Last reviewed 2026-04-20 · How we verify

Tekturna (ALISKIREN)

Tekturna works by blocking the renin enzyme, which is involved in the production of angiotensin II, a potent vasoconstrictor.

Tekturna (Aliskiren) is a small molecule renin inhibitor developed by Novartis and currently owned by Lxo Ireland. It targets the renin enzyme to treat hypertension. Approved by the FDA in 2007, Tekturna is a patented medication with a half-life of 24 hours and bioavailability of 2%. The drug is off-patent, with a generic manufacturer available. Key safety considerations include potential kidney damage and increased risk of stroke.

At a glance

Mechanism of action

Renin is secreted by the kidney in response to decreases in blood volume and renal perfusion. Renin cleaves angiotensinogen to form the inactive decapeptide angiotensin (Ang I). Ang is converted to the active octapeptide angiotensin II (Ang II) by angiotensin-converting enzyme (ACE) and non-ACE pathways. Ang II is powerful vasoconstrictor and leads to the release of catecholamines from the adrenal medulla and prejunctional nerve endings. It also promotes aldosterone secretion and sodium reabsorption. Together, these effects increase blood pressure. Ang II also inhibits renin release, thus providing negative feedback to the system. This cycle, from renin through angiotensin to aldosterone and its associated negative feedback loop, is known as the renin-angiotensin-aldosterone system (RAAS). Aliskiren is direct renin inhibitor, decreasing plasma renin activity (PRA) and inhibiting the conversion of angiotensinogen to Ang I. Whether aliskiren affects other RAAS c

Approved indications

• Hypertensive disorder

Boxed warnings

• WARNING: FETAL TOXICITY When pregnancy is detected, discontinue Tekturna as soon as possible. ( 5.1 , 8.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 , 8.1 ) WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. When pregnancy is detected, discontinue Tekturna as soon as possible. ( 5.1 , 8.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 , 8.1 )

Common side effects

• Diarrhea
• Cough
• Rash
• Elevated uric acid
• Gout
• Renal stones
• Angioedema
• Edema involving the face, hands or whole body
• Abdominal pain
• Dyspepsia
• Gastroesophageal reflux
• Headache

Drug interactions

• atorvastatin
• benazepril
• ciclosporin
• enalapril
• eprosartan
• fosinopril
• furosemide
• irbesartan
• itraconazole
• ketoconazole
• lisinopril
• losartan

Key clinical trials

• Evaluation of a Renin Inhibitor, Aliskiren, Compared to Enalapril, in C3 Glomerulopathy (PHASE2)
• Non-Inferiority Study of Aliskiren vs Losartan in the Treatment of Hypertension With Hyperuricemia (PHASE4)
• A Long Term Safety Study to Test the Combination of Aliskiren/ Amlodipine / Hydrochlorothiazide in Participants With Essential Hypertension (PHASE3)
• ACEI or ARB and COVID-19 Severity and Mortality in US Veterans
• Effect of Light Meal on Pharmacokinetic and Pharmacodynamics of Aliskiren in Patients With Mild to Moderate Hypertension (PHASE1)
• Pharmacokinetic and Pharmacodynamic Profiles of Aliskiren in Japanese Patients With Mild to Moderate Essential Hypertension (PHASE1)
• Efficacy and Tolerability of an Aliskiren-based Treatment Algorithm in Patients With Mild to Moderate Hypertension (PHASE4)
• Effect of Aliskiren and Hydrochlorothiazide on Kidney Oxygenation in Patients With Hypertension (PHASE4)

Patents

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Tekturna CI brief — competitive landscape report
• Tekturna updates RSS · CI watch RSS
• Lxo Ireland portfolio CI