^
5d
Trial completion date
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • RUNX1 (RUNX Family Transcription Factor 1) • KMT2A (Lysine Methyltransferase 2A) • ETV6 (ETS Variant Transcription Factor 6)
|
MLL rearrangement • MLL rearrangement
|
dasatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • methotrexate • vincristine • daunorubicin • clofarabine • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine • Hemady (dexamethasone tablets) • Starasid (cytarabine ocfosfate)
12d
Dasatinib induces apoptosis and autophagy by suppressing the PI3K/Akt/mTOR pathway in bladder cancer cells. (PubMed, Investig Clin Urol)
These results confirmed that dasatinib is a potent chemotherapeutic drug which induces apoptosis and autophagy by suppressing the PI3K/Akt/mTOR pathway in bladder cancer cells.
Journal • PARP Biomarker • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2)
|
cisplatin • dasatinib
13d
Exploration on the construction of a bladder cancer prognostic model based on disulfidptosis-related lncRNAs and its clinical significance. (PubMed, Sci Rep)
Lastly, the drug sensitivity analysis revealed that the BLCA cells in the high-risk group showed an increased sensitivity to cisplatin, sunitinib, cetuximab, axitinib, docetaxel, saracatinib, vinblastine and pazopanib compared with those in the low-risk group. According to the Quantitative real time PCR results, we found that five lncRNAs of the risk model were more highly expressed in BCa cell lines than human immortalized uroepithelial cell line. The disulfidptosis-related lncRNA risk model has a valuable effect in assessing the prognosis of BLCA patients.
Journal • Tumor mutational burden • IO biomarker
|
TMB (Tumor Mutational Burden)
|
TMB-L
|
Erbitux (cetuximab) • cisplatin • docetaxel • sunitinib • pazopanib • Inlyta (axitinib) • saracatinib (AZD0530) • vinblastine
15d
Co-delivery of Interferon Regulatory Factor 5 (IRF5) siRNA and dasatinib by a disulfide bond bearing polymeric carrier for enhanced anti-inflammatory effects. (PubMed, Int J Biol Macromol)
The optimum micelles exhibited a dramatic reduction in IRF5 expression and revealed a notably higher anti-inflammatory effect than either DB or psiRF5, as indicated by more IL-10 and less IL-6 and TNF-α production by LPS-stimulated RAW264.7 macrophages incubated with the co-delivery system. The resultant nanocarriers might be promising for more effective treatment of inflammatory diseases.
Journal
|
IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • IRF5 (Interferon Regulatory Factor 5)
|
dasatinib
18d
Reciprocal inhibition of NOTCH and SOX2 shapes tumor cell plasticity and therapeutic escape in triple-negative breast cancer. (PubMed, EMBO Mol Med)
To counteract monotherapy-induced tumor relapse, we assessed GSI-paclitaxel and dasatinib-paclitaxel combination treatments in NOTCH inhibitor-sensitive and -resistant TNBC xenotransplants, respectively. These distinct preventive combinations and second-line treatment option dependent on NOTCH1 and SOX2 expression in TNBC are able to induce tumor growth control and reduce metastatic burden.
Journal • Tumor cell
|
NOTCH1 (Notch 1) • SOX2
|
NOTCH1 expression • SOX2 expression
|
dasatinib • paclitaxel
23d
A Multi-Omics Prognostic Model Capturing Tumor Stemness and the Immune Microenvironment in Clear Cell Renal Cell Carcinoma. (PubMed, Biomedicines)
The CRCS2 subtype was in a hypoxic state and was characterized by suppression and exclusion of immune function, which was sensitive to gefitinib, erlotinib, and saracatinib. Our findings highlight the key role of CSCs in shaping the ccRCC tumor microenvironment, crucial for therapy research and clinical guidance. Recognizing tumor stemness helps to predict treatment efficacy, recurrence, and drug resistance, informing treatment strategies and enhancing ccRCC patient outcomes.
Journal
|
SAA2 (Serum Amyloid A2)
|
erlotinib • gefitinib • saracatinib (AZD0530)
23d
Metabolic regulation of the glioblastoma stem cell epitranscriptome by malate dehydrogenase 2. (PubMed, Cell Metab)
Pharmacological inhibition of MDH2 in GSCs augmented efficacy of dasatinib, an orally bioavailable multi-kinase inhibitor, including PDGFRβ. Collectively, stem-like tumor cells reprogram their metabolism to induce changes in their epitranscriptomes and reveal possible therapeutic paradigms.
