ALISKIREN HEMIFUMARATE

EUEMA:by INNUSDailyMed:AliskirenUSFDA:Tekturna C in first trimesterD in second and third trimesters C09XA02(WHO)C09XA52(WHO) (withHCT) UK:POM(Prescription only)US:℞-only (2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide 173334-57-1Y 5493444 4812 DB01258Y 4591452N 502FWN4Q32 D03208Y CHEBI:601027N ChEMBL1639N C41 (PDBe,RCSB PDB) DTXSID40891494 Interactive image O=C(N)C(C)(C)CNC(=O)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)Cc1cc(OCCCOC)c(OC)cc1 InChI=1S/C30H53N3O6/c1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36/h10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35)/t22-,23-,24-,25-/m0/s1NKey:UXOWGYHJODZGMF-QORCZRPOSA-NN Aliskiren(brand namesTekturnaandRasilez) is the first in a class of drugs called directrenin inhibitors.‍​‍‍‍​‍‍‍‍‍‍‍‍​‍ It is used foressential (primary) hypertension.While used for high blood pressure, other better studied medications are typically recommended due to concerns of higher side effects and less evidence of benefit. In December 2011, Novartis halted a trial of the drug after discovering increased nonfatalstroke, kidney complications,high blood potassium, andlow blood pressurein people withdiabetesandkidney problems. As a result, in 2012: A new contraindication was added to the product label concerning the use of aliskiren withangiotensin receptor blockers(ARBs) orangiotensin-converting enzyme inhibitors(ACEIs) in patients with diabetes because of the risk of kidney impairment, low blood pressure, and high levels of potassium in the blood.A warning to avoid use of aliskiren with ARBs or ACEIs was also added for patients with moderate to severe kidney impairment (i.e., where glomerular filtration rate is less than 60 ml/min).Novartis decided to stop marketing Valturna (aliskiren/valsartan). Aliskiren was co-developed by the Swiss pharmaceutical companiesNovartisand Speedel.