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DRUG CLASS:

Apoptosis inhibitor

2d
HELIOS: AMX0035 in Adult Patients With Wolfram Syndrome (clinicaltrials.gov)
P2, N=12, Active, not recruiting, Amylyx Pharmaceuticals Inc. | Trial completion date: Jan 2026 --> Dec 2026
Trial completion date
15d
Ursodeoxycholic and chenodeoxycholic bile acids alleviate endotoxininduced acute lung injury in rats by modulating aquaporin expression and pathways associated with apoptosis and inflammation. (PubMed, Front Pharmacol)
Although the results indicate a significant association between the expression of these proteins and histopathological changes, the potential influence of additional factors cannot be excluded. These findings suggest that UDCA and CDCA provide lung protection by acting through complex mechanisms involving inflammatory, oxidative, and apoptotic pathways.
Preclinical • Journal • IO biomarker
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BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • AQP1 (Aquaporin 1)
16d
OSOPOLAR: Ursodeoxycolic Acid for the Prevention of Relapsing Complications After Gallstone Acute Pancreatitis (clinicaltrials.gov)
P3, N=332, Recruiting, Hospital General Universitario de Alicante | Trial completion date: Jul 2025 --> Jul 2027 | Trial primary completion date: Jul 2025 --> Jul 2027 | Not yet recruiting --> Recruiting
Enrollment open • Trial completion date • Trial primary completion date
17d
Discovery of dual CDK4/6 and BRD4 inhibitor as apoptosis and autophagy inducers against NSCLC in vitro and in vivo. (PubMed, Eur J Med Chem)
Importantly, it also showed good pharmacokinetic properties in rats, meanwhile, B15 effectively inhibited tumor growth in vivo (TGI = 85.3 %) without causing significant toxicity. Overall, our results introduce a promising strategy of dual CDK4/6 and BRD4 inhibitors for the treatment of NSCLC.
Preclinical • Journal
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BRD4 (Bromodomain Containing 4)
18d
A Mechanistic Study of the Feasibility of Ursodeoxycholic Acid in the Treatment of Colon Adenocarcinoma. (PubMed, Drug Des Devel Ther)
In vitro experiment showed UDCA effectively inhibited the proliferation, migration, invasion and neovascularization in colon cancer cells. The antitumor activity of ursodeoxycholic acid may be related to cell apoptosis, proliferation, migration and vascular neogenesis.
Journal
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MMP2 (Matrix metallopeptidase 2) • CASP3 (Caspase 3)
18d
Ursodeoxycholic Acid in Patients With NAFLD - Clinical Observation (clinicaltrials.gov)
P=N/A, N=20, Active, not recruiting, General University Hospital, Prague | Recruiting --> Active, not recruiting | Trial completion date: Dec 2024 --> Jun 2025 | Trial primary completion date: Dec 2024 --> Jun 2025
Enrollment closed • Trial completion date • Trial primary completion date
1m
Coordinating interleukin-2 encoding circRNA with immunomodulatory lipid nanoparticles to potentiate cancer immunotherapy. (PubMed, Sci Adv)
To tackle these, a circular RNA (cRNA)-based IL-2 therapy using immunomodulatory lipid nanoparticles [ursodeoxycholic acid lipid nanoparticles (ULNPs)] and sustained-release hydrogel was developed...Furthermore, a locally administrated hydrogel loading with ULNPs-cRNAIL-2F sustains the release, enhancing efficacy and reducing toxicity. This innovative approach achieves remarkable tumor inhibition in both melanoma and orthotopic glioma models with or without surgery, offering a promising future for cancer immunotherapy.
