^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

Lck inhibitor

Associations
over1year
Discovery of a Novel and Potent LCK Inhibitor for Leukemia Treatment via Deep Learning and Molecular Docking. (PubMed, J Chem Inf Model)
In addition, complementary molecular dynamics simulations provided deeper insight into the binding kinetics between 1232030-35-1 and LCK, highlighting the formation of a hydrogen bond with Met319. Collectively, our study established a robust and effective screening strategy that integrates AI-driven and conventional methodologies for the identification of LCK inhibitors, positioning 1232030-35-1 as a highly promising and novel drug-like candidate for potential applications in treating T-ALL.
Journal
|
LCK (LCK Proto-Oncogene, Src Family Tyrosine Kinase)
2years
Identification of 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one scaffolds as potent Lck inhibitors as anti-cancer agents. (PubMed, Bioorg Med Chem Lett)
Notably, 12a inhibited the phosphorylation of Lck in Colo201 cells. Overall, the anti-proliferative effects of 12a on diverse cancer cell lines highlights its potential application for the treatment of various cancer types.
Journal • IO biomarker
|
LCK (LCK Proto-Oncogene, Src Family Tyrosine Kinase)
almost3years
Integrated CRISPR screening and drug profiling identifies combination opportunities for EGFR, ALK, and BRAF/MEK inhibitors. (PubMed, Cell Rep)
Data from drug combination screens with EGF816 and ceritinib indicate that dasatinib and agents disrupting microtubules act synergistically across many cell lines. Finally, we show that a higher-order-combination screen with 26 selected drugs in two resistant EGFR-mutant lung cancer cell lines identified active triplet combinations.
Journal
|
EGFR (Epidermal growth factor receptor) • BCL2L1 (BCL2-like 1) • YAP1 (Yes associated protein 1)
|
EGFR mutation
|
dasatinib • Zykadia (ceritinib) • nazartinib (EGF816)
almost3years
Antifibrotic mechanism of avitinib in bleomycin-induced pulmonary fibrosis in mice. (PubMed, BMC Pulm Med)
At present, only two drugs are approved by the FDA for the treatment of IPF, including the synthetic pyridinone drug, pirfenidone, and the tyrosine kinase inhibitor, nintedanib. The cellular experiments also indicated that avitinib improved alveolar epithelial cell injury in A549 cells. In conclusion, the present findings demonstrated that avitinib attenuates bleomycin-induced pulmonary fibrosis in mice by inhibiting alveolar epithelial cell injury and myofibroblast activation.
Preclinical • Journal
|
TGFB1 (Transforming Growth Factor Beta 1) • SMAD3 (SMAD Family Member 3)
|
nintedanib • bleomycin • Fujovee (abivertinib)
almost3years
Pralsetinib for RET Fusion-Positive Advanced Non-small-Cell Lung Cancer: An Evidence Review Group Perspective of a NICE Single Technology Appraisal. (PubMed, Pharmacoeconomics)
The comparators in the untreated population were pembrolizumab + pemetrexed + chemotherapy and pembrolizumab monotherapy. The comparators for the pre-treated population were docetaxel monotherapy, docetaxel + nintedanib, and platinum-based chemotherapy ± pemetrexed...The uncertainty of the clinical evidence and the estimates of cost effectiveness were too high to be considered a cost-effective use of NHS resources. Therefore, pralsetinib was not recommended for routine use.
NICE • Review • Journal • Metastases
|
RET (Ret Proto-Oncogene)
|
RET fusion • RET positive
|
Keytruda (pembrolizumab) • docetaxel • pemetrexed • Gavreto (pralsetinib) • nintedanib
almost3years
An immune-related signature for optimizing prognosis prediction and treatment decision of hepatocellular carcinoma. (PubMed, Eur J Med Res)
This study developed a robust IGS model for survival prediction of HCC patients, providing new insights into integrating tailored risk stratification with precise immunotherapy and screening potentially targeted agents.
Journal • IO biomarker
|
TP53 (Tumor protein P53) • IL6 (Interleukin 6)
|
TP53 mutation
|
dasatinib • ispinesib (SB-715992) • vindesine
almost3years
Constructing a novel mitochondrial-related gene signature for evaluating the tumor immune microenvironment and predicting survival in stomach adenocarcinoma. (PubMed, J Transl Med)
Our results suggest that the mitochondrial-related risk model could be a reliable prognostic biomarker for personalized treatment of STAD patients.
