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DRUG CLASS:

Ca2+ channel antagonist

5d
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
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nitroglycerin
9d
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
16d
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
18d
Enrollment change • Head-to-Head
22d
New P3 trial
1m
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
1m
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
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STING (stimulator of interferon response cGAMP interactor 1)
2ms
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)
2ms
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
2ms
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
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TNFA (Tumor Necrosis Factor-Alpha) • HMOX1 (Heme Oxygenase 1) • CASP3 (Caspase 3) • TLR4 (Toll Like Receptor 4)
2ms
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
2ms
New P2 trial
2ms
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
2ms
Bioequivalence test of trimetazidine hydrochloride tablets (ChiCTR2400088581)
P4, N=56, Completed, Guangzhou Panyu Central Hospital; Guangzhou Panyu Central Hospital
New P4 trial
2ms
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
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papaverine
2ms
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)
2ms
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)
2ms
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
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NFKBIA (NFKB Inhibitor Alpha 2)
2ms
Efficacy & Safety of Zonisamide in newly diagnosed partial epilepsy patients. (ACTRN12607000142437)
P3, N=582, Completed, Eisai Ltd | Not yet recruiting --> Completed
Trial completion
2ms
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
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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)
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temozolomide
2ms
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
3ms
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
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
3ms
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
3ms
Enrollment change
3ms
The Effects of Combination Zonisamide and Bupropion on Switching to an Electronic Cigarette (clinicaltrials.gov)
P3, N=180, Recruiting, Rose Research Center, LLC | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Feb 2024 --> Dec 2024
Trial completion date • Trial primary completion date
3ms
Papaverine and Oxytocin vs Oxytocin Alone in Labor Induction (clinicaltrials.gov)
P=N/A, N=126, Not yet recruiting, Western Galilee Hospital-Nahariya
New trial
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papaverine
3ms
Efficacy and Safety Study of Etripamil Nasal Spray Self-Administration for the Termination of Spontaneous Episodes of Paroxysmal Supraventricular Tachycardia (clinicaltrials.gov)
P3, N=500, Active, not recruiting, Ji Xing Pharmaceuticals (Shanghai) Co., Ltd. | Recruiting --> Active, not recruiting
Enrollment closed
3ms
TRIESTE: Transradial Evaluation Study of Diameter Increase After Vasodilatory Drugs Administration. (clinicaltrials.gov)
P=N/A, N=165, Completed, University of Lausanne Hospitals | Active, not recruiting --> Completed
Trial completion
3ms
Diltiazem in Jervell and Lange-Nielsen Syndrome (clinicaltrials.gov)
P4, N=2, Enrolling by invitation, Vanderbilt University Medical Center
New P4 trial
3ms
AFF RVR: Diltiazem in the Treatment of Atrial Fibrillation or Atrial Flutter With Rapid Ventricular Rate (clinicaltrials.gov)
P4, N=92, Recruiting, Aurora Health Care | Trial primary completion date: Jun 2024 --> Nov 2024
Trial primary completion date
4ms
Comparative Evaluation of MEBO Ointment and Topical Diltiazem Ointment in the Treatment of Acute Anal Fissure (clinicaltrials.gov)
P2, N=183, Recruiting, American University of Beirut Medical Center | Trial completion date: Jan 2024 --> Jan 2025 | Trial primary completion date: Jan 2024 --> Jan 2025
Trial completion date • Trial primary completion date
4ms
Zonisamide Ameliorated the Apoptosis and Inflammation in Cerebellar Tissue of Induced Alcohol Addiction Animal Model. (PubMed, Life (Basel))
Zonisamide improved locomotor function and reduced serum TNF-α levels, as well as APAF-1 and TNF-α expression in cerebellar tissues. These findings suggest that zonisamide exerts its protective effects by modulating immune and inflammatory pathways, thereby preserving cerebellar integrity and function.
Preclinical • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • APAF1 (Apoptotic peptidase activating factor 1)
4ms
Tetrandrine Activates STING/TBK1/IRF3 Pathway to Potentiate Anti-PD-1 Immunotherapy Efficacy in Non-Small Cell Lung Cancer. (PubMed, Pharmacol Res)
We further revealed that the combination of TET with αPD-1 monoclonal antibody (αPD-1 mAb) yields significant anti-cancer effects by promoting CD8+ T cell infiltration and enhancing its cell-killing effect, which in turn reduced the growth of tumors and prolonged survival of NSCLC mice. Therefore, TET effectively eliminates NSCLC cells and enhances immunotherapy efficacy through the activation of the STING pathway, and combining TET with anti-PD-1 immunotherapy deserves further exploration for applications.
