Vericiguat, sold under the brand name Verquvo, is a medication used to reduce the risk of cardiovascular death and hospitalization in certain patients with heart failure after a recent acute decompensation event.
Pregnancy category AU: D
Routes of administration By mouth
Drug class Soluble guanylate cyclase activator
Common side effects include low blood pressure and anemia.
Considers it to be a first-in-class medication.
Vericiguat is indicated to reduce the risk of cardiovascular death and hospitalization for heart failure following a prior hospitalization for heart failure or need for outpatient intravenous diuretics, in adults with symptomatic chronic heart failure and an ejection fraction of less than 45%.
Vericiguat is usually given orally once every day with food.
No dose adjustments are required in the elderly, in people with mild-to-moderate liver failure, or in those with impaired kidney function.
It is contraindicated in pregnancy.
Animals studies suggest higher rates of birth defects, as well as increased number of abortions and resorptions.
It may also pass into breast milk, but the effects on breastfed infants is unknown.
Vericiguat is a direct stimulator of soluble guanylate cyclase, an important enzyme in vascular smooth muscle cells.
Specifically, vericiguat binds to the beta-subunit of the target site on the soluble guanylate cyclase enzyme.
Soluble guanylate cyclase catalyzes the formation of cyclic GMP upon interaction with nitric oxide, activating a number of downstream signaling cascades, which can compensate for defects in this pathway and resulting losses in regulatory myocardial and vascular cellular processes due to cardiovascular complications.
After vericiguat is administered 100 mg by mouth once daily, with a Tmax of one hour.
Vericiguat is an advised to consume food with the drug for an oral bioavailability of 93%.
It is extensively protein bound in plasma.
Vericiguat is primarily metabolized via conjugation reactions, with a minor CYP-mediated oxidative metabolite.
The major metabolite is glucuronidated and inactive.
The typical half-life profile for patients with heart failure is 30 hours.
Vericiguat has a decreased clearance in patients with systolic heart failure.