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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.
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.
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.
Backbone ribbon from PDB 9PI9. RCSB PDB 9PI9. The ribbon widens where the chain is folded into a regular pattern and narrows where it is a loose loop.
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.
Regulates calcium signalling and cell adhesion; overexpression correlates with shorter survival. Expression is heterogeneous within tumours, which limits the value of IHC selection.
7 products aim at TROP2: antibodies, antibody-drug conjugates and cell therapies. 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.
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
Tests the ADC as the first chemotherapy after endocrine therapy. Timing is a registry-based estimate. Source
Tumour-associated overexpression: 6 cell-killing or cell-finding medicines (AK146D1, BIO-106, Datopotamab deruxtecan and more) aim at the antigen, which HPA finds stained high in 1 normal tissue; the medicine relies on the tumour carrying more of it than the normal tissue it shares it with. HPA TACSTD2: RNA tissue enhanced (esophagus 1,245 nTPM, salivary gland 585 nTPM, skin 1 555 nTPM); blood lineage group enriched (dendritic cells 4 nTPM, granulocytes 15 nTPM, monocytes 4 nTPM); high antibody staining in 1 normal tissue; highest cancer staining urothelial cancer (1 of 11 high). Distribution: 4 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Breast cancer (all types), Lung cancer (all types), Bladder & urothelial cancer, Pancreatic ductal adenocarcinoma); approvals of single-target medicines aimed at it also list Endometrial cancer, Cervical cancer, not counted; Open Targets associates it with 3 specific cancer types at or above 0.5 (breast cancer, non-small cell lung carcinoma, triple-negative breast carcinoma). (Rule 5 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas TACSTD2 tissue; Human Protein Atlas TACSTD2 pathology; Open Targets ENSG00000184292 associations
First described 1989. Earliest sequence paper UniProt cites for the protein: Linnenbach A.J. et al, Proc. Natl. Acad. Sci. U.S.A, 1989, "Sequence investigation of the major gastrointestinal tumor-associated antigen gene family, GA733". Source.
What a pathology or genomic report can say about this target, each with the thresholds approvals use.
Cell lines and mouse models for this target →
Regulates calcium signalling and cell adhesion; overexpression correlates with shorter survival. 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.
RNA: tissue enhanced (esophagus 1,245 nTPM, salivary gland 585 nTPM, skin 1 555 nTPM), detected in many normal tissues. Blood: group enriched (dendritic cells 4 nTPM, granulocytes 15 nTPM, monocytes 4 nTPM).
Medium: Bronchus, Cervix, Esophagus, Kidney, Nasopharynx, Oral mucosa, Seminal vesicle, Urinary bladder.
Medium only: cervical cancer, liver cancer, lung cancer, ovarian cancer.
HPA TACSTD2 tissue · HPA TACSTD2 pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Triple-negative breast cancer | 80-90% | IHC, any/moderate-high expression | ASCENT benefit was independent of TROP2 IHC level | PMC |
| Bladder & urothelial cancer | 80-90% | IHC, any expression | PMC | |
| HR-positive / HER2-negative breast cancer | 75-90% | IHC, any expression | PMC | |
| Non-small-cell lung cancer | 60-70% | IHC, moderate-high | Adenocarcinoma and squamous | PMC |
| Pancreatic ductal adenocarcinoma | 50% | IHC, any expression | Approximate; heterogeneous | PMC |
| Triple-negative breast cancer | 2-4% | Protein expression (H-score) and amplification | Trop-2 expression was assessable in 290 of 468 ASCENT patients and sacituzumab govitecan benefit was seen at high and medium expression (progression-free survival 6.9 and 5.6 versus 2.5 and 2.2 months), with the low group too small to judge (Bardia 2021); cBioPortal: TACSTD2 amplification in 3 of 119, 2.5%, in brca_tcga_pan_can_atlas_2018 and 14 of 320, 4.4%, in brca_metabric; no TACSTD2 mutation in either. | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
AK146D1 is Akeso's Nectin-4 × TROP2 bispecific ADC, combining the two most validated ADC addresses in one molecule.
BIO-106 is an experimental antibody-drug conjugate from BiOneCure Therapeutics in phase 2 trials, aimed at TROP2.
Datopotamab deruxtecan (Datroway) is the second TROP2 ADC and shares Enhertu's payload. In 2026 it became a first-line option for triple-negative breast cancer patients who cannot receive immunotherapy.
EB-NK-301 is an experimental CAR-NK cell therapy from Beijing Biotech in phase 2 trials, aimed at TROP2.
LCB84 is an experimental monoclonal antibody from LigaChem Biosciences in phase 2 trials, aimed at TROP2.
The first TROP2-targeted ADC. It delivers a strong chemotherapy directly to breast and bladder cancer cells and is now a first-line option in triple-negative breast cancer.
Sacituzumab tirumotecan is Kelun-Biotech's TROP2 ADC, approved in China in 2024 for pretreated triple-negative breast cancer and then EGFR-mutant lung cancer. Merck holds rights outside Greater China and runs the TroFuse programme of more than ten phase 3 trials across breast, lung, endometrial and cervical cancer; in the US it holds a priority voucher but no approval yet.
The first-line overall survival result that made an antibody-drug conjugate the standard for PD-L1-negative or immunotherapy-ineligible metastatic triple-negative disease, and the reason the sequencing question (which TROP2 drug first, what after it) is now urgent.
For hormone-receptor-positive metastatic breast cancer that has already had chemotherapy, Dato-DXd controls the disease for longer with fewer severe side effects than chemotherapy, but does not help patients live longer, so it is not a standard option here. The result is a reminder that progression-free survival is a surrogate; regulators and clinicians should wait for survival data before adopting an ADC in a setting where later therapies are effective.
Confirms that the TROP2 antibody-drug conjugates are given without a TROP2 test and that PD-L1 remains the one selection assay in metastatic triple-negative disease, which is why assay harmonisation matters.
Sacituzumab govitecan is a standard second-line or later treatment for metastatic triple-negative breast cancer, roughly doubling survival compared with the chemotherapies it was tested against. Patients should expect neutropenia and diarrhoea, which are manageable with growth factor support and loperamide. Trials are now testing it earlier, in first-line combinations with pembrolizumab and after surgery for residual disease.
TROP2 IHC does not gate sacituzumab govitecan: the label requires no test, and the corpus records TROP2 as an expression readout without a threshold.
Query for this target: (TITLE:"TROP2" OR ABSTRACT:"TROP2" OR TITLE:"TACSTD2" OR ABSTRACT:"TACSTD2") 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 TROP2, not a curated reading list.
Shares Clinical Trial of VBC103 in Patients With Advanced Malignant Solid Tumors, Overexpression, Avenzo Therapeutics, AK146D1 and the tag adc-target.
Shares Overexpression, Alpha radioligands after ADC failure, Re-map the tumour's surface proteins before choosing the next antibody drug, Bispecific ADC and the tag adc-target.
Shares Re-map the tumour's surface proteins before choosing the next antibody drug, Endometrial cancer, Antibody-drug conjugate (ADC), Triple-negative breast cancer (TNBC) and the tag adc-target.
Shares Cervical cancer, Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC), Triple-negative breast cancer (TNBC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC) and the tag adc-target.
Shares Antibody-drug conjugate (ADC) and the tag adc-target.