Ticagrelor
Tablet · Oral
Uses
Ticagrelor tablets are a P2Y 12 platelet inhibitor indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI. For at least the first 12 months following ACS, it is superior to clopidogrel. Ticagrelor tablets also reduces the risk of stent thrombosis in patients who have been stented for treatment of ACS. (1.1) to reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events. While use is not limited to this setting, the efficacy of ticagrelor tablets were established in a population with type 2 diabetes mellitus (T2DM). (1.2) to reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score ≤ 5) or high-risk transient ischemic attack (TIA). ( 1.3 ) 1.1 Acute Coronary Syndrome or a History of Myocardial Infarction Ticagrelor tablets are indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI. For at least the first 12 months following ACS, it is superior to clopidogrel. Ticagrelor tablets also reduces the risk of stent thrombosis in patients who have been stented for treatment of ACS [see Clinical Studies (14.1) ] . 1.2 Coronary Artery Disease but No Prior Stroke or Myocardial Infarction Ticagrelor tablets are indicated to reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events [see Clinical Studies (14.2) ] . While use is not limited to this setting, the efficacy of ticagrelor tablets were established in a population with type 2 diabetes mellitus (T2DM). 1.3 Acute Ischemic Stroke or Transient Ischemic Attack (TIA) Ticagrelor tablets are indicated to reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score ≤ 5) or high-risk transient ischemic attack (TIA) [see Clinical Studies (14.3) ] .
Dosage and administration
2 DOSAGE AND ADMINISTRATION ACS or History of MI Initiate treatment with 180 mg oral loading dose of ticagrelor tablets. Then administer 90 mg twice daily during the first year. After one year, administer 60 mg twice daily. ( 2.2 ) Patients with CAD and No Prior Stroke or MI Administer 60 mg ticagrelor tablets twice daily. ( 2.3 ) Acute Ischemic Stroke Initiate treatment with a 180 mg loading dose of ticagrelor tablets then continue with 90 mg twice daily for up to 30 days. ( 2.4 ) Use ticagrelor tablets with a daily maintenance dose of aspirin of 75 mg to 100 mg. ( 2 ) However, in patients who have undergone PCI, consider single antiplatelet therapy with ticagrelor tablets based on the evolving risk for thrombotic versus bleeding events. ( 2.2 ) 2.1 General Instructions Advise patients who miss a dose of ticagrelor tablets to take their next dose at its scheduled time. For patients who are unable to swallow tablets whole, ticagrelor tablets can be crushed, mixed with water, and drunk. The mixture can also be administered via a nasogastric tube (CH8 or greater) [see Clinical Pharmacology (12.3) ] . Do not administer ticagrelor tablets with another oral P2Y 12 platelet inhibitor. Avoid aspirin at doses higher than recommended [see Clinical Studies (14.1) ] . 2.2 Acute Coronary Syndrome or a History of Myocardial Infarction Initiate treatment with a 180 mg loading dose of ticagrelor tablets. Administer the first 90 mg maintenance dose of ticagrelor tablets, 6 to 12 hours after the loading dose. Administer 90 mg of ticagrelor tablets twice daily during the first year after an ACS event. After one year, administer 60 mg of ticagrelor tablets twice daily. Initiate ticagrelor tablets with a daily maintenance dose of aspirin of 75 mg to 100 mg. However, in patients who have undergone percutaneous coronary intervention (PCI), consider single antiplatelet therapy with ticagrelor tablets based on the evolving risk for thrombotic versus bleeding events [see Warnings and Precautions (5.1) and Clinical Studies (14) ] . 2.3 Coronary Artery Disease but No Prior Stroke or Myocardial Infarction Administer 60 mg of ticagrelor tablets twice daily. Generally, use ticagrelor tablets with a daily maintenance dose of aspirin of 75 mg to 100 mg [see Clinical Studies (14) ] . 2.4 Acute Ischemic Stroke or Transient Ischemic Attack (TIA) Initiate treatment with a 180 mg loading dose of ticagrelor tablets and then continue with 90 mg twice daily for up to 30 days. Administer the first maintenance dose 6 to 12 hours after the loading dose. Use ticagrelor tablets with a loading dose of aspirin (300 mg to 325 mg) and a daily maintenance dose of aspirin of 75 mg to 100 mg [see Clinical Studies (14) ] .
