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Association details:
| Biomarker: | PIK3CA H1047R |
|---|---|
| Cancer: | Melanoma |
| Drug: | Tafinlar (dabrafenib) (BRAF inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma
Excerpt:
...one patient (Patient 48) whose pre-treatment tumor harbored PTENY86fs frameshift exhibited a new PIK3CAH1047R mutation in the resistant tumor biopsy (PIK3CAH1047R is a well-characterized oncogenic mutation in the catalytic PI3 kinase alpha subunit27).
DOI:
10.1158/2159-8290.CD-13-0617
Source:
Title:
The PIK3CA H1047R Mutation Confers Resistance to BRAF and MEK Inhibitors in A375 Melanoma Cells through the Cross-Activation of MAPK and PI3K-Akt Pathways
Published date:
03/08/2022
Excerpt:
CONTRADICTING EVIDENCE: An MTT analysis showed that A375-H1047R had a higher resistance to dabrafenib (IC50: 3.41 ± 0.35 nM) compared to that of A375-PIK3CA and A375-pLNCX2 cells (IC50: 1.42 ± 0.19 nM and 1.30 ± 0.14 nM, respectively) (p ≤ 0.05) (Figure 3A). Similarly, A375H1047R showed increased resistance to trametinib (IC50: 2.06 ± 0.08 nM) compared to that of other cell lines (IC50: 0.88 ± 0.23 nM for A375PIK3CA and 0.85 ± 0.14 nM for A375pLNCX2) (p ≤ 0.05) (Figure 3E).
DOI:
10.3390/pharmaceutics14030590
