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Drug intelligence / Profile preview
tilarginine + nab-paclitaxel + alpelisib
- Development stage
- Unknown
- Lead developer
- Obsidian Therapeutics
- Modality
- Small Molecules, Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous, Oral
01
Overview
Tilarginine + nab-paclitaxel + alpelisib is a combination regimen in clinical development for the treatment of metaplastic breast cancer, a rare and aggressive subtype of triple-negative breast cancer (TNBC). The regimen consists of **tilarginine** (L-NMMA), a pan-inhibitor of nitric oxide synthase (NOS); **alpelisib**, a selective PI3K inhibitor; and **nab-paclitaxel**, an albumin-bound nanoparticle formulation of the microtubule-stabilizing chemotherapy agent paclitaxel. Tilarginine functions by inhibiting NOS to modulate the tumor microenvironment and enhance the efficacy of chemotherapy, while alpelisib targets the PI3K pathway, which is frequently dysregulated in metaplastic breast cancer. The combination is being evaluated in Phase 1/2 trials sponsored by Galera Therapeutics in collaboration with Houston Methodist and the University of Texas MD Anderson Cancer Center.
- Other names
- tilarginine + nab-paclitaxel + PI3KiL-NMMA + nab-paclitaxel + alpelisib
02
Targets
NOS1 (nNOS)PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))
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