypercholesterolemia. Moreover, elevated ox-LDL may serve as a biomarker for UBC.
Journal
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JAK1 (Janus Kinase 1) • CD36 (thrombospondin receptor)