Last week, pacritinib, an oral tyrosine kinase inhibitor drug-candidate with dual activity against JAK2 and FLT, has been granted Fast Track designation by the U.S. Food & Drug Administration Continue reading
Category Archives: Signal Transduction
Targeted therapies for cancer – overview
The National Cancer Institute has a very informative, yet easy to understand overview presented as a Q&A – Targeted Cancer Therapies. Continue reading
Monoclonal antibodies + kinase inhibitors are better than antibodies alone in breast cancer and B-cell lymphoma
The combination of Herceptin plus pan-HER (EGFR and Her 2 an 4) kinase inhibitor neratinib resulted in a 33% improvement in progression free survival versus Herceptin alone in breast cancer patients. Rituxan combined with idelalisib, PI3K inhibitor, resulted in a near doubling of progression-free survival at 24 weeks versus Rituxan, alone in patients with Chronic Lymphocytic Leukemia, non-Hodgkin’s Lymphoma, and small cell lymphoma. The news for neratinib tripled the valuation of Puma Biotechnology, while the FDA granted approval of Gilead’s drug Zydelig (idelalisib). Continue reading
Cancer diagnostics in clinical use
Diagnostics that not only diagnose cancer, but also help select the appropriate therapy and monitor response are a mainstay in modern oncology, and their use is growing. Precision medicine, identifying genetic markers of disease and designing treatments to exploit these, is the essence of targeted cancer therapy. Continue reading
Genspera G-202 – anti-cancer hand grenade
Genspera is a company developing novel prodrugs for the treatment of cancer. In a phase 2 study in patients with hepatocellular carcinoma who have failed treatment with Nexavar (sorafenib), a tyrosine kinase inhibitor that blocks KIT, FLT-3 RET, raf, VEGFR1-3, and PDGF kinases, a doubling of time to progression was seen in patients taking G-202. Continue reading
Ras – targeting the “undruggable”
The Ras onogene has been studied for 30 years, with over 40,000 scientific articles published on it. However, an inhibitor of the mutated form of Ras has not been able to be developed. So, researchers have developed downstream blockers of the Ras cascade – MEK inhibitors and Raf inhibitors, for example. But why can’t a molecule that blocks mutated Ras be identified? Continue reading
Genentech Acquires Seragon – Selective Estrogen Receptor Degraders for breast cancer
Roche /Genentech announced that it acquired a company called Seragon for its new class of compound – SERD (selective Estrogen Receptor Degraders). Blocking estrogen production (aromatse inhibitors) and the binding to the estrogen receptor (tamoxifen) are mainstays of treatment for patients with ER (estrogen receptor) and PR (progesterone receptor) positive breast cancer. However, patients relapse subsequent to treatment with these agents. Continue reading
EGFRm+ non-small cell lung cancer – new treatments in development
For patients with activating mutations to the EGFR receptor kinase, small molecule specific inhibitors Iressa (gefintinib) or Tarceva (erlotinib) are administered as front-line treatments. But, non-small cell lung cancers develop resistance after about one year of treatment via a single recurrent missense mutation (T790M) to the tyrosine kinase. This is similar to resistance observed in patients with CML (Chronic Myeloid Leukemia) following treatment Gleevec (imatinib), which is mediated by a mutation to the Bcr-Abl transgene. Continue reading
Precision Medicine: SWOG Lung-MAP study – unique public/private collaboration
Using genomics to take-on advanced non-small cell lung cancer, the Southwest Oncology Group announced the start of a master protocol that will screen patients for optimal eligibility into one of five clinical trials with experimental drugs… Continue reading
OncoMed’s Wnt-targeted experimental cancer drugs and bone-related adverse events
OncoMed is a biotech company that is developing therapies directed at the Wnt and Notch signaling pathways. Clinical studies with two products directed at the Wnt pathway (Vantictumab – anti-Fzd-7, and Fzd-8 Fc) have been halted by the company while it explores findings of bone toxicity. Continue reading