Table 2.

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

Name	Target	Indication	Clinical status/Trial ID	Refs.
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)