Journal
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CD8 (cluster of differentiation 8) • IL2 (Interleukin 2) • TGFB1 (Transforming Growth Factor Beta 1)
1m
PD-L1 Inhibitor + RT ± Ursodeoxycholic Acid in Recurrent/Metastatic HER2-Neg Breast Cancer (clinicaltrials.gov)
P2, N=70, Not yet recruiting, Cancer Institute and Hospital, Chinese Academy of Medical Sciences
New P2 trial
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Ariely (adebrelimab)
1m
The effects of ursodeoxycholic acid on cardiometabolic risk factors: a systematic review and meta-analysis of randomized controlled trials. (PubMed, BMC Cardiovasc Disord)
This systematic review and meta-analysis suggest that UDCA supplementation may improve BMI and DBP, whereas it may increase SBP and have no effect on weight or inflammation. Further long-term and well-designed RCTs are needed to further assess and confirm these results.
Retrospective data • Review • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha)
1m
Severe Hepatotoxicity From Capmatinib: A Case Report and Therapeutic Approach. (PubMed, Cureus)
Here, we present a case of a 60-year-old male with MET exon mutated NSCLC who developed grade 4 liver injury after capmatinib initiation, which did not respond to drug discontinuation and eventually responded to N-acetyl cysteine (NAC) and ursodeoxycholic acid (ursodiol) therapy. This case demonstrates that NAC plus ursodiol can be an effective treatment strategy in such patients.
Journal
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MET (MET proto-oncogene, receptor tyrosine kinase)
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MET exon 14 mutation
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Tabrecta (capmatinib)
2ms
Viral IL-10 can promote the proliferation, migration and invasion of nasopharyngeal carcinoma cells and inhibit their apoptosis. (PubMed, Discov Oncol)
vIL-10 regulates the JAK1-STAT3 signalling pathway, promotes the proliferation of NPC cells, enhances their migration and invasion capabilities, inhibits tumour cell apoptosis, and participates in the progression of nasopharyngeal carcinoma.
Journal
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JAK1 (Janus Kinase 1) • IL10 (Interleukin 10)
2ms
The IRF2-INPP4B pathway is activated in CD4+ T cells and aggravates acute myeloid leukemia development by inhibiting apoptosis. (PubMed, Turk J Haematol)
We demonstrated that the IRF2-INPP4B signaling in CD4+ T cells activated the JAK2/STAT3 signaling pathway and downregulated caspase 3 expression, causing inhibition on AML cell apoptosis to aggravate AML development. This study proposes a novel regulatory mechanism in AML development, suggesting that the IRF2/INPP4B pathway might influence the JAK2-STAT3 signaling pathway, adding a new layer to our understanding of the complex interplay of these pathways in AML development.
Journal
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IFNG (Interferon, gamma) • CD4 (CD4 Molecule) • CASP3 (Caspase 3) • INPP4B (Inositol polyphosphate-4-phosphatase type II B) • IL4 (Interleukin 4) • IRF2 (Interferon Regulatory Factor 2)
2ms
Novel ethyl 2-hydrazineylidenethiazolidin-5-ylidene acetate clubbed with coumarinylthiazolyl pyrazole system as potential VEGFR-2 inhibitors and apoptosis inducer: synthesis, cytotoxic evaluation, cell cycle, autophagy, in silico ADMET and molecular docking studies. (PubMed, RSC Adv)
Among these, compounds 5d and 5g demonstrated notable antiproliferative effects, which were benchmarked against the standard drug doxorubicin...Further, both compounds 5d and 5g showed strong interactions with the VEGFR-2 receptor when they were studied using molecular docking. The ADMET prediction indicated that these bioactive compounds have the potential to serve as effective to fight liver cancer.
