Table 1.

Drugs against RGD‐binding integrins and against TGF‐β

Drug	Target	Disease	Clinical Stage	Company
A: Chemical or peptide/protein based drugs
Abciximab ( a )	α IIbβ3 ( b )	Thrombosis	approved	Janssen Biologics
Tirofiban	α IIbβ3	Thrombosis	approved	Medicure Pharma
Intrifiban	α IIbβ3	Thrombosis	approved	Millennium Pharmaceuticals
GSK3008348	α vβ6	idiopathic pulmonary fibrosis (IPF)	Phase I	GSK
PLN‐74809	α vβ1 and α vβ6	IPF	Phase IIa	Pliant
THR‐687	pan RGD integrin inhibitor	Diabetic macular edema	Phase II planned	Oxurion NV
GLPG0187	α vβ1, α vβ3, α vβ5, α vβ6, and α 5β1	Solid tumors	Phase I	Galapagos NV
IDL2965	α vβ1, α vβ3, and α vβ6	IPF	Phase IIa	Indalo Therapeutics
Risuteganib	α 5β1, α vβ1, α vβ3, and α vβ5	Dry age‐related macular degeneration, diabetic macular edema	Phase IIa	Allegro
MK‐0429	αvβ1, but has also been shown to block α 5β1, α vβ3, α vβ5, α vβ6, α vβ8, α 5β1139	Prostate cancer, Post‐Menopausal Osteoporosis	Phase I, II	Merck Sharp & Dohme
Cilengitide	α 5β1, α vβ3 and α vβ5	Solid tumors	Phase II/III	Merck KGaA
ATN161	α 5β1	Renal cancer, glioma	Phase II	Attenuon
B: Antibodies against RGD‐binding integrins
Intetumumab	α vβ1, α vβ3, α vβ5, and α vβ6	Prostate cancer, melanoma	Phase II	Centocor, Inc.
BG00011 (STX‐100)	α vβ6	IPF	Phase II	Biogen
Abituzumab (EMD525797)	α vβ1, α vβ3, α vβ5, α vβ6, and α vβ8	Prostate cancer, colorectal cancer	Phase II	Merck KGaA
C: TGF‐β inhibitors
OT‐101 (Trabedersen)	TGF‐β2	Solid cancer/ COVID‐19	Phase III/IND filed for phase II study	Mateon Therapeutics
Galunisertib	TGF‐beta receptor type‐1 (TGF‐βR1)	Myelodysplastic syndrome and solid tumors	Phase II/III	Eli Lilly & Company (Lilly)
TEW‐7197	TGF‐βR1	Solid tumors	Phase I	MedPacto Inc.
LY3022859	TGF‐βR2	Advanced solid tumors	Phase I	Lilly
LY2157299	TGF‐βR2	Hepatocellular carcinoma	Phase II	Lilly
LY2382770	TGF‐β1	Diabetic kidney disease, diabetic nephropathy, diabetic glomerulosclerosis	Phase II	Lilly
Fresolimumab (GC‐1008)	Pan TGF‐β	Systemic sclerosis, focal segmental glomerulosclerosis, myelofibrosis, and solid tumors	Phase II	Genzyme
Luspartecept	TGF‐β superfamily inhibitor	β‐thalassaemia; anaemia in patients with MDS	Phase II	Acceleron Pharma
NIS793	Pan TGF‐β	Solid tumors	Phase I	Novartis
LY2382770	TGF‐β1	Diabetic kidney disease (fibrosis)	Phase II	Lilly &
CAT‐192	TGF‐β1	Systemic sclerosis scleroderma	Phase I/II	Genzyme
AVID200	TGF‐β1 & ‐β3	Scleroderma, myelofibrosis, solid tumors	Phase I	Icahn School of Medicine at Mount Sinai

IND, Investigational New Drug.

^aAbciximab is a Fab fragment. We listed it in this table because it is not a full length antibody.

^bWe only show approved drugs against αIIbβ3. There are more inhibitors in different stages of clinical trials.