Brand name (Active ingredient/route of administration) | Types of molecule | Signs | Year of approval/sponsor/review classification | Chemical class | Major drug metabolizing enzyme(s) | Target | ROE |
---|---|---|---|---|---|---|---|
Uptravi (Selexipag/PO) | Small molecules | PAH | 2015/Actelion/S, O | Organonitrogen compounds | Carboxylesterases, CYP2C8, CYP3A4 | Prostacyclin receptor agonist | 93% in feces and only 12% in urine |
Entresto (Selexipag/PO) | Small molecules | Heart failure | 2015/Novartis/P | Benzene and substituted derivatives | Esterase | Neprilysin inhibitor | Urine (50–70%) |
Entresto (Valsartan/PO) | Carboxylic acids and derivatives | Minimal metabolism | Angiotensin II receptor blocker | Feces (86%) | |||
Kengreal (Cangrelr/IV) | Small molecules | Avoid blood clots | 2015/Medicines company/S | Purine nucleotide | Dephosphorylation | P2Y12 platelet inhibitor | 58% via urine, 35% feces |
Corlanor (Ivabradine/PO) | Small molecule | Heart failure | 2015/Amgen/P | Benzazepines | CYP3A4 | HCN-channels inhibitor | Feces (50%) and Urine (50%) |
Savaysa (Edoxaban/PO) | Small molecule | Systemic embolism | 2015/Daiichi/Sankyo/S | Carboxylic acids and derivatives | Carboxylesterase I | Factor Xa inhibitor | Feces (50%) and urine (50%) |
Praxbind (Idarucizumab/IV) | Antibody fragment | Reverse Pradaxa’s blood thinning effects | 2015/BoehringerIngelheim/P, O, A, B | Fab derived from an IgG2 | Hydrolytic Enzymes | Binds to dabigatran | Similar to endogenous IgG |
Repathan (Evolocumab/SC) | Monoclonal antibody | High cholesterol | 2015/Amgen/S, O | Humanized IgG2 | Hydrolytic Enzymes | PCSK9 inhibitor | Similar to endogenous IgG |
Praluent (Alirocumab/SC) | Monoclonal antibody | High cholesterol | 2015/Sanofi/P | Humanized IgG1 | Hydrolytic Enzymes | PCSK9 inhibitor | Similar to endogenous IgG |
Defitelio (Defibrotide sodium/IV) | Oligonucleotide | Hepatic venoocclusive disease | 2016/Gentium/P, O | Single-stranded oligodeoxyribonucleotides | Nucleases | Increase levels of Prostaglandin I2, E2 and prostacyclin | NA |
Bevyxxa (Betrixaban/PO) | Small molecule | Venous thromboembolism | 2017/Portola pharma/P | Anilids | Predominantly remain unchanged | Factor Xa inhibitor | 85% feces and 11% urine |
Hemlibra (Emicizumab/SC) | Monoclonal antibody | Hemophilia A | 2017/Roche/Genetech/P, O, B | Humanized IgG4 | Hydrolytic Enzymes | Factor Ixa and X inhibitor | Similar to endogenous IgG |
Giapreza (Angiotensin II/IV) | Small molecule | Septic or other shocks | 2017/La Jolla pharma/P | Amino acids, peptides and analogues | Aminopeptidase A and ACE2 to angiotensin | Angiotensin II agonist | NA |
Vyndaqel (Tafamidis meglumine/PO) | Small molecule | Cardiomyopathy | 2019/Pfizer/Foldrx/P, O, B | Benzoxazole derivatives | Glucuronidation | Transthyretin stabilizers | 59% feces and 22% urine |
Cablivi (Caplacizumab-yhdp/IV or SC) | Antibody fragment | Acquired thrombotic thrombocytopenic purpura | 2019/Sanofi/Ablynx/P, O | Vwf-directed Fab | Hydrolytic Enzymes | A1-domain of vWF | Similar to endogenous IgG |
Nexletol (Bempedoic acid/PO) | Small molecule | Familial hypercholesterolemia | 2020/Esperion/S | Fatty acids and conjugates | Glucuronidation | Adenosine triphosphate citrate lyase inhibitor | NA |