Drug intelligence / Profile preview

tilarginine + nab-paclitaxel + alpelisib

Development stage
Unknown
Lead developer
Galera Therapeutics
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
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.

Brand names
AbraxanePiqray
Other names
tilarginine + nab-paclitaxel + PI3KiL-NMMA + nab-paclitaxel + alpelisib
02

Targets

TUBB (Tubulin (alpha and beta subunits))PIK3CA (Phosphoinositide 3-kinase alpha)NOS1 (nNOS)

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