Journal
|
PDGFRB (Platelet Derived Growth Factor Receptor Beta) • ALKBH5 (AlkB Homolog 5, RNA Demethylase)
|
dasatinib
24d
Ubiquitin-related gene markers predict immunotherapy response and prognosis in patients with epithelial ovarian carcinoma. (PubMed, Sci Rep)
It also exhibited lower tumor mutation burden, mRNAsi, and EREG-mRNAsi and reduced sensitivity to other chemotherapy drugs, except dasatinib. These findings serve as a valuable indicator for personalized treatment strategies and clinical stratification in managing patients with EOC. Additionally, our study will serve as a foundation for future mechanistic research to explore the association between the ubiquitin-proteasome pathway and EOC.
Journal • Tumor mutational burden • IO biomarker
|
TMB (Tumor Mutational Burden) • CD4 (CD4 Molecule) • EREG (Epiregulin) • STAT1 (Signal Transducer And Activator Of Transcription 1) • VPS18 (VPS18 Core Subunit Of CORVET And HOPS Complexes) • AKAP12 (A-Kinase Anchoring Protein 12) • FBXO9 (F-Box Protein 9) • HSP90AB1 (Heat Shock Protein 90 Alpha Family Class B Member 1) • PPM1G (Protein Phosphatase, Mg2+/Mn2+ Dependent 1G)
|
TMB-L
|
dasatinib
26d
Correlation of T Regulatory Cells, Cytotoxic T-lymphocyte-associated Antigen 4, and Transforming Growth Factor-β1 with Treatment Response in Patients with Chronic Myeloid Leukemia Receiving Dasatinib Therapy. (PubMed, Ann Afr Med)
The study concluded that dasatinib treatment improved response in CML patients with decreased Treg cells. Dasatinib reduces Treg-mediated immunological suppression, reducing CTLA-4 and TGF-β1 levels.
Journal
|
BCR (BCR Activator Of RhoGEF And GTPase) • CTLA4 (Cytotoxic T-Lymphocyte Associated Protein 4) • TGFB1 (Transforming Growth Factor Beta 1)
|
dasatinib • imatinib
1m
TIRBASKIN: A Study of Tirbanibulin on the Wellbeing of Participants With Actinic Keratoses (clinicaltrials.gov)
P4, N=342, Completed, Almirall, S.A. | Trial completion date: Jan 2023 --> Jan 2024 | Trial primary completion date: Jan 2023 --> Jan 2024
Trial completion date • Trial primary completion date
|
Klisyri (tirbanibulin ointment)
1m
HTSS: Hematopoietic Stem Cell Transplant Survivors Study (clinicaltrials.gov)
P1, N=9, Completed, Mayo Clinic | Recruiting --> Completed | Phase classification: PN/A --> P1 | Trial completion date: Oct 2024 --> Jul 2024 | Trial primary completion date: Oct 2024 --> Jul 2024
Trial completion • Phase classification • Trial completion date • Trial primary completion date
|
dasatinib
1m
Integrative multi-omic and machine learning approach for prognostic stratification and therapeutic targeting in lung squamous cell carcinoma. (PubMed, Biofactors)
Notably, the high LMS group was more inclined toward "cold" tumors, characterized by immune suppression and exclusion, but drugs like dasatinib may represent promising therapeutic options for these patients. Notably, we also validated the model gene SERPINB13 through cell experiments, confirming its role as a potential oncogene influencing the progression of LUSC and as a promising therapeutic target. Our research provides new insights into refining the molecular classification of LUSC and further optimizing immunotherapy strategies.
Journal • IO biomarker • Machine learning
|
SERPINB3 (Serpin family B member 3)
|
dasatinib
1m
Journal
|
KIT (KIT proto-oncogene, receptor tyrosine kinase)
|
KIT mutation
|
dasatinib
2ms
Dasatinib-Induced Bilateral Chylothorax: A Case Report. (PubMed, Cureus)
Dasatinib was discontinued and bosutinib was initiated. Six months later, the patient remained stable with no recurrence of chylothorax. The mechanism of dasatinib-induced chylothorax is currently under investigation. The purpose of this report is to raise awareness about dasatinib-induced chylothorax, aid in identifying predisposing risk factors, and enhance understanding of the proper management of this rare complication.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • Bosulif (bosutinib)
2ms
PDIA2 is associated with the prognosis of prostate cancer, and downregulation of PDIA2 delays the progression of prostate cancer cells. (PubMed, Sci Rep)
The prostate cancer treatment efficacy of dasatinib is hampered by PDIA2, which is intimately linked to the growth, invasion, and metastasis of PCa cells. In summary, our research highlights the potential of PDIA2 as a biomarker for the diagnosis and management of PCa.
