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DRUG CLASS:

Ca2+ channel antagonist

6d
Safety and tolerability of Trimetazidine in amyotrophic lateral sclerosis (ALS) (ACTRN12620000945921)
P1/2, N=36, Completed, The University of Queensland | Not yet recruiting --> Completed
Trial completion
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IL6 (Interleukin 6)
8d
Trial completion
15d
ReVeRA-301: Etripamil in Atrial Fibrillation Phase 3 (clinicaltrials.gov)
P3, N=750, Not yet recruiting, Milestone Pharmaceuticals Inc.
New P3 trial
17d
AFF RVR: Diltiazem in the Treatment of Atrial Fibrillation or Atrial Flutter With Rapid Ventricular Rate (clinicaltrials.gov)
P4, N=92, Completed, Wake Forest University Health Sciences | Recruiting --> Completed | Trial completion date: Jun 2026 --> Nov 2024
Trial completion • Trial completion date
20d
Phototoxicity of Frequently Prescribed Medicines (clinicaltrials.gov)
P=N/A, N=12, Completed, Medical University of Vienna
New trial
21d
Combined Bisoprolol and Trimetazidine ameliorate Arsenic trioxide -Induced Acute Myocardial Injury in Rats: Targeting PI3K/GSK-3β/Nrf2/HO-1 and NF-κB/iNOS Signaling Pathways, Inflammatory Mediators and Apoptosis. (PubMed, Immunopharmacol Immunotoxicol)
The present research depicted that BIS and TMZ have the potential to protect the heart and provide therapeutic benefits by preventing acute heart injury induced by ATO. This is achieved by reversing the redox-sensitive pathway, reducing inflammation, and inhibiting apoptosis.
Preclinical • Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • CASP3 (Caspase 3) • IL1B (Interleukin 1, beta) • CAT (Catalase) • PI3K (Phosphoinositide 3-kinases)
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BCL2 expression • HMOX1 expression
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arsenic trioxide
22d
Dilution of Verapamil During Intraarterial Administration (clinicaltrials.gov)
P1, N=55, Completed, University of Illinois at Chicago | Recruiting --> Completed | N=100 --> 55
Trial completion • Enrollment change
23d
REPAIR: Reducing the Risk of Chronic Hypertension and Improving Vascular Function Following Preeclampsia (clinicaltrials.gov)
P=N/A, N=618, Recruiting, Medical College of Wisconsin | Not yet recruiting --> Recruiting
Enrollment open
23d
P-PAT: Preeclampsia Postpartum Antihypertensive Treatment (clinicaltrials.gov)
P3, N=300, Recruiting, Medical College of Wisconsin | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Jun 2024 --> Jun 2025
Trial completion date • Trial primary completion date
24d
Calcium Channel Blocker Lacidipine Promotes Antitumor Immunity by Reprogramming Tryptophan Metabolism. (PubMed, Adv Sci (Weinh))
Mechanistically, lacidipine targets calcium channels (CaV1.2/1.3) to inhibit Pyk2-JAK1-calmodulin complex-mediated IDO1 transcription suppression, which suppresses the kynurenine pathway and maintains the total nicotinamide adenine dinucleotide (NAD) pool by regulating NAD biosynthesis. These results reveal a new function of calcium channels in IDO1-mediated tryptophan metabolism in tumor immunity and warrant further development of lacidipine for the metabolic immunotherapy in breast cancer.
Journal • IO biomarker
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JAK1 (Janus Kinase 1) • IDO1 (Indoleamine 2,3-dioxygenase 1)
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IDO1 expression
24d
Decoding neuronal genes in stroke-induced pain: insights from single-nucleus sequencing in mice. (PubMed, BMC Neurol)
This study identified the role of key genes in thalamic hemorrhage-induced CPSP through snRNA-seq, providing a scientific basis for further exploration of the molecular mechanisms underlying CPSP.
Preclinical • Journal
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GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase) • HSP90AB1 (Heat Shock Protein 90 Alpha Family Class B Member 1)
27d
Diltiazem in Jervell and Lange-Nielsen Syndrome (clinicaltrials.gov)
P4, N=1, Completed, Vanderbilt University Medical Center | Enrolling by invitation --> Completed | Trial completion date: Jul 2025 --> Oct 2024 | Trial primary completion date: Jul 2025 --> Oct 2024
Trial completion • Trial completion date • Trial primary completion date
28d
Trimetazidine Efficacy in Attenuating Paclitaxel-Induced Peripheral Neuropathy (clinicaltrials.gov)
P1/2, N=60, Recruiting, Minia University | Trial completion date: Nov 2024 --> Mar 2025 | Trial primary completion date: Nov 2024 --> Feb 2025
Trial completion date • Trial primary completion date
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paclitaxel
28d
Treatment of Elevated Blood Pressures in Early Pregnancy (clinicaltrials.gov)
P2, N=2, Terminated, Marshall University | N=234 --> 2 | Trial completion date: Dec 2024 --> May 2024 | Recruiting --> Terminated; The study has closed due to difficulty in enrollment.
