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DRUG:

dasatinib

i
Other names: BMS 354825, BMS-354825, BMS354825
Company:
Generic mfg.
Drug class:
c-KIT inhibitor, Bcr-abl tyrosine kinase inhibitor, Src kinase inhibitor, EphA2 receptor antagonist, PDGFR β antagonist
Related drugs:
23h
Ma-Spore ALL 2020 Study (clinicaltrials.gov)
P2, N=500, Recruiting, National University Hospital, Singapore
New P2 trial
|
dasatinib • Rituxan (rituximab) • imatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • vincristine • fludarabine IV • mercaptopurine • thioguanine
1d
PDGFRA K385 mutants in myxoid glioneuronal tumors promote receptor dimerization and oncogenic signaling. (PubMed, Sci Rep)
Furthermore, we evaluated the sensitivity of these mutants to three FDA-approved tyrosine kinase inhibitors: imatinib, dasatinib, and avapritinib, which effectively suppressed the constitutive activity of the mutant receptors. Interestingly, K385M was reported in a few cases of brain tumors but not in MGNT. Our results provide valuable insights into the molecular mechanism underlying the activation of PDGFRα by the K385I/L mutations, highlighting their potential as actionable targets in the treatment of myxoid glioneuronal tumors.
Journal
|
PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
|
PDGFRA mutation
|
dasatinib • imatinib • Ayvakit (avapritinib)
2d
The immune regulation and therapeutic potential of the SMAD gene family in breast cancer. (PubMed, Sci Rep)
Interestingly, patients with high expression of SMAD3 exhibited significant resistance to dasatinib and staurosporine, while high sensitivity to tamoxifen and auranofin. In addition, SMAD3 knockdown promoted the apoptosis of BT-549 cells and decreased cell activity, and BAY-1161909 and XK-469 increased drug efficacy. In conclusion, genes of the SMAD family play a crucial role in the development of breast cancer.
Journal
|
SMAD4 (SMAD family member 4) • TGFB1 (Transforming Growth Factor Beta 1) • SMAD7 (SMAD Family Member 7) • SMAD2 (SMAD Family Member 2) • SMAD3 (SMAD Family Member 3)
|
dasatinib • tamoxifen • empesertib (BAY1161909)
7d
Dasatinib In Waldenström Macroglobulinemia (clinicaltrials.gov)
P1, N=3, Terminated, Jorge J. Castillo, MD | Recruiting --> Terminated; Lack of efficacy
Trial termination
|
MYD88 (MYD88 Innate Immune Signal Transduction Adaptor) • PLCG2 (Phospholipase C Gamma 2)
|
MYD88 mutation
|
dasatinib • Imbruvica (ibrutinib)
9d
Synergistic effect of cannabidiol with dasatinib on lung cancer by SRC/PI3K/AKT signal pathway. (PubMed, Biomed Pharmacother)
The xenograft mouse model suggested that the combination was more efficient and safer. In short, CBD and low-dose dasatinib exhibited a synergistic effect on anticancer by targeting the SRC/PI3K/AKT signaling pathway, suggesting a potential therapeutic option for the treatment of lung cancer.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • CASP3 (Caspase 3)
|
dasatinib
14d
Drug-induced chylothorax as a rare pleural complication in dasatinib therapy for chronic myeloid leukaemia. (PubMed, J R Coll Physicians Edinb)
Chylothorax is a lymphatic chylous pleural effusion typically associated with traumatic (iatrogenic, non-iatrogenic) and non-traumatic (infections, malignancy, lymphatic disorders) aetiologies. Drug-induced chylothorax is uncommon and mostly reported in association with BCR-ABL tyrosine kinase inhibitor therapy.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib
14d
Bioresponsive nanocomplex integrating cancer-associated fibroblast deactivation and immunogenic chemotherapy for rebuilding immune-excluded tumors. (PubMed, Nanomedicine)
The GNC co-loaded dasatinib, a CAF inhibitor, and paclitaxel, a chemotherapeutic agent, to deactivate CAFs and enhance the effects of immunogenic chemotherapy. Moreover, GNC treatment exhibited remarkable immunostimulatory efficacy, including CD8+ T cell expansion and PD-L1 downregulation, facilitating immune checkpoint blockade therapy. In summary, the integration of CAF deactivation and immunogenic chemotherapy using the GNC nanoplatform holds promise for rebuilding immune-excluded tumors.
