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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.
31 products aim at TROP2: 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's exploratory biomarker analysis supported benefit in the high/medium H-score groups; the low-expression group was too small for definitive conclusions (290 of 468 assessable patients had TROP2 data). No TROP2 companion test is required for the breast-cancer indications. | 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 | 2.5-4.4% | Gene amplification (copy number) | 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 the TNBC-filtered copy-number cohorts, 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. | cBioPortal (TCGA) |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
9MW2921 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
AK146D1 is Akeso's Nectin-4 × TROP2 bispecific ADC, combining the two most validated ADC addresses in one molecule.
An experimental drug that uses an antibody to deliver a cancer-killing drug and an immune activator to cells carrying TROP2. An early human study is recruiting; benefit and safety are still being tested.
AVZO-103 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
BAT8008 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
BCG033 is an experimental drug designed to carry chemotherapy to cancer cells. Its published evidence is from laboratory and animal studies.
BHV-1510 is an experimental chemotherapy-delivering antibody being studied alone and with immunotherapy. Early response findings need confirmation in larger trials.
BIO-106 is an experimental antibody-drug conjugate from BiOneCure Therapeutics in phase 2 trials, aimed at TROP2.
CAN020 is an experimental drug designed to carry chemotherapy to cancer cells. Its published evidence is from laboratory and animal studies.
CATB-101 is an experimental drug designed to carry chemotherapy to cancer cells. Its published evidence is from laboratory and animal studies.
CBB-120 is an experimental drug designed to carry chemotherapy to cancer cells. Its published evidence is from laboratory and animal studies.
CTPH-03 is an experimental drug designed to carry chemotherapy to cancer cells. Its published evidence is from laboratory and animal studies.
Datopotamab deruxtecan delivers chemotherapy to cells bearing TROP2. Its FDA approvals cover specific advanced breast-cancer and EGFR-mutated lung-cancer settings.
DB-1305 / BNT325 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
EB-NK-301 is an experimental donor-derived immune-cell therapy aimed at TROP2. Its registered trial combines phase 1 and phase 2 testing; no clinical benefit is established.
ESG401 is an experimental drug that delivers chemotherapy to cells bearing TROP2. Early breast-cancer response results are being followed by larger trials.
FDA018-ADC, also called F0024, is an experimental drug that carries chemotherapy to TROP2-bearing cells. Early response results do not establish a benefit over standard treatment.
IBI130 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
IBI3014 is an experimental antibody-drug conjugate being studied in people with advanced cancer. Its benefit and safety are still being evaluated.
JS108 is an experimental TROP-2 antibody-drug conjugate whose first clinical study was terminated.
JSKN016 is an experimental drug that targets two proteins on cancer cells and carries chemotherapy. It has reached phase 3 testing; earlier response findings do not prove comparative benefit.
An experimental antibody drug that carries two cancer-killing payloads to cells carrying TROP2. A first human study is registered but is still listed as not yet recruiting in an older record.
LCB84 is an experimental antibody-drug conjugate from LigaChem Biosciences. It links an antibody aimed at TROP2 to an MMAE prodrug and is being studied in a phase 1/2 trial.
MT-302 programs myeloid immune cells inside the body to recognise TROP-2-bearing cancers. It is an experimental treatment in an early clinical trial.
This early TROP-2 antibody-drug conjugate was tested in a study that stopped before completing development.
Sacituzumab govitecan carries chemotherapy to cancer cells bearing TROP2. It is FDA-approved for specific advanced breast-cancer settings, including two first-line triple-negative indications.
Sacituzumab tirumotecan is a TROP2 antibody-drug conjugate approved for specific advanced breast- and lung-cancer settings in China. It remains investigational in the United States.
SHR-A1921 is an experimental drug that delivers chemotherapy to TROP2-bearing cells. Early solid-tumor findings are distinct from the later trials testing its comparative benefit.
The first registered STI-3258 TROP-2 study was withdrawn before enrolling any participants.
These experimental immune cells are designed to recognize TROP2 on cancer cells. Early trials are studying their safety and activity.
VBC103 is an experimental drug designed to recognize two proteins on cancer cells. Its early trial is testing safety and activity.
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 unresectable or metastatic hormone-receptor-positive, HER2-negative breast cancer after endocrine-based therapy and chemotherapy for advanced disease, Dato-DXd is an FDA-approved option. TROPION-Breast01 showed longer progression-free survival and fewer severe treatment-related adverse events than chemotherapy; the final overall survival analysis did not show a statistically significant improvement. Approval in this setting does not establish a survival advantage or apply to postoperative early-stage disease.
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 AVZO-103, VBC103, Clinical Trial of VBC103 in Patients With Advanced Malignant Solid Tumors, Overexpression 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 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) 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.
Every source this page cites, grouped by who published it. Grouping is read from the web address, not assigned by hand.
A source that has moved or gone is reported by the weekly link check. /audit/