Journal
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KDR (Kinase insert domain receptor)
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doxorubicin hydrochloride
2ms
New trial
2ms
Journal
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CDH1 (Cadherin 1) • TGFB1 (Transforming Growth Factor Beta 1) • CDH2 (Cadherin 2) • SMAD2 (SMAD Family Member 2) • SMAD3 (SMAD Family Member 3)
2ms
Multifunctional Liposome Delivery System Based on Ursodeoxycholic Acid Sodium for the Encapsulation of Silibinin and Combined Treatment of Alcoholic Liver Injury. (PubMed, Mol Pharm)
Furthermore, it also modulated apoptosis-related factors, including B-cell lymphoma-2 (Bcl-2), BCL-2-associated X (Bax), cysteinyl aspartate specific proteinase-3 (Caspase-3), and cleaved caspase-3, to mitigate hepatocyte apoptosis. In summary, SUL demonstrates enhanced therapeutic efficacy against ALD, offering a novel approach for the clinical application of SLB in the prevention and treatment of ALD.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • KEAP1 (Kelch Like ECH Associated Protein 1) • HMOX1 (Heme Oxygenase 1) • CASP3 (Caspase 3)
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Legalon (silibinin)
2ms
Corticosterone-Induced Myocardial Dysfunctions and the Cardioprotective Role of Tauroursodeoxycholic Acid: An Experimental Study in Mice. (PubMed, Clin Exp Pharmacol Physiol)
Overall, our results suggest that corticosterone induces depression-like behaviours, cardiac dysfunction, elevated serum NE levels, reduced ATP and a decreased Bcl-2/Bax ratio, disrupting myocardial contraction and mitochondrial function. TUDCA effectively reversed these effects and modulated genes linked to muscle contraction and ion transport, highlighting its potential in mitigating corticosterone-induced behavioural and cardiac impairments.
Preclinical • Journal • IO biomarker
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BAX (BCL2-associated X protein)
2ms
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3) • SIRT1 (Sirtuin 1)
2ms
The effects of ursodeoxycholic acid on Parkinson's disease, a mechanistic review of the recent evidence. (PubMed, Metab Brain Dis)
Parkinson`s disease stands as the second-most widespread neurodegenerative disorder. Second, their antioxidant property is marked by an increase in the expression of superoxide dismuthase, glutathione peroxidase and other antioxidant enzymes. The third property is the antiapoptotic activity, characterized by decreased caspase-3 activity and lower expression of pro-apoptotic Bax in the striatum. Conclusion. Based on this comprehensive review, UDCA and TUDCA have the potential to be considered as a therapeutic agent in the management of the Parkinson's disease.
Review • Journal
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TNFA (Tumor Necrosis Factor-Alpha) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • IL1B (Interleukin 1, beta)
2ms
Remimazolam inhibits apoptosis of endothelial and epithelial cells by activating the PI3K/AKT pathway in acute lung injury. (PubMed, Int Immunopharmacol)
This study presents novel findings elucidating the beneficial effect of REM in ALI. This effect can be attributed to REM's ability to inhibit apoptosis by activating of the PI3K/AKT pathway in endothelial and epithelial cells. Additionally, REM targeted TSPO to regulate this pathway in endothelial cells. These results suggested a potential protective role for REM in ALI/ARDS management.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • CASP7 (Caspase 7) • BAK1 (BCL2 Antagonist/Killer 1)
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LY294002
2ms
New molecular hybrids integrated with quinoxaline and pyrazole structural motifs: VGFR2 inhibitors and apoptosis inducers. (PubMed, Bioorg Chem)
The synthesized compounds were assessed in vitro using the MTT assay with doxorubicin serving as a reference standard for their cytotoxic properties against the HCT-116 and MCF-7 cell lines...Notably, it was discovered that our target compound, 13, was 1.1 times more potent than sorafenib and 3.19 times more potent than sunitinib as a VGFRA2 inhibitor...For every hybrid, in silico physicochemical attributes, drug likeness metrics, and ligand efficiency were plausible. It's interesting to note that 13 and 15 are plausible medication candidates.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3)
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sorafenib • sunitinib • doxorubicin hydrochloride
2ms
Early warning of recurrence risk after NOTES Gallbladder Preserving Surgery based on serum bile acid profile (ChiCTR2400094465)
P=N/A, N=270, The 909th hospital (Southeast Hospital of Xiamen University); The 909th hospital
New trial
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APOA1 (Apolipoprotein A-I) • APOB (Apolipoprotein B)
2ms
Ursodeoxycholic Acid Attenuates Statin-Induced Impaired Glucose Tolerance: A Randomized Controlled Clinical Trial (ChiCTR2400091742)
P4, N=128, The First Affiliated Hospital of Xi'an Jiaotong University; The First Affiliated Hospital of Xi'an Jiaotong University
New P4 trial
3ms
LARP3 inhibits the apoptosis of hepatocellular carcinoma via the ROS/PI3K/c-Fos axis. (PubMed, PLoS One)
Finally, through biological means such as RNA sequencing, flow cytometry, western blotting, and the construction of a subcutaneous tumorigenesis model in nude mice, we concluded that inhibition of HCC apoptosis by LARP3 is related to LARP3 negatively regulating ROS level and inhibiting the PI3K/c-Fos/apoptosis axis. This study will provide potential targets for the treatment of HCC.
