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Ticagrelor | CAS No: 274693-27-5 | GMP-certified suppliers
A medication that helps reduce the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or established coronary artery disease.
Therapeutic categories
Primary indications
- Ticagrelor is indicated to reduce the risk of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome or a history of myocardial infarction
- Ticagrelor is also indicated to reduce the risk of a first myocardial infarction or stroke in high risk patients with coronary artery disease
Product Snapshot
- Ticagrelor is an oral small‑molecule API supplied for solid dose tablet formulations
- It is used in products aimed at reducing risks of cardiovascular death, myocardial infarction, and stroke in acute coronary syndrome, prior myocardial infarction, or high‑risk coronary artery disease populations
- It is approved in the US, EU, and Canada
Clinical Overview
Ticagrelor acts as a direct, reversible antagonist of the P2Y12 receptor on platelets. This receptor normally couples to Gi family proteins, inhibiting adenylyl cyclase and activating downstream pathways including PI3K, Akt, Rap1b, and specific potassium channels. These pathways support platelet activation and aggregation. By blocking P2Y12 signalling, ticagrelor decreases platelet aggregation and limits development of occlusive thrombosis, contributing to the prevention of myocardial infarction and ischemic stroke.
Pharmacodynamically, ticagrelor demonstrates a moderate duration of action consistent with twice‑daily dosing. It does not require metabolic activation, differentiating it from prodrug P2Y12 inhibitors. Clinically relevant adverse effects include bleeding, dyspnea, and bradyarrhythmias. The agent has a wide therapeutic index, though patient monitoring for bleeding risk remains essential.
Ticagrelor undergoes hepatic metabolism, with CYP3A4 identified as the major metabolic pathway. Both ticagrelor and its active metabolite are substrates of CYP3A enzymes and may act as weak inhibitors or inducers of several CYP isoforms, including CYP2C9 and CYP3A4. The compound is also reported to interact with P‑glycoprotein transport pathways. Absorption, protein binding, and elimination parameters vary across studies, but the drug is known to reach clinically active plasma concentrations without requiring prodrug conversion.
For API sourcing, ensure suppliers provide material manufactured under ICH‑compliant GMP with full impurity profiling, control of chiral and structural isomers, and validated analytical methods suitable for regulatory submissions. Consistency in particle properties and residual solvent levels is important for formulation development and global market registration.
Identification & chemistry
| Generic name | Ticagrelor |
|---|---|
| Molecule type | Small molecule |
| CAS | 274693-27-5 |
| UNII | GLH0314RVC |
| DrugBank ID | DB08816 |
Pharmacology
| Summary | Ticagrelor is an oral antagonist of the P2Y12 receptor, a Gi‑coupled platelet ADP receptor that regulates intracellular signaling pathways involved in platelet activation. By blocking P2Y12‑mediated inhibition of adenylyl cyclase and downstream signaling through PI3K, Akt, and Rap1b, it reduces platelet aggregation. This antiplatelet activity supports its use in preventing thrombotic events such as myocardial infarction and ischemic stroke. |
|---|---|
| Mechanism of action | Ticagrelor is a P2Y<sub>12</sub> receptor antagonist. The P2Y<sub>12</sub> receptor couples with Gα<sub>i2</sub> and other G<sub>i</sub> proteins which inhibit adenylyl cyclase.G<sub>i</sub> mediated signalling also activates PI3K, Akt, Rap1b, and potassium channels.The downstream effects of these activities mediate hemostasis and lead to platelet aggregation. Antagonism of the P2Y<sub>12</sub> receptor reduces development of occlusive thromboses, which can reduce the risk of myocardial infarction and ischemic stroke. |
| Pharmacodynamics | Ticagrelor is a P2Y<sub>12</sub> receptor antagonist that inhibits the formation of thromboses to reduce the risk of myocardial infarction and ischemic stroke.It has a moderate duration of action as it is given twice daily, and a wide therapeutic index as high single doses are well tolerated.Patients should be counselled regarding the risk of bleeding, dyspnea, and bradyarrhythmias. |
Targets
| Target | Organism | Actions |
|---|---|---|
| P2Y purinoceptor 12 | Humans | inhibitor |
ADME / PK
| Absorption | Ticagrelor is 36% orally bioavailable.A single 200mg oral dose of ticagrelor reaches a C<sub>max</sub> of 923ng/mL, with a T<sub>max</sub> of 1.5 hours and an AUC of 6675ng\*h/mL.The active metabolite of ticagrelor reaches a C<sub>max</sub> of 264ng/mL, with a T<sub>max</sub> of 3.0 hours and an AUC of 2538ng\*h/mL. |
|---|---|
| Half-life | Ticagrelor has a plasma half life of approximately 8 hours, while the active metabolite has a plasma half life of approximately 12 hours. |
| Protein binding | Ticagrelor and its active metabolite ate >99% protein bound in plasma, particularly albumin. |
| Metabolism | The complete structure of all ticagrelor metabolites are not well defined.Ticagrelor can be dealkylated at postition 5 of the cyclopentane ring to form the active AR-C124910XX.AR-C124910XX's cyclopentane ring can be further glucuronidated or the alkyl chain attached to the sulfur can be hydroxylated.Ticagrelor can also be glucuronidated or hydroxylated.Ticagrelor can also be N-dealkylated to form AR-C133913XX, which is further glucuronidated or hydroxylated. |
| Route of elimination | A radiolabelled dose of ticagrelor is 57.8% recovered in feces and 26.5% recovered in urine.Less than 1% of the dose is recovered as the unmetabolized parent drug.The active metabolite AC-C124910XX makes up 21.7% of the recovery in the feces.The metabolite AR-C133913XX makes up 9.2% of the recovery in the urine and 2.7% of the recovery in the feces.Other minor metabolites are predominantly recovered in the urine. |
| Volume of distribution | The steady state volume of distribution of ticagrelor is 88 L. |
| Clearance | The renal clearance of ticagrelor is 0.00584L/h. |
Formulation & handling
- Low aqueous solubility and moderate lipophilicity may require solubility‑enhancing strategies for robust oral solid‑dose formulations.
