The renin–angiotensin–aldosterone system (RAAS) is a major hormone pathway that regulates blood pressure and body fluid levels, and is involved in organ injuries. Angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), both of which block the downstream components of RAAS, are highly effective in controlling blood pressure and have organ protective effects, mainly on the heart and kidneys. Renin is a key upstream molecule of RAAS and its inhibition seems to result in more effective treatment than that of downstream components. However, the clinical application of a renin inhibitor is largely limited owing to the lack of efficacy.

Imarikiren (SCO-272, formerly TAK-272) is a long-acting renin inhibitor that shows excellent pharmacokinetic profiles in humans. Imarikiren has been shown to be effective in the treatment of hypertension, kidney diseases, and heart failure in preclinical studies. In addition, imarikiren sustains renin inhibition and decreases albuminuria in patients with type 2 diabetes.

These observations suggest that imarikiren is a novel drug candidate for the treatment of hypertension, kidney diseases, and heart failure. As imarikiren shows high water solubility, imarikiren is likely a new option for patients who require drug administration via injection.

Indication

  • Diabetic kidney disease
  • Hypertension
  • Change
  • Activation
  • Benefits
  • Inhibition
Angiotensinogen
Angiotensin Ⅰ
Angiotensin Ⅱ
ACE inhibitors
ACE
SCO-272
Renin
AT1 receptor
ARB
Hypertension

Hypertension

Renal dysfunction

Renal dysfunction

Heart failure

Heart failure

ACE : Angiotensin-converting enzyme

ARB : Angiotensin receptor blocker