iobenguane sulfate i-131
Trade name: iobenguane sulfate i-131
Approved
Mar 25, 1994
Iobenguane I-131 is a radioactive therapeutic agent. The drug contains radioactive isotope I-131, which decays by electron emission with a half-life of about 8 days. By the chemical structure, iobenguane is similar to the neurotransmitter norepinephrine and is subject to the same uptake and regulation pathways. After intravenous administration, iobenguane I-131 accumulates within pheochromocytoma and paraganglioma cells, and radiation from the radioactive decay causes cell death and tumor necrosis. Iobenguane I-131 was approved by the FDA for the treatment of adult and pediatric patients with iobenguane scan positive, unresectable, locally advanced or metastatic pheochromocytoma or paraganglioma who require systemic anticancer therapy. Iobenguane I-131 is investigated in clinical trials as a treatment of neuroblastoma, ganglioneuroblastoma and other tumors of neuroendocrinal origin. — NCATS
Clinical trial activity
24 trials · 34 clinical orgs · 2 marketing orgs
Earliest trial started May 1, 1991 (NCT01413503)
Timeline
1980s
- Nov 14, 1984
Orphan Drug Designation
1990s
- Jan 1, 1991
Earliest Phase 2 Sponsor(trial)
- Mar 25, 1994
Pharmalucence — Earliest FDA Approval
- Mar 25, 1994
Pharmalucence — NDA Secondary Org
- Mar 25, 1994
Pharmalucence — NDA Organization
2010s
- Jul 30, 2018
Progenics — NDA Secondary Org
Indications
Studied for
Mechanism of action
- Norepinephrine transporterSUBSTRATE
Norepinephrine transporter substrate
Is similar in structure to the neurotransmitter norepinephrine (NE) and is taken up by the NE transporter and accumulates in adrenergically innervated tissues, including tumors of neural crest origin that express high levels of surface NE transporter. Radiation causes cell death.
- contrast mediumRadiopaque
contrast medium radiopaque
Approval history
- approvedPriority reviewMar 25, 1994
Chemistry & pharmacology
SMILES
N=C(N)NCc1cccc([131I])c1.N=C(N)NCc1cccc([131I])c1.O=S(=O)(O)O- Mol. weight
- 656.27 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Discontinued
Oral
No
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL3989511 ↗
- NCATSQ461L7AK4R ↗
- ChEMBLCHEMBL1626569 ↗
- ChEMBLCHEMBL1615779 ↗
Also known as
- 131i mibg
- 131i mibg
- 131i-mibg
- 131i-mibg
- i-131 metaiodobenzylguanidine (mibg)
- i-131 mibg
- i-131 mibg
- iobenguane (131i)
- iobenguane (131i)
- iobenguane (131i)
- iobenguane (131i)
- iobenguane (131i)
- iobenguane i 131
- iobenguane i 131
- iobenguane i 131
- iobenguane i 131
- iobenguane i-131
- iobenguane i-131
- iobenguane i-131
- iobenguane sulfate (131i)
- iobenguane sulfate (131i)
- iobenguane sulfate i 131
- iobenguane sulfate i 131
- iobenguane sulfate i 131
- iobenguane sulfate i-131
- m131ibg
- m131ibg
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07261241 | Phase 2 | Jul 31, 2026 | Jubilant DraxImage Inc., National Cancer Institute (NCI), United Therapeutics |
| NCT04614766 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2020 | National Cancer Institute (NCI), National Institutes of Health (NIH), Progenics, University of Iowa |
| NCT03561259 | Phase 2 | Jul 31, 2018 | Jubilant DraxImage Inc. |
| NCT03126916 | Phase 3 | Aug 1, 2017 | National Cancer Institute (NCI) |
| NCT03165292 | Phase 2 | Jun 1, 2017 | Institut Gustave Roussy, National Cancer Institute, France |
| NCT03044977 | Early Phase 1 (Phase 1) | May 7, 2017 | National Cancer Institute (NCI), National Institutes of Health (NIH), University of Iowa |
| NCT01941849 | Phase 1 | Oct 1, 2014 | AstraZeneca, Cancer Research UK, University of London |
| NCT02035137 | Phase 2 | Jul 1, 2014 | Harvard University, National Cancer Institute (NCI) |
| NCT01838187 | N/A | Apr 8, 2013 | University of Cincinnati |
| NCT01590680 | N/A | May 1, 2012 | Cook Children's Medical Center, Duke University, Emory University, Harvard University, Jubilant DraxImage Inc., The University of Texas, Dallas, University of Chicago, University of Cincinnati, University of Colorado, University of Michigan, University of Washington, University of Wisconsin, Vanderbilt University |
| NCT01175356 | N/A | Oct 1, 2010 | National Cancer Institute (NCI) |
| NCT03061656 | Phase 2 | Jan 1, 2009 | Government of Korea, Sungkyunkwan University |
| NCT00960739 | Phase 2 | Nov 1, 2008 | National Cancer Institute, France, Novartis, University of Lille |
| NCT00798148 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2008 | Isfahan University |
| NCT00526318 | N/A | Jan 1, 2007 | Gesellschaft fur Padiatrische Onkologie und Hamatologie - Germany, University of Cincinnati |
| NCT00509353 | Phase 1 | Jan 1, 2007 | National Cancer Institute (NCI), University of California, San Francisco, University of Southern California |
| NCT00107289 | Phase 2 | May 1, 2006 | Cornell University, National Cancer Institute (NCI) |
| NCT00253435 | Phase 2 | Sep 1, 2005 | National Cancer Institute (NCI), University of California, San Francisco, University of Michigan, University of Pennsylvania, University of Southern California |
| NCT00293319 | Phase 2 | Apr 1, 2005 | National Cancer Institute (NCI), University of California, San Francisco, University of Pennsylvania |
| NCT00410631 | Phase 3 | Oct 1, 2004 | Gesellschaft fur Padiatrische Onkologie und Hamatologie - Germany, University of Cincinnati |
Organizations
Research & Development (34)
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Pharmalucence | For profit | NDA2 | Mar 25, 1994 |
| Pharmalucence | For profit | NDA | Mar 25, 1994 |
| Progenics | For profit | NDA2 | Jul 30, 2018 |