Table 3.

Clinical small molecules inhibitors targeting IKK complex in NF-κB pathway.

Drug	Originator/ Developer	Stage	Indication	Trail No.	Other Information
IKK α/β Inhibitors
CHS-828	Leo Pharma	Discontinued at phase 2	Solid tumor	NCT00003979	Originally Nicotinamide phosphoribosyl transferase (NAMPT) inhibitor. Dose-limiting toxicities; thrombosis, thrombocytopenia, esophagitis, diarrhea, and constipation [120].
IMD-1041 (Pro-drug of IMD-0354)	Institute of Medicinal Molecular Design	Phase 2	COPD	NCT00883584	No further development reported for COPD. Clinical phases for other indication unknown.
		NA	Age-related macular degeneration, DM, Glaucoma, PF	NA
SAR-113945	Sanofi	Discontinued at Phase 2	OA	NCT01598415	SAR-113945 gave as intra-articular injection. Phase 1 studies was promising but Phase 2b proof-of-concept study failed to show efficacy in a larger patient sample size [121].
		Discontinued at Phase 1	OA	NCT01113333, NCT01463488, NCT01511549
MLN-0415	Millennium Pharmaceuticals	Discontinued at Phase 1	Arthritis, Inflammation, MS	NA	Unfavorable safety profile in Phase 1.
VGX-1027	VGX Pharmaceuticals	Phase 1	Healthy subjects (RA)	NCT00627120	No development reported for RA or other diseases.
		Phase 1	Healthy subjects (RA)	NCT00760396
Teglarinad Chloride (EB-1627; GMX1777)	Leo Pharma	Phase 1	Malignant melanoma	NCT00724841,	Multi dose study conducted with combination of Temozolomide.
		Phase 1	Lymphoma, Solid tumors	NCT00457574	Single therapy was performed.
AS-602868	Merck	Discontinued at Phase 1	Hematological malignancies	NA	Also, inhibit FLT3.

Abbreviations: COPD—chronic obstructive pulmonary disease; DM—Diabetes mellitus; FLT3—FMS-like tyrosine kinase 3; MS—Multiple sclerosis; NA—not available; OA—osteoarthritis; PF—Pulmonary fibrosis; RA—rheumatoid arthritis.