Cangrelor Monograph for Professionals - Drugs.com

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# Cangrelor

Brand name: Kengreal
Drug class: Platelet-aggregation Inhibitors
Chemical name: N-[2-(Methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]-5′-adenylic acid monoanhydride with (dichloromethylene)bis[phosphonic acid] tetrasodium salt
Molecular formula: C17H21Cl2F3N5Na4O12P3S2
CAS number: 163706-36-3

Medically reviewed by Drugs.com on Dec 15, 2021. Written by ASHP.

## Introduction

Platelet-activation and -aggregation inhibitor; nonthienopyridine, reversible, P2Y12 platelet adenosine diphosphate (ADP)-receptor antagonist.

## Uses for Cangrelor

### Acute Ischemic Complications of PCI

Used as an adjunct to PCI to reduce the risk of periprocedural MI, repeat coronary revascularization, and stent thrombosis in patients who have not been treated with a P2Y12-receptor antagonist and are not being given a glycoprotein IIb/IIIa (GP IIb/IIIa) inhibitor.

Dual antiplatelet therapy with aspirin and a P2Y12 receptor inhibitor is considered the current standard of care in patients undergoing PCI.

Cangrelor is the only currently available IV P2Y12 receptor inhibitor. Compared with oral P2Y12 inhibitors (clopidogrel, prasugrel, ticagrelor), cangrelor has a rapid onset and offset of action; following an IV bolus dose, platelet inhibition is immediate and can be maintained with continuous IV infusion.

May be useful in patients who cannot take oral medications (e.g., intubated patients or those with shock, cardiac arrest, or nausea/vomiting) or patients who may benefit from a rapidly acting or reversible agent (e.g., those who have bleeding complications with PCI or are candidates for emergent invasive procedures such as CABG).

## Cangrelor Dosage and Administration

### General

- Intended to be given to patients prior to PCI in conjunction with other standard-of-care therapy (e.g., aspirin, anticoagulants).

### Administration

#### IV Administration

For solution and drug compatibility information, see Compatibility under Stability.

Must reconstitute commercially available lyophilized powder and further dilute prior to administration.

Administer by rapid IV (“bolus”) injection (over <1 minute) from the prepared IV infusion bag via manual IV push or infusion pump, followed by IV infusion.

##### Reconstitution

Reconstitute vial containing 50 mg of lyophilized cangrelor with 5 mL of sterile water for injection (swirl gently).

##### Dilution

Dilute reconstituted solution in 250 mL of 5% dextrose or 0.9% sodium chloride injection to a final concentration of 200 mcg/mL.

##### Rate of Administration

Rapid IV (“bolus”) injection: Administer over <1 minute.

Continuous IV infusion: Administer for at least 2 hours or for duration of PCI, whichever is longer.

### Dosage

Available as cangrelor tetrasodium; dosage expressed in terms of cangrelor.

#### Adults

##### Acute Ischemic Complications of PCI

###### IV

30 mcg/kg by rapid IV (“bolus”) injection prior to PCI, immediately followed by 4 mcg/kg per minute by continuous IV infusion for at least 2 hours or for the duration of the procedure, whichever is longer.

###### Transitioning to Oral Therapy

After discontinuance of cangrelor infusion, administer an oral P2Y12-receptor antagonist (clopidogrel, prasugrel, or ticagrelor) to maintain platelet inhibition.

If ticagrelor used, administer 180 mg any time during cangrelor infusion or immediately after discontinuance of the infusion.

If clopidogrel used, administer 600 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor. (See Specific Drugs under Interactions.)

If prasugrel used, administer 60 mg immediately after discontinuance of cangrelor infusion; do not administer concurrently with cangrelor. (See Specific Drugs under Interactions.)

### Special Populations

#### Renal Impairment

Dosage adjustment not required.

#### Hepatic Impairment

Dosage adjustment not required.

Detailed Cangrelor dosage information

## Cautions for Cangrelor

### Contraindications

- Substantial active bleeding.

- Known hypersensitivity to cangrelor or any ingredient in the formulation.

### Warnings/Precautions

#### Bleeding

Possible bleeding, especially hematoma at the site of vascular access. (See Contraindications.)

In pivotal clinical trial, greater incidence of bleeding events of all severities with cangrelor compared with clopidogrel; however, rate of severe bleeding (per the Global Use of Strategies to Open Occluded Coronary Arteries [GUSTO] criteria) not substantially different between treatment groups.

Antiplatelet effect negligible 1 hour after discontinuance of cangrelor infusion.

#### Sensitivity Reactions

##### Hypersensitivity

Hypersensitivity reactions (e.g., anaphylaxis, bronchospasm, angioedema, stridor) reported. (See Contraindications.)

