[HTML][HTML] Pathway-directed therapy in multiple myeloma
Multiple Myeloma (MM) is a malignant plasma cell disorder with an unmet medical need, in
particular for relapsed and refractory patients. Molecules within deregulated signaling …
particular for relapsed and refractory patients. Molecules within deregulated signaling …
The discovery of exarafenib (KIN-2787): overcoming the challenges of pan-RAF kinase inhibition
YK Chen, T Kanouni, LD Arnold, JM Cox… - Journal of Medicinal …, 2024 - ACS Publications
RAF, a core signaling component of the MAPK kinase cascade, is often mutated in various
cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were …
cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were …
TAS-117, a novel selective Akt inhibitor demonstrates significant growth inhibition in multiple myeloma cells in vitro and in vivo
Abstract Abstract 942 The PI3K/Akt pathway mediates multiple myeloma (MM) cell growth
and drug resistance, and targeting this molecule is a promising therapeutic option. In this …
and drug resistance, and targeting this molecule is a promising therapeutic option. In this …
[HTML][HTML] An open-label, dose escalation, multi-center phase 1 study of PRLX 93936, an agent synthetically active against the activated ras pathway, in the treatment of …
PM Voorhees, RL Schlossman, CJ Gasparetto… - Blood, 2014 - Elsevier
Introduction: Overall survival for patients with multiple myeloma (MM) has improved, but
most patients relapse and eventually succumb to complications of the disease. The …
most patients relapse and eventually succumb to complications of the disease. The …
Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor
DD Stuart, N Li, DJ Poon, K Aardalen, S Kaufman… - Cancer Research, 2012 - AACR
Selective RAF inhibitors have significant activity in patients with metastatic melanoma whose
tumors express BRAFV600E. However, not all patients respond equally well to treatment …
tumors express BRAFV600E. However, not all patients respond equally well to treatment …
Discovery of a highly potent pan-RAF inhibitor IHMT-RAF-128 for cancer treatment
A Wang, J Liu, X Li, F Zou, Z Qi, S Qi, Q Liu… - European Journal of …, 2023 - Elsevier
Although rat sarcoma viral oncogene homolog (RAS) mutations occur in about 30% of solid
tumors, targeting RAS mutations other than KRAS-G12C is still challenging. As an …
tumors, targeting RAS mutations other than KRAS-G12C is still challenging. As an …
[HTML][HTML] Open label, multicenter, dose-escalation/expansion phase Ib study to evaluate safety and activity of BET Inhibitor RO6870810 (RO), given as monotherapy to …
Introduction Multiple myeloma (MM), relapsed or refractory (R/R) to standard of care
therapies, represents a treatment indication with a significant unmet clinical need …
therapies, represents a treatment indication with a significant unmet clinical need …
A phase I study of LY3009120, a pan-RAF inhibitor, in patients with advanced or metastatic cancer
Mutations in ERK signaling drive a significant percentage of malignancies. LY3009120, a
pan-RAF and dimer inhibitor, has preclinical activity in RAS-and BRAF-mutated cell lines …
pan-RAF and dimer inhibitor, has preclinical activity in RAS-and BRAF-mutated cell lines …
[HTML][HTML] KSP inhibitor SB743921 induces death of multiple myeloma cells via inhibition of the NF-κB signaling pathway
IS Song, YJ Jeong, B Nyamaa, SH Jeong, HK Kim… - BMB …, 2015 - ncbi.nlm.nih.gov
SB743921 is a potent inhibitor of the spindle protein kinesin and is being investigated in
ongoing clinical trials for the treatment of myeloma. However, little is known about the …
ongoing clinical trials for the treatment of myeloma. However, little is known about the …
Abstract LB-114: RAF inhibitor LXH254 effectively inhibits B-and-CRAF, but not ARAF
KA Monaco, S Delach, P Fordjour, S Parikh, Y Feng… - Cancer Research, 2019 - AACR
RAS mutant tumors have proven largely refractory to inhibitors of the MAPK pathway in
clinic. In contrast, selective inhibitors of BRAFV600E but not wild type RAF have been …
clinic. In contrast, selective inhibitors of BRAFV600E but not wild type RAF have been …