Evidence & regulatory context
- Mechanism
- Direct renin inhibitor (target CHEMBL286, renin); action type INHIBITOR, direct interaction true, disease efficacy true. First-in-class, USAN stem -kiren. ATC C09XA02. Approved 2007; carries an FDA black box warning (fetal toxicity). ChEMBL max_phase 4.
- Target
- CHEMBL286
- Injury models
- Ischaemia-reperfusion · Chemical/toxin
- Reported indication
- Not recorded
- First approval
- 2007
- Development stage
- Not recorded
- ChEMBL record
- CHEMBL1639 ↗
- ChEMBL max phase
- 4 / 4 (development scale, not regulatory approval)
- Synonyms
- Aliskiren; Aliskirene; Aliskireno; Rasilez; Tekturna; SPP-100; SPP100
- Note
- Not recorded
Clinical trials 10
0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.
An 8-week Multicenter, Randomized, Double-blind, Active Controlled, Parallel Group, Forced Titration Study to Evaluate Aliskiren/Amlodipine/HCTZ Compared to Aliskiren/Amlodipine in US Minority Patients With Stage 2 Hypertension
Hypertension
Enrolment: 412 · Results not recorded
Effect of Aliskiren on Muscle Sympathetic Nerve Activity in Hypertensive Patients With Chronic Kidney Disease
Chronic Kidney Disease · Hypertension · Muscle Sympathetic Nerve Activity
Enrolment: 30 · Results not recorded
Effect of Aliskiren 300mg and Hydrochlorothiazide 25mg on Kidney Oxygenation in Patients With Stage 1 and 2 Hypertension: a BOLD-MRI Study
Hypertension
Enrolment: 24 · Results not recorded
Study of Triple Blockade of the Renin Angiotensin Aldosterone System in Diabetic (Type 1 and 2) Proteinuric Patients
Microalbuminuria · Macroalbuminuric Diabetic Nephropathy · Diabetes · Proteinuria · Albuminuria
Enrolment: 2 · Results not recorded
An 8-week Multi-center, Dose Escalation Study to Evaluate the Efficacy and Safety of Aliskiren (150 mg and 300 mg) Administered Alone and in Combination With Valsartan in Patients With Hypertension
Hypertension
Enrolment: 1797 · Results not recorded
A Twenty Six-week, Dose Titration Study to Evaluate the Efficacy and Safety of Aliskiren Compared to HCTZ With the Optional Addition of Amlodipine in Patients With Essential Hypertension
Hypertension
Enrolment: 976 · Results not recorded
An Eight-week Multicenter Study to Evaluate the Efficacy and Safety of the Combination of Aliskiren/HCTZ in Comparison With HCTZ 25 mg in Patients With Essential Hypertension
Hypertension
Enrolment: 726 · Results not recorded
Aliskiren Effect on Plaque Progression In Established Atherosclerosis Using High Resolution 3D MRI (ALPINE)
Atherosclerosis
Enrolment: 71 · Results not recorded
Interstitial and Tissue Concentrations of Aliskiren and Effects on the Renin-Angiotensin System in Fat and Skeletal Muscle of Hypertensive Patients With Abdominal Obesity
Hypertension · Abdominal Obesity
Enrolment: 46 · Results not recorded
Relative Bioavailability of Fixed Combination Aliskiren/Valsartan 75/160 mg Tablets vs Free Combination in Healthy Subjects
Healthy
Enrolment: 32 · Results not recorded
Preclinical evidence 2
2 studies reported at therapy level; 2 evidence entries itemised.
MouseIschaemia-reperfusionCerebral (MCAO/stroke)C57BL/6MaleIntragastric10 or 25 mg/kg per dayAfter transient middle cerebral artery occlusion
Model: Transient middle cerebral artery occlusion
Aliskiren significantly improved neurological deficit, infarct volume, brain water content and Nissl body counts without altering systemic blood pressure. Protection was associated with reduced apoptosis, increased phosphorylation of PI3K and AKT, higher Bcl-2 and lower Bax, and was reversed by the…
Extraction: extract · Subtype source: rule · Supplied extraction confidence: 0.75. Machine-extracted fields require source verification.
RatChemical/toxinWistarOral100 mg/kgPretreatment before doxorubicin challenge
Model: Doxorubicin-induced acute cardiotoxicity and nephrotoxicity, doxorubicin 15 mg/kg intraperitoneally as a single dose
Aliskiren 100 mg/kg orally for 14 days significantly prevented the doxorubicin-induced rises in angiotensin I, caspase-3, lactate dehydrogenase, malondialdehyde, urea and creatinine and the falls in albumin, total protein, glutathione and superoxide dismutase, and limited myocardial and renal ultra…
Extraction: extract · Supplied extraction confidence: 0.75. Machine-extracted fields require source verification.