Journal
|
PDIA2 (Protein Disulfide Isomerase Family A Member 2)
|
dasatinib
2ms
A SRC-slug-TGFβ2 signaling axis drives poor outcomes in triple-negative breast cancers. (PubMed, Cell Commun Signal)
Targeting the SRC-Slug-TGFβ2 axis may therefore lead to better treatment options and improve patient outcomes in this highly aggressive subpopulation of TNBCs.
Journal
|
SNAI2 (Snail Family Transcriptional Repressor 2) • TGFB2 (Transforming Growth Factor Beta 2)
|
dasatinib • epirubicin
2ms
Unprecedented Megakaryocytic Blast Phase Transformation in Chronic Myeloid Leukemia After 16 Years of Tyrosine Kinase Inhibitor Therapy. (PubMed, Cureus)
For 16 years, the patient maintained chronic phase (CP) under treatment with first- and second-generation tyrosine kinase inhibitors (TKIs), including imatinib, dasatinib, and bosutinib, none of which resulted in ABL1 mutations. This case illustrates the critical role of third-generation TKIs like ponatinib in managing advanced CML phases, especially when previous therapies fail. It also emphasizes the necessity of vigilant long-term monitoring during the chronic phase to detect and address any signs of disease progression promptly.
Journal
|
ABL1 (ABL proto-oncogene 1)
|
dasatinib • imatinib • Iclusig (ponatinib) • Bosulif (bosutinib)
2ms
Critical review of clinical data and expert-based recommendations for the use of bosutinib in the treatment of chronic myeloid leukemia. (PubMed, Front Oncol)
The current availability of six different TKIs (imatinib, dasatinib, nilotinib, bosutinib, ponatinib, and asciminib) in clinical practice makes it important to know their efficacy and toxicity profile for treatment optimization. In summary, the latest research highlights the versatility of bosutinib in CML treatment and underscores its pivotal role in optimizing patient management in challenging cases. Continuing research and investigation will further establish bosutinib's place in the evolving landscape of CML therapy, offering an alternative for CML patients across different treatment stages.
Clinical data • Review • Journal
|
ABL1 (ABL proto-oncogene 1)
|
ABL1 fusion
|
dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib) • Scemblix (asciminib)
2ms
Manifesting the Dasatinib-gallic acid co-amorphous system to augment anticancer potential: Physicochemical characterization, in silico molecular simulation, ex vivo permeability, and in vitro efficacy. (PubMed, Int J Pharm)
The mitochondrial membrane depolarization, apoptotic index, and reactive oxygen species formation in MCF-7 cells were also notably higher in the DAB-GA-CA system than in free DAB. Hence, this research suggests that the DAB-GA-CA system could substantially enhance oral delivery, solubility, and therapeutic efficacy.
Preclinical • Journal
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • BCL2 (B-cell CLL/lymphoma 2)
|
dasatinib
3ms
Dasatinib interferes with HIV-1 proviral integration and the inflammatory potential of monocyte-derived macrophages from people with HIV. (PubMed, Biochem Pharmacol)
Due to the production of M2-related anti-inflammatory cytokines like IL-1RA and IL-10 was also impaired, dasatinib appeared to interfere with MDMs differentiation. The use of dasatinib along with ART could be used against HIV-1 reservoir in CD4 and macrophages and to alleviate the chronic inflammation characteristic of PWH.
Journal
|
IFNG (Interferon, gamma) • IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • CXCL9 (Chemokine (C-X-C motif) ligand 9) • CD4 (CD4 Molecule) • IL10 (Interleukin 10) • IL1B (Interleukin 1, beta) • IL1R1 (Interleukin 1 receptor, type I)
|
dasatinib
3ms
Construction of a prognostic model for colon cancer by combining endoplasmic reticulum stress responsive genes. (PubMed)
Finally, based on the cMAP database, we identified several potential drugs that could target high-risk groups, such as Dasatinib, GNF-2, Saracatinib, and WZ-1-84. This model can be used as a predictor of prognosis and immunotherapy response in colon cancer patients. At the same time, model-based prediction of drugs can also be a potential option for colon cancer treatment in the future.