Journal • Tumor mutational burden • Gene Signature • IO biomarker
|
TMB (Tumor Mutational Burden) • NOX4 (NADPH Oxidase 4) • FKBP10 (FKBP Prolyl Isomerase 10)
|
dasatinib • methotrexate • Gomekli (mirdametinib) • sirolimus • lestaurtinib (CEP-701) • AZD-7762
almost3years
A Novel Quantum Dots-Based Fluorescent Sensor for Determination of the Anticancer Dacomitinib: Application to Dosage Forms. (PubMed, Molecules)
Finally, the proposed method was applied to a pharmaceutical dosage form of the drug (Vizimpro Tablets) and the obtained results were satisfactory. Considering the eco-friendly aspect of the suggested methodology, using natural materials to synthesize N-CQDs and water as a diluting solvent added to its greenness profile.
Journal
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation
|
Vizimpro (dacomitinib)
almost3years
Patient-guided dose reduction of tyrosine kinase inhibitors in chronic myeloid leukaemia (RODEO study): study protocol for a prospective, multicentre, single-arm trial. (PubMed, BMC Cancer)
Outcomes of this trial using a personalised approach will provide clinical and patient-reported data to guide future dose reduction of TKIs in CML. If the strategy appears to be effective, it may be implemented as another valid option to offer next to standard of care to prevent potential unnecessary exposure to higher TKI doses in this selected group of patients.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib • Iclusig (ponatinib) • nilotinib • bosutinib
almost3years
New therapies in non-small cell lung cancer with EGFR exon 20 insertion mutations. (PubMed, J Oncol Pharm Pract)
The efficacy of mobocertinib, amivantamab and poziotinib in NSCLC with EGFR exon 20 insertion mutations is promising. However, therapies were assessed in single-arm CTs with low-quality evidence. Comparative studies with more extensive patient follow-up, larger sample size and better design are needed to reliably quantify the effect of these drugs.
Review • Journal • EGFR exon 20
|
EGFR (Epidermal growth factor receptor)
|
EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation
|
Tagrisso (osimertinib) • erlotinib • docetaxel • Perjeta (pertuzumab) • Kadcyla (ado-trastuzumab emtansine) • Vizimpro (dacomitinib) • Rybrevant (amivantamab-vmjw) • Pozenveo (poziotinib) • Exkivity (mobocertinib) • luminespib (AUY922) • onalespib (AT13387)
almost3years
Modulating tumor-stromal crosstalk via a redox-responsive nanomedicine for combination tumor therapy. (PubMed, J Control Release)
Herein, we prepared a redox-responsive chondroitin sulfate (CS)-based nanomedicine, in which hydrophobic cabazitaxel (CTX) was conjugated to the backbone of CS via glutathione (GSH)-sensitive dithiomaleimide (DTM) to form an amphipathic CS-DTM-CTX (CDC) conjugate, and dasatinib (DAS) co-assembled with the CDC conjugate to obtain DAS@CDC. Meanwhile, the nanomedicine internalized by tumor cells could effectively inhibit tumor proliferation and metastasis, leading to shrinkage of the tumor volume and inhibition of lung metastasis in a subcutaneous 4 T1 tumor model with low side effects. Collectively, the nanomedicine showed a remarkably synergistic therapy effect against breast cancer by modulating tumor-stromal crosstalk.
Journal • Stroma
|
FN1 (Fibronectin 1)
|
dasatinib • cabazitaxel
almost3years
ImmunoPET Imaging Identifies the Optimal Timepoint for Combination Therapy in Xenograft Models of Triple-Negative Breast Cancer. (PubMed, Cancers (Basel))
(4) Dasatinib upregulated gpNMB expression in gpNMB-positive MDA-MB-468 xenografted tumors at 14 days post treatment initiation, which can be quantified by PET imaging with [Zr]Zr-DFO-CR011. Furthermore, combination therapy with dasatinib and CDX-011 appears to be a promising therapeutic strategy for TNBC and warrants further investigation.
Preclinical • Journal • Combination therapy
|
GPNMB (Glycoprotein Nmb)
|
dasatinib • glembatumumab vedotin (CDX-011)