Journal
|
CD8 (cluster of differentiation 8)
|
dasatinib • paclitaxel
16d
Trial completion date • Surgery • Metastases
|
erlotinib • dasatinib • gemcitabine
17d
Imatinib Mesylate or Dasatinib in Treating Patients With Previously Untreated Chronic Phase Chronic Myelogenous Leukemia (clinicaltrials.gov)
P2, N=406, Active, not recruiting, National Cancer Institute (NCI) | Phase classification: P2b --> P2
Phase classification • Trial completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib
23d
YES1 as a potential target to overcome drug resistance in EGFR-deregulated non-small cell lung cancer. (PubMed, Arch Toxicol)
Epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) such as gefitinib and osimertinib have primarily been used as first-line treatments for patients with EGFR-activating mutations in non-small cell lung cancer (NSCLC)...Furthermore, the combination of gefitinib and dasatinib demonstrated a synergistic effect in suppressing the proliferation of HCC827/GR cells. Notably, YES1- and Nrf2-regulated genes showed a positive regulatory relationship in patients with lung cancer and in TKI-resistant NSCLC cell lines. Taken together, these findings suggest that modulation of YES1 expression and activity may be an attractive therapeutic strategy for the treatment of drug-resistant NSCLC.
Journal • IO biomarker
|
EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • BCL2L1 (BCL2-like 1) • YAP1 (Yes associated protein 1)
|
EGFR mutation • CCND1 expression
|
Tagrisso (osimertinib) • dasatinib • gefitinib
23d
Clinical efficacy and safety of flumatinib versus dasatinib combined with multi-drug chemotherapy in adults with Philadelphia-positive acute lymphoblastic leukemia. (PubMed, Hematol Transfus Cell Ther)
These findings suggest that flumatinib is a safe and effective tyrosine kinase inhibitor (TKI) for achieving CMR and MRD negativity in patients with Ph+ ALL, as supported by this small series of patients.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib • Hansoh Xinfu (flumatinib)
23d
Characteristics and literature review of ETV6::ABL1 fusion gene-positive acute myeloid leukemia. (PubMed, Int J Hematol)
ETV6::ABL1 is a rare but recurrent genetic aberration in AML, and the combined use of fluorescence in situ hybridization and PCR can better identify this fusion gene. Patients carrying ETV6::ABL1 have a high relapse rate and a poor prognosis. TKIs are a reasonable treatment option for this group, and allo-HSCT may be curative.
Review • Journal
|
ABL1 (ABL proto-oncogene 1) • ETV6 (ETS Variant Transcription Factor 6)
|
ABL1 fusion • ETV6-ABL1 fusion
|
dasatinib
24d
Trial initiation date
|
ABL1 (ABL proto-oncogene 1) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • CD19 (CD19 Molecule) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CSF1R (Colony stimulating factor 1 receptor)
|
CD19 expression
|
TruSight RNA Pan-Cancer Panel
|
dasatinib • imatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • Blincyto (blinatumomab) • methotrexate • vincristine • daunorubicin • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • Asparlas (calaspargase pegol-mknl) • thioguanine • Starasid (cytarabine ocfosfate)
25d
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial (clinicaltrials.gov)
P1, N=2, Terminated, OHSU Knight Cancer Institute | Active, not recruiting --> Terminated; Low accrual
Trial termination
|
Keytruda (pembrolizumab) • Opdivo (nivolumab) • Avastin (bevacizumab) • Venclexta (venetoclax) • Lynparza (olaparib) • Mekinist (trametinib) • erlotinib • Gilotrif (afatinib) • Yervoy (ipilimumab) • Ibrance (palbociclib) • dasatinib • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • carboplatin • Imfinzi (durvalumab) • sorafenib • Rozlytrek (entrectinib) • imatinib • Sutent (sunitinib) • everolimus • Nerlynx (neratinib) • Iclusig (ponatinib) • Kadcyla (ado-trastuzumab emtansine) • Cotellic (cobimetinib) • Lorbrena (lorlatinib) • Lenvima (lenvatinib) • bortezomib • doxorubicin hydrochloride • capecitabine • Verzenio (abemaciclib) • enzalutamide capsule • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Stivarga (regorafenib) • abiraterone acetate • oxaliplatin • Aliqopa (copanlisib) • Vizimpro (dacomitinib) • Zydelig (idelalisib) • daunorubicin • Zolinza (vorinostat) • Idhifa (enasidenib) • Farydak (panobinostat) • Erivedge (vismodegib) • Nubeqa (darolutamide) • bicalutamide • leucovorin calcium • cabazitaxel • Vesanoid (tretinoin) • fluorouracil topical
25d
High-dose methotrexate pharmacokinetics and its impact on prognosis of paediatric acute lymphoblastic leukaemia patients: A population pharmacokinetic study. (PubMed, Br J Haematol)
Additionally, utilizing population pharmacokinetic modelling (6051 concentrations from 815 patients), we identified the significant impact of physiological maturation, estimated glomerular filtration rate, sex and concurrent dasatinib administration on MTX pharmacokinetics...The findings underscore the critical role of HDMTX in treating IR/HR populations and call for a reassessment of its application in lower-risk groups. An individualized pharmacokinetic dosage regimen could achieve the most optimal results, ensuring the largest proportion of steady-state concentrations within the optimal range.