Journal • IO biomarker
|
Oncotype DX® Colon Recurrence Score test
|
dasatinib • saracatinib (AZD0530)
3ms
A transcriptomic biomarker predictive of cell proliferation for use in adverse outcome pathway-informed testing and assessment. (PubMed, Toxicol Sci)
The biomarker identified suppression of CP 1) under conditions of p53 activation by DNA damaging agents in human cells, 2) in human A549 lung cells exposed to therapeutic anticancer kinase inhibitors (dasatinib, nilotnib) and 3) in the mouse liver when comparing high levels of CP at birth to the low background levels in the adult. The responses using the biomarker were similar to those observed using conventional markers of CP including PCNA, Ki67, and BrdU labeling. The CP biomarker will be a useful tool for interpretation of HTTr data streams to identify cell proliferation status after exposure to chemicals in human cells or in rodent tissues.
Journal • Adverse events
|
ER (Estrogen receptor) • PCNA (Proliferating cell nuclear antigen)
|
dasatinib
3ms
Philadelphia chromosome-like acute lymphoblastic leukemia with concomitant rearrangements of CRLF2 and ABL1: a pediatric case report. (PubMed, BMC Pediatr)
Our results identified that ABL1 rearrangement and CRLF2 rearrangement can coexist. The application of FISH, whole transcription sequencing, PCR can help us to have a more comprehensive understanding of ALL cytogenetics and molecular biology. Further studies are needed to explore the role of targeted therapies in such rare clinical scenarios.
Journal
|
ABL1 (ABL proto-oncogene 1) • CRLF2 (Cytokine Receptor Like Factor 2) • P2RY8 (P2Y Receptor Family Member 8)
|
dasatinib
3ms
Targeting the tyrosine kinase Src in endothelium attenuates inflammation and atherogenesis induced by disturbed flow. (PubMed, Br J Pharmacol)
Disturbed flow promotes endothelial inflammation and atherogenesis through the Piezo1-Src-Stat3 pathway. Therefore, inhibiting Src in endothelial cells could be a promising therapeutic strategy to treat atherogenesis.
Journal
|
APOE (Apolipoprotein E) • CDH5 (Cadherin 5)
|
dasatinib
3ms
Exploration of ETV6::ABL1-positive AML with concurrent NPM1 and FLT3-ITD mutations. (PubMed, Ann Hematol)
After haplo-HSCT, a combination of sorafenib and dasatinib was administered as maintenance therapy. The patient achieved complete remission (CR) and maintained it for 11 months. The intricate genetic landscape observed in this case presents diagnostic dilemmas and therapeutic challenges, emphasizing the importance of a comprehensive understanding of its implications for disease classification, risk stratification, and treatment selection.
Journal
|
FLT3 (Fms-related tyrosine kinase 3) • ABL1 (ABL proto-oncogene 1) • NPM1 (Nucleophosmin 1) • ETV6 (ETS Variant Transcription Factor 6)
|
dasatinib • sorafenib
4ms
A Study to Learn About the Study Medicine Bosulif in Adult Patients With Chronic Myeloid Leukemia(CML). (clinicaltrials.gov)
P=N/A, N=600, Not yet recruiting, Pfizer | Initiation date: Mar 2024 --> Aug 2024
Trial initiation date
|
Bosulif (bosutinib)
4ms
T-cell dysfunction in CLL is mediated through expression of SIGLEC-10 ligands CD24 and CD52 on CLL cells. (PubMed, Blood Adv)
Inhibition of kinases involved in the CD40-signaling cascade revealed that the SRC-kinase inhibitor dasatinib prevented rescue of T-cell function independent of CD40-mediated increased levels of costimulatory and adhesion ligands on CLL cells...These results demonstrate that T cells derived from CLL patients can be reinvigorated by manipulating CLL-T cell interactions. Targeting CD24- and CD52-mediated CLL-T cell interaction could be a promising therapeutic strategy to enhance T-cell function in CLL.
