Radioligands
A ligand that binds the target, a chelator that holds the metal, and an isotope whose emission does the work; beta emitters travel millimetres, alpha emitters micrometres. The grid below is target against isotope: 7 by 7 from 16 medicines, 7 combinations approved, 5 in development, 0 tried and stopped, 37 untried in this corpus.
Antibody-drug conjugatesRadioligandsCAR cell therapiesTCR-T cell therapiesBispecific antibodiesDegraders and molecular gluesSmall-molecule inhibitorsNaked antibodiesCytokinesCancer vaccinesOncolytic virusesOther cell therapies
Approved 7In development 5Tried and stopped 0Recorded, state unclear 0Untried here 377 target rows x 7 isotope columns. Click a cell to filter the table.
Every tried combination
12 combinations
| Medicines | Records | Stopped, and why | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| PSMA | Lutetium-177 | Approved | 1 | 1 | 0 | Small-molecule ligand | DOTAGADOTA | - | |||
| PSMA | Actinium-225 | In development | 0 | 3 | 0 | Small-molecule ligand | - | - | |||
| PSMA | Radium-223 | Approved | 1 | 0 | 0 | Bone-seeking mimetic | - | - | |||
| PSMA | Samarium-153 | Approved | 1 | 0 | 0 | Bone-seeking mimetic | EDTMP | - | |||
| Somatostatin receptor 2 | Lutetium-177 | Approved | 1 | 1 | 0 | DOTA | - | ||||
| Somatostatin receptor 2 | Actinium-225 | In development | 0 | 1 | 0 | DOTA | - | ||||
| Somatostatin receptor 2 | Lead-212 | In development | 0 | 1 | 0 | DOTA | - | ||||
| CD20 | Yttrium-90 | Approved | 1 | 0 | 0 | - | Zevalin authorised 16 Jan 2004; marketing stopped May 2020 (manufacturing) and the authorisation lapsed under the sunset clause 4 Jan 2024 | ||||
| FAP | Lutetium-177 | In development | 0 | 1 | 0 | DOTA | - | ||||
| Norepinephrine transporter | Iodine-131 | Approved | 1 | 0 | 0 | Small-molecule ligand | - | - | |||
| PTPRC | Iodine-131 | In development | 0 | 1 | 0 | - | - | ||||
| Sodium-iodide symporter (NIS) | Iodine-131 | Approved | 1 | 0 | 0 | Transporter substrate | - | - |
Stopped, and why
0 medicines recorded as stopped; 1 recorded reason, including stopped studies of medicines still in development- Ibritumomab tiuxetanApproved
Zevalin authorised 16 Jan 2004; marketing stopped May 2020 (manufacturing) and the authorisation lapsed under the sunset clause 4 Jan 2024
EMA / European Commission (EU): withdrawn 2024 · regulator row
Proposed, not yet tried
11 proposals from the open pipeline, scored and searched (docs/OPEN-PIPELINE.md); hypotheses, not records of a medicineClinical evidence 6Preclinical 2No public evidence 3
| Score | Target | Isotope | Status | Rationale | Evidence | Now in the corpus |
|---|---|---|---|---|---|---|
| 79 | DLL3 | Lutetium-177 | Clinical evidence | DLL3 radioligand labelled with lutetium-177. DLL3 is validated by an approved T-cell engager (tarlatamab) and lutetium-177 by two approved radioligands (pluvicto, lutathera). No corpus product pairs DLL3 with a radionuclide, despite small-cell lung cancer's radiosensitivity and the tumour-restricted antigen. Small-cell lung cancer is the most radiosensitive common solid tumour and DLL3 has no normal-tissue surface expression, so the target-to-background is favourable; low antigen density is the objection, which the crossfire of a beta emitter partly answers.Caveat: Low DLL3 density and the rapid kinetics of small-cell disease mean an antibody carrier may deliver too little dose too slowly; a fast-clearing fragment or a pre-targeting approach may be required.Proposed by OnCo open pipeline, searched 2026-09-23. | Trial: Memorial Sloan Kettering Cancer Center (2025-04-23)Trial: Novartis Pharmaceuticals (2025-06-05), neighbouring cellTrial: Molecular Partners AG (2025-12-12), neighbouring cellTrial: Abdera Therapeutics Inc. (2024-12-16), neighbouring cellLutetium-177 dotatateLutetium-177 vipivotide tetraxetanTarlatamab | Untried |
