Table 1.

Targeted therapies in clinical trials affecting STAT3 phosphorylation status

Name	Mechanism	Condition	Clinical Trial Phase	ClinicalTrials.gov Identifier	Preclinical effects on vascular function
Direct inhibition
STA-21	STAT3 SH2 domain inhibition	Psoriasis	Phase 1/27	NCT01047943	Not investigated
STAT3 DECOY	Disruption of STAT3-DNA interaction	Head and neck cancer	Phase 08	NCT00696176	Inhibition of tumour angiogenesis9
STATTIC	STAT3 SH2 domain inhibition		Preclinical		Inhibition of neointima formation,10 tumour angiogenesis,11 and vascular dysfunction12
S3I-201	STAT3 SH2 domain inhibition		Preclinical		Inhibition of tumour angiogenesis13 and vascular dysfunction12
Indirect inhibition by targeting STAT3 upstream signalling
Ruxolitinib	JAK1/2 inhibition	Myelofibrosis	FDA approved		Not investigated
Tocilizumab	IL-6 receptor antibody	Rheumatoid arthritis	FDA approved		Inhibition of tumour angiogenesis14
Tofacitinib	pan-JAK inhibition	Rheumatoid arthritis	FDA approveda		Inhibition of tumour angiogenesis15
AZD1480	JAK1/2 inhibition	Solid malignancies, primary myelofibrosis	Phase 1	NCT00910728, NCT01112397, NCT01219543	Inhibition of tumour angiogenesis16
sb1578	JAK2 inhibition	Rheumatoid arthritis	Phase 1	NCT01235871	Not investigated
WP1066	JAK2 inhibition	Brain cancer	Phase 1	NCT01904123	Inhibition of neointima formation17 and tumour angiogenesis,18 increased atherosclerotic plaque stability,19

^aTofacitinib is currently approved for the treatment of rheumatoid arthritis in the USA and Russia. It was not approved by the European regulatory agencies because of concerns over efficacy and safety.