Table 2 Some key features of anticancer peptidomimetics that have entered the clinical studies

68Ga-NODAGA-THERANOST™

αvβ3 integrin

✓ Non-small-cell lung cancer

✓ Breast cancer

✓ Phase 2

✓ NCT04480619

Baum et al. (2015), Kim et al. (2012)

64Cu-LLP2A

α4β1 integrin

Multiple myeloma (MM)

✓ Early Phase 1

✓ NCT03804424

Beaino and Anderson (2014), Walker et al. (2016), Laforest et al. (2022)

FAP-2286

Fibroblast Activation Protein (FAP)

Solid tumors

✓ Phase 1

✓ NCT04621435

Zboralski et al. (2022)

Cilengitide

αvβ3, αvβ5, α5β1 integrins

✓ Malignant glioblastoma (GBM)

✓ Malignant primary brain tumors

✓ Phase 3

✓ NCT00689221

Mas-Moruno et al. (2010), Dechantsreiter et al. (1999), Stupp et al. (2014)

GDC-0152

ANGPTL2

Solid tumors

✓ Phase 1

✓ NCT00689221

Shin et al. (2013), Yang et al. (2015)

KX2-391

Src kinase inhibitor

Solid tumors

✓ Phase 2

✓ NCT02838628

Kempers et al. (2020)

Cyclic RGD

VEGF related pathways

Colon and pancreatic malignancies

✓ Phase 2

✓ NCT05518071

Valk et al. (2020)

XK469

DNA topoisomerase II (topo II) inhibition

Liver tumors

✓ Phase 1

✓ NCT00028548

Xia et al. (2016)