Dosage forms and strengths
Ticagrelor tablets 60 mg are supplied as light pink, round shaped, film coated tablets debossed with “521” on one side and “SG” on the other side. Ticagrelor tablets 90 mg are supplied as yellow, round shaped, film coated tablets debossed with “522” on one side and “SG” on the other side. 60mg and 90 mg tablets. ( 3 )
Contraindications
History of intracranial hemorrhage. ( 4.1 ) Active pathological bleeding. ( 4.2 ) Hypersensitivity to ticagrelor or any component of the product. ( 4.3 ) 4.1 History of Intracranial Hemorrhage Ticagrelor tablets are contraindicated in patients with a history of intracranial hemorrhage (ICH) because of a high risk of recurrent ICH in this population [see Clinical Studies (14.1) , (14.2) ] . 4.2 Active Bleeding Ticagrelor tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . 4.3 Hypersensitivity Ticagrelor tablets are contraindicated in patients with hypersensitivity (e.g., angioedema) to ticagrelor or any component of the product.
Warnings and precautions
Dyspnea was reported more frequently with ticagrelor than with control agents in clinical trials. Dyspnea from ticagrelor is self-limiting. ( 5.3 ) Severe Hepatic Impairment: Likely increase in exposure to ticagrelor. ( 5.5 ) Laboratory Test Interference: False negative platelet functional test results have been reported for Heparin Induced Thrombocytopenia (HIT). Ticagrelor is not expected to impact PF4 antibody testing for HIT. ( 5.7 ) 5.1 Risk of Bleeding Drugs that inhibit platelet function including ticagrelor increase the risk of bleeding [see Warnings and Precautions (5.2) and Adverse Reactions (6.1) ]. Patients treated for acute ischemic stroke or TIA Patients at NIHSS > 5 and patients receiving thrombolysis were excluded from THALES and use of ticagrelor in such patients is not recommended. 5.2 Discontinuation of Ticagrelor in Patients Treated for Coronary Artery Disease Discontinuation of ticagrelor will increase the risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease. If ticagrelor must be temporarily discontinued (e.g., to treat bleeding or for significant surgery), restart it as soon as possible. When possible, interrupt therapy with ticagrelor for five days prior to surgery that has a major risk of bleeding. Resume ticagrelor as soon as hemostasis is achieved. 5.3 Dyspnea In clinical trials, about 14% (PLATO and PEGASUS) to 21% (THEMIS) of patients treated with ticagrelor developed dyspnea. Dyspnea was usually mild to moderate in intensity and often resolved during continued treatment but led to study drug discontinuation in 0.9% (PLATO), 1.0% (THALES), 4.3% (PEGASUS), and 6.9% (THEMIS) of patients. In a substudy of PLATO, 199 subjects underwent pulmonary function testing irrespective of whether they reported dyspnea. There was no indication of an adverse effect on pulmonary function assessed after one month or after at least 6 months of chronic treatment. If a patient develops new, prolonged, or worsened dyspnea that is determined to be related to ticagrelor, no specific treatment is required; continue ticagrelor without interruption if possible. In the case of intolerable dyspnea requiring discontinuation of ticagrelor, consider prescribing another antiplatelet agent. 5.4 Bradyarrhythmias Ticagrelor can cause ventricular pauses [see Adverse Reactions (6.1) ] . Bradyarrhythmias including AV block have been reported in the post-marketing setting. Patients with a history of sick sinus syndrome, 2 nd or 3 rd degree AV block or bradycardia-related syncope not protected by a pacemaker were excluded from clinical studies and may be at increased risk of developing bradyarrhythmias with ticagrelor. 5.5 Severe Hepatic Impairment Avoid use of ticagrelor in patients with severe hepatic impairment. Severe hepatic impairment is likely to increase serum concentration of ticagrelor. There are no studies of ticagrelor patients with severe hepatic impairment [see Clinical Pharmacology (12.3) ] . 5.6 Central Sleep Apnea Central sleep apnea (CSA) including Cheyne-Stokes respiration (CSR) has been reported in the post-marketing setting in patients taking ticagrelor, including recurrence or worsening of CSA/CSR following rechallenge. If central sleep apnea is suspected, consider further clinical assessment. 5.7 Laboratory Test Interferences False negative functional tests for Heparin Induced Thrombocytopenia (HIT) Ticagrelor has been reported to cause false negative results in platelet functional tests (including the heparin-induced platelet aggregation (HIPA) assay) for patients with Heparin Induced Thrombocytopenia (HIT). This is related to inhibition of the P2Y 12 -receptor on the healthy donor platelets in the test by ticagrelor in the affected patient’s serum/plasma. Information on concomitant treatment with ticagrelor is required for interpretation of HIT functional tests. Based on the mechanism of ticagrelor interference, ticagrelor is not expected to impact PF4 antibody testing for HIT.