Enrollment change • Trial completion date • Trial termination
30d
Eco-Friendly Synthesis and Molecular Modelling of 2-Phenylimidazo[1,2-b]pyridazine Derivatives: In Vitro and In Vivo Studies for Lead Optimization. (PubMed, ChemMedChem)
To lay the groundwork for the future rational optimization of this promising class of compounds, the molecular bases of DM1 and DM2 activity were investigated by modelling their interaction with hCav3.1 channels. The calculated binding modes of DM1 and DM2 to hCav3.1 channels partially mirrored that of the selective Cav3.1 blocker Z944, paving the way for future lead optimization.
Preclinical • Journal
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CAV3 (Caveolin 3)
1m
New P1 trial
1m
Diltiazem mitigates acute liver injury by targeting NFκB-TXNIP/NLRP3 axis in Rats: New insights beyond calcium channel blockade. (PubMed, Int Immunopharmacol)
In conclusion, diltiazem shows promise as a protective agent for liver inflammatory diseases. Further research is warranted to translate these preclinical results into effective strategies for improving liver health.
Preclinical • Journal • IO biomarker
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BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • IL18 (Interleukin 18) • TXN (Thioredoxin) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • TXNIP (Thioredoxin Interacting Protein)
1m
Preventing radial artery spasm during cerebral angiography via transradial access by intra-arterial administration of spasmolytic and using The Glidesheath Slender Sheath (ChiCTR2400089250)
P=N/A, N=248, Not yet recruiting, Tongji Medical College, Huazhong University of Science and Technology; Tongji Hospital, Tongji Medical College, Huazhong University of Science and Tec
New trial
|
nitroglycerin
1m
Neuroprotective Effects of Trimetazidine against Cisplatin-Induced Peripheral Neuropathy: Involvement of AMPK-Mediated PI3K/mTOR, Nrf2, and NF-κB Signaling Axes. (PubMed, Oxid Med Cell Longev)
In conclusion, AMPK-mediated PI3K/mTOR, Nrf2, and NF-κB signaling pathways may all be involved in the therapeutic benefits of TRI for CIPN. These results indicate that TRI may be useful for reducing the side effects of CIPN and enhancing patient outcomes during cisplatin chemotherapy.
Journal
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mTOR (Mechanistic target of rapamycin kinase) • AMPK (Protein Kinase AMP-Activated Catalytic Subunit Alpha 1)
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AMPK expression
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cisplatin
2ms
Ver-A-T1D: Verapamil SR in Adults With Type 1 Diabetes (clinicaltrials.gov)
P2, N=138, Active, not recruiting, Medical University of Graz | Recruiting --> Active, not recruiting
Enrollment closed
2ms
Enrollment change • Head-to-Head
2ms
New P3 trial
2ms
Dronedarone hydrochloride inhibits gastric cancer proliferation in vitro and in vivo by targeting SRC. (PubMed, Transl Oncol)
Our research has revealed that Dronedarone hydrochloride, an FDA-approved drug, is an SRC inhibitor that can suppress the growth of GC cells by blocking the SRC/AKT1 signaling pathway. It provides a scientific basis for use in the clinical treatment of GC.
Preclinical • Journal
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AKT1 (V-akt murine thymoma viral oncogene homolog 1)
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dasatinib
3ms
Dronedarone hydrochloride (DH) induces pancreatic cancer cell death by triggering mtDNA-mediated pyroptosis. (PubMed, Cell Death Dis)
Finally, we assessed the anti-cancer effects of DH in a pancreatic cancer mouse model and found that DH treatment suppressed pancreatic tumor development in vivo. Collectively, our investigation demonstrates that DH triggers pyroptosis in PDAC and proposes its potential effects on anti-PDAC growth.
Journal
|
STING (stimulator of interferon response cGAMP interactor 1)
3ms
Tetrandrine Tablets Used in Hospitalized Adults With COVID-19 (clinicaltrials.gov)
P4, N=0, Withdrawn, Peking University Third Hospital | N=414 --> 0 | Not yet recruiting --> Withdrawn
Enrollment change • Trial withdrawal
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CBT-1 (tetrandrine)
3ms
Cancer stem cells in meningiomas: novel insights and therapeutic implications. (PubMed, Clin Transl Oncol)
The use of combination therapies, such as hydroxyurea alongside diltiazem, suggests more efficient and effective MG management compared to monotherapy. Since the efficacy of traditional therapies is limited in most cases due to resistance mechanisms in CSCs, further studies on the biology of CSCs are warranted to develop therapeutic interventions that are likely to be effective in MG. Consequently, improved diagnostic approaches may lead to personalised treatment plans tailored to the specific needs of each patient.
Review • Journal • Cancer stem
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SOX2 • POU5F1 (POU Class 5 Homeobox 1) • NANOG (Nanog Homeobox)
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hydroxyurea
3ms
Targeting Toll-like Receptor 4/Nuclear Factor-κB and Nrf2/Heme Oxygenase-1 Crosstalk via Trimetazidine Alleviates Lipopolysaccharide-Induced Depressive-like Behaviors in Mice. (PubMed, J Neuroimmune Pharmacol)
Male Swiss albino mice were injected with LPS (500 µg/kg, i.p) every other day alone or parallel with oral doses of either escitalopram (Esc) (10 mg/kg/day) or TMZ (20 mg/kg/day) for 14 days. Here we showed that TMZ is an affluent nominee for depression management via targeting TLR4/NF-κB and Nrf2/HO-1 pathways. Future research addressing TMZ-antidepressant activity in humans is mandatory to enroll it as a novel therapeutic strategy for depression.
