BETHESDA, MD 09 October 2013—FDA on October 8 announced the approval of riociguat oral tablets to improve symptoms and prevent or delay loss of function in adults with certain types of pulmonary hypertension.
Riociguat is a soluble guanylate cyclase (sGC) stimulator and the first drug in this class with an approved indication for pulmonary hypertension, according to FDA.
for riociguat states that the drug affects the binding and action of nitric oxide (NO) in two ways, resulting in stimulation of the NO–sGC–cyclic guanosine monophosphate (cGMP) molecular pathway. This, in turn, leads to increased cGMP generation and improvements in vascular endothelial function, which is impaired in patients with pulmonary hypertension.
Riociguat will be marketed as Adempas by Bayer HealthCare Pharmaceuticals and will begin shipping the drug as early as today, a company spokeswoman said.
Labeling for riociguat states that it is indicated to improve exercise capacity and activity level in patients with persistent recurrent or chronic thromboembolic pulmonary hypertension (CTEPH) after surgical treatment or if surgery is not an option.
The drug is also indicated to improve exercise capacity and activity level and delay clinical worsening of pulmonary arterial hypertension.
According to FDA, riociguat is the only agency-approved drug that has been shown to be effective in patients with CTEPH, which is characterized by clots in pulmonary blood vessels.
Concomitant administration of riociguat and nitrates, nitric oxide donors, or phosphodiesterase inhibitors is contraindicated.
The recommended starting dosage of riociguat is 1 mg taken three times daily, but therapy may be initiated at 0.5 mg three times daily if the patient is unlikely to tolerate the drug's hypotensive effects. Doses may be increased in 0.5-mg increments up to a maximum of 2.5 mg taken three times daily, if tolerated. At least two weeks should lapse between dose increases.
The labeling states that dosage levels above 2.5 mg three times daily may be considered, if tolerated, for patients who smoke. A lower dose may be required if a patient quits smoking.
Labeling for riociguat includes a medication guide and a boxed warning describing the risk of fetal harm if a woman takes the drug during pregnancy.
A risk evaluation and mitigation strategy (REMS) program has been developed for all women who take the drug. According to FDA, the REMS program includes a restricted distribution program and mandatory prescriber and pharmacy certification.
In clinical trials, the adverse events reported most often by patients receiving riociguat included headache, dizziness, gastrointestinal symptoms, and anemia. Rare but serious bleeding episodes, including a fatal incident of hemoptysis, also occurred during the clinical studies.
Riociguat will be available in 90-tablet bottles and 42-tablet blister packs in 0.5-, 1.0, 1.5-, 2.0-, and 2.5-mg strengths. The tablets should be stored at controlled room temperature.