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APR-246 + dabrafenib
- Development stage
- Unknown
- Lead developer
- Aprea Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
APR-246 + dabrafenib is an investigational combination therapy being studied primarily for the treatment of patients with **BRAF V600 mutant unresectable or metastatic cutaneous melanoma** who are resistant to prior dabrafenib/trametinib therapy[1][4][6]. **APR-246** (also known as eprenetapopt, PRIMA-1MET) is a small molecule designed to restore the normal wild-type conformation and function of mutant TP53 (tumor suppressor protein p53), leading to tumor cell apoptosis. **Dabrafenib** is a small molecule **BRAF inhibitor** that targets and inhibits BRAF V600-mutant kinases, thus blocking aberrant MAPK pathway signaling and cell proliferation. The rationale for combining APR-246 with dabrafenib is to potentially overcome resistance to BRAF inhibitors by restoring TP53 tumor suppressor function and simultaneously inhibiting BRAF V600-driven signaling. The combination's development is led by Aprea Therapeutics, including clinical evaluation in collaboration with Jules Bordet Institute[1][4][6].
- Brand names
- Tafinlar (dabrafenib)
- Other names
- APR-246 + dabrafenibeprenetapopt + dabrafenibPRIMA-1MET + dabrafenib
02
Targets
CAPN3 (B-Raf proto-oncogene, serine/threonine kinase)TP53 (Cellular Tumor Antigen p53 R175H)
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