#### Specific Populations

##### Pregnancy

No adequate and well-controlled studies of cangrelor in pregnant women. In animal studies, cangrelor produced dose-related fetal growth retardation and increased incidences of abortion and/or intrauterine losses, but did not produce malformations; not considered to be a teratogen.

##### Lactation

Not known whether cangrelor is distributed into human milk; discontinue nursing or the drug.

##### Pediatric Use

Safety and efficacy not established.

##### Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.

##### Renal Impairment

No dosage adjustment required; however, worsening renal function reported in some patients with severe renal impairment (Clcr <30 mL/minute) receiving cangrelor in clinical studies.

##### Hepatic Impairment

Safety and efficacy not established in patients with hepatic impairment. Hepatic impairment not expected to affect pharmacokinetics because metabolism not dependent on hepatic function.

### Common Adverse Effects

Bleeding; transient dyspnea reported in some patients.

## Interactions for Cangrelor

### Drugs Metabolized by Hepatic Microsomal Enzymes

Neither cangrelor nor its major metabolites inhibit activity of the hepatic CYP isoenzymes at therapeutic concentrations in vitro. Cangrelor not expected to interact with drugs metabolized by these microsomal enzymes.

### Specific Drugs

Drug | Interaction | Comments
--- | --- | ---
Aspirin | No effect on pharmacokinetics or pharmacodynamics of cangrelor |
Bivalirudin | No clinically detectable interactions |
Heparin | No effect on pharmacokinetics or pharmacodynamics of cangrelor |
Heparin, low molecular weight | No clinically detectable interactions |
Nitroglycerin | No effect on pharmacokinetics or pharmacodynamics of cangrelor |
Ticagrelor | Antiplatelet effect of ticagrelor 180 mg not substantially altered when given during cangrelor infusion | Administer ticagrelor at any time during or immediately after cangrelor infusion
Thienopyridines (clopidogrel, prasugrel) | Decreased antiplatelet effect of clopidogrel 600 mg or prasugrel 60 mg when given during cangrelor infusion | Do not administer clopidogrel or prasugrel until cangrelor infusion discontinued

Cangrelor drug interactions (more detail)

## Cangrelor Pharmacokinetics

### Absorption

#### Bioavailability

Peak plasma concentrations achieved within 2 minutes after administration of rapid IV (“bolus”) injection followed by continuous infusion.

#### Onset

Immediate antiplatelet effect.

#### Duration

Platelet function returns to normal within 1 hour after discontinuance of infusion.

### Distribution

#### Extent

Not known whether the drug is distributed into human milk.

#### Plasma Protein Binding

Approximately 97–98%.

### Elimination

#### Metabolism

Rapidly deactivated in circulation by dephosphorylation to its primary metabolite, which has negligible antiplatelet activity.

#### Elimination Route

Excreted in urine (58%) and feces (35%).

#### Half-life

3–6 minutes.

#### Special Populations

Pharmacokinetics not affected by gender, age, renal status, or hepatic function. Body weight has effect on pharmacokinetics but accounted for by weight-based infusion regimen.

## Stability

### Storage

#### Parenteral

##### Powder for Injection

20–25°C (may be exposed to 15–30°C).

Diluted IV solutions (200 mcg/mL) are stable at room temperature for up to 12 hours in 5% dextrose injection and 24 hours in 0.9% sodium chloride injection.

### Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

#### Parenteral

##### Solution Compatibility1

Compatible
Dextrose 5% in water
Sodium chloride 0.9%

## Actions

- Nonthienopyridine, direct-acting P2Y12 platelet ADP-receptor antagonist; unlike thienopyridines (e.g., clopidogrel, prasugrel), but like ticagrelor, cangrelor binds reversibly to P2Y12 receptor and does not require hepatic transformation to exert its pharmacologic effects.

- Prevents signal transduction of the cyclic adenosine monophosphate (cAMP) pathway, resulting in reduced exposure of fibrinogen binding sites to the GP IIb/IIIa complex and subsequent inhibition of platelet activation and aggregation.

- Compared with clopidogrel, cangrelor produces more rapid and effective inhibition of platelet aggregation and has a faster onset and offset of action.

## Advice to Patients

- Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

- Importance of patients informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant diseases.

- Importance of informing patients of other important precautionary information. (See Cautions.)

## Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Cangrelor Tetrasodium
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer
--- | --- | --- | --- | ---
Parenteral | For injection, for IV use | 50 mg (of cangrelor) | Kengreal | Chiesi

AHFS DI Essentials™. © Copyright 2023, Selected Revisions December 15, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

Reload page with references included

## More about cangrelor

- Check interactions
- Side effects
- Dosage information
- During pregnancy
- Drug class: platelet aggregation inhibitors

### Patient resources

- Advanced Reading
- Cangrelor

### Professional resources

#### Other brands

Kengreal

### Related treatment guides

- Percutaneous Coronary Intervention

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