Journal • IO biomarker
|
CD24 (CD24 Molecule) • CD52 (CD52 Molecule) • CD40 (CD40 Molecule)
|
dasatinib
4ms
BCR-ABL kinase domain mutations in CML patients, experience from a tertiary care center in North India. (PubMed, Leuk Res Rep)
Other generation ABL tyrosine kinase inhibitors such as dasatinib, nilotinib, bosutinib and ponatinib help to overcome imatinib resistance [3]. ATP binding P-Loop (42.42 %), Direct binding site (36.36 %), C-Loop (10.60 %), A-Loop (6.06 %), SH2 contact (3.03 %), SH3 contact (1.51 %). Total 20.06 % patients (66/329) show mutation in at least one of the structural motifs of BCR-ABL kinase domain, which further confer the resistance to a particular generation of TKI.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib)
4ms
Prognostic analysis of anoikis-related genes in bladder cancer: An observational study. (PubMed, Medicine (Baltimore))
The IC50 of 56 drugs showed significant differences between 2 risk groups, such as imatinib, docetaxel, and dasatinib. At last, the results of real time quantitative-polymerase chain reaction (RT-qPCR) demonstrated that the expression trend of CALR, HGF, and INHBB was consistent with the result obtained previously based on public databases. Taken together, this study identified 6 anoikis-related characteristic genes (CALR, FASN, CSPG4, HGF, INHBB, SATB1) for the prognosis of BLCA patients, providing a scientific reference for further research on BLCA.
Observational data • Journal
|
CSPG4 (Chondroitin Sulfate Proteoglycan 4) • CALR (Calreticulin) • FASN (Fatty acid synthase) • SATB1 (SATB Homeobox 1)
|
dasatinib • imatinib • docetaxel
4ms
Proof of Concept Study to Access Superficial Basal Cell Carcinoma in Adults (clinicaltrials.gov)
P2, N=5, Completed, Austin Institute for Clinical Research | Recruiting --> Completed | N=10 --> 5
Trial completion • Enrollment change
|
Klisyri (tirbanibulin ointment)
4ms
PI3K/AKT and STAT3 pathways mediate the neuroprotective effect of dasatinib from acute cerebral injury in endotoxemic mice. (PubMed, Res Pharm Sci)
Histopathology demonstrated that dasatinib might considerably reduce brain damage and the intensity of neuroinflammation when compared to sepsis and vehicle groups that showed extensive brain inflammation and damage. Dasatinib attenuated endotoxemia-induced acute brain damage in mice via modulating effects on TLR4, PI3K, AKT, and STAT3 downstream signaling pathways.
Preclinical • Journal • IO biomarker
|
IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL10 (Interleukin 10) • TLR4 (Toll Like Receptor 4) • IL1B (Interleukin 1, beta)
|
dasatinib
4ms
Blastic Plasmacytoid Dendritic Cell Neoplasm Developed in Chronic Myeloid Leukemia in Molecular Remission During a Four-Year Treatment-Free Interval After Six Years of Dasatinib Treatment. (PubMed, Cureus)
To the best of our knowledge, this is the first case report of the development of BPDCN in a patient with CML in molecular remission. Further studies are required to clarify the pathogenesis of BPDCN in patients with hematological malignancies in remission.
Journal
|
CD123 (Interleukin 3 Receptor Subunit Alpha) • NCAM1 (Neural cell adhesion molecule 1) • IL3RA (Interleukin 3 Receptor Subunit Alpha)
|
dasatinib
4ms
Coexistence of BCR∷ABL1 translocation and JAK2V617F mutations in indian patients with myeloproliferative neoplasms: A case series. (PubMed, Indian J Pathol Microbiol)
All were treated with imatinib and hydroxyurea and attained major molecular response after 2-7 months. She was treated with dasatinib but no hematologic or molecular response was attained after 6 months despite good compliance. In conclusion, BCR∷ABL1 and JAK2V617F may rarely coexist in MPN with variable temporal evolution, clinicopathological profile, and treatment response.
Journal
|
ABL1 (ABL proto-oncogene 1)
|
dasatinib • imatinib • hydroxyurea
4ms
Development of an Orally Bioavailable LCK PROTAC Degrader as a Potential Therapeutic Approach to T-Cell Acute Lymphoblastic Leukemia. (PubMed, J Med Chem)
We have recently shown that a subset of T-ALL cases exhibited constitutive activation of the lymphocyte-specific protein tyrosine kinase (LCK) and were consequently responsive to treatments with LCK inhibitors and degraders such as dasatinib and dasatinib-based PROTACs. Here we report the design, synthesis and in vitro/vivo evaluation of SJ45566, a potent and orally bioavailable LCK PROTAC.
