Table 1.
Cancer genes included in the assay and available targeted cancer therapies
| Gene | SNaPshot coverage | Relevant drugs: launched (developer) | Relevant drugs in clinical testing (number of compounds)1 |
|---|---|---|---|
| APC | 15% | None | None |
| BRAF | 94% | Sorafenib (Bayer HealthCare Pharmaceuticals, Onyx Pharmaceuticals) | Raf inhibitors (4) |
| MEK inhibitors (12) | |||
| ERK inhibitor (1) | |||
| CTNNB1 | 74% | None | None |
| Gefitinib (AstraZeneca) | |||
| EGFR | 69% | Cetuximab (ImClone Systems, Merck Serono, Bristol-Myers Squibb) Erlotinib hydrochloride (Genentech, OSI Pharmaceuticals, Roche) Panitumumab (Amgen) Nimotuzumab (YM BioSciences, Biotech Pharmaceuticals, Oncoscience, Daiichi Sankyo) Lapatinib (GlaxoSmithKline) | EGFR inhibitors (26) |
| FLT3 | 22% | Sorafenib (Bayer HealthCare Pharmaceuticals, Onyx Pharmaceuticals) Sunitinib (Pfizer) | FLT3 inhibitors (10) |
| JAK2 | 99% | None | JAK2 inhibitors (4) |
| Imatinib mesylate (Novartis Oncology) | |||
| KIT | 24% | Sorafenib (Bayer HealthCare Pharmaceuticals, Onyx Pharmaceuticals) Sunitinib (Pfizer) | KIT inhibitors (11) |
| KRAS | 98% | None | Raf inhibitors (4) |
| MEK inhibitors (12) | |||
| ERK inhibitor (1) | |||
| NOTCH1 | 9% | None | Notch1/Gamma-Secretase inhibitors (3) |
| NRAS | 97% | None | Raf inhibitors (4) |
| MEK inhibitors (12) | |||
| ERK inhibitor (1) | |||
| PIK3CA | 76% | mTOR inhibitors: Sirolimus (Wyeth Pharmaceuticals) Everolimus (Novartis Pharmaceuticals) Temsirolimus (Wyeth Pharmaceuticals) | PI3K inhibitors (10) |
| PKB/AKT inhibitors (6) | |||
| mTOR inhibitors (13) | |||
| PTEN | 15% | Sirolimus (Wyeth Pharmaceuticals) Everolimus (Novartis Pharmaceuticals) Temsirolimus (Wyeth Pharmaceuticals) | mTOR inhibitors: |
| PI3K inhibitors (10) | |||
| PKB/AKT inhibitors (6) | |||
| mTOR inhibitors (13) | |||
| TP53 | 29% | None | None |
The numbers on the second column reflect the frequency of somatic mutations described for each gene (COSMIC database v42 release) that are captured by SNaPshot genotyping. The data on targeted agents was compiled using the Prous Science database (www.prous.com). Of note, many compounds have multiple targets or overlapping activities.
1
Cancer trials.