[HTML][HTML] Anti-tumor activities of the new oral pan-RAF inhibitor, TAK-580, used as monotherapy or in combination with novel agents in multiple myeloma

R Suzuki, Y Kitamura, Y Nakamura, H Akashi… - Oncotarget, 2020 - ncbi.nlm.nih.gov
Many RAS pathway inhibitors, including pan-RAF inhibitors, have shown significant anti-
tumor activities in both solid and hematological tumors. The pan-RAF inhibitor, TAK-580, is a …

Anti-tumor activity of the pan-RAF inhibitor TAK-580 in combination with KPT-330 (selinexor) in multiple myeloma

R Suzuki, Y Kitamura, D Ogiya, Y Ogawa… - International Journal of …, 2022 - Springer
Abstract RAS/RAF/MEK/ERK pathway inhibitors exhibit significant anti-tumor effects against
various tumor types, including multiple myeloma (MM), and they are predicted to play a …

The combination of the farnesyl transferase inhibitor lonafarnib and the proteasome inhibitor bortezomib induces synergistic apoptosis in human myeloma cells that is …

E David, SY Sun, EK Waller, J Chen, FR Khuri, S Lonial - Blood, 2005 - ashpublications.org
The identification of signaling pathways critical to myeloma growth and progression has
yielded an array of novel agents with clinical activity. Multiple myeloma (MM) growth is IL-6 …

Results from the biomarker-driven basket trial of RO5126766 (CH5127566), a potent RAF/MEK inhibitor, in RAS-or RAF-mutated malignancies including multiple …

M Chenard-Poirier, M Kaiser, K Boyd, P Sriskandarajah… - 2017 - ascopubs.org
2506 Background: RO5126766 is a potent RAF and MEK inhibitor with activity in xenografts
models of RAS and RAF-mutated cancers. We present data from the RAS/RAF-mutated …

Pan-Raf co-operates with PI3K-dependent signalling and critically contributes to myeloma cell survival independently of mutated RAS

E Müller, S Bauer, T Stühmer, A Mottok, CJ Scholz… - Leukemia, 2017 - nature.com
Direct therapeutic targeting of oncogenic RAS is currently still impossible due to lack of
suitable pharmacological inhibitors. Because specific blockade of druggable RAS effectors …

[PDF][PDF] Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers

SB Peng, JR Henry, MD Kaufman, WP Lu, BD Smith… - Cancer cell, 2015 - cell.com
LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and
occupies both protomers in RAF dimers. Biochemical and cellular analyses revealed that …

OTX015, a novel BET inhibitor, is a promising anticancer agent for multiple myeloma

M Todaro, M Boi, V Vurchio, E Ercole, R Machiorlatti… - Cancer Research, 2014 - AACR
Introduction. The activity of BET inhibitors in several models human hematologic disorders,
including multiple myeloma (MM) has recently been demonstrated. Exposure of cancer cells …

364 First-in-human phase 1 study of MLN2480, an investigational oral pan-RAF kinase inhibitor, in patients (pts) with relapsed or refractory solid tumors, including …

M Middleton, DW Rasco… - … Journal of Cancer, 2014 - research.manchester.ac.uk
Background: Activating mutations in the MAPK pathway are common in many solid tumors.
RAF kinases play a key role in this pathway and represent a valid target for therapy. This …

[HTML][HTML] Rapid response in a patient with relapsed/refractory multiple myeloma treated with BRAF/MEK inhibitors

SB Otieno, S Nasir, A Weir, R Johnson - Case Reports in …, 2020 - hindawi.com
Patients with relapsed and refractory multiple myeloma have a poor prognosis. The mitogen-
activated protein kinase (MAPK) pathway has been implicated in the pathogenesis of …

Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in preclinical models of human RAF/RAS mutant melanoma

NLG Miller, TS Wang, P Severson, P Jiang, M Perez… - Cancer Research, 2022 - AACR
Background: In the US in 2021, invasive melanoma will account for an estimated 106,000
new cases and> 7,000 deaths. Somatic mutations that activate the MAPK signaling pathway …