Journal
|
LCK (LCK Proto-Oncogene, Src Family Tyrosine Kinase)
|
dasatinib
4ms
Enrollment open
|
dasatinib • carboplatin • capecitabine • Halaven (eribulin mesylate) • vinorelbine tartrate
5ms
Tirbanibulin decreases cell proliferation and downregulates protein expression of oncogenic pathways in human papillomavirus containing HeLa cells. (PubMed, Arch Dermatol Res)
Tirbanibulin 1% ointment is a synthetic antiproliferative agent approved in 2021 by the European Union for treating actinic keratoses (AK). These results demonstrate that tirbanibulin may impact expression of HPV oncoproteins via the Src- MEK- pathway. Tirbanibulin significantly downregulates oncogenic proteins related to cell cycle regulation and cell proliferation while upregulating apoptosis pathways.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • E2F1 (E2F transcription factor 1) • RBL2 (RB Transcriptional Corepressor Like 2)
|
Klisyri (tirbanibulin ointment) • tirbanibulin oral (KX2-391 oral)
5ms
ECT2 promotes the occurrence and is a prognostic biomarker of head and neck squamous cell carcinoma. (PubMed, J Cancer)
There are also significant differences in the sensitivity to drugs such as bortezomib and dasatinib between the two groups. Integration of scRNA-seq data identified Monocyte clusters as high-scoring cell clusters based on genes interacting with ECT2.Mendelian randomization analysis identified three genes (LGALS2, SLC11A1, and TKT) causally related to HNSCC within this cell cluster. The findings suggest that ECT2 overexpression is associated with the survival rate of HNSCC, indicating its potential as a prognostic biomarker for this malignancy.
Journal
|
LGALS3 (Galectin 3)
|
dasatinib • bortezomib
5ms
Current Status and Management of Chronic Myeloid Leukemia in the Gulf Region: Survey Results and Expert Opinion. (PubMed, Cancers (Basel))
Most patients were reported to be in first-line therapy, and the most common treatments were imatinib/imatinib generic in first-line and dasatinib in second- and third-lines. The most important treatment objectives were "MMR" and "early molecular response followed by prolongation of overall survival" in the short term and "treatment-free remission" in the long term. The current practices in CML in the Gulf region appear to be similar to global figures.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib
5ms
EGFRvIII Confers Sensitivity to Saracatinib in a STAT5-Dependent Manner in Glioblastoma. (PubMed, Int J Mol Sci)
Our findings reveal that exogenous expression of paralogs STAT5A and STAT5B augments cell proliferation and that inhibition of STAT5 phosphorylation in vivo improves overall survival in combination with temozolomide (TMZ). Constitutively active STAT5A or STAT5B mitigates saracatinib sensitivity in EGFRvIII+ cells. In vivo, saracatinib treatment decreased survival in mice bearing EGFR WT tumors compared to the control, yet in EGFRvIII+ tumors, treatment with saracatinib in combination with TMZ preferentially improves survival.
Journal
|
JAK1 (Janus Kinase 1) • STAT5B (Signal Transducer And Activator Of Transcription 5B) • STAT5A (Signal Transducer And Activator Of Transcription 5A)
|
temozolomide • saracatinib (AZD0530)
5ms
Identifying proteomic risk factors for overall, aggressive, and early onset prostate cancer using Mendelian Randomisation and tumour spatial transcriptomics. (PubMed, EBioMedicine)
Our findings emphasise the importance of proteomics for improving our understanding of prostate cancer aetiology and of opportunities for novel therapeutic interventions. Additionally, we demonstrate the added benefit of in-depth functional analyses to triangulate the role of risk proteins in the clinical aggressiveness of prostate tumours. Using these integrated methods, we identify a subset of risk proteins associated with aggressive and early onset disease as priorities for investigation for the future prevention and treatment of prostate cancer.
Journal
|
TPM3 (Tropomyosin 3) • PRSS3 (Serine Protease 3)
|
PP2
6ms
Study to Assess Efficacy and Safety of NS-018 Compared to BAT in Patients With Myelofibrosis (clinicaltrials.gov)
P2, N=7, Terminated, NS Pharma, Inc. | N=120 --> 7 | Recruiting --> Terminated; The study was stopped due to a business decision.
Enrollment change • Trial termination
6ms
ASP210: a potent oligonucleotide-based inhibitor effective against TKI-resistant CML cells. (PubMed, Am J Physiol Cell Physiol)
Imatinib- and dasatinib-resistant sublines of BCR-ABL1 positive MOLM-7 and CML-T1 cells were established and exposed to 0.25 and 2.5 µM ASP210 for 10 days. Furthermore, the spontaneous uptake and high intracellular concentrations of ASP210 suggest its potential to be effective at relatively low doses. The present findings suggest that ASP210 is a promising therapeutic avenue for CML patients who fail to respond to TKI therapy.
Journal
|
ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
|
dasatinib • imatinib