Tipifarnib is an oral investigational monotherapy drug candidate for HRAS-mutant HNSCC. In preclinical models, tipifarnib blocks the activity of an enzyme called farnesyltransferase (FT). It is the only farnesyltransferase inhibitor (FTI) under investigation for HRAS-dependent HNSCC.
Alpelisib is an oral inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα. It received FDA approval as PIQRAY®, a kinase inhibitor indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen. Important Safety Information can be found here.4