PK/PD data • Journal
|
KMT2A (Lysine Methyltransferase 2A)
|
MLL rearrangement • MLL rearrangement
|
dasatinib • methotrexate
25d
Targeting HER2-positive breast cancer cells by a combination of dasatinib and BMS-202: Insight into the molecular pathways. (PubMed, Cancer Cell Int)
Our findings implicate that a combination of DA and BMS-202 could have a significant impact on the management of HER2-positive breast cancer.
Journal • PD(L)-1 Biomarker • IO biomarker
|
HER-2 (Human epidermal growth factor receptor 2) • CDH1 (Cadherin 1) • VIM (Vimentin) • MAPK8 (Mitogen-activated protein kinase 8)
|
HER-2 positive • CDH1 expression • VIM expression
|
dasatinib • BMS-202
26d
Trial Treating Relapsed Acute Lymphoblastic Leukemia With Venetoclax and Navitoclax (clinicaltrials.gov)
P1/2, N=90, Recruiting, St. Jude Children's Research Hospital | Trial primary completion date: Aug 2024 --> Aug 2025
Trial primary completion date
|
Venclexta (venetoclax) • dasatinib • cytarabine • cyclophosphamide • etoposide IV • Blincyto (blinatumomab) • vincristine • navitoclax (ABT 263) • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • Asparlas (calaspargase pegol-mknl)
26d
Dasatinib, Temsirolimus, and Cyclophosphamide in Treating Patients With Advanced, Recurrent, or Refractory Solid Tumors (clinicaltrials.gov)
P1, N=14, Active, not recruiting, M.D. Anderson Cancer Center | Trial completion date: Oct 2023 --> Oct 2024 | Trial primary completion date: Oct 2023 --> Oct 2024
Trial completion date • Trial primary completion date • Metastases
|
dasatinib • cyclophosphamide • Torisel (temsirolimus)
28d
Immune-related long noncoding RNA zinc finger protein 710-AS1-201 promotes the metastasis and invasion of gastric cancer cells. (PubMed, World J Gastrointest Oncol)
Immune-related lncRNA ZNF710-AS1-201 facilitates the metastasis and invasion of GC cells. It appears that ZNF710-AS1-201 and ZNF710 have potential as effective targets for therapeutic intervention in GC. Nevertheless, it is still necessary to determine the specific targets of the ZNF710 TF.
Journal
|
CD8 (cluster of differentiation 8) • CD4 (CD4 Molecule) • MIR93 (MicroRNA 93)
|
Mekinist (trametinib) • cisplatin • dasatinib • gemcitabine • 5-fluorouracil • Zolinza (vorinostat)
29d
Pharmacovigilance study of BCR-ABL1 tyrosine kinase inhibitors: a safety analysis of the FDA adverse event reporting system. (PubMed, BMC Pharmacol Toxicol)
The results of this study demonstrated that AE signals differ among the five BCR-ABL1 TKIs. Furthermore, each BCR-ABL1 TKI displayed several new signals. These findings provide valuable information for clinicians aiming to reduce the risk of AEs during BCR-ABL1 TKI treatment.
Journal • Adverse events
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib)
1m
High-resolution transcriptomics analysis of CXCL13+ EPSTI1+ CDK1+ cells with a specific focus on lung adenocarcinoma. (PubMed, J Thorac Dis)
Finally, the subpopulation-enriched targets and drugs were confirmed through ConnectivityMap (CMAP) analysis and multi-omics, respectively. In this study, positive samples for CXCL13, EPSTI1, and CDK1 exhibited poor prognostic significance in treatment-naïve LUAD cases but demonstrated benefits from PD-L1 blockade and dasatinib therapies.
Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
|
TMB (Tumor Mutational Burden) • STK11 (Serine/threonine kinase 11) • CD74 (CD74 Molecule) • CXCL13 (Chemokine (C-X-C motif) ligand 13) • CDK1 (Cyclin-dependent kinase 1) • EPSTI1 (Epithelial Stromal Interaction 1)
|
dasatinib
1m
Machine learning reveals diverse cell death patterns in lung adenocarcinoma prognosis and therapy. (PubMed, NPJ Precis Oncol)
Additionally, we found that patients with a high PCDI score may exhibit resistance to immunotherapy and standard adjuvant chemotherapy regimens; however, they may benefit from other FDA-supported drugs such as docetaxel and dasatinib. In conclusion, the PCDI holds potential as a prognostic signature and can facilitate personalized treatment for LUAD patients.
Journal • IO biomarker • Machine learning
|
CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • CHEK2 (Checkpoint kinase 2) • CD79A (CD79a Molecule) • RRM2 (Ribonucleotide Reductase Regulatory Subunit M2) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase) • MMP1 (Matrix metallopeptidase 1) • ITGB4 (Integrin Subunit Beta 4) • KRT18 (Keratin 18) • TMPRSS4 (Transmembrane Serine Protease 4)
|
dasatinib • docetaxel
1m
Tyrosine kinase inhibitor response of ABL-class acute lymphoblastic leukemia: The role of kinase type and SH3 domain. (PubMed, Blood)
We showed that ALL samples with fusions of any of the four tyrosine kinase genes were relatively sensitive to imatinib. In contrast, PDGFRB-fused ALL samples were less sensitive to dasatinib and bosutinib. Variation in ex vivo TKI response within the subset of samples with the same ABL-class tyrosine kinase gene was not associated with ALL immunophenotype, 5' fusion partner, the presence or absence of the Src-homology-2/3 domains, or deletions of IKZF1, PAX5, or CDKN2A/B. In conclusion, the tyrosine kinase gene involved in ABL-class ALL is the main determinant for TKI sensitivity and is relevant for specific TKI selection.
Journal
|
ABL1 (ABL proto-oncogene 1) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • IKZF1 (IKAROS Family Zinc Finger 1) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • PAX5 (Paired Box 5) • ABL2 (ABL Proto-Oncogene 2, Non-Receptor Tyrosine Kinase) • CSF1R (Colony stimulating factor 1 receptor)
|
CDKN2A deletion
|
dasatinib • imatinib • Bosulif (bosutinib)
1m
Association of changes in expression of HDAC and SIRT genes after drug treatment with cancer cell line sensitivity to kinase inhibitors. (PubMed, Epigenetics)
HDAC5 was upregulated by dasatinib and erlotinib in the majority of the cell lines. HDAC5 was not upregulated in the UACC-257 cell line resistant to dasatinib. The effects of cancer drug treatment on expression of HDAC and SIRT genes may influence chemosensitivity and may need to be considered during chemotherapy.
Preclinical • Journal
|
HDAC1 (Histone Deacetylase 1) • HDAC5 (Histone Deacetylase 5)
|
erlotinib • dasatinib
1m
Randomized Phase III Study of Intensive Chemotherapy With or Without Dasatinib (Sprycel™) (clinicaltrials.gov)
P3, N=204, Completed, University of Ulm | Active, not recruiting --> Completed
Trial completion
|
RUNX1 (RUNX Family Transcription Factor 1) • RUNX1T1 (RUNX1 Partner Transcriptional Co-Repressor 1)
|
RUNX1-RUNX1T1 fusion • CBFB-MYH11 fusion
|
dasatinib • daunorubicin • idarubicin hydrochloride
1m
Pediatric-Inspired Chemotherapy Plus Tyrosine Kinase Inhibitor in Adult Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia (clinicaltrials.gov)
P2, N=0, Withdrawn, University of Michigan Rogel Cancer Center | N=23 --> 0 | Recruiting --> Withdrawn
Enrollment change • Trial withdrawal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • cytarabine • Iclusig (ponatinib) • doxorubicin hydrochloride • cyclophosphamide
1m
Pharmacokinetics of Dasatinib in Rats: a Potential Food-Drug Interaction with Naringenin. (PubMed, Eur J Drug Metab Pharmacokinet)
Concurrent use of naringenin-containing supplements, herbs, or foods with dasatinib may cause serious and potentially life-threatening drug interactions. Further studies are necessary to determine the clinical significance of these findings.
