Category Archives: Receptor Tyrosine Kinase Inhibitors

JAK-inhibitors for myelofibrosis

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

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

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

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