Brand Name
Effient
Generic Name
Prasugrel
View Brand Information FDA approval date: July 12, 2017
Classification: P2Y12 Platelet Inhibitor
Form: Tablet
What is Effient (Prasugrel)?
Effient is a P2Y 12 platelet inhibitor indicated for the reduction of thrombotic cardiovascular events in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention as follows: Patients with unstable angina or non-ST-elevation myocardial infarction .
Approved To Treat
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Brand Information
Effient (Prasugrel Hydrochloride)
WARNING: BLEEDING RISK
- Effient can cause significant, sometimes fatal, bleeding
- Do not use Effient in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke
- In patients ≥75 years of age, Effient is generally not recommended, because of the increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk situations (patients with diabetes or a history of prior myocardial infarction [MI]) where its effect appears to be greater and its use may be considered
- Do not start Effient in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue Effient at least 7 days prior to any surgery
- Additional risk factors for bleeding include: body weight <60 kg, propensity to bleed, concomitant use of medications that increase the risk of bleeding (e.g
- Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of Effient
- If possible, manage bleeding without discontinuing Effient. Discontinuing Effient, particularly in the first few weeks after acute coronary syndrome, increases the risk of subsequent cardiovascular (CV) events
1DOSAGE AND ADMINISTRATION
Initiate Effient treatment as a single 60 mg oral loading dose and then continue at 10 mg orally once daily. Patients taking Effient should also take aspirin (75 mg to 325 mg) daily
2DOSAGE FORMS AND STRENGTHS
Effient 5 mg is available as a yellow, elongated hexagonal, film-coated, non-scored tablet debossed with "5121" on one side and 3 parallel arched lines followed by a "5" on the other side.
Effient 10 mg is available as a beige, elongated hexagonal, film-coated, non-scored tablet debossed with "5123" on one side and 3 parallel arched lines followed by a "10" on the other side.
3ADVERSE REACTIONS
The following serious adverse reactions are also discussed elsewhere in the labeling:
- Bleeding
- Thrombotic Thrombocytopenic Purpura
- Hypersensitivity Including Angioedema
3.1Clinical Trials Experience
Safety in patients with ACS undergoing PCI was evaluated in a clopidogrel-controlled study, TRITON-TIMI 38, in which 6741 patients were treated with Effient (60 mg loading dose and 10 mg once daily) for a median of 14.5 months (5802 patients were treated for over 6 months; 4136 patients were treated for more than 1 year). The population treated with Effient was 27 to 96 years of age, 25% female, and 92% Caucasian. All patients in the TRITON-TIMI 38 study were to receive aspirin. The dose of clopidogrel in this study was a 300 mg loading dose and 75 mg once daily.
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with the rates observed in other clinical trials of another drug and may not reflect the rates observed in practice.
3.2Postmarketing Experience
The following adverse reactions have been identified during post-approval use of Effient. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Blood and lymphatic system disorders — thrombocytopenia, thrombotic thrombocytopenic purpura (TTP) [see
Immune system disorders — hypersensitivity reactions including anaphylaxis [see
4DESCRIPTION
Effient contains prasugrel, a thienopyridine class inhibitor of platelet activation and aggregation mediated by the P2Y
Prasugrel hydrochloride is a white to practically white solid. It is soluble at pH 2, slightly soluble at pH 3 to 4, and practically insoluble at pH 6 to 7.5. It also dissolves freely in methanol and is slightly soluble in 1- and 2-propanol and acetone. It is practically insoluble in diethyl ether and ethyl acetate.
Effient is available for oral administration as 5 mg or 10 mg elongated hexagonal, film-coated, non-scored tablets, debossed on each side. Each yellow 5 mg tablet is manufactured with 5.49 mg prasugrel hydrochloride, equivalent to 5 mg prasugrel and each beige 10 mg tablet with 10.98 mg prasugrel hydrochloride, equivalent to 10 mg of prasugrel.
