DRUG INTERACTIONS-(summary)

 Clopidogrel: Do not administer during KENGREAL infusion. 

DRUG INTERACTIONS- (details)-

1 Thienopyridines If clopidogrel or prasugrel are administered during KENGREAL infusion, they will have no antiplatelet effect until the next dose is administered. Clopidogrel and prasugrel, therefore, should not be administered until KENGREAL infusion is discontinued

PRODUCT DETAILS 

Name of the drug-   KENGREAL

Active ingriendents-    Cangrelor

FDA approved use-    To prevent the formation of harmful blood clots in the coronary                                                arteries for adult patients undergoing coronary intervention

Date of Approval         6/22/2015

HIGHLIGHTS OF PRESCRIBING INFORMATION-

These highlights do not include all the information needed to use                              KENGREAL safely and effectively.

See full prescribing information for KENGREAL. KENGREAL™ (cangrelor) for injection, for intravenous use

Initial U.S. Approval: 2015-

 INDICATIONS AND USAGE -

 KENGREAL is a P2Y12 platelet inhibitor indicated as an adjunct to percutaneous coronary intervention (PCI) for reducing the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients in who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor

ADVERSE REACTIONS-

 The most common adverse reaction is bleeding

CONTRAINDICATIONS-

 Significant active bleeding

Hypersensitivity to KENGREAL or any component of the product (4.2)

WARNINGS AND PRECAUTIONS-

 Bleeding: Like other drugs that inhibit platelet P2Y12 function, KENGREAL can increase the risk of bleeding

DOSAGE AND ADMINISTRATION-

 KENGREAL is intended for administration via a dedicated IV line, only after reconstitution and dilution.

 Administer 30 µg/kg intravenous (IV) bolus prior to PCI followed immediately by a 4 µg/kg/min IV infusion for at least 2 hours or duration of procedure, whichever is longer.

 To maintain platelet inhibition after discontinuation of KENGREAL infusion, an oral P2Y12 platelet inhibitor should be administered.

 DOSAGE FORMS AND STRENGTHS-

 Single-use 10 mL vial containing 50 mg KENGREAL as a lyophilized powder for reconstitution

OVERDOSAGE -

There is no specific treatment to reverse the antiplatelet effect of KENGREAL but the effect is gone within one hour after the drug is discontinued.

In clinical trials, 36 patients received an overdose of KENGREAL, ranging from 36 to 300 mcg/kg (bolus dose) or 4.8 to 13.7 mcg/kg/min (infusion dose).

The maximum overdose received was 10 times the PCI bolus dose or 3.5 times the PCI infusion dose in 4 patients. No clinical sequela were noted as a result of overdose following completion of KENGREAL therapy.

HOW SUPPLIED/STORAGE AND HANDLING-

KENGREAL is supplied as a sterile lyophilized powder in single use 10 mL vials.

 10 mL vial containing 50 mg cangrelor

 10 count of 10 mL vials containing 50 mg cangrelor Vials of KENGREAL should be stored at USP Controlled Room Temperature, [20°C to 25°C (68°F to 77°F) with excursions between 15°C and 30°C (59°F and 86°F) permitted].

Distributed by: The Medicines Company Parsippany, NJ 07054

3 Pharmacokinetics-

KENGREAL administered intravenously has linear pharmacokinetics in both healthy volunteers and patients. KENGREAL is rapidly distributed and metabolized, reaching Cmax within 2 minutes after administration of an intravenous bolus followed by infusion.

Distribution-

In a study in healthy volunteers, KENGREAL administration at a dose of 30 mcg/kg bolus plus 4 mcg/kg/min showed a volume of distribution of 3.9 L. Plasma protein binding of KENGREAL is about 97-98%.

Metabolism-

 KENGREAL is deactivated rapidly in the circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible anti-platelet activity. KENGREAL’s metabolism is independent of hepa

 USE IN SPECIFIC POPULATIONS

1. Pregnancy-                                                                                                             Pregnancy Category C-                                                                                                  There are no adequate and well-controlled studies of KENGREAL in pregnant women. Cangrelor did not produce malformations in either the rat or rabbit reproductive studies, and is not considered to be a teratogen.

In embryo-fetal development studies in rats, cangrelor produced dose-related fetal growth retardation characterized by increased incidences of incomplete ossification and unossified hind limb metatarsals at plasma concentration of approximately 5 times lower than that achieved in the PCI setting at the maximum recommended human dose (MRHD). In rabbits, cangrelor was associated with increased incidences of abortion and intrauterine losses, as well as fetal growth retardation at plasma concentrations of approximately 12 times higher than the PCI setting at the MRHD.

2.Nursing Mothers-

 It is not known whether KENGREAL is excreted in human milk.

3. Pediatric Use-                                                                                                               Safety and effectiveness in pediatric patients have not been established. 

4. Geriatric Use-                                                                                                                In CHAMPION PHOENIX, 18% of patients were =75 years. No overall differences in safety or effectiveness were observed between these patients and those patients <75 years 

5.Renal Impairment-                                                                                                          No dosage adjustment is required for patients with mild, moderate, or severe renal impairment

6. Hepatic Impairment-                                                                                                 KENGREAL has not been studied in patients with hepatic impairment. However, the metabolism of KENGREAL is not dependent of hepatic function, so that dosage adjustment is not required for patients with hepatic impairment

OVERDOSAGE-                                                                                                                       There is no specific treatment to reverse the antiplatelet effect of KENGREAL but the effect is gone within one hour after the drug is discontinued.

In clinical trials, 36 patients received an overdose of KENGREAL, ranging from 36 to 300 mcg/kg (bolus dose) or 4.8 to 13.7 mcg/kg/min (infusion dose).

The maximum overdose received was 10 times the PCI bolus dose or 3.5 times the PCI infusion dose in 4 patients.

No clinical sequela were noted as a result of overdose following completion of KENGREAL therapy.