Side effects
The following adverse reactions are also discussed elsewhere in the labeling: Bleeding [see Warnings and Precautions (5.1) ] Dyspnea [see Warnings and Precautions (5.3) ] Most common adverse reactions (> 5%) are bleeding and dyspnea. ( 5.1 , 5.3 , 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ScieGen Pharmaceuticals, Inc. at (1-855-724-3436) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Ticagrelor has been evaluated for safety in more than 58,000 patients. Bleeding in PLATO (Reduction in risk of thrombotic events in ACS) Figure 1 is a plot of time to the first non-CABG major bleeding event. Figure 1: Kaplan-Meier estimate of time to first non-CABG PLATO-defined major bleeding event (PLATO) Frequency of bleeding in PLATO is summarized in Tables 1 and 2. About half of the non-CABG major bleeding events were in the first 30 days. Table 1: Non-CABG related bleeds (PLATO) Ticagrelor * N=9,235 Clopidogrel N=9,186 n (%) patients with event n (%) patients with event PLATO Major + Minor 713 (7.7) 567 (6.2) Major 362 (3.9) 306 (3.3) Fatal/Life-threatening 171 (1.9) 151 (1.6) Fatal 15 (0.2) 16 (0.2) Intracranial hemorrhage (Fatal/Life-threatening) 26 (0.3) 15 (0.2) PLATO Minor bleed: requires medical intervention to stop or treat bleeding. PLATO Major bleed: any one of the following: fatal; intracranial; intrapericardial with cardiac tamponade; hypovolemic shock or severe hypotension requiring intervention; significantly disabling (e.g., intraocular with permanent vision loss); associated with a decrease in Hb of at least 3 g/dL (or a fall in hematocrit (Hct) of at least 9%); transfusion of 2 or more units. PLATO Major bleed, fatal/life-threatening: any major bleed as described above and associated with a decrease in Hb of more than 5 g/dL (or a fall in hematocrit (Hct) of at least 15%); transfusion of 4 or more units. Fatal: A bleeding event that directly led to death within 7 days. * 90 mg BID No baseline demographic factor altered the relative risk of bleeding with ticagrelor compared to clopidogrel. In PLATO, 1,584 patients underwent CABG surgery. The percentages of those patients who bled are shown in Figure 2 and Table 2. Figure 2: ‘Major fatal/life-threatening’ CABG-related bleeding by days from last dose of study drug to CABG procedure (PLATO) X-axis is days from last dose of study drug prior to CABG. The PLATO protocol recommended a procedure for withholding study drug prior to CABG or other major surgery without unblinding. If surgery was elective or non-urgent, study drug was interrupted temporarily, as follows: If local practice was to allow antiplatelet effects to dissipate before surgery, capsules (blinded clopidogrel) were withheld 5 days before surgery and tablets (blinded ticagrelor) were withheld for a minimum of 24 hours and a maximum of 72 hours before surgery. If local practice was to perform surgery without waiting for dissipation of antiplatelet effects capsules and tablets were withheld 24 hours prior to surgery and use of aprotinin or other hemostatic agents was allowed. If local practice was to use IPA monitoring to determine when surgery could be performed both the capsules and tablets were withheld at the same time and the usual monitoring procedures followed. T = Ticagrelor; C = Clopidogrel. Table 2: CABG-related bleeding (PLATO) Ticagrelor * N=770 Clopidogrel N=814 n (%) patients with event n (%) patients with event PLATO Total Major 626 (81.3) 666 (81.8) Fatal/Life-threatening 337 (43.8) 350 (43.0) Fatal 6 (0.8) 7 (0.9) PLATO Major bleed: any one of the following: fatal; intracranial; intrapericardial with cardiac tamponade; hypovolemic shock or severe hypotension requiring intervention; significantly disabling (e.g., intraocular with permanent vision