Journal
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FOS (Fos Proto-Oncogene AP-1 Transcription Factor Subunit 2)
3ms
Adiponectin facilitates the cell cycle, inhibits cell apoptosis and induces temozolomide resistance in glioblastoma via the Akt/mTOR pathway. (PubMed, Oncol Lett)
Adiponectin (ADN) regulates DNA synthesis, cell apoptosis and cell cycle to participate in the pathology and progression of glioblastoma. Markedly, ADN-mediated TMZ resistance was further attenuated by LY294002, suggesting that ADN activated the Akt/mTOR pathway to induce TMZ resistance in glioblastoma cell lines. In conclusion, ADN activated the Akt/mTOR pathway to facilitate cell cycle, inhibit cell apoptosis and induce TMZ resistance in glioblastoma.
Journal
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CCND1 (Cyclin D1) • CASP3 (Caspase 3) • ANXA5 (Annexin A5) • CCNB1 (Cyclin B1)
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CCND1 expression
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temozolomide • LY294002
3ms
Extension Study Evaluating The Safety And Tolerability of AMX0035 (clinicaltrials.gov)
P3, N=352, Completed, Amylyx Pharmaceuticals Inc. | Enrolling by invitation --> Completed | N=600 --> 352 | Trial completion date: Aug 2026 --> Oct 2024 | Trial primary completion date: Mar 2026 --> Oct 2024
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
3ms
Fenofibrate in Primary Biliary Cholangitis: a Real World Study (clinicaltrials.gov)
P3, N=300, Recruiting, Xijing Hospital of Digestive Diseases
New P3 trial • Real-world evidence
3ms
New P3 trial • Real-world evidence
3ms
New P3 trial • Real-world evidence
3ms
Remimazolam inhibits apoptosis of endothelial and epithelial cells by activating the PI3K/AKT pathway in acute lung injury. (PubMed, Int Immunopharmacol)
This study presents novel findings elucidating the beneficial effect of REM in ALI. This effect can be attributed to REM's ability to inhibit apoptosis by activating of the PI3K/AKT pathway in endothelial and epithelial cells. Additionally, REM targeted TSPO to regulate this pathway in endothelial cells. These results suggested a potential protective role for REM in ALI/ARDS management.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • CASP7 (Caspase 7) • BAK1 (BCL2 Antagonist/Killer 1)
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LY294002
3ms
Inhibition of AKT enhances chemotherapy efficacy and synergistically interacts with targeting of the Inhibitor of apoptosis proteins in oesophageal adenocarcinoma. (PubMed, Sci Rep)
A high degree of synergism was also observed in patient-derived OAC organoids indicating the potential clinical relevance of the combination. This study demonstrates the role for dual AKT/IAP inhibition in OAC and provides a strong rationale for the further investigation of this highly efficacious combination strategy.
