BETHESDA, MD 13 July 2009—Prasugrel, a thienopyridine, has been approved for reducing the rate of myocardial infarctions and strokes in patients with acute coronary syndrome who are undergoing a catheter-based procedure to reopen an occluded coronary artery, FDA announced July 10.
Daiichi Sankyo Inc. and Eli Lilly and Company will market the drug under the brand name Effient.
During and after a catheter-based procedure such as angioplasty, FDA said, platelets in the blood can aggregate around the procedure site. The resultant clumps can lead to myocardial infarction, stroke, and death.
Prasugrel reduces platelet aggregation through the action of the drug`s active metabolite. According to the labeling (PDF) for prasugrel, the active metabolite irreversibly binds to the P2Y12 class of receptors on platelets.
The labeling recommends that patients receive an initial 60-mg dose of prasugrel and then 10 mg once daily and also 75–325 mg of aspirin daily.
Clinicians are advised by the labeling to consider using a 5-mg/day maintenance dosage in patients weighing less than 60 kg, although the effectiveness and safety of this lower dosage was not studied prospectively. About 10% of patients weighing less than 60 kg who received a maintenance dosage of 10 mg/day in the major clinical study had a bleeding episode.
Patients with a previous transient ischemic attack or stroke or active pathological bleeding, such as peptic ulcer or intracranial hemorrhage, must not receive prasugrel.
The labeling for prasugrel includes a boxed warning that states the drug can cause "significant, sometimes fatal, bleeding." Risk factors for bleeding include age 75 years or older, coronary artery bypass graft surgery, body weight of less than 60 kg, propensity to bleed, and concomitant use of medications that increase the risk of bleeding.
In addition to bleeding, the most commonly reported adverse events in prasugrel-treated patients in a major clinical trial were hypertension, hyperlipidemia, headache, and back pain.
Effient will be available in 5- and 10-mg film-coated tablets. The 5-mg tablets will be packaged in 7- and 30-count bottles; the 10-mg tablets will come in 30-count bottles and 90-count blister packs.
According to a press release from Daiichi Sankyo and Lilly, the companies will start selling Effient in the United States "in the coming weeks."