loss); associated with a decrease in Hb of at least 3 g/dL (or a fall in hematocrit (Hct) of at least 9%); transfusion of 2 or more units. PLATO Major bleed, fatal/life-threatening: any major bleed as described above and associated with a decrease in Hb of more than 5 g/dL (or a fall in hematocrit (Hct) of at least 15%); transfusion of 4 or more units. * 90 mg BID When antiplatelet therapy was stopped 5 days before CABG, major bleeding occurred in 75% of ticagrelor treated patients and 79% on clopidogrel. Other Adverse Reactions in PLATO Adverse reactions that occurred at a rate of 4% or more in PLATO are shown in Table 3. Table 3: Percentage of patients reporting non-hemorrhagic adverse reactions at least 4% or more in either group and more frequently on ticagrelor (PLATO) Ticagrelor * N=9,235 Clopidogrel N=9,186 Dyspnea 13.8 7.8 Dizziness 4.5 3.9 Nausea 4.3 3.8 * 90 mg BID Bleeding in PEGASUS (Secondary Prevention in Patients with a History of Myocardial Infarction) Overall outcome of bleeding events in the PEGASUS study are shown in Table 4. Table 4: Bleeding events (PEGASUS) Ticagrelor * N=6,958 Placebo N=6,996 Events/1,000 patient years Events/1,000 patient years TIMI Major 8 3 Fatal 1 1 Intracranial hemorrhage 2 1 TIMI Major or Minor 11 5 TIMI Major: Fatal bleeding, OR any intracranial bleeding, OR clinically overt signs of hemorrhage associated with a drop in hemoglobin (Hgb) of ≥ 5 g/dL, or a fall in hematocrit (Hct) of ≥ 15%. Fatal: A bleeding event that directly led to death within 7 days. TIMI Minor: Clinically apparent with 3 g/dL to 5 g/dL decrease in hemoglobin. * 60 mg BID The bleeding profile of ticagrelor 60 mg compared to aspirin alone was consistent across multiple pre-defined subgroups (e.g., by age, gender, weight, race, geographic region, concurrent conditions, concomitant therapy, stent, and medical history) for TIMI Major and TIMI Major or Minor bleeding events.
Drug interactions
Avoid use with strong CYP3A inhibitors or CYP3A inducers. ( 7.1 , 7.2 ) Opioids: Decreased exposure to ticagrelor. Consider use of parenteral anti-platelet agent. ( 7.3 ) Patients receiving more than 40 mg per day of simvastatin or lovastatin, or more than 20 mg per day of rosuvastatin may be at increased risk of statin-related adverse effects. ( 7.4 ) Monitor digoxin levels with initiation of or any change in ticagrelor. ( 7.5 ) 7.1 Strong CYP3A Inhibitors Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir and telithromycin) [see Clinical Pharmacology (12.3) ] . 7.2 Strong CYP3A Inducers Strong CYP3A inducers substantially reduce ticagrelor exposure and so decrease the efficacy of ticagrelor. Avoid use with strong inducers of CYP3A (e.g., rifampin, phenytoin, carbamazepine and phenobarbital) [see Clinical Pharmacology (12.3) ] . 7.3 Opioids As with other oral P2Y 12 inhibitors, co-administration of opioid agonists delay and reduce the absorption of ticagrelor and its active metabolite presumably because of slowed gastric emptying [see Clinical Pharmacology (12.3) ] . Consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring co-administration of morphine or other opioid agonists. 7.4 Simvastatin, Lovastatin, Rosuvastatin Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses greater than 40 mg [see Clinical Pharmacology (12.3) ] . Ticagrelor increases serum concentrations of rosuvastatin because rosuvastatin is a BCRP substrate. Avoid rosuvastatin doses greater than 20 mg [see Clinical Pharmacology (12.3) ]. In patients at increased risk for rhabdomyolysis, consider rosuvastatin dosages less than 20 mg per day. 7.5 Digoxin Ticagrelor inhibits the P-glycoprotein transporter; monitor digoxin levels with initiation of or change in ticagrelor therapy [see Clinical Pharmacology (12.3) ] .
