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. 2021 Sep 17;21(1):60–78. doi: 10.1038/s41573-021-00284-4

Table 3.

Selected integrin inhibitors in clinical trials with reported clinical safety and efficacy data

Name (sponsor) Modality Delivery route Population or indication Integrin targets Highest human dose reported ClinicalTrials.gov identifiers Safety and efficacy
BG00011 (Biogen) Humanized mAb s.c. IPF αvβ6 56 mg weekly NCT03573505 Toxicity observed174
Intetumumab (CNTO-95) (Centocor) Humanized mAb i.v. Melanoma, prostate cancer Pan-αv 10 mg kg−1 every 3 weeks NCT00246012, NCT00537381 Tolerated but no efficacy188,189
Abituzumab (DI17E6) (Merck KGaA) Humanized mAb i.v. Colorectal cancer Pan-αv 1,500 mg every 4 weeks NCT01008475 Acceptable tolerability; did not meet primary end points106
GLPG0187 (Galapagos NV) 7 Small molecule Continuous infusion Solid tumours Pan-αv, α5β1 400 mg daily NCT01313598 Well tolerated; no efficacy42
GSK3008348 (GSK) 5 Small molecule Inhalation Healthy volunteers αvβ6 3 mg NCT02612051 Well tolerated190
Cilengitide (EMD Serono) 1 Cyclic peptide i.v. Glioblastoma αvβ3, αvβ5 2,000 mg twice a week NCT00689221 Well tolerated; no efficacy39
MK-0429 (Merck & Co.) 13 Small molecule Oral Metastatic bone disease Pan-αv 1,600 mg twice daily for 4 weeks NCT00302471 Safe191
Etrolizumab (Roche) Humanized mAb s.c. Ulcerative colitis α4β7 105 mg every 4 weeks NCT02136069 Well tolerated192
VPI-2690B (Vascular Pharmaceuticals) Humanized mAb s.c. Diabetic nephropathy αvβ3 48 mg every 2 weeks NCT02251067 Safe; significant levels of drug exposure193
THR-687 (Oxurion) Small molecule Intravitreal injection DME Pan-αv, α5β1 2.5 mg NCT03666923 Safe and well tolerated194
SF0166/OT-166 (Scifluor Life Sciences/OcuTerra Therapeutics) 11 Small molecule Topical Age-related macular degeneration, DME αvβ3, αvβ6, αvβ8 5% solution twice a day for 28 days NCT02914613, NCT02914639 Well tolerated; one potential mild-to-moderate drug-related adverse event195
Risuteganib (Luminate, ALG-1001; Allegro Ophthalmics) 4 Small molecule Intravitreal injection DME, dry age-related macular degeneration αvβ3, αvβ5, α5β1 1.0 mg NCT03626636 Well tolerated196
PLN-74809 (Pliant Therapeutics) 15 Small molecule Oral IPF αvβ6, αvβ1 40 mg daily for 7 days197 NCT04396756 Good tolerability
SB-273005 (GSK) 14 Small molecule Oral Osteoporosis αvβ3/αvβ5 2,000 mg daily Historic No toxicity in humans; dose-dependent heart valve lesions in mice (species-specific)198

Studies that have published safety, tolerability or efficacy data are included. Numbers in bold refer to the molecule structures in Figs 2,3. DME, diabetic macular oedema; GSK, GlaxoSmithKline; IPF, idiopathic pulmonary fibrosis; i.v., intravenous; mAb, monoclonal antibody; s.c., subcutaneous.