Other ingredients include mannitol, hypromellose, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, sucrose stearate, and glyceryl behenate. The color coatings contain lactose, hypromellose, titanium dioxide, triacetin, iron oxide yellow, and iron oxide red (only in Effient 10 mg tablet).
5CLINICAL STUDIES
The clinical evidence for the effectiveness of Effient is derived from the TRITON-TIMI 38 (
Patients with UA/NSTEMI presenting within 72 hours of symptom onset were to be randomized after undergoing coronary angiography. Patients with STEMI presenting within 12 hours of symptom onset could be randomized prior to coronary angiography. Patients with STEMI presenting between 12 hours and 14 days of symptom onset were to be randomized after undergoing coronary angiography. Patients underwent PCI, and for both UA/NSTEMI and STEMI patients, the loading dose was to be administered anytime between randomization and 1 hour after the patient left the catheterization lab. If patients with STEMI were treated with thrombolytic therapy, randomization could not occur until at least 24 hours (for tenecteplase, reteplase, or alteplase) or 48 hours (for streptokinase) after the thrombolytic was given.
Patients were randomized to receive Effient (60 mg loading dose followed by 10 mg once daily) or clopidogrel (300 mg loading dose followed by 75 mg once daily), with administration and follow-up for a minimum of 6 months (actual median 14.5 months). Patients also received aspirin (75 mg to 325 mg once daily). Other therapies, such as heparin and intravenous glycoprotein IIb/IIIa (GPIIb/IIIa) inhibitors, were administered at the discretion of the treating physician. Oral anticoagulants, other platelet inhibitors, and chronic NSAIDs were not allowed.
The primary outcome measure was the composite of cardiovascular death, nonfatal MI, or nonfatal stroke in the UA/NSTEMI population. Success in this group allowed analysis of the same endpoint in the overall ACS and STEMI populations. Nonfatal MIs included both MIs detected solely through analysis of creatine kinase muscle-brain (CK-MB) changes and clinically apparent (investigator-reported) MIs.
The patient population was 92% Caucasian, 26% female, and 39% ≥65 years of age. The median time from symptom onset to study drug administration was 7 hours for patients with STEMI and 30 hours for patients with UA/NSTEMI. Approximately 99% of patients underwent PCI. The study drug was administered after the first coronary guidewire was placed in approximately 75% of patients.
Effient significantly reduced total endpoint events compared to clopidogrel (see
The treatment effect of Effient was apparent within the first few days, and persisted to the end of the study (see
The Kaplan-Meier curves (see
Effient reduced the occurrence of the primary composite endpoint compared to clopidogrel in both the UA/NSTEMI and STEMI populations (see
The effect of Effient in various subgroups is shown in Figures 4 and 5. Results are generally consistent across pre-specified subgroups, with the exception of patients with a history of TIA or stroke
Effient is generally not recommended in patients ≥75 years of age, except in high-risk situations (diabetes mellitus or prior MI) where its effect appears to be greater and its use may be considered. These recommendations are based on subgroup analyses (see
There were 50% fewer stent thromboses (95% C.I. 32% - 64%; p<0.001) reported among patients randomized to Effient (0.9%) than among patients randomized to clopidogrel (1.8%). The difference manifested early and was maintained through one year of follow-up. Findings were similar with bare metal and drug-eluting stents.
In TRITON-TIMI 38, prasugrel reduced ischemic events (mainly nonfatal MIs) and increased bleeding events
6PATIENT COUNSELING INFORMATION
Advise the patient to read the FDA-approved patient labeling (Medication Guide).
7PRINCIPAL DISPLAY PANEL - 5 mg Tablet Bottle Label
30 Tablets
Effient
Rx only
5 mg
Keep and dispense only in original
Dispense accompanying
Cosette Pharmaceuticals, Inc.
8PRINCIPAL DISPLAY PANEL - 10 mg Tablet Bottle Label
30 Tablets
Effient
Rx only
10 mg
Keep and dispense only in original
Dispense accompanying
Cosette Pharmaceuticals, Inc.
