TABLE 3.

Therapeutic drugs and clinical trials for treatment of CKD by targeting TGF-β.

Drug and trials	Mechanisms	Disease	Drug administration and period	Results	Side effects	References
LY2382770
NCT01113801	TGF-β1	DN	Subcutaneous injection given monthly for 12 months	No efficacy on improvements in eGFR, Scr and proteinuria	Risk of toxicity and loss of renal efficacy	Voelker et al., 2017
Fresolimumab
NCT01665391	TGF-β1,2,3	FSGS	Administered intravenously at 1 mg/kg or 4 mg/kg for 112 days, followed double-blind for 252 days	No efficacy in proteinuria reduction; non-significant trend on eGFR decline	Herpes zoster; skin lesions, bleeding events and cancers	Vincenti et al., 2017
NCT00464321	TGF-β1,2,3	FSGS	Administered intravenously at one of four single-dose (0.3,1,2 and 4 mg/kg), followed for 112 days	Less eGFR decline (non-significant)	Pustular rash	Trachtman et al., 2011
Pirfenidone
NCT02689778	TGF-β1,2,3	DN	Administrated orally 600 mg with breakfast and 1200 mg with dinner for 12 months	Phase 3 ongoing	N/A
NCT00063583	TGF-β1,2,3	DN	Administered orally at a dose of 1200 mg or 2400 mg per day for 12 months	eGFRs increased significantly in the 1200 mg/d pirfenidone group compared with placebo	Gastrointestinal disorders, fatigue and photosensitivity rash	Sharma et al., 2011
NCT02408744	TGF-β1,2,3	CKD	Prolonged-released tablets, orally administered 2 time per day for 36 months	Phase 2 ongoing	N/A
NCT02530359	TGF-β1,2,3	Septic AKI	Pirfenidone extended release 600 mg per month every 12 h for 7 days	Phase 4 ongoing	N/A
NCT00001959	TGF-β1,2,3	FSGS	Orally administrated 3 times daily for 12 months	Improved eGFR decline; no effect on BP or proteinuria	Dyspepsia, sedation, and photosensitive dermatitis	Cho et al., 2007

DN, diabetic nephropathy; FSGS, focal and segmental glomerulosclerosis; CKD, chronic kidney disease; AKI, acute kidney disease.