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alpelisib + L-NMMA + nab-paclitaxel
- Development stage
- Unknown
- Lead developer
- Methodist Hospital Research Institute
- Modality
- Nanoparticles → Drug Delivery Systems, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This combination therapy consists of alpelisib, L-NMMA (tilarginine), and nab-paclitaxel. It is being evaluated in a Phase II clinical trial sponsored by The Methodist Hospital Research Institute for the treatment of HER2-negative metaplastic breast cancer (MpBC) and triple-negative breast cancer (TNBC). Alpelisib is an orally bioavailable, alpha-specific inhibitor of Class I phosphatidylinositol 3-kinase (PI3K). L-NMMA is a pan-nitric oxide synthase (NOS) inhibitor that targets the inducible NOS (iNOS) pathway, which is often upregulated in MpBC and contributes to chemoresistance. Nab-paclitaxel is an albumin-bound nanoparticle formulation of the taxane chemotherapy agent paclitaxel. The rationale for the triple combination is to overcome resistance mechanisms in aggressive breast cancer subtypes by simultaneously inhibiting the PI3K/Akt pathway and nitric oxide production while delivering cytotoxic chemotherapy.
- Brand names
- PiqrayAbraxane
- Other names
- NG-monomethyl-L-argininetilarginineL-NMMA
02
Targets
NOS2 (Nitric Oxide Synthase 2)TUBB (Tubulin (alpha and beta subunits))PIK3CA (Phosphoinositide 3-kinase alpha)
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