Actinium-225 DOTATATE
An alpha-particle version of Lutathera for neuroendocrine tumours that have stopped responding to the beta version.
Overview
RYZ101 is actinium-225 DOTATATE, a targeted alpha therapy: the same SSTR2-binding peptide as Lutathera but chelating 225Ac, whose alpha decay chain delivers dense, short-range double-strand DNA breaks that beta particles cannot match. Bristol Myers Squibb acquired it with RayzeBio in 2024 for $4.1B. The ACTION-1 phase 3 trial tests it in SSTR-positive GEP-NETs progressing after 177Lu-SSTR therapy, at 10.5 MBq/kg every 8 weeks for 4 cycles, and it is also being combined with chemo-immunotherapy in extensive-stage small-cell lung cancer. Nausea, fatigue and lymphopenia are expected, and renal function is monitored because the kidneys clear the peptide. Whether alpha emission overcomes resistance to beta therapy, and whether 225Ac supply can meet demand, are the open questions. For a newcomer: an alpha-particle upgrade of an approved neuroendocrine radioligand.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
PubChem holds the unlabelled ligand, so the radionuclide itself is not in this drawing.
DOTATATE chelating 225Ac; alpha decay chain. Connects to Somatostatin receptor 2.
- PSMA / SSTR-positive cell
1.Radioligand circulates and binds Somatostatin receptor 2 on tumour cells
- Route
- IV infusion
- Schedule
- 10.5 MBq/kg every 8 weeks for 4 cycles (ACTION-1)
- Monitoring
- Renal function, blood counts, amino acid co-infusion
Source: clinicaltrials.gov/study/NCT05477576. Doses are for orientation; the current label governs.
Deals
Deal map| Date | Deal | Type | Upfront | Total | Source |
|---|---|---|---|---|---|
| 2023-12-26 | RayzeBio (BMS) to Bristol Myers Squibb RYZ101 (actinium-225 DOTATATE) and an actinium-based radiopharmaceutical platform | Acquisition | $62.50 per share in cash | about $4.1bn equity value, $3.6bn net of estimated cash acquired | source |
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- 26 Feb 2024Filing / dealUS
BMS completes RayzeBio acquisition ($4.1B) source
| Adverse event |
|---|
| Nausea |
| Fatigue |
| Lymphopenia |
| Renal toxicity (monitor) |
Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
| Country | Reimbursement | List price | Assistance |
|---|---|---|---|
| United States | Investigational | not disclosed | - |
List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.
Trials
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Landmark trials
Latest papers
topQuery for this drug: (TITLE:"Actinium-225 DOTATATE" OR ABSTRACT:"Actinium-225 DOTATATE" OR TITLE:"RYZ101" OR ABSTRACT:"RYZ101") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR 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 Actinium-225 DOTATATE, not a curated reading list.
Similar pages
not linked directly; found by shared links- CompanyOrano Med
Shares Recover legacy radium-226 sources worldwide as the feedstock for actinium-225, Actinium-225 supply, Alpha-emitter roadmap: radium-223 → 225Ac-PSMA-617 → a phase 3 pipeline, Radiopharmaceutical roadmap: iodine → lutetium → actinium.
- CompanyMolecular Targeting Technologies
Shares Small-cell lung cancer, Pancreatic neuroendocrine tumours, Small intestinal neuroendocrine tumours, Somatostatin receptor 2.
- CompanyTerraPower Isotopes
Shares Recover legacy radium-226 sources worldwide as the feedstock for actinium-225, Actinium-225 supply, Alpha-emitter roadmap: radium-223 → 225Ac-PSMA-617 → a phase 3 pipeline, Radiopharmaceutical roadmap: iodine → lutetium → actinium.
- Agent212Pb-DOTAMTATE
Shares SSTR theranostics roadmap: octreotide scintigraphy → 68Ga-DOTATATE → 177Lu-DOTATATE → alpha, Alpha-emitter roadmap: radium-223 → 225Ac-PSMA-617 → a phase 3 pipeline, Actinium-225 supply: thorium stocks, accelerators and radium targets, Pancreatic neuroendocrine tumours.
- IdeaSSTR antagonist radioligands to increase tumour dose
Shares SSTR theranostics roadmap: octreotide scintigraphy → 68Ga-DOTATATE → 177Lu-DOTATATE → alpha, Small intestinal neuroendocrine tumours, Somatostatin receptor 2, Peptide receptor radionuclide therapy (PRRT).
- TermPRRT (peptide receptor radionuclide therapy)
Shares Pancreatic neuroendocrine tumours, Small intestinal neuroendocrine tumours, Somatostatin receptor 2, Peptide receptor radionuclide therapy (PRRT).
- CompanyITM Isotope Technologies Munich
Shares Radiopharmaceutical roadmap: iodine → lutetium → actinium, Actinium-225 supply: thorium stocks, accelerators and radium targets, Somatostatin receptor 2, Peptide receptor radionuclide therapy (PRRT).
- AgentLutetium-177 dotatate (radioligand equivalent)
Shares Pancreatic neuroendocrine tumours, Small intestinal neuroendocrine tumours, Somatostatin receptor 2, Peptide receptor radionuclide therapy (PRRT).