PK/PD data • Preclinical • Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
dasatinib
1m
Neoadjuvant Tislelizumab in Combination With Dasatinib and Quercetin in Resectable HNSCC (COIS-01) (clinicaltrials.gov)
P2, N=24, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Trial primary completion date: Sep 2023 --> Jun 2024
Trial primary completion date • Combination therapy
|
dasatinib • Tevimbra (tislelizumab)
1m
Combination Chemotherapy With or Without Donor Stem Cell Transplant in Treating Patients With Acute Lymphoblastic Leukemia (clinicaltrials.gov)
P2, N=97, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jan 2024 --> Jan 2025
Trial completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CD22 (CD22 Molecule) • CD5 (CD5 Molecule) • CD79A (CD79a Molecule) • MME (Membrane Metalloendopeptidase) • CD7 (CD7 Molecule) • ANPEP (Alanyl Aminopeptidase, Membrane) • MPO (Myeloperoxidase)
|
dasatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • methotrexate • vincristine • sirolimus • leucovorin calcium • Hemady (dexamethasone tablets) • Neupogen (filgrastim) • Starasid (cytarabine ocfosfate)
1m
Study of Brexucabtagene Autoleucel Plus Dasatinib in Adults With Acute Lymphoblastic Leukemia (clinicaltrials.gov)
P1, N=20, Recruiting, Stanford University | Phase classification: P1b --> P1
Phase classification
|
CD19 (CD19 Molecule)
|
CD19 expression
|
dasatinib • Tecartus (brexucabtagene autoleucel)
1m
A Six-gene Prognostic Model Based on Neutrophil Extracellular Traps (NETs)-related Gene Signature for Lung Adenocarcinoma. (PubMed, Comb Chem High Throughput Screen)
Altogether, this study has identified a novel NET-score signature based on six novel NET-related genes to predict the prognosis of LUAD and ABCC2 and has also explored a new method for personalized chemo-/immuno-therapy of LUAD.
Journal • Gene Signature • IO biomarker
|
ABCC2 (ATP Binding Cassette Subfamily C Member 2) • UPK1B (Uroplakin 1B)
|
dasatinib • lapatinib • zorifertinib (AZD3759)
1m
TPX2 overexpression promotes sensitivity to dasatinib in breast cancer by activating YAP transcriptional signaling. (PubMed, Mol Oncol)
We find that the overexpression of targeting protein for Xklp2 (TPX2) enhances sensitivity to the proto-oncogene c-Src (SRC) inhibitor dasatinib due to activation of the Yes-associated protein 1 (YAP) pathway. Furthermore, using breast cancer data from The Cancer Genome Atlas (TCGA) and a cohort of cancer-derived patient samples, we find that both TPX2 overexpression and YAP activation are present in a significant percentage of cancer tumor samples and are associated with poor prognosis; therefore, they are putative biomarkers for selection for dasatinib therapy.
Journal
|
YAP1 (Yes associated protein 1) • TPX2 (TPX2 Microtubule Nucleation Factor)
|
dasatinib
1m
UPP1 promotes lung adenocarcinoma progression through the induction of an immunosuppressive microenvironment. (PubMed, Nat Commun)
Using patient-derived organoids (PDOs), we discover that UPP1high tumors exhibit relatively increased sensitivity to Bosutinib and Dasatinib. Collectively, our study highlights the immunosuppressive role of UPP1 in LUAD, and these findings may provide insights into the molecular features of LUAD and facilitate the development of personalized treatment strategies.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • CD8 (cluster of differentiation 8) • TGFB1 (Transforming Growth Factor Beta 1)
|
PD-L1 expression
|
dasatinib • Bosulif (bosutinib)
1m
Superbinder based phosphoproteomic landscape revealed PRKCD_pY313 mediates the activation of Src and p38 MAPK to promote TNBC progression. (PubMed, Cell Commun Signal)
Collectively, the heterogeneity of phosphorylation exists in different molecular subtypes of breast cancer. PRKCD_pY313 activates Src and accelerates TNBC progression, which could be inhibited by Dasatinib.
Journal
|
BCL2L1 (BCL2-like 1) • CASP3 (Caspase 3) • VIM (Vimentin) • TJP1 (Tight Junction Protein 1)
|
dasatinib
2ms
The novel TERF2::PDGFRB fusion gene enhances tumorigenesis via PDGFRB/STAT5 signalling pathways and sensitivity to TKI in ph-like ALL. (PubMed, J Cell Mol Med)
Our study has unveiled a newfound fusion gene, TERF2::PDGFRB, and we have found that patients carrying this fusion gene exhibit sensitivity to dasatinib. When transfused into mice, Ba/F3 cells with the TERF2::PDGFRB fusion gene induce tumorigenesis and a shortened lifespan in cell-derived graft models, but this outcome can be improved with imatinib treatment. In summary, we have identified the novel TERF2::PDGFRB fusion gene, which exhibits oncogenic potential both in vitro and in vivo, making it a potential therapeutic target for tyrosine kinase inhibitors (TKIs).