Journal
|
STING (stimulator of interferon response cGAMP interactor 1)
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CBT-1 (tetrandrine)
4ms
Prognostic Value of Precision Medicine in Patients With MINOCA (PROMISE Trial). (clinicaltrials.gov)
P4, N=120, Active, not recruiting, Fondazione Policlinico Universitario Agostino Gemelli IRCCS | Recruiting --> Active, not recruiting | N=180 --> 120
Enrollment closed • Enrollment change
4ms
STOP-PA: Statin Combined With Amlodipine Treats Primary Aldosteronism (clinicaltrials.gov)
P4, N=150, Not yet recruiting, Third Military Medical University
New P4 trial
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amlodipine/atorvastatin
4ms
A randomized controlled study on the effect of abandoning anti-spasmodic drugs after finger replantation on finger survival (ChiCTR2200058130)
P=N/A, N=144, Recruiting, Subei people's Hospital; Subei people's Hospital | Not yet recruiting --> Recruiting
Enrollment open
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papaverine
4ms
Exploring bat-inspired cyclic tryptophan diketopiperazines as ABCB1 Inhibitors. (PubMed, Commun Chem)
By molecular simulations of ABCB1-substrate interactions, we generated a benzylated Cyclo-tryptophan (C3N-Dbn-Trp2) that inhibits ABCB1 activity with efficacy comparable to or better than the classical inhibitor, verapamil. C3N-Dbn-Trp2 restored chemotherapy sensitivity in drug-resistant human cancer cells with no adverse effect on cell proliferation. Our unique approach presents a promising lead toward developing effective ABCB1 inhibitors to treat drug-resistant cancers.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1)
4ms
RAPID: Efficacy and Safety of Etripamil for the Termination of Spontaneous Paroxysmal Supraventricular Tachycardia (PSVT). (clinicaltrials.gov)
P3, N=1097, Terminated, Milestone Pharmaceuticals Inc. | N=748 --> 1097 | Completed --> Terminated; The closure of the event-driven study was terminated due to the total sample size was reached.
Enrollment change • Trial termination
4ms
Inhibition of autophagy induced by tetrandrine promotes the accumulation of reactive oxygen species and sensitizes efficacy of tetrandrine in pancreatic cancer. (PubMed, Cancer Cell Int)
The results of treating subcutaneous xenograft tumors with a combination of tetrandrine and chloroquine validated that autophagy inhibition enhances the toxicity of tetrandrine against pancreatic cancer in vivo. Altogether, our study demonstrates that tetrandrine induces cytoprotective autophagy in pancreatic cancer cells. Inhibiting tetrandrine-induced autophagy promotes the accumulation of ROS and enhances its toxicity against pancreatic cancer.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • ATG7 (Autophagy Related 7) • BECN1 (Beclin 1)
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CBT-1 (tetrandrine) • chloroquine phosphate
4ms
Trial completion date • Trial primary completion date • Combination therapy • Metastases
|
temozolomide
4ms
Effect of a Proposed Cav1.3 Inhibitor in Primary Aldosteronism (clinicaltrials.gov)
P=N/A, N=15, Completed, Queen Mary University of London | Active, not recruiting --> Completed | Trial completion date: May 2024 --> Sep 2023 | Trial primary completion date: Apr 2024 --> Sep 2023
Trial completion • Trial completion date • Trial primary completion date
|
CAV1 (Caveolin 1)
4ms
Reduction Efficacy of OLOMAX for Blood Pressure and Low-density Lipoprotein Cholesterol in Hypertensive Patients With Dyslipidemia (clinicaltrials.gov)
P=N/A, N=4000, Active, not recruiting, Daewoong Pharmaceutical Co. LTD. | Recruiting --> Active, not recruiting | Trial completion date: Oct 2024 --> Apr 2025 | Trial primary completion date: Apr 2024 --> Nov 2024
Enrollment closed • Trial completion date • Trial primary completion date • Real-world evidence • Real-world