Use in specific populations
Lactation: Breastfeeding not recommended. ( 8.2 ) 8.1 Pregnancy Risk Summary Available data from case reports with ticagrelor use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Ticagrelor given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times the maximum recommended human dose (MRHD) based on body surface area. When ticagrelor was given to rats during late gestation and lactation, pup death and effects on pup growth were seen at approximately 10 times the MRHD (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In reproductive toxicology studies, pregnant rats received ticagrelor during organogenesis at doses from 20 to 300 mg/kg/day. 20 mg/kg/day is approximately the same as the MRHD of 90 mg twice daily for a 60 kg human on a mg/m 2 basis. Adverse outcomes in offspring occurred at doses of 300 mg/kg/day (16.5 times the MRHD on a mg/m 2 basis) and included supernumerary liver lobe and ribs, incomplete ossification of sternebrae, displaced articulation of pelvis, and misshapen/misaligned sternebrae. At the mid-dose of 100 mg/kg/day (5.5 times the MRHD on a mg/m 2 basis), delayed development of liver and skeleton was seen. When pregnant rabbits received ticagrelor during organogenesis at doses from 21 to 63 mg/kg/day, fetuses exposed to the highest maternal dose of 63 mg/kg/day (6.8 times the MRHD on a mg/m 2 basis) had delayed gall bladder development and incomplete ossification of the hyoid, pubis and sternebrae occurred. In a prenatal/postnatal study, pregnant rats received ticagrelor at doses of 10 to 180 mg/kg/day during late gestation and lactation. Pup death and effects on pup growth were observed at 180 mg/kg/day (approximately 10 times the MRHD on a mg/m 2 basis). Relatively minor effects such as delays in pinna unfolding and eye opening occurred at doses of 10 mg/kg and 60 mg/kg (approximately one-half and 3.2 times the MRHD on a mg/m 2 basis). 8.2 Lactation Risk Summary There are no data on the presence of ticagrelor or its metabolites in human milk, the effects on the breastfed infant, or the effects on milk production. Ticagrelor and its metabolites were present in rat milk at higher concentrations than in maternal plasma. When a drug is present in animal milk, it is likely that the drug will be present in human milk. Breastfeeding is not recommended during treatment with ticagrelor. 8.4 Pediatric Use The safety and effectiveness of ticagrelor tablets have not been established in pediatric patients. Effectiveness was not demonstrated in an adequate and well-controlled study conducted in 101 ticagrelor tablets-treated pediatric patients, aged 2 to < 18 for reducing the rate of vaso-occlusive crises in sickle cell disease. 8.5 Geriatric Use About half of the patients in PLATO, PEGASUS, THEMIS, and THALES were ≥ 65 years of age and at least 15% were ≥ 75 years of age. No overall differences in safety or effectiveness were observed between elderly and younger patients. 8.6 Hepatic Impairment Ticagrelor is metabolized by the liver and impaired hepatic function can increase risks for bleeding and other adverse events. Avoid use of ticagrelor in patients with severe hepatic impairment. There is limited experience with ticagrelor in patients with moderate hepatic impairment; consider the risks and benefits of treatment, noting the probable increase in exposure to ticagrelor. No dosage adjustment is needed in patients with mild hepatic impairment [see Warnings and Precautions (5.5) and Clinical Pharmacology (12.3) ] . 8.7 Renal Impairment No dosage adjustment is needed in patients with renal impairment [see Clinical Pharmacology (12.3) ] . Patients with End-Stage Renal Disease on dialysis Clinical efficacy and safety studies with ticagrelor did not enroll patients with end-stage renal disease (ESRD) on dialysis. In patients with ESRD maintained on intermittent hemodialysis, no clinically significant difference in concentrations of ticagrelor and its metabolite and platelet inhibition are expected compared to those observed in patients with normal renal function [see Clinical Pharmacology (12.3) ] . It is not known whether these concentrations will lead to similar efficacy and safety in patients with ESRD on dialysis as were seen in PLATO, PEGASUS, THEMIS and THALES.