Journal
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XIAP (X-Linked Inhibitor Of Apoptosis)
3ms
Fenofibrate for Compensated Cirrhosis Patients with Primary Biliary Cholangitis (clinicaltrials.gov)
P2/3, N=104, Recruiting, Xijing Hospital of Digestive Diseases | Trial primary completion date: Dec 2024 --> Dec 2025
Trial primary completion date
3ms
Fenofibrate Combined with Ursodeoxycholic Acid in Subjects with Primary Biliary Cholangitis (clinicaltrials.gov)
P3, N=150, Recruiting, Xijing Hospital of Digestive Diseases | Trial primary completion date: Dec 2024 --> Dec 2025
Trial primary completion date
4ms
YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. (PubMed, JCI Insight)
We further demonstrated that dasatinib and MYF-03-176 notably enhance the efficacy of KRAS inhibitors by reducing SRC kinase activity and TEAD activity. Overall, targeting the Hippo-YAP/TAZ pathway has the potential to overcome resistance to KRAS inhibitors.
Journal
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KRAS (KRAS proto-oncogene GTPase) • BCL2L11 (BCL2 Like 11) • SLC7A5 (Solute Carrier Family 7 Member 5)
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KRAS mutation • KRAS G12D
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dasatinib
4ms
ORION: AMX0035 and Progressive Supranuclear Palsy (clinicaltrials.gov)
P2/3, N=110, Active, not recruiting, Amylyx Pharmaceuticals Inc. | Recruiting --> Active, not recruiting
Enrollment closed
4ms
Rhodium complex [RhLI2]I: a novel anticancer agent inducing tumor inhibition and apoptosis. (PubMed, Discov Oncol)
No long-term adverse effects on hematological or biochemical parameters or tissue levels were observed in the mice. Given these findings, this compound demonstrates significant cytotoxic effects and has the potential to serve as a promising chemotherapeutic agent, warranting further investigation at more advanced stages.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3) • CASP8 (Caspase 8)
4ms
The Potential Therapeutic Approach of Ursodeoxycholic Acid as a Potent Activator of ACE-2 on Cerebral Disorders Induced by γ-irradiation in Rats. (PubMed, Cell Biochem Funct)
In conclusion, UDCA treatment efficiently normalizes the above-mentioned pathological abnormalities and avoids the development of IRR-associated neurological dysfunction by upregulating the beneficial axis of RAS in the brain. Hence, ursodeoxycholic acid presents a novel option for patient care during radiotherapy.
Preclinical • Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • NOX4 (NADPH Oxidase 4)
4ms
Design of a Magnetic Nanoplatform Based on CD26 Targeting and HSP90 Inhibition for Apoptosis and Ferroptosis-Mediated Elimination of Senescent Cells. (PubMed, ACS Biomater Sci Eng)
MNP@CD26@17D-mediated ferroptosis might be executed by ferritinophagy as judged by elevated levels of the ferritinophagy marker NCOA4 and a decreased pool of ferritin. As 24 h treatment with MNP@CD26@17D did not induce hemolysis in human erythrocytes in vitro, this newly designed nanoplatform could be considered as an optimal multifunctional tool to target and eliminate senescent cells of skin origin, overcoming their apoptosis resistance.
Journal
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NCOA4 (Nuclear Receptor Coactivator 4) • DPP4 (Dipeptidyl Peptidase 4) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
4ms
Colon-targeted self-assembled nanoparticles loaded with berberine double salt ameliorate ulcerative colitis by improving intestinal mucosal barrier and gut microbiota. (PubMed, Colloids Surf B Biointerfaces)
Berberine hydrochloride and ursodeoxycholic acid were combined to form a double salt (BeU), enhancing solubility and encapsulation. Remarkably, the mean colon length in the FU-PA/BeU NPs@MS group was 1.2 times longer than that in the sulfasalazine group. These dual-targeted FU-PA/BeU NPs@MS show great potential for UC treatment.
Journal
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IL6 (Interleukin 6) • IL10 (Interleukin 10)