Tracers / [177Lu]Lu-DOTA-trastuzumab
[177Lu]Lu-DOTA-trastuzumab
Also written as [Lu-177]Lu-DOTA-Trastuzumab; [Lu-177]Lu-DOTA-trastuzumab; Lu-177-DOTA-trastuzumab; Lu-177-DOTA-Trastuzumab; [Lu-177]Lu-Trastuzumab; [Lu-177]trastuzumab; [Lu-177]Lu-trastuzumab
- Radionuclide
- Lu-177 t½ 9584.6 min
- Modality
- Therapy
- Production route
- —
- Stage
- clinical evaluation
- Syntheses indexed
- 5
What it is
- Compound class
- DOTA-conjugated monoclonal antibody (radioimmunoconjugate)
- Target / mechanism
- Targets HER2 (human epidermal growth factor receptor 2) via trastuzumab antibody binding PMID 37857502
- Clinical application
- Radioimmunotherapy for HER2-positive cancers (breast cancer, gastric cancer, ovarian peritoneal carcinomatosis) PMID 41256994
- Theranostic pair
- —
Regulatory status
- FDA
- —
- EMA (centralised)
- —
- Other approvals
- —
- Brand names
- —
Clinical use
- Typical injected activity
- —
- Uptake time
- —
Reported in the literature. Not a dosing recommendation.
Published syntheses
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| — | — | — | — | — | DOTA-Trastuzumab | 41256994 2025 ACS Med Chem Lett |
| — | — | — | — | — | — | 40794258 2025 EJNMMI Res |
| — | — | — | — | — | — | 37857502 2023 J Nucl Med |
| Manual synthesis | — | SPE | — | >99% | p-SCN-Bn-DOTA Macrocyclics | 36972439 2023 Proc Natl Acad Sci U S A Trastuzumab (Genentech) or isotope control antibody (IgG1) (MP Biomedicals) was conjugated with 20-fold molar excess of p-SCN-Bn-DOTA (Macrocyclics, Inc.) chelator at a pH of 9 and 37 °C for 90 min on a thermomixer at 350 rpm. |
| — | — | — | — | — | DOTA-Trastuzumab | 41590403 2026 Bioconjug Chem |
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Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 9 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Compound class inferred from precursor name (not stated outright) -- PMID 36972439: 'conjugated with 20-fold molar excess of p-SCN-Bn-DOTA (Macrocyclics, Inc.) chelator'. Stage set/updated at stage 23 from PMID 41256994: '[177Lu]-Lu-DOTA-Trastuzumab is currently under clinical evaluation for radioimmunotherapy (RIT) for HER2-positive breast cancer.'. | Stage 29 (2026-09-14): merged lu177-trastuzumab into this row -- bare '[177Lu]Lu-trastuzumab' had 0 parsed syntheses of its own; its discovery cluster (4 Lu-177 PMIDs, via the '[Tb-161]Tb-trastuzumab' bulk-discovery group) overlaps 4 PMIDs with this agent's own discovery cluster, and the literature commonly names DOTA-trastuzumab and plain trastuzumab conjugates interchangeably. Its alternative-name spellings folded in above.