Pregnancy
8.1 Pregnancy Risk Summary Available data from case reports with ticagrelor use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Ticagrelor given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times the maximum recommended human dose (MRHD) based on body surface area. When ticagrelor was given to rats during late gestation and lactation, pup death and effects on pup growth were seen at approximately 10 times the MRHD (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In reproductive toxicology studies, pregnant rats received ticagrelor during organogenesis at doses from 20 to 300 mg/kg/day. 20 mg/kg/day is approximately the same as the MRHD of 90 mg twice daily for a 60 kg human on a mg/m 2 basis. Adverse outcomes in offspring occurred at doses of 300 mg/kg/day (16.5 times the MRHD on a mg/m 2 basis) and included supernumerary liver lobe and ribs, incomplete ossification of sternebrae, displaced articulation of pelvis, and misshapen/misaligned sternebrae. At the mid-dose of 100 mg/kg/day (5.5 times the MRHD on a mg/m 2 basis), delayed development of liver and skeleton was seen. When pregnant rabbits received ticagrelor during organogenesis at doses from 21 to 63 mg/kg/day, fetuses exposed to the highest maternal dose of 63 mg/kg/day (6.8 times the MRHD on a mg/m 2 basis) had delayed gall bladder development and incomplete ossification of the hyoid, pubis and sternebrae occurred. In a prenatal/postnatal study, pregnant rats received ticagrelor at doses of 10 to 180 mg/kg/day during late gestation and lactation. Pup death and effects on pup growth were observed at 180 mg/kg/day (approximately 10 times the MRHD on a mg/m 2 basis). Relatively minor effects such as delays in pinna unfolding and eye opening occurred at doses of 10 mg/kg and 60 mg/kg (approximately one-half and 3.2 times the MRHD on a mg/m 2 basis).
Pediatric use
8.4 Pediatric Use The safety and effectiveness of ticagrelor tablets have not been established in pediatric patients. Effectiveness was not demonstrated in an adequate and well-controlled study conducted in 101 ticagrelor tablets-treated pediatric patients, aged 2 to < 18 for reducing the rate of vaso-occlusive crises in sickle cell disease.
Geriatric use
8.5 Geriatric Use About half of the patients in PLATO, PEGASUS, THEMIS, and THALES were ≥ 65 years of age and at least 15% were ≥ 75 years of age. No overall differences in safety or effectiveness were observed between elderly and younger patients.
Overdosage
There is currently no known treatment to reverse the effects of ticagrelor, and ticagrelor is not dialyzable. Treatment of overdose should follow local standard medical practice. Bleeding is the expected pharmacologic effect of overdosing. If bleeding occurs, appropriate supportive measures should be taken. Platelet transfusion did not reverse the antiplatelet effect of ticagrelor in healthy volunteers and is unlikely to be of clinical benefit in patients with bleeding. Other effects of overdose may include gastrointestinal effects (nausea, vomiting, diarrhea) or ventricular pauses. Monitor the ECG.
Description
Ticagrelor tablets contain ticagrelor, a cyclopentyltriazolopyrimidine, inhibitor of platelet activation and aggregation mediated by the P2Y 12 ADP-receptor. Chemically it is (1 S ,2 S ,3 R ,5 S )-3-[7-{[(1 R ,2 S )-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3 H -[1,2,3]-triazolo[4,5- d ]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol. The molecular formula of ticagrelor is C 23 H 28 F 2 N 6 O 4 S and its molecular weight is 522.57 g/mol. The chemical structure of ticagrelor is: Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10 mcg/mL at room temperature. Ticagrelor 90 mg tablets for oral administration contain 90 mg of ticagrelor and the following ingredients: crospovidone, magnesium stearate, mannitol, microcrystalline cellulose, povidone. The film coating contains, hypromellose, polyethylene glycol, titanium dioxide, talc, and yellow iron oxide. Ticagrelor 60 mg tablets for oral administration contain 60 mg of ticagrelor and the following ingredients: crospovidone, magnesium stearate, mannitol, microcrystalline cellulose, povidone. The film coating contains, hypromellose, polyethylene glycol, titanium dioxide, talc, iron oxide red and black iron oxide. abc
Mechanism of action
12.1 Mechanism of Action Ticagrelor and its major metabolite reversibly interact with the platelet P2Y 12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent.
How supplied
Ticagrelor tablets 60 mg are supplied as light pink, round shaped, film coated tablets debossed with ‘521’ on one side and ‘SG’ on the other side. Bottle of 30's NDC 50228-521-30 Bottle of 60’s NDC 50228-521-60 Bottle of 1000's NDC 50228-521-10 Ticagrelor tablets 90 mg are supplied as yellow, round shaped, film coated tablets debossed with ‘522’ on one side and ‘SG’ on the other side. Bottle of 30's NDC 50228-522-30 Bottle of 60’s NDC 50228-522-60 Bottle of 1000's NDC 50228-522-10 Storage and Handling Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP controlled room temperature].
