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GDC-0084 + trastuzumab
- Development stage
- Unknown
- Lead developer
- Kazia Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
GDC-0084 + trastuzumab is a combination therapy under investigation for the treatment of HER2-positive breast cancer with brain metastases. GDC-0084 (also known as paxalisib) is a brain-penetrant small molecule inhibitor targeting both PI3K and mTOR pathways, which are frequently activated in cancers with PIK3CA mutations or PTEN loss. Trastuzumab (Herceptin) is a monoclonal antibody that targets the human epidermal growth factor receptor 2 (HER2), inhibiting its signaling and mediating antibody-dependent cellular cytotoxicity. The rationale for this combination stems from evidence that activation of the PI3K/mTOR pathway can confer resistance to HER2-targeted therapies like trastuzumab; thus, dual inhibition may overcome resistance and improve outcomes in patients with central nervous system involvement[1][3][4][7]. Clinical trials are ongoing to evaluate efficacy and safety in this population.
- Brand names
- Herceptin
- Other names
- GDC-0084 + Herceptinpaxalisib + trastuzumab
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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