Table 1.

Radioimmunoconjugates in clinical trials for therapeutic applications under active development according to the Thomson Reuters Integrity database

NameBrand nameHighest phaseDescriptionConditionOrganizationStudy identifier
SHL-749 (Ibritumomab tiuxetan)ZevalinLaunched 2002Murine CD20 targeting antibody ibritumomab linked by the chelator tiuxetan to 90Y (or 111In for imaging purposes)B-cell lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, mantle cell lymphoma, non-Hodgkin's lymphomaBayer HealthCare Pharmaceuticals; Bayer Schering Pharma; Ben-Gurion University Negev; Biogen Idec; Nordion; Rigshospitalet; Spectrum PharmaceuticalsIDEC 106-04 IDEC 106-06 PMID 12074764
A phase III trial with 143 non-Hodgkin's lymphoma patients showed an overall response rate of 80% with 90Y-ibritumomab tiuxetan, compared with 56% with rituximab (68). A second trial found an overall response rate of 74% in rituximab refractory patients (IDEC 106-06). These and other studies led to FDA approval in 2002 for the treatment of patients with relapsed or refractory low-grade, follicular, or transformed B-cell non-Hodgkin's lymphoma, including patients with rituximab refractory follicular non-Hodgkin's lymphoma. In 2008, Zevalin was approved as first-line consolidation for follicular lymphoma in the European Union.
131I-tositumomabBexxarLaunched 2003Combination regimen consisting of the unlabeled and 131I-labeled murine CD20 targeting antibody tositumomabB-cell lymphoma, Hodgkin's lymphoma, diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, multiple myelomaCorixa; Fred Hutchinson Cancer Research Center; GlaxoSmithKline; NordionNCT00989664 NCT00996593
In a pivotal study of 40 patients (69) that led to the approval for the treatment of rituximab-refractory, low-grade, follicular non-Hodgkin's lymphoma in 2003, a response rate of 65% with progression-free survival of 24.5 months for responders was measured. In 2004, the indication was expanded for the treatment of non-Hodgkin's lymphoma patients who have not received rituximab, after a study showed superiority to last qualifying chemotherapy in 60 patients (70).
131I ch-TNT-1/BCotaraPhase II131I-labeled chimeric monoclonal antibody chTNT-1/B for tumor necrosis therapyAnaplastic astrocytoma, biliary cancer, colorectal cancer, liver cancer, pancreas cancer, glioblastoma multiforme, glioma, sarcomaPeregrine PharmaceuticalsNCT00004017
131I-BC8Phase II131I-labeled murine anti-CD45 monoclonal IgG1 antibodyAcute myeloid leukemiaFred Hutchinson Cancer Research Center; National Cancer Institute; University of WashingtonNCT00008177 PMID 19786617
111In-J591, 177Lu-J591Phase II111In/177Lu labeled humanized monoclonal antibody to prostate specific membrane antigen/extracellular domain (PSMAext)Prostate cancerBZL Biologics; Cornell University; Memorial Sloan-Kettering Cancer Center; Millennium PharmaceuticalsNCT00859781
131I-MetuximabLicartinPhase II131I-labeled murine monoclonal antibody HAb18 F(ab′)2 fragment against the HCC-associated antigen HAb18G/CD147Liver cancerEastern Hepatobiliary Surgery Hospital; Fourth Military Medical UniversityNCT00819650 NCT00829465
177Lu-DOTA-cG250Phase IIChimeric monoclonal antibody G250 conjugated to DOTA and radiolabeled with 177LuKidney cancer (renal cell carcinoma)Ludwig Institute for Cancer Research; Radboud Universiteit NijmegenNCT00142415
131I-3F8Phase II131I-labeled anti-GD2 ganglioside murine IgG3 monoclonal antibodyCancer, medulloblastoma, neuroblastomaMemorial Sloan-Kettering Cancer Center; National Cancer Institute; National Cancer InstituteNCT00003022 PMID 18048828
131I-L19Radre-tumabPhase II131I-labeled SIP composed of L19 that binds to the ED-B domain of human fibronectinNon–small cell lung cancer, solid tumors, hematologic/blood cancerPhilogenNCT01125085
131I-F16Tena-RadPhase II131I-labeled human monoclonal antibody against the A1 domain of tenascin-CHematological cancer, solid tumorsPhilogenNCT01240720
177Lu-J591Phase II177Lu-labeled humanized monoclonal antibody J591 targeting prostate-specific membrane antigen (PSMA)Metastatic prostate cancerCornell University; Memorial Sloan-Kettering Cancer CenterNCT00195039 NCT00859781
90Y-hLL2 IgG; (Epratuzu-mab-90Y)LymphoCide 90YPhase I/II90Y/111In-labeled human-mouse monoclonal IMMU-hLL2 targeting CD22Follicular lymphoma, non-Hodgkin's lymphoma, acute lymphoblastic leukemiaGarden State Cancer Center; ImmunomedicsNCT00421395 NCT00061425 PMID 16033839
Pretargeted antibody-guided radioimmunotherapyPhase I/IIPretargeted antibody-guided radioimmunotherapy using biotinylated anti-tenascin antibody (BC4), avidin, and 90Y-biotinGlioma, non-Hodgkin's lymphomaSigma-Tau
90Y-hPAM4 (90Y Clivatuzumab tetraxetan)hPAM4-CidePhase I/IIHuman-mouse monoclonal hPAM4 IgG1 targeting human Mucin-1 conjugated to DOTA and radiolabeled with 90YPancreas cancerGarden State Cancer Center; ImmunomedicsNCT00603863 NCT00597129

Phase I drugs 177Lu-CYT-500, 188Re-6D2, 90Y-cG250, 131I-huA33, 225Ac-HuM195, 131I-CHT-25, F16-131I are not listed in the table. Important studies are referenced with their identifier; for selected publications, the PubMed ID (PMID) is given.