Patient information
Advise the patient to read the FDA-approved patient labeling (Medication Guide). Advise patients daily doses of aspirin should not exceed 100 mg and to avoid taking any other medications that contain aspirin. Advise patients that they: Will bleed and bruise more easily Will take longer than usual to stop bleeding Should report any unanticipated, prolonged or excessive bleeding, or blood in their stool or urine. Advise patients to contact their doctor if they experience unexpected shortness of breath, especially if severe. Advise patients to inform physicians and dentists that they are taking ticagrelor before any surgery or dental procedure. Advise women that breastfeeding is not recommended during treatment with ticagrelor [see Use in Specific Populations (8.2) ]. Manufactured by: ScieGen Pharmaceuticals, Inc. Hauppauge, NY 11788, USA Revised: 5/2026
Label text from the FDA structured product label by ScieGen Pharmaceuticals INC (revised Aug 31, 2026). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Ticagrelor in 52 products
Ticagrelor NDC products (52)
| NDC | Strength & form | Labeler | Type |
|---|---|---|---|
| 11788-157 | Ticagrelor 60 mg/1 Tablet | AiPing Pharmaceutical, Inc | ANDA |
| 11788-158 | Ticagrelor 90 mg/1 Tablet | AiPing Pharmaceutical, Inc | ANDA |
| 62332-500 | Ticagrelor 60 mg/1 Tablet, Film Coated | Alembic Pharmaceuticals Inc. | ANDA |
| 62332-241 | Ticagrelor 90 mg/1 Tablet, Film Coated | Alembic Pharmaceuticals Inc. | ANDA |
| 46708-500 | Ticagrelor 60 mg/1 Tablet, Film Coated | Alembic Pharmaceuticals Limited | ANDA |
| 46708-241 | Ticagrelor 90 mg/1 Tablet, Film Coated | Alembic Pharmaceuticals Limited | ANDA |
| 60687-935 | Ticagrelor 60 mg/1 Tablet | American Health Packaging | ANDA |
| 60687-928 | Ticagrelor 90 mg/1 Tablet | American Health Packaging | ANDA |
| 71610-914 | Ticagrelor 90 mg/1 Tablet, Film Coated | Aphena Pharma Solutions - Tennessee, LLC | ANDA |
| 71610-958 | Ticagrelor 90 mg/1 Tablet | Aphena Pharma Solutions - Tennessee, LLC | ANDA |
| 53401-028 | Ticagrelor 90 mg/1 Tablet | Aphena Pharma Solutions - Tennessee, LLC | ANDA |
| 60505-4453 | Ticagrelor 60 mg/1 Tablet | Apotex Corp. | ANDA |
| 60505-4452 | Ticagrelor 90 mg/1 Tablet | Apotex Corp. | ANDA |
| 67877-491 | Ticagrelor 90 mg/1 Tablet | Ascend Laboratories, LLC | ANDA |
| 67877-522 | Ticagrelor 60 mg/1 Tablet, Film Coated | Ascend Laboratories, LLC | ANDA |
| 73190-003 | Ticagrelor 60 mg/1 Tablet | AvKARE | ANDA |
| 73190-008 | Ticagrelor 90 mg/1 Tablet | AvKARE | ANDA |
| 50268-826 | Ticagrelor 90 mg/1 Tablet | AvPAK | ANDA |
| 69452-509 | Ticagrelor 90 mg/1 Tablet | BIONPHARMA INC. | ANDA |
| 69452-508 | Ticagrelor 60 mg/1 Tablet | BIONPHARMA INC. | ANDA |
| 55488-0543 | Ticagrelor 90 mg/1 Tablet | Changzhou Pharmaceutical Factory | ANDA |
| 55488-0544 | Ticagrelor 60 mg/1 Tablet | Changzhou Pharmaceutical Factory | ANDA |
| 69097-989 | Ticagrelor 60 mg/1 Tablet, Film Coated | Cipla USA Inc. | ANDA |
| 69097-991 | Ticagrelor 90 mg/1 Tablet, Film Coated | Cipla USA Inc. | ANDA |
| 43598-629 | Ticagrelor 60 mg/1 Tablet | Dr. Reddys Laboratories Inc | ANDA |
| 43598-480 | Ticagrelor 90 mg/1 Tablet | Dr. Reddys Laboratories Inc | ANDA |
