Potent and selective Bruton's tyrosine kinase inhibitors: Discovery of GDC-0834.
San Francisco, United States. In Bioorg Med Chem Lett, 15 Apr 2015
SAR studies focused on improving the pharmacokinetic (PK) properties of the previously reported potent and selective Btk inhibitor CGI-1746 (1) resulted in the clinical candidate GDC-0834 (2), which retained the potency and selectivity of CGI-1746, but with much improved PK in preclinical animal models.
Multiple myeloma: Updates for pharmacists in the treatment of relapsed and refractory disease.
Ann Arbor, United States. In J Oncol Pharm Pract, 17 Mar 2015
New therapies currently in the drug development pipeline for relapsed and refractory disease include additional proteasome inhibitors (oprozomib, marizomib, ixazomib), histone deacetylase inhibitors (panobinostat, ricolinostat, quisinostat), monoclonal antibodies (daratumumab, elotuzumab, SAR650984), Bruton's tyrosine kinase inhibitors (ibrutinib), a selective inhibitor of nuclear export, and others.
MicroRNAs in B cell lymphomas: How a complex biology gets more complex.
Brno, Czech Republic. In Leukemia, Jan 2015
We focus on miR-contribution to the regulation of important signalling pathways (like NF-κB, PI3K/AKT, TGF-β), BCR signalling and its modulators (like PTEN, SHIP-1, ZAP-70, GAB1, BTK), anti- and pro-apoptotic proteins (like BCL2, MCL1, TCL1, BIM, p53, SIRT1), and transcription factors (like MYC, MYB, PU.1, FOXP1, BCL6).
Bortezomib for the treatment of non-Hodgkin's lymphoma.
Richmond, United States. In Expert Opin Pharmacother, Nov 2014
Rational combinations, for example, with Bruton's tyrosine kinase inhibitors or BH3-mimetics, may hold the key to optimizing the therapeutic potential of PIs in NHL.
[State of the art treatment of progressive or refractory multiple myeloma].
Freiburg, Germany. In Dtsch Med Wochenschr, Oct 2014
Therefore, inclusion of patients in therapeutic trials and use of novel agent combinations is highly recommended, e.g. with 3(rd) generation-IMIDs (pomalidomide), new proteasome inhibitors, such as carfilzomib, ixazomib or oprozomib, antibodies, such as elotuzumab, daratumumab or SAR650984, siltuximab, tabalumab, denosumab, romosozumab, BTK-, HSP-inhibitors and other innovative phase I/II agents.