| 77 | Claudin 18.2 | Lutetium-177 | Preclinical | Claudin 18.2 radioligand labelled with lutetium-177. Claudin 18.2 is validated by an approved antibody (zolbetuximab) and an approved CAR-T (satricabtagene-autoleucel), and lutetium-177 by two approved radioligands (pluvicto, lutathera). No corpus product pairs Claudin 18.2 with a radionuclide, though the antigen's tumour-selective exposure is the property radioligand targets need. Claudin 18.2 is exposed on cancer cells but hidden in tight junctions of normal stomach, giving a tumour-selective epitope; gastric and pancreatic cancers are moderately radiosensitive, and a nanobody or peptide carrier would give the fast clearance a radioligand needs.Caveat: Normal gastric mucosa does express Claudin 18.2 at the tight junction; whether a radioligand's crossfire spares it, as a large antibody does, needs to be shown in dosimetry first.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 75 | HER2 | Lutetium-177 | Clinical evidence | HER2 radioligand labelled with lutetium-177. HER2 is the corpus's most validated delivery antigen (trastuzumab-deruxtecan, trastuzumab-emtansine, zanidatamab) and lutetium-177 is validated by two approved radioligands (pluvicto, lutathera). No corpus product pairs HER2 with a therapeutic radionuclide, although HER2 imaging tracers already show the antigen can be targeted in vivo. HER2 is a proven delivery target, but a full antibody circulates for weeks and delivers a high marrow dose with lutetium-177; a small HER2-binding scaffold (affibody, nanobody) with fast clearance is the format that would make this work, and HER2 on heart tissue is the safety question.Caveat: An intact antibody carrier would give too much marrow dose; the proposal requires a small, fast-clearing HER2 binder with kidney retention solved, which is engineering work before any efficacy question.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 75 | Nectin-4 | Lutetium-177 | Preclinical | Nectin-4 radioligand labelled with lutetium-177. Nectin-4 is validated by an approved ADC (enfortumab-vedotin) and lutetium-177 by two approved radioligands (pluvicto, lutathera). No corpus product pairs Nectin-4 with a radionuclide, although the antigen's density and restricted expression are the properties the radioligand field selects for. Nectin-4 is highly expressed in urothelial cancer with limited normal-tissue expression apart from skin; a small peptide or bicyclic ligand with fast clearance is the plausible carrier, and skin dose is the toxicity to model.Caveat: A radioligand needs a small ligand with good tumour retention, which for Nectin-4 is not yet an established chemistry; the first evidence would be a PET tracer showing uptake in patients.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 75 | TROP2 | Lutetium-177 | No public evidence | TROP2 radioligand labelled with lutetium-177. TROP2 carries three approved ADCs (sacituzumab-govitecan, datopotamab-deruxtecan, sacituzumab-tirumotecan) and lutetium-177 is validated on two targets (pluvicto, lutathera). No corpus product pairs TROP2 with a radionuclide. TROP2 is broadly expressed on epithelial cancers but also on skin, oesophagus and other normal epithelia, which a radioligand cannot spare as an ADC can through antigen-density thresholds; the case is weaker than for Nectin-4 or PSMA.Caveat: Normal-tissue TROP2 expression is the objection; a PET tracer study showing tumour-to-background ratios comparable to PSMA would be needed before therapy is credible.