Furthermore, CHL reduced p-p65 expression by 5-fold, indicating its effective inhibition of NF-κB transcriptional activity and thereby alleviating inflammatory responses. Therefore, the LAP-activable co-prodrug CHL holds promising potential as a candidate for the synergistic treatment of liver injury.

1 month ago

Journal

NQO1 (NAD(P)H dehydrogenase, quinone 1) • RELA (RELA Proto-Oncogene)

Vandetanib and Everolimus in Treating Patients With Advanced or Metastatic Cancer (clinicaltrials.gov)

P1, N=151, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed | Trial completion date: May 2026 --> Oct 2025 | Trial primary completion date: May 2026 --> Oct 2025

1 month ago

Trial completion • Trial completion date • Trial primary completion date

everolimus • Caprelsa (vandetanib)

2ms

A Clinical Study of Neflamapimod in Patients With Dementia With Lewy Bodies (clinicaltrials.gov)

P2, N=25, Active, not recruiting, EIP Pharma Inc | Recruiting --> Active, not recruiting

2 months ago

Enrollment closed

2ms

Design, Synthesis, and 2D QSAR Analysis of Some Novel Pyrazolo[1,5-a]pyrimidine Derivatives as Pim-1 Kinase Inhibitors for the Treatment of MCF-7 Breast Cancer. (PubMed, Drug Dev Res)

Compound 4d exhibited a 1.5-fold increased cytotoxic activity compared to doxorubicin against the MCF-7 cell line, whereas compound 9a showed an analogous activity to doxorubicin...Besides, docking of the desired compounds into Pim-1 ATP binding site showed a noteworthy binding mode for the enzyme inhibition. Additionally, a 2D QSAR identified the potential structural features controlling the Pim-1 inhibitory activity attained via the targeted pyrazolo[1,5-a]pyrimidines.

2 months ago

Journal

TP53 (Tumor protein P53) • PIM1 (Pim-1 Proto-Oncogene)

doxorubicin hydrochloride

2ms

Stereotactic Body Radiotherapy and Focal Adhesion Kinase Inhibitor in Advanced Pancreas Adenocarcinoma (clinicaltrials.gov)

P2, N=42, Active, not recruiting, Washington University School of Medicine | Trial primary completion date: Sep 2025 --> Dec 2025

2 months ago

Trial primary completion date

Fakzynja (defactinib)

3ms

Design and synthesis of new Thieno[2,3-d]pyrimidine-based derivatives as anti-breast cancer: Biological evaluation, PIM-1 kinase inhibition, and in silico studies. (PubMed, Bioorg Chem)

Compound 15 demonstrated the strongest anticancer activity, with IC50 value of 34.49 ± 1.32 μM, compared to doxorubicin (IC50 = 34.20 ± 0.28 μM)...Additionally, the binding relationships produced between compound 15 and the PIM-1 kinase active site were investigated using molecular docking experiments, providing insights into their inhibitory potential. Finally, to further assess the stability of the compound 15-PIM-1 kinase complex and validate the docking results, molecular dynamics (MD) simulations were performed.

3 months ago

Journal • IO biomarker

BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • PIM1 (Pim-1 Proto-Oncogene)

doxorubicin hydrochloride

3ms

KC1036, a multi-kinase inhibitor with anti-angiogenic activity, can effectively suppress the tumor growth of Ewing sarcoma. (PubMed, Angiogenesis)

The novel anti-angiogenic inhibitor, KC1036, is effective in treating ES in the preclinical models.

3 months ago

Journal

FGFR (Fibroblast Growth Factor Receptor) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • FLT1 (Fms-related tyrosine kinase 1) • NPY1R (Neuropeptide Y Receptor Y1)

doxorubicin hydrochloride • pazopanib • Cabometyx (cabozantinib tablet) • KC1036

3ms

ACCRU-GI-2008: Atezolizumab in Combination With a Multi-Kinase Inhibitor for the Treatment of Unresectable, Locally Advanced, or Metastatic Liver Cancer (clinicaltrials.gov)

P2, N=122, Recruiting, Academic and Community Cancer Research United | Trial primary completion date: Dec 2024 --> Dec 2025

3 months ago

Trial primary completion date

Avastin (bevacizumab) • Tecentriq (atezolizumab) • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet)

3ms

CA209-8LC: Study of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer (clinicaltrials.gov)

P1/2, N=48, Completed, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Active, not recruiting --> Completed

3 months ago

Trial completion • Mismatch repair • pMMR

KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)

KRAS wild-type • BRAF wild-type • NRAS wild-type

Opdivo (nivolumab) • Aliqopa (copanlisib)

3ms

Synergy of advanced machine learning and deep neural networks with consensus molecular docking for virtual screening of anaplastic lymphoma kinase inhibitors. (PubMed, J Comput Aided Mol Des)

Combining these two approaches, we virtually screened 120,571 compounds, identifying three promising ALK inhibitors, CHEMBL1689515, CHEMBL2380351, and CHEMBL102714, that bind to the protein's pocket and establish hydrophobic contacts in the hinge region through their ketone groups, resembling Alectinib's interaction...The study recommends further in vitro testing to validate the prospective screening performance of these models. A graphical user interface is available at https://huggingface.co/spaces/thechuongtrinh/ALK_inhibitors_classification .

3 months ago

Journal

ALK (Anaplastic lymphoma kinase)

ALK positive • ALK mutation

Alecensa (alectinib)