- Developed exclusively as an oral small‑molecule API; film‑coated and ODT formats support protection from moisture and aid swallowability.
- Metabolism via CYP3A4 makes the API sensitive to excipient choices that may affect oxidative stability during processing and storage.
Regulatory status
| Lifecycle | Most key patents for the API in Canada and the United States expired between 2018 and 2021, indicating that the product has transitioned into a post‑exclusivity phase. With availability across Canada, the US, and the EU, the market is consistent with a mature, largely genericized stage. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Ticagrelor is supported by a single originator developer, with multiple branded and authorized generic presentations indicating a mature commercialization stage across the US, EU, and Canada. The product has broad global availability, including continued branded presence in major regulated markets. With key patents in the US and Canada expiring between 2018 and 2021, the molecule is already subject to generic competition in several regions. |
|---|
Safety
| Toxicity | Patients experiencing an overdose may present with bleeding, nausea, vomiting, diarrhea, and ventricular pauses.Overdose can be managed through symptomatic and supportive treatment, including ECG monitoring.Dialysis is not expected to remove ticagrelor from the blood due to it being highly protein bound. |
|---|
- Overexposure may lead to bleeding events and gastrointestinal symptoms, with potential for ventricular pauses
- The compound’s high plasma‑protein binding limits clearance by dialysis
- Toxicity assessment typically involves cardiac rhythm observation due to reported conduction disturbances
Ticagrelor is a type of Platelet Aggregation Inhibitors
Platelet Aggregation Inhibitors are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) used in the field of cardiology and thrombosis management. These inhibitors play a vital role in preventing platelet aggregation, a process responsible for the formation of blood clots. By inhibiting platelet aggregation, these APIs reduce the risk of arterial thrombosis, which can lead to severe cardiovascular events like heart attacks and strokes.
Platelet Aggregation Inhibitors primarily work by targeting specific receptors on platelet cells, thereby impeding their activation and subsequent aggregation. The most commonly utilized APIs in this category include acetylsalicylic acid (aspirin), clopidogrel, ticagrelor, and prasugrel. These drugs are available in various forms, such as tablets, capsules, and intravenous formulations, allowing flexibility in their administration.
The effectiveness of Platelet Aggregation Inhibitors lies in their ability to prevent platelets from adhering to each other and forming clots within blood vessels. This property is especially crucial in patients with a high risk of cardiovascular events, such as those with a history of heart disease, diabetes, or peripheral artery disease.
While Platelet Aggregation Inhibitors are generally safe and effective, they can also carry potential side effects, including bleeding complications. Therefore, their administration requires careful consideration of individual patient characteristics and risk factors.
In conclusion, Platelet Aggregation Inhibitors represent a significant category of pharmaceutical APIs used for the prevention of platelet aggregation and subsequent blood clot formation. By inhibiting this process, they contribute to the management and reduction of cardiovascular events, offering critical benefits to patients at risk.
Ticagrelor API manufacturers & distributors
Compare qualified Ticagrelor API suppliers worldwide. We currently have 32 companies offering Ticagrelor API, with manufacturing taking place in 8 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Acura Labs | Producer | India | India | CoA, GMP | 18 products |
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF | 229 products |
| Apollo Healthcare Resourc... | Distributor | Singapore | Singapore | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, ISO9001, JDMF, KDMF, MSDS, USDMF, WC | 200 products |
| Arshine Pharmaceutical Co... | Distributor | China | China | CoA | 176 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, ISO9001, MSDS, USDMF, WC | 250 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Changzhou Pharma | Producer | China | China | CoA, USDMF | 9 products |
| ChemExpress | Producer | United States | China | CoA, GMP, ISO9001, MSDS, WC | 197 products |
| Chr. Olesen Group | Distributor | Denmark | China | CoA, USDMF | 252 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, KDMF, MSDS, USDMF, WC | 170 products |
| Dr. Sahu's Laboratories | Producer | India | India | BSE/TSE, CEP, CoA, FDA, GMP, MSDS | 70 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| HEC Pharm | Producer | Germany | Unknown | CoA, USDMF | 31 products |
| Honour Lab | Producer | India | India | CoA, GMP, USDMF, WC | 30 products |
| Lek Pharma | Producer | Slovenia | India | CoA, USDMF | 32 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| MSN Organics | Producer | India | India | CoA, GMP, USDMF, WC | 21 products |
| Mylan | Producer | India | India | CoA, USDMF | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF | 64 products |
| Raks Pharma | Producer | India | India | CoA, USDMF | 58 products |
| Rochem International, Inc... | Distributor | United States | United States | BSE/TSE, CoA, GMP, ISO9001, MSDS | 144 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, ISO9001 | 157 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sichuan Benepure | Producer | China | China | CoA | 23 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, MSDS, USDMF | 762 products |
| Solfyn International LLP | Distributor | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, USDMF, WHO-GMP | 24 products |
| Suzhou Lixin Pharmaceutic... | Producer | China | China | BSE/TSE, CEP, CoA, EDMF/ASMF, GMP, MSDS | 34 products |
| Valence Labs | Producer | India | India | CoA, GMP | 32 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 140 products |
| Wuhan ZhongYou | Producer | China | China | CoA, USDMF | 4 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Ticagrelor API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Ticagrelor API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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