TABLE 2.
Overview of anti-TGF-β therapies based on integrin inhibitors used in cancer clinical trials.
| Drug (Target) | Clinical trial (Phase) | Status | Cancer type | Patients enrolled | Arms | Outcomes |
| EMD 121974 (Integrins αvβ3 and αvβ5) | NCT01122888 (Phase I) | Terminated | Adult giant cell glioblastoma, adult glioblastoma, adult gliosarcoma, adult solid neoplasms and recurrent adult brain neoplasms | 41 | Sunitinib + EMD 121974 Sunitinib |
NA |
| EMD 121974 (Integrins αvβ3 and αvβ5) | NCT00705016 (Phases I/II) | Completed | Head and NeckSquamous Cell Carcinoma | 184 | Cilengitide (2000 mg) once weekly + cetuximab + 5-FU + cisplatin Cilengitide (2000 mg) twice weekly + cetuximab + 5-FU + cisplatin Cetuximab + 5-FU + Cisplatin |
No improvement in PFS No improvement in OS |
| EMD 121974 (Integrins αvβ3 and αvβ5) | NCT00689221 (Phase III) | Completed | Glioblastoma | 545 | Cilengitide + temozolomide + radiotherapy Temozolomide + radiotherapy |
No improvement in PFS No improvement in OS |
| SF1126 (Integrin-targeted PI3 kinase) | NCT02337309 (Phase I) | Terminated | Neuroblastoma | 4 | Single-arm: SF1126 | NA |
| IMGN388 (Integrins αv) | NCT00721669 (Phase I) | Completed | Melanoma, breast carcinomas, lung carcinomas and ovary carcinomas | 60 | Single-arm: IMGN388 | NA |
| MEDI-522 (Integrin αvβ3) | NCT00284817 (Phases I/II) | Completed | Colorectal cancer | 17 | MEDI-522 (D0: 4 mg/kg; W1–W51: 1 mg/kg) MEDI-522 (D0: 4 mg/kg; W1–W51: 2 mg/kg) MEDI-522 (D0: 6 mg/kg; W1–W51: 2 mg/kg) MEDI-522 (D0: 6 mg/kg; W1–W51: 3 mg/kg) |
NA |
| M200 (Integrin α5β1) | NCT00635193 (Phases I/II) | Completed | Ovarian cancer and primary peritoneal cancer | 138 | Liposomal doxorubicin (40 mg/m2) + M200 (7.5 mg/kg) Liposomal doxorubicin (40 mg/m2) + M200 (15.0 mg/kg) Liposomal doxorubicin (40 mg/m2) |
NA |
5-FU, 5-fluoracil; D0, First day of treatment; W1–W51, weeks 1–51 of treatment; PFS, progression-free survival; OS, overall survival; NA, not available.