| 76282-584 | Ticagrelor 60 mg/1 Tablet, Film Coated | Exelan Pharmaceuticals, Inc | ANDA |
| 76282-550 | Ticagrelor 90 mg/1 Tablet, Film Coated | Exelan Pharmaceuticals, Inc | ANDA |
| 51407-861 | Ticagrelor 90 mg/1 Tablet | Golden State Medical Supply, Inc. | ANDA |
| 42658-115 | Ticagrelor 90 mg/1 Tablet, Film Coated | Hisun Pharmaceuticals USA, Inc. | ANDA |
| 42385-994 | Ticagrelor 90 mg/1 Tablet | Laurus Labs Limited | ANDA |
| 42385-993 | Ticagrelor 60 mg/1 Tablet | Laurus Labs Limited | ANDA |
| 70756-048 | Ticagrelor 90 mg/1 Tablet, Film Coated | Lifestar Pharma LLC | ANDA |
| 70756-047 | Ticagrelor 60 mg/1 Tablet, Film Coated | Lifestar Pharma LLC | ANDA |
| 33342-432 | Ticagrelor 90 mg/1 Tablet, Film Coated | Macleods Pharmaceuticals Limited | ANDA |
| 33342-431 | Ticagrelor 60 mg/1 Tablet, Film Coated | Macleods Pharmaceuticals Limited | ANDA |
| 0378-2215 | Ticagrelor 90 mg/1 Tablet, Film Coated | Mylan Pharmaceuticals Inc. | ANDA |
| 0378-2214 | Ticagrelor 60 mg/1 Tablet, Film Coated | Mylan Pharmaceuticals Inc. | ANDA |
| 72603-940 | Ticagrelor 60 mg/1 Tablet, Film Coated | NorthStar RxLLC | ANDA |
| 72603-941 | Ticagrelor 90 mg/1 Tablet, Film Coated | NorthStar RxLLC | ANDA |
| 72205-368 | Ticagrelor 90 mg/1 Tablet | Novadoz Pharmaceuticals LLC | ANDA |
| 72205-406 | Ticagrelor 60 mg/1 Tablet | Novadoz Pharmaceuticals LLC | ANDA |
| 72516-017 | Ticagrelor 60 mg/1 Tablet | Oryza Pharmaceuticals, Inc. | ANDA |
| 72516-018 | Ticagrelor 90 mg/1 Tablet | Oryza Pharmaceuticals, Inc. | ANDA |
| 77771-521 | Ticagrelor 60 mg/1 Tablet | Radha Pharmaceuticals INC | ANDA |
| 77771-522 | Ticagrelor 90 mg/1 Tablet | Radha Pharmaceuticals INC | ANDA |
| 67296-2268 | Ticagrelor 90 mg/1 Tablet, Film Coated | Redpharm Drug | ANDA |
| 50228-522 | Ticagrelor 90 mg/1 Tablet | ScieGen Pharmaceuticals INC | ANDA |
| 50228-521 | Ticagrelor 60 mg/1 Tablet | ScieGen Pharmaceuticals INC | ANDA |
| 43547-657 | Ticagrelor 90 mg/1 Tablet, Film Coated | Solco Healthcare U.S., LLC | ANDA |
| 0480-2695 | Ticagrelor 90 mg/1 Tablet, Film Coated | Teva Pharmaceuticals, Inc. | ANDA |
| 0480-2688 | Ticagrelor 60 mg/1 Tablet, Film Coated | Teva Pharmaceuticals, Inc. | ANDA |
Frequently asked questions
What is Ticagrelor used for?
Ticagrelor tablets are a P2Y 12 platelet inhibitor indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI. For at least the first 12 months following ACS, it is superior to clopidogrel. Ticagrelor tablets also reduces the risk of stent thrombosis in patients who have been stented for…
What are the side effects of Ticagrelor?
The following adverse reactions are also discussed elsewhere in the labeling: Bleeding [see Warnings and Precautions (5.1) ] Dyspnea [see Warnings and Precautions (5.3) ] Most common adverse reactions (> 5%) are bleeding and dyspnea. ( 5.1 , 5.3 , 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact ScieGen Pharmaceuticals, Inc. at (1-855-724-3436) or FDA at 1-800-FDA-1088 or… See the full label for the complete list.
Who makes Ticagrelor?
Ticagrelor is listed by 28 labelers in the FDA NDC directory, including AiPing Pharmaceutical, Inc, Alembic Pharmaceuticals Inc., Alembic Pharmaceuticals Limited, American Health Packaging.