Tracers / [212Pb]Pb-212-TCMC-trastuzumab
[212Pb]Pb-212-TCMC-trastuzumab
Also written as Pb-212-TCMC-trastuzumab
- Radionuclide
- Pb-212 t½ 638.4 min
- Modality
- Therapy
- Production route
- —
- Stage
- Phase I clinical trial (first-in-human)
- Syntheses indexed
- 5
What it is
- Compound class
- Radiolabeled monoclonal antibody (TCMC-conjugated anti-HER2 antibody trastuzumab, alpha-particle immunoconjugate)
- Target / mechanism
- HER2-targeting via trastuzumab antibody delivering alpha-emitting 212Pb PMID 24229395
- Clinical application
- Intraperitoneal targeted alpha-particle radioimmunotherapy for HER-2-expressing peritoneal carcinomatosis (e.g., ovarian cancer) PMID 25157044
- 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 |
|---|---|---|---|---|---|---|
| Manual synthesis | — | — | — | — | TCMC | 26858987 2015 AIMS Med Sci conjugation of mAbs with the chelator is routinely performed at molar chelate to antibody/peptide ratios of 5–20:1 |
| Manual synthesis | — | SPE | 92.2% to 99.6% | 90.2% to 100% | TCMC-trastuzumab Goodwin Biotechnology, Inc. | 26230702 2015 Pharmaceuticals (Basel) TCMC-trastuzumab was then labeled with 212Pb as previously described — Radiolabelling efficiency of the cGMP TCMC-trastuzumab with 212Pb ranged from 92.2% to 99.6% |
| Manual synthesis | — | SPE | — | 82.1% and 83% | TCMC-trastuzumab Goodwin Biotechnology, Inc. | 26230702 2015 Pharmaceuticals (Basel) The 203Pb solution was neutralized and the cGMP TCMC-trastuzumab (100 µg) added, vortexed and incubated at 37 °C for 1 h |
| — | — | — | — | — | TCMC-trastuzumab Genentech | 25157044 2014 J Nucl Med |
| — | — | — | — | — | — | 24229395 2014 Cancer Biother Radiopharm |
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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) -- 5 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 26230702: '1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoylmethyl)-cyclododecane-trastuzumab (212Pb-TCMC-trastuzumab)'. Stage set/updated at stage 23 from PMID 25157044: 'Dose escalation and dosimetry of first-in-human α radioimmunotherapy with 212Pb-TCMC-trastuzumab.'.