A gene fusion in about 1-2% of lung cancers that responds for years to targeted pills, now in their third generation. This dossier gathers the 4 products (4 approved), 0 trials, 0 pathways and 0 resistance routes in the corpus that involve it, with external identifiers so it can be joined to UniProt, ChEMBL, Open Targets and the rest of biology.
Biology
Receptor tyrosine kinase with homology to ALK; fusions constitutively activate MAPK, PI3K, and JAK-STAT.
- NSCLC (~1-2%)
- Cholangiocarcinoma, glioblastoma, Spitz tumours (rare)
Elsewhere: identifiers and databases
Built from HGNC, Ensembl, UniProt and ChEMBL idsMutation hotspots and which drugs address them
| Residue | Kind | How common | What it does | Addressed by | Defeats | Source |
|---|---|---|---|---|---|---|
| G2032R (solvent front) 2032 | Resistance | The most common ROS1 resistance mutation after crizotinib | Defeats crizotinib and entrectinib; repotrectinib and taletrectinib were designed to fit past it. | Gainor et al., JCO Precision Oncology 2017 | ||
| L2026M (gatekeeper) and D2033N, S1986F/Y 2026 | Resistance | not sourced | Less common escapes; sensitivity varies by drug. | — | Gainor et al., JCO Precision Oncology 2017 |
Frequencies are quoted from the source on each row; a blank means no figure was sourced, not that it is rare. Domain boundaries are approximate. Sources for the map: COSMIC: ROS1.
Products by modality and phase
Browse products →| Modality | Approved |
|---|---|
| Small molecule 1 | |
| Small-molecule ALK/ROS1/MET TKI 1 | |
| Small-molecule ROS1 TKI 1 | |
| Small-molecule TRK/ROS1/ALK TKI 1 |
Trials
Evidence ranking →No trial in the corpus names this target or one of its products.
Resistance routes that involve this target
Unaddressed routes →The resistance atlas has no route that names this target.
Pathways where it is a node
Pathway-to-drug matrix →No pathway diagram carries this target as a node.
Companion diagnostics and assays
Assay registry →| Assay | Platform | Cut-off | Gates |
|---|---|---|---|
| Oncomine Dx Target Test Thermo Fisher Scientific · FDA CDx 2017 | NGS tissue | Per companion claim: BRAF V600E (dabrafenib plus trametinib), ROS1 fusions (crizotinib), EGFR (gefitinib), RET fusions (pralsetinib), MET exon 14 (tepotinib), EGFR exon 20 insertions |
Preclinical models
All models →No model entry for this target yet; check the cancer entries on the models page.
Open questions
All open questions →No open questions recorded for this target yet. Suggest one.
Ideas and companies
Key papers and the live literature
Preprints →Query for this target: (TITLE:"ROS1" OR ABSTRACT:"ROS1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about ROS1, not a curated reading list.
Export
The dossier as machine-readable JSON: identifiers from HGNC, Ensembl, UniProt and ChEMBL, products with status, trials, pathways, hotspots, open questions and assays. The full entity record is in the open API at /api/v1/entities/ros1.json. Licence CC BY 4.0.