Table 1.

Classification of hepcidin agonists

Hepcidin agonistsCompanyDrugTargetClinical trialsReference
Class 1: hepcidin mimetics University of California, Los Angeles MHs (PR65, PR73, M009, M012) Ferroportin Validated in preclinical studies See articles cited in the review 
 La Jolla Pharmaceutical Company LJPC-401 (hepcidin formulation) Ferroportin Phase 1: no toxicity reported; expected hypoferremia observed 45  
 Protagonist Therapeutics PTG-300 Ferroportin Phase 1: no serious adverse events reported; expected hypoferremia observed 58  
Class 2: stimulators of hepcidin production Ionis Pharmaceuticals Tmprss6-ASO Tmprss6 Phase 1 ongoing 59  
 Alnylam Pharmaceuticals Tmprss6-siRNA Tmprss6 Validated in preclinical studies See articles cited in the review 
Class 3: ferroportin inhibitors Vifor Pharma VIT-2763 Ferroportin Phase 1 planned in 2018 60  
Hepcidin agonistsCompanyDrugTargetClinical trialsReference
Class 1: hepcidin mimetics University of California, Los Angeles MHs (PR65, PR73, M009, M012) Ferroportin Validated in preclinical studies See articles cited in the review 
 La Jolla Pharmaceutical Company LJPC-401 (hepcidin formulation) Ferroportin Phase 1: no toxicity reported; expected hypoferremia observed 45  
 Protagonist Therapeutics PTG-300 Ferroportin Phase 1: no serious adverse events reported; expected hypoferremia observed 58  
Class 2: stimulators of hepcidin production Ionis Pharmaceuticals Tmprss6-ASO Tmprss6 Phase 1 ongoing 59  
 Alnylam Pharmaceuticals Tmprss6-siRNA Tmprss6 Validated in preclinical studies See articles cited in the review 
Class 3: ferroportin inhibitors Vifor Pharma VIT-2763 Ferroportin Phase 1 planned in 2018 60  

ASO, antisense oligonucleotide; siRNA, small-interfering RNA.

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