Re: Neratinib clinical trials
Evlin
Neratinib is basically like Lapatanib. The main side effect is diarrhea. There are other side effects, fatigue and even thrombocytopenia, but it should be less harsh than iv chemo. This isnt true of all oral oncology drugs. Read the side effects of Mekinist, Xalkori and Zelboraf.
Neratinib bonds more strongly to the drug active sight of the Tyrosine Kinase Enzyme. The cancer cells are smart. They make one amino acid change and the Lapatanib cant bond to the drug receptor sight anymore. I dont know the exact mutation involved with Lapatanib. In melanoma there is a switch from a valine amino acid residue to glutamate. In Chronic Myelogenous Leukemia there is a switch from a threonine to IsoLeucine. This one amino acid switch makes Gleevec ineffective. This is where Iclusig is effective
The dose of Neratinib is 240mg daily. It seems the most obvious side effect is diarrhea. When they were doing double blind studies with Tykerb (Lapatanib) there was a problem. The Lapatanib diarrhea made it obvious who was getting the active drug, and who was
not.
Paul
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