Table 1 Recent integrin-targeting drugs in clinical studies

Monoclonal antibodies

SAN-300

α 1β 1

RA

IV

Phase I

[114]

Vatelizumab

α2β1

MS and IBD

IV

Phase I

[115]

OS2966

β1

Glioma

Intratumoural infusion

Phase I

[116]

BG00011(STX-100)

αvβ6

IPF

SC

Phase II/I

[78]

Volociximab

α5β1

NSCLC and AMD

IV

Phase II

[117, 118]

Etaracizumab

αvβ3

Melanoma

SC

Phase II

[119]

Intetumumab

Pan-αv

Melanoma and prostate cancer

IV

Phase II

[120, 121]

Abituzumab

^Pan−αv

Colorectal cancer and melanoma

IV

Phase II

[122, 123]

Abrilumab

α4β7

UC

SC

Phase II

[124, 125]

VPI-2690B

αvβ3

Diabetic nephropathy

SC

Phase II

(http://www.vascularpharma.com/science/vpi-2690b)

ASP-5094

α 9β 1

RA

IV

Phase II

[126]

Natalizumab biosimilar

α4β1, α4β7

IBD

IV

Phase III

[127, 128]

Etrolizumab

α4β7, αEβ7

UC and Crohn’s

SC

Phase III

[129, 130]

Peptides

AXT-107

αvβ3, α5β1

DME, nAMD

Intravitreal Injection

Recruiting

[131]

PN-943

α4β7

UC

Oral

Recruiting

[129]

PTG-100

α4β7

UC

Oral

Phase II

[132]

ATN-161

α5β1

Cancer, Crohn’s and SARS-CoV-2

IV

Phase II ?

[133, 134]

Cilengitide

αvβ3, αvβ5

Glioblastoma

IV

Phase III

[135]

Small molecules

inhibitors

MK-0429

Pan−αv

MBD

Oral

Not mentioned

[136]

ELND-002

α4

MS

SC

Phase I

(https://adisinsight.springer.com/trials/700056998)

7HP-349

αLβ2, α4β1

Solid tumor

Oral

Phase I

[137]

GLPG-0187

Pan-αv, α5β1

Solid tumor

IV/Oral/SC

Phase I

[138]

GSK3008348

αvβ6

IPF

Inhalation

Phase I

[139]

THR-687

Pan-αv, α5β1

DME

Intravitreal injections

Phase I

(https://www.oxurion.com/content/oxurion-nv-expert-presentation-positive-topline-data-phase-1-study-evaluating-thr-687)

Firategrast

α4β1

MS and Crohn’s

Oral

Phase II

[140]

AXR-159

α4

DED

Topical

Phase II

(https://clinicaltrials.gov/ct2/show/NCT03598699?cond=AXR-159&draw=2&rank=1)

RO-0506997

α4

MS

Oral

Phase II

(https://adisinsight.springer.com/trials/700201021)

PLN-74809

αvβ1, αvβ6

IFP

Oral

Phase II

[141]

OT-166

αvβ3, αvβ6, αvβ8

AMD

Topical

Phase II

(https://www.businesswire.com/news/home/20171218005625/en/SciFluor-Announces-Positive-Top-Line-Results-Phase-12)

Risuteganib

αvβ3, αvβ5, α5β1

DME and dry agerelated macular degeneration

Intravitreal injections

Phase II

[142]

SAR-1118

αLβ2

DED and conjunctivitis

Topical

Phase II

[143]

MDL-819767

α4β1

Arthritis

Inhalation

Phase II

[144]

TRK-170

α4β7

Crohn’s

Oral

Phase II

(https://clinicaltrials.gov/ct2/show/NCT01345799)

RO-27–0608

α4

Asthma

Oral

Phase II

[145]

Zalunfiban

αIIbβ3

STEMI with PCI

SC

Phase III

[146]

AJM-300

α4

IBD, UC and Crohn’s

Oral

Phase III

[147]

Orbofiban

αIIbβ3

Thrombosis

Oral

Phase III

[148]