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DRUG CLASS:

Fatty acid inhibitor

6d
Targeting fatty acid synthase suppresses tumor development in NF2/CDKN2A-deficient pleural mesothelioma. (PubMed, Cell Death Dis)
Our drug screening assay showed that the fatty acid synthase (FASN) inhibitor cerulenin demonstrates strong and selective antiproliferative properties against NF2/CDKN2A(p16)-deficient PM cells, surpassing the effects of C75, cisplatin or pemetrexed. These findings suggest that FASN might play a role in the tumorigenesis of PM cells through the regulation of mitochondrial dynamics. This research offers a novel perspective on the potential development of precision medicine for PM.
Journal
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CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • FASN (Fatty acid synthase)
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cisplatin • pemetrexed • cerulenin
18d
Gemfibrozil Prevents Myocardial Ischemia-Reperfusion Injury in Mice Through AMPK Activation. (PubMed, Clin Exp Pharmacol Physiol)
Myocardial ischemia-reperfusion injury (MIRI) causes severe clinical complications in patients. Further analysis showed that GEM administration prevented the I/R-induced decrease in phospho-AMPK levels in ischemic cardiac tissue, and pharmacological inhibition of AMPK with dorsomorphin (DSMF) abolished all cardioprotective effects of GEM. Taken together, these results suggest that GEM mitigates MIRI-induced cardiac injury by inhibiting apoptosis and oxidative stress via modulation of AMPK, supporting its potential for reducing MIRI-related cardiac damage.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CASP3 (Caspase 3) • CASP9 (Caspase 9) • IL1B (Interleukin 1, beta)
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dorsomorphin (Compound C)
3ms
Chinese herbal injections combined with EGFR-TKIs for intervention of non-small cell lung cancer: a systematic review and meta-analysis. (PubMed, Front Pharmacol)
The objective response rate (ORR) was significantly increased by Kanglaite injection (RR = 1.52, 95% confidence interval [CI]: 1.07-2.15, p = 0.02)...Due to limitations in the assessed research, high-quality clinical studies with rigorous designs are required to confirm the findings. https://www.crd.york.ac.uk/PROSPERO/view/CRD42024561845, Identifier CRD42024561845.
Retrospective data • Review • Journal
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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EGFR mutation • EGFR expression
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Kanglaite Injection (KLTi)
4ms
Lipidomics and single-cell transcriptomics uncover aberrant lipid metabolism in metaplasia lesions during gastric carcinogenesis. (PubMed, J Gastroenterol)
Our study reveals a distinct lipid signature in gastric metaplasia characterized by TG and LD accumulation, providing novel therapeutic insights into targeting lipid metabolism to prevent GIM malignant transformation and reduce cancer risk.
Journal
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DDIT4 (DNA Damage Inducible Transcript 4) • FABP1 (Fatty Acid Binding Protein 1)
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tamoxifen • TVB-3664
4ms
Efficacy and safety of Chinese medicine injection combined with concurrent chemoradiotherapy in the treatment of esophageal cancer: a Bayesian network meta-analysis. (PubMed, Front Med (Lausanne))
Kanglaite injection (KLT) combined with CCRT (SUCRA: 85.1%; 90.1%) was optimal for enhancing performance status and one-year survival rate...Nevertheless, the findings shall be validated in multicenter, better-designed RCTs. The PRISMA registration details for this study can be found at: https://www.crd.york.ac.uk/PROSPERO/view/CRD42024574242.
Retrospective data • Review • Journal
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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Kanglaite Injection (KLTi)
5ms
8 specific Chinese herbal injections combined with chemotherapy for breast cancer: a systematic review and network meta-analysis of comparative safety and efficacy. (PubMed, Front Pharmacol)
Kanglaite Injection (KLT) combined with chemotherapy had the best effect on reducing tumor markers CEA and CA153. Although a 2021 network meta-analysis (Comparative Efficacy and Safety of Chinese Herbal Injections Combined With Cyclophosphamide and 5-Fluorouracil Chemotherapies in Treatment of Breast Cancer: A Bayesian Network Meta-Analysis) examined chemotherapy combined with Chinese medicine injections for breast cancer, it was limited to the CF regimen and assessed few outcomes, with some lower-quality studies included (excluded herein)...This provides more comprehensive results, identifying SQFZ as most effective for improving response rate and Karnofsky Performance Status (KPS), thereby enhancing clinical utility. https://www.crd.york.ac.uk/PROSPERO/myprospero, identifier [CRD42024589306].
Retrospective data • Review • Journal
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CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule)
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5-fluorouracil • cyclophosphamide • Kanglaite Injection (KLTi)
5ms
The Effect of Omega 3 Supplementation on Postoperative Delirium in Elderly Patients Undergoing Major Cardiac Surgery (clinicaltrials.gov)
P2, N=90, Enrolling by invitation, University of Missouri-Columbia | Not yet recruiting --> Enrolling by invitation
Enrollment open
6ms
Phase II Trial to Modulate Intermediate Endpoint Biomarkers in Former and Current Smokers (clinicaltrials.gov)
P2, N=19, Active, not recruiting, H. Lee Moffitt Cancer Center and Research Institute | Trial primary completion date: Jun 2025 --> Mar 2025
Trial primary completion date
7ms
Synergistic targeting of FASN and HMGCS1 by cerulenin enhances tumor cell ferroptosis sensitivity through rewiring lipid metabolism and blocking GPX4 biosynthesis. (PubMed, Cancer Lett)
In vivo, cerulenin synergized with classic ferroptosis inducer erastin to suppress xenograft tumor growth without observable toxicity. Collectively, this study revealed that cerulenin dual-targets FASN/HMGCS1 and obtained with remarkable pro-ferroptosis properties, providing a mechanistically distinct therapeutic paradigm for precision cancer therapy.
Journal
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GPX4 (Glutathione Peroxidase 4) • FASN (Fatty acid synthase) • SLC7A11 (Solute Carrier Family 7 Member 11) • HMGCS1 (3-Hydroxy-3-Methylglutaryl-CoA Synthase 1)
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erastin • cerulenin
7ms
Reduced Muscle Loss in Patients With NSCLC Taking Fibrates: Findings From a Retrospective Observational Study. (PubMed, J Cachexia Sarcopenia Muscle)
Patients with NSCLC taking fibrates at the time of diagnosis lost less muscle area over time. In a secondary analysis, this change was not associated with a change in overall survival, though this study was likely underpowered for this analysis.
Observational data • Retrospective data • Journal
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PPARA (Peroxisome Proliferator Activated Receptor Alpha)
7ms
A Prospective, Multicenter, Randomized, Controlled, Open-Label, Blinded Endpoint Trial Evaluating the Efficacy, Safety, and Cost-Effectiveness of Omega-3 Ethyl Esters in Mixed Dyslipidemia (ChiCTR2500104485)
P=N/A, N=492, Not yet recruiting, Beiing Anzhen Hospital. Capital Medical University; Beijing Association of Holistic Integrative Medicine
New trial • HEOR
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atorvastatin
8ms
IN VITRO ASSESSMENT OF REVERSIBLE AND METABOLISM-DEPENDENT INHIBITORY EFFECTS OF PROPOXAZEPAM ON CYP2C8 ACTIVITY. (PubMed, Exp Oncol)
Based on the indicators used (Ki, IC50, IC50 shift, and [I]/Ki ratios), propoxazepam is not expected to be a significant CYP2C8 inhibitor in vitro.
Preclinical • Journal
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CYP2C8 (Cytochrome P450 Family 2 Subfamily C Member 8)