Journal
|
PDGFRB (Platelet Derived Growth Factor Receptor Beta)
|
PDGFRB fusion
|
dasatinib • imatinib
2ms
Trial completion
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • methotrexate • vincristine • daunorubicin • Starasid (cytarabine ocfosfate)
2ms
Monitoring drug metabolic pathways through extracellular vesicles in mouse plasma. (PubMed, PNAS Nexus)
Out of 44 known ADME proteins in plasma EVs, previously annotated mouse cytochrome P450 3A11 (Cyp3a11), homolog to human CYP3A4, and uridine 5'-diphospho (UDP) glucuronosyltransferase 2A3 (Ugt2a3), increased upon daily rifampicin dosage. Dasatinib, a tyrosine kinase inhibitor to treat leukemia, also elevated Cyp3a11 levels in plasma EVs, but to a lesser extent. Altogether, this study demonstrates that measuring drug enzymes in circulating EVs as an effective surrogate is highly feasible and may transform today's drug discovery and development for personalized medicine.
Preclinical • Journal
|
CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
|
dasatinib • rifampicin
2ms
Bioinformatics analysis identifies coagulation factor II receptor as a potential biomarker in stomach adenocarcinoma. (PubMed, Sci Rep)
Drug sensitivity analysis demonstrated positive correlations between F2R and several drugs, including BEZ235, CGP-60474, Dasatinib, HG-6-64-1, Aazopanib, Rapamycin, Sunitinib and TGX221, while negative correlation with CP724714, FH535, GSK1904529A, JNK-9L, LY317615, pyrimidine, rTRAIL and Vinorelbine. In conclusion, this study underscores the significance of F2R as a potential biomarker in gastric adenocarcinoma, shedding light on its molecular mechanisms in tumorigenesis. F2R holds promise for aiding in the diagnosis, prognosis, and targeted therapy of STAD.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1)
|
dasatinib • Sutent (sunitinib) • dactolisib (RTB101) • vinorelbine tartrate • sirolimus • Kinenza (enzastaurin) • TGX-221
2ms
Unraveling T cell exhaustion in the immune microenvironment of osteosarcoma via single-cell RNA transcriptome. (PubMed, Cancer Immunol Immunother)
Drug sensitivity analysis revealed that OS patients with a low Tex risk were responsive to Dasatinib and Pazopanib. Finally, immunohistochemistry verified that MYC and FCGR2B were significantly upregulated in OS tissues compared with adjacent tissues. This study investigates the role of Tex within the TIME of OS, and offers novel insights into the mechanisms underlying disease progression as well as the potential treatment strategies for OS.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-1 (Programmed cell death 1) • LAG3 (Lymphocyte Activating 3) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • ENTPD1 (Ectonucleoside Triphosphate Diphosphohydrolase 1) • FCGR2B (Fc Fragment Of IgG Receptor IIb)
|
PD-1 expression
|
dasatinib • Votrient (pazopanib)
2ms
Single Nuclei RNA-seq to Map Adipose Cellular Populations and Senescent Cells in Older Subjects (clinicaltrials.gov)
P2/3, N=160, Recruiting, Cedars-Sinai Medical Center | Not yet recruiting --> Recruiting
Enrollment open
|
dasatinib
2ms
Molecular prognostic of nine parthanatos death-related genes in glioma, particularly in COL8A1 identification. (PubMed, J Neurochem)
Low-score glioma patients were sensitive to AZD3759_1915, AZD5582_1617, AZD8186_1918, Dasatinib_1079, and Temozolomide_1375, while high-score patients were less sensitive to these drugs. Silencing COL8A1 inhibited the malignant characterization. Temozolomide and AZD3759 inhibited COL8A1 expression and cell viability and promoted apoptosis and parthanatos gene expression, which is a target to improve glioma.
Journal
|
CD58 (CD58 Molecule) • COL8A1 (Collagen Type VIII Alpha 1 Chain) • FABP5 (Fatty Acid Binding Protein 5) • TNFRSF11B (Tumor necrosis factor receptor superfamily member 11B)
|
dasatinib • temozolomide • AZD8186 • zorifertinib (AZD3759)