TROP2
TROP2 is a surface glycoprotein present at high levels on most epithelial cancers (breast, lung, urothelial, gastric, pancreatic) and at low levels on normal tissue. It does not drive the cancer; it is a delivery address, used by the approved ADCs sacituzumab govitecan and datopotamab deruxtecan and by sacituzumab tirumotecan, with a TROP2 PET tracer in development to pick patients.
Overview
Trophoblast cell-surface antigen 2 is a transmembrane glycoprotein overexpressed in most epithelial cancers (breast, lung, urothelial, gastric, pancreatic) with low normal-tissue expression. It is not an oncogenic driver; it is a delivery address. Three TROP2 ADCs are approved or in registration (sacituzumab govitecan, datopotamab deruxtecan, sacituzumab tirumotecan) and a TROP2 PET tracer is in development to select patients.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · TROP2 is a surface glycoprotein present at high levels on most epithelial cancers (breast, lung, urothelial, gastric, pancreatic) and at low levels on normal tissue. It does not drive the cancer; it is a delivery address, used by the approved ADCs sacituzumab govitecan and datopotamab deruxtecan and by sacituzumab tirumotecan, with a TROP2 PET tracer in development to pick patients.
- 1 · What it is
TROP2 is a surface glycoprotein present at high levels on most epithelial cancers (breast, lung, urothelial, gastric, pancreatic) and at low levels on normal tissue. It does not drive the cancer; it is a delivery address, used by the approved ADCs sacituzumab govitecan and datopotamab deruxtecan and by sacituzumab tirumotecan, with a TROP2 PET tracer in development to pick patients.
- 2 · What goes wrong in cancer
Regulates calcium signalling and cell adhesion; overexpression correlates with poor prognosis. Expression is heterogeneous within tumours, which limits the value of IHC selection.
- 3 · How drugs use it
No product in this corpus aims at TROP2 yet. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
Catalysts
Catalyst calendar- 2027expectedTROPION-Lung14: datopotamab deruxtecan plus osimertinib, first-line EGFR-mutant NSCLC
Would move the TROP2 ADC into the first-line EGFR-mutant setting on top of the standard TKI. Timing is a registry-based estimate. Source
- 2027expectedASCENT-07: sacituzumab govitecan versus chemotherapy, first-line HR-positive HER2-negative metastatic breast cancer
Tests the ADC as the first chemotherapy after endocrine therapy. Timing is a registry-based estimate. Source
External identifiers
Biology
Regulates calcium signalling and cell adhesion; overexpression correlates with poor prognosis. Expression is heterogeneous within tumours, which limits the value of IHC selection. Internalises on antibody binding and traffics to lysosomes, which is what makes it a good ADC target.
- Triple-negative breast cancer (~80-90% express)
- HR+ breast cancer
- NSCLC
- Urothelial carcinoma
- Gastric, pancreatic, endometrial cancers
Latest papers
topQuery for this target: (TITLE:"TROP2" OR ABSTRACT:"TROP2" OR TITLE:"TACSTD2" OR ABSTRACT:"TACSTD2") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR 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 TROP2, not a curated reading list.
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