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c-Kit

Early Long-Term Administration of the CSF1R Inhibitor PLX3397 Ablates Microglia and Reduces Accumulation of Intraneuronal Amyloid, Neuritic Plaque Deposition and Pre-Fibrillar Oligomers in 5XFAD Mouse Model of Alzheimer

16 views | May 22 2020

Justyna Sosna et al. demonstrate that CSF1R signaling, either directly on neurons or mediated by microglia, was crucial for the accumulation of intraneuronal amyloid and formation of neuritic plaques, suggesting that these two events were serially linked in a causal pathway leading to neurodegeneration and neuritic plaque formation. [Read the Full Post]

Pexidartinib: First Approval

25 views | May 21 2020

Yvette N Lamb et al. summarized the milestones in the development of pexidartinib leading to its first approval for TGCT. [Read the Full Post]

Cerebrospinal fluid penetration of the colony-stimulating factor-1 receptor (CSF-1R) inhibitor, pexidartinib

27 views | May 18 2020

Shankarappa PS et al. found that pexidartinib was well-tolerated in NHPs, with no Grade 3 or Grade 4 toxicities. The CSF penetration of pexidartinib after single-dose oral administration to NHPs was limited. [Read the Full Post]

Clinical activity and molecular correlates of response to atezolizumab alone or in combination with bevacizumab versus sunitinib in renal cell carcinoma

125 views | Feb 25 2020

McDermott DF et al. suggested that prediction of outcomes with anti-VEGF and immunotherapy may be possible and offer mechanistic insights into how blocking VEGF may overcome resistance to immune checkpoint blockade. [Read the Full Post]

Early diagnosis, clinical management, and follow-up of cardiovascular events with ponatinib

201 views | Feb 07 2020

Casavecchia G et al. reported and discussed most relevant evidence currently available on cardiovascular events associated with the use of ponatinib. [Read the Full Post]

Targeting mitochondrial oxidative phosphorylation eradicates therapy-resistant chronic myeloid leukemia stem cells

291 views | Dec 10 2019

Kuntz EM et al. provided a strong rationale for investigation of the use of TKIs in combination with tigecycline to treat patients with CML with minimal residual disease. [Read the Full Post]

Treatment Patterns in Patients with Chronic-Phase Chronic Myeloid Leukaemia in Routine Clinical Practice: the SIMPLICITY Italian Population

699 views | Aug 10 2019

Abruzzese E et al. provided valuable insights into management and treatment patterns in Italian patients with CML within routine clinical practice. [Read the Full Post]

Phase Ib study of the combination of pexidartinib (PLX3397), a CSF-1R inhibitor, and paclitaxel in patients with advanced solid tumors

154 views | Aug 03 2019

Wesolowski R et al. showed the combination of pexidartinib and paclitaxel was generally well tolerated. RP2D for pexidartinib was 1600 mg/day. Pexidartinib blocked CSF-1R signaling, indicating potential for mitigating macrophage tumor infiltration. [Read the Full Post]

Sustained inhibition of receptor tyrosine kinases and macrophage depletion by PLX3397 and rapamycin as a potential new approach for the treatment of MPNSTs

139 views | Jul 18 2019

Patwardhan PP et al. suggested that PLX3397 is superior to imatinib in the treatment of MPNSTs, and the combination of PLX3397 with a TORC1 inhibitor could provide a new therapeutic approach for the treatment of this disease. [Read the Full Post]

TKI-Related Platelet Dysfunction Does Not Correlate With Bleeding in Patients With Chronic Phase-Chronic Myeloid Leukemia With Complete Hematological Response

418 views | Jun 21 2019

Sener Y et al. concluded that TKIs may impair in vitro platelet aggregation but this impairment is not associated with bleeding diathesis. [Read the Full Post]