Preclinical • Journal
|
TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • CASP3 (Caspase 3) • TLR4 (Toll Like Receptor 4)
3ms
Diltiazem in Jervell and Lange-Nielsen Syndrome (clinicaltrials.gov)
P4, N=2, Enrolling by invitation, Vanderbilt University Medical Center | Initiation date: Aug 2024 --> Nov 2024
Trial initiation date
3ms
New P2 trial
3ms
REPAIR: Reducing the Risk of Chronic Hypertension and Improving Vascular Function Following Preeclampsia (clinicaltrials.gov)
P=N/A, N=618, Not yet recruiting, Medical College of Wisconsin | Phase classification: P4 --> P=N/A
Phase classification
3ms
Bioequivalence test of trimetazidine hydrochloride tablets (ChiCTR2400088581)
P4, N=56, Completed, Guangzhou Panyu Central Hospital; Guangzhou Panyu Central Hospital
New P4 trial
3ms
Effects of papaverine on hepatic, splenic and renal hemodynamics in patients after liver transplantation: a randomized controlled trial (ChiCTR2400087258)
P1, N=62, Completed, Huashan Hospital Affiliated to Fudan University; Huashan Hospital Affiliated to Fudan University
New P1 trial
|
papaverine
3ms
Short Communication: Novel Di- and Triselenoesters as Effective Therapeutic Agents Inhibiting Multidrug Resistance Proteins in Breast Cancer Cells. (PubMed, Int J Mol Sci)
The cytometric analysis showed that the tested compounds (especially EDAG-8) are inhibitors of BCRP, MDR1, and MRP1 efflux pumps (more potent than the reference compounds-novobiocin, verapamil, and MK-571). An in silico study correlates with these results, suggesting that the compound with the lowest binding energy to these transporters (EDAG-8) has a more favorable spatial structure affecting its anticancer activity, making it a promising candidate in the development of a novel anticancer agent for future breast cancer therapy.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
3ms
Dronedarone inhibits the proliferation of esophageal squamous cell carcinoma through the CDK4/CDK6-RB1 axis in vitro and in vivo. (PubMed, Front Med)
Furthermore, dronedarone suppressed the growth of ESCC in patient-derived tumor xenograft models in vivo. Thus, our study demonstrated that dronedarone could be repurposed as a CDK4/6 inhibitor for ESCC chemoprevention.
Preclinical • Journal
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RB1 (RB Transcriptional Corepressor 1) • CDK4 (Cyclin-dependent kinase 4) • CDK6 (Cyclin-dependent kinase 6)
3ms
Lacidipine Inhibits NF-κB and Notch Pathways and Mitigates DSS-Induced Colitis. (PubMed, Dig Dis Sci)
Lacidipine demonstrated a protective effect in UC, reducing inflammation and modulating key signaling pathways. These findings suggest that lacidipine could be a promising candidate for the treatment of UC.
Journal
|
NFKBIA (NFKB Inhibitor Alpha 2)
3ms
Efficacy & Safety of Zonisamide in newly diagnosed partial epilepsy patients. (ACTRN12607000142437)
P3, N=582, Completed, Eisai Ltd | Not yet recruiting --> Completed
Trial completion
4ms
Eslicarbazepine induces apoptosis and cell cycle arrest in C6 glioma cells in vitro and suppresses tumor growth in an intracranial rat model. (PubMed, BMC Cancer)
Based on these novel findings, ESL has the potential for further experimental and clinical studies in glioblastoma.
Preclinical • Journal
|
BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CCNB1 (Cyclin B1)
|
temozolomide
4ms
The Efficacy of Botulinum Toxin Alone Versus Combined Botulinum Toxin and Topical Diltiazem in Chronic Anal Fissure (clinicaltrials.gov)
P=N/A, N=217, Completed, Istanbul Medipol University Hospital | Trial completion date: Jun 2022 --> Aug 2024
Trial completion date
4ms
Development of Natural-Product-Inspired ABCB1 Inhibitors Through Regioselective Tryptophan C3-Benzylation. (PubMed, Chemistry)
We have reported that exo-C3-N-Dbn--Trp2 (13) as a lead ABCB1 inhibitor that is more effective than Verapamil...We correlate that the predictions based on the inhibitor interactions at the access tunnel provide clues about the design of improved ABCB1 inhibitors. This work lays the foundation for the design of a new class of inhibitors from a cyclo-L-Trp-L-Trp DKP scaffold.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1)
4ms
REPAIR: Reducing the Risk of Chronic Hypertension and Improving Vascular Function Following Preeclampsia (clinicaltrials.gov)
P4, N=618, Not yet recruiting, Medical College of Wisconsin | Phase classification: P3 --> P4
Phase classification