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An alpha-particle version of Lutathera for neuroendocrine tumours that have stopped responding to the beta version.
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
DOTATATE chelating 225Ac; alpha decay chain. Connects to Somatostatin receptor 2.
1.Radioligand circulates and binds Somatostatin receptor 2 on tumour cells
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
Source: clinicaltrials.gov/study/NCT05477576. Doses are for orientation; the current label governs.
| 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 | not disclosed | $4.1bn | source |
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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.
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Query for this drug: (TITLE:"Actinium-225 DOTATATE" OR ABSTRACT:"Actinium-225 DOTATATE" OR TITLE:"RYZ101" OR ABSTRACT:"RYZ101") 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 Actinium-225 DOTATATE, not a curated reading list.
Shares Recover legacy radium-226 sources worldwide as the feedstock for actinium-225, Actinium-225 supply: thorium stocks, accelerators and radium targets, Radiopharmaceutical roadmap: iodine → lutetium → actinium, Peptide receptor radionuclide therapy (PRRT).
Shares Actinium-225 supply: thorium stocks, accelerators and radium targets, Peptide receptor radionuclide therapy (PRRT), Somatostatin receptor 2, Small intestinal neuroendocrine tumours.
Shares Somatostatin receptor expression by PET (SSTR-positive), Peptide receptor radionuclide therapy (PRRT), Somatostatin receptor 2, Small intestinal neuroendocrine tumours.
Shares Recover legacy radium-226 sources worldwide as the feedstock for actinium-225, Actinium-225 supply: thorium stocks, accelerators and radium targets, Radiopharmaceutical roadmap: iodine → lutetium → actinium, Targeted alpha therapy.
Shares Actinium-225 supply: thorium stocks, accelerators and radium targets, Radiopharmaceutical roadmap: iodine → lutetium → actinium, Peptide receptor radionuclide therapy (PRRT), Somatostatin receptor 2.
Shares Recover legacy radium-226 sources worldwide as the feedstock for actinium-225, Beta radioligand → alpha radioligand, Actinium-225 supply: thorium stocks, accelerators and radium targets, Radiopharmaceutical roadmap: iodine → lutetium → actinium.
Shares Peptide receptor radionuclide therapy (PRRT), Somatostatin receptor 2, Small intestinal neuroendocrine tumours, Pancreatic neuroendocrine tumours.
Shares Somatostatin receptor expression by PET (SSTR-positive), Peptide receptor radionuclide therapy (PRRT), Somatostatin receptor 2, Small intestinal neuroendocrine tumours.