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 68 | CD20 | Lutetium-177 | No public evidence | CD20 radioligand labelled with lutetium-177. CD20 is validated as a radioimmunotherapy target by an approved yttrium-90 conjugate (ibritumomab-tiuxetan) and lutetium-177 is the most validated therapeutic isotope in the corpus (pluvicto, lutathera). No corpus product pairs CD20 with lutetium-177, although the lutetium infrastructure built for prostate and neuroendocrine cancer now exists in most large centres. CD20 radioimmunotherapy is proven with yttrium-90 (ibritumomab-tiuxetan); lutetium-177's gamma emission allows dosimetry and its shorter beta range spares marrow, so it may revive a modality abandoned for logistics rather than efficacy.Caveat: Radioimmunotherapy of lymphoma lost to rituximab combinations and bispecifics on convenience, not efficacy; a lutetium-177 CD20 agent would need a defined place, most plausibly consolidation in follicular lymphoma.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 68 | PSMA | Iodine-131 | Clinical evidence | PSMA radioligand labelled with iodine-131. PSMA is validated by an approved lutetium-177 radioligand (pluvicto) and iodine-131 is the oldest approved therapeutic isotope (radioactive-iodine, i131-mibg). No corpus product pairs PSMA with iodine-131, though the isotope's supply is independent of the reactor bottlenecks the corpus flags for lutetium and actinium (actinium-225-supply). Iodine-131 is cheap and reactor-independent of the lutetium supply chain (therapy-isotope-supply-chain), and its 8-day half-life suits slowly clearing ligands; the gamma emission and long marrow dose are the reasons lutetium is preferred.Caveat: It would need to show equivalence to lutetium-177 with acceptable marrow dose and radiation-protection burden; the argument is access and cost in countries without lutetium supply rather than efficacy.Proposed by OnCo open pipeline, searched 2026-09-23. | Trial: Progenics Pharmaceuticals, Inc. (2019-05-07)Paper: Yu EY et al. (2026-05-01)Paper: Afshar-Oromieh A et al. (2017-03-09)Actinium-225 supply: thorium stocks, accelerators and radium targets131I-MIBG (iobenguane I-131) therapyLutetium-177 vipivotide tetraxetanRadioactive iodine (I-131)Therapeutic isotope supply chain (Mo-99, Lu-177, Ac-225) | Untried |
| 68 | PSMA | Lead-212 | Clinical evidence | PSMA radioligand labelled with lead-212. PSMA is validated by an approved radioligand (pluvicto) and lead-212 is in phase 2 on SSTR2 (alphamedix), while the corpus actinium-225 PSMA programmes are in phase 3 (aaa817, ac225-psma). No corpus product pairs PSMA with lead-212, an isotope whose generator supply avoids the actinium bottleneck the corpus records (actinium-225-supply). Lead-212's 10.6-hour half-life matches the fast kinetics of small PSMA ligands better than actinium-225's ten days, and it can be produced from generators (alpha-nanogenerators) rather than the scarce actinium supply; the short half-life makes distribution the hard part.Caveat: A 10.6-hour half-life means the dose must be made close to the patient; the proposal stands or falls on a distribution network, not on the biology.Proposed by OnCo open pipeline, searched 2026-09-23. | Trial: AdvanCell Pty Limited (2023-02-09)Trial: ARTBIO Inc. (2025-10-09)Paper: Høyvik AJK et al. (2025-05-21)AAA817Actinium-225 PSMA agentsActinium-225 supply: thorium stocks, accelerators and radium targetsAlpha-emitter nanogenerators and daughter trapping212Pb-DOTAMTATELutetium-177 vipivotide tetraxetan | Untried |
| 64 | CD33 | Actinium-225 | Clinical evidence | CD33 radioligand labelled with actinium-225. CD33 is validated by an approved ADC (gemtuzumab-ozogamicin) and actinium-225 is in phase 3 on PSMA and SSTR2 (aaa817, ryz101). No corpus product pairs CD33 with an alpha emitter, though the corpus already carries a CD45 iodine-131 antibody as transplant conditioning (iomab-b) showing the marrow-targeted radioimmunotherapy route is workable. CD33 is on most AML blasts and alpha particles kill without needing internalisation or cell division, which suits quiescent blasts and low antigen density; marrow toxicity is the design constraint and a transplant-conditioning use is the natural fit (iomab-b uses the same logic with CD45).Caveat: The place for this agent is probably conditioning before transplant or a bridge to it; as a stand-alone therapy in unfit older patients, cytopenias would compete with the disease.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 63 | GPRC5D | Lutetium-177 | No public evidence | GPRC5D radioligand labelled with lutetium-177. GPRC5D is validated by an approved T-cell engager (talquetamab) and lutetium-177 by two approved radioligands (pluvicto, lutathera). No corpus product pairs GPRC5D with a radionuclide, although its restricted expression is the property that made SSTR2 a good radioligand target. GPRC5D is a GPCR restricted to plasma cells and keratinised tissue, the same target class as SSTR2 that made lutathera possible; myeloma is radiosensitive, but no small-molecule or peptide GPRC5D ligand is known, so the carrier would have to be an antibody fragment.Caveat: Without a small ligand, an antibody-fragment carrier and its kidney retention are the engineering problems; and the hair, nail and tongue expression that gives talquetamab its toxicity would receive radiation too.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried | |
| 60 | CD38 | Actinium-225 | Clinical evidence | CD38 radioligand labelled with actinium-225. CD38 is validated by two approved antibodies (daratumumab, isatuximab) and actinium-225 is in phase 3 on two other targets (aaa817, ryz101). No corpus product pairs CD38 with a therapeutic radionuclide, although the antigen's density and the radiosensitivity of plasma cells make it a natural radioimmunotherapy target. Myeloma is radiosensitive and CD38 is dense on plasma cells; an alpha emitter's 2-3 cell range suits marrow-infiltrating disease, but CD38 on NK cells and the long antibody half-life mean marrow toxicity is the limit, as with any haematological radioimmunotherapy.Caveat: Daratumumab pre-treatment lowers CD38 on residual cells and free daratumumab in serum would compete for the antigen; timing after antibody washout is a prerequisite for any dose to reach tumour.Proposed by OnCo open pipeline, searched 2026-09-23. | Untried |
Not placed
1 of 17 medicines in this format (6%)These medicines belong to the format but their target is on no record the engine reads: the targets field is empty, the target lists no such drug, the trials linked to it name no target of its own, and the modality, mechanism and summary text name none the corpus knows. They are listed here rather than placed by guesswork; adding the target to the record puts them in the grid on the next build.
How this grid is read from the records
Each medicine's parts come from its own record: the targets field first, else the target records that list the medicine, else a sibling conjugate that shares its antibody name, else the trials linked to it, else the target names the corpus knows found in its modality, mechanism or summary text. The isotope is read from the name, modality or mechanism (177Lu, 225Ac, 212Pb, 223Ra, 131I and the rest); its emission is a fixed physics table; the chelator and ligand class from the mechanism text. Every part carries the fields it was read from and a confidence in the JSON file.
What the states mean, and do not
Approved: a medicine in the cell has an approval row or a regulator's approved entry and is not recorded as withdrawn. In development: a recruiting, active or planned trial, a development-phase record status, or active studies in the ClinicalTrials.gov index, and no approval. Tried and stopped: every medicine in the cell is withdrawn, negative or historic, or its only trial evidence is a terminated, withdrawn or negative study, or its approval was withdrawn. Untried: no medicine in this corpus combines the two parts.
A cell is coloured by its strongest medicine; the table shows each medicine with its own state. The reasons quoted under Stopped, and why are the records' words, including the registry's whyStopped text where the sponsor wrote one, and include stopped studies of medicines that are still in development elsewhere. Nothing here is medical advice.