Eptifibatide API CAS 881997-86-0

Eptifibatide API | Eptifibatide acetate cGMP production | GP IIb/IIIa antagonist | Science-Peptide

Eptifibatide API CAS 881997-86-0--Antiplatelet peptide for acute coronary syndrome. Science-Peptidelogicals provides cGMP-compliant eptifibatide acetate, with mature technology, clear impurity profile, support for China, the United States and Europe to declare, and has served a number of pharmaceutical companies to pass the consistency evaluation. Welcome to contact us.

At the scene of acute coronary syndrome (ACS), time is myocardium. When a patient is put on the operating table to undergo percutaneous coronary intervention (PCI), how to rapidly inhibit platelet aggregation and prevent thrombosis is a critical step in determining the prognosis. Eptifibatide (Eptifibatide) is the drug that plays this role - it is like a precise "brake", stuck on the platelet surface of the GP IIb/IIIa receptor, so that the fibrinogen can't "stick" to the platelets. It acts as a precise "brake" on the GP IIb/IIIa receptors on the platelet surface, preventing fibrinogen from "sticking" platelets together.

 

Science-Peptide is one of the early enterprises in China to carry out the development of efebatide API process. More than ten years ago, we started to study this 7 amino acid cyclic peptide, from the laboratory trial to the cGMP production of 100