Biological Activity

• Target

  Renin IC50:1.5nM

• DescriptionAliskiren is an orally active renin inhibitor with IC50 value of 0.6nM, used as antihypertensive drugs that block the first step in the renin–angiotensin system, which can interrupt the negative feedback effects of angiotensin II on renin secretion. Administration of Aliskiren at dose of 150mg alone significantly inhibited plasma renin activity by 65% in patients with hypertension. Inhibition of renin by Aliskiren in combinations with hydrochlorothiazide, ramipril, or irbesartan increased renin–angiotensin system suppression, improved 24-hour blood pressure control.
• MechanismAliskiren interacts with several binding pockets in distinct regions around the active site of renin.^[2]

• Animal Study
  Dose	Rat: 3 mg/kg - 30 mg/kg[4] (s.c.); 10 mg/kg[4] (i.v.); 1 mg/kg - 30 mg/kg[5] (p.o.), 200 mg/kg[6] (p.o.) Mice: 25 mg/kg[7] (osmotic minipump) Mice: 3 mg/kg - 25 mg/kg[8] (s.c.)
  Administration	s.c., i.v.
  Pharmacokinetics	Animal Rats[9] Dose 100 mg/kg (p.o.) 10 mg/kg (i.v.) Administration p.o. i.v. F 2.4% (p.o.) T1/2 23.1 h (i.v.) Cmax 0.27 μmol/L (p.o.) 29.20 μmol/L (i.v.) AUC 3.01 μmol·h/L (p.o.) 12.60 μmol·h/L (i.v.) Tmax 0.25 h (p.o.) 0.083 h (i.v.) Vss 7.8 L/kg (i.v.) CL 1.2 L/h/kg (i.v.)

• Clinical Study

• NCT Number	Condition or disease	Phase	Recruitment Status	Estimated Study Completion Date	Locations
  NCT00865020	-	-	Completed	-	-
  NCT00841672	Moderate to Severe Hypertensio... more >>n Collapse <<	Phase 3	Completed	-	Germany ... more >> Investigative Site Berlin, Germany Philippines Investigative Site Manilla, Philippines Romania Investigative Site Bucharest, Romania Russian Federation Investigative Site Moscow, Russian Federation Singapore Investigative Site Singapore, Singapore Spain Investigative Site Madrid, Spain Collapse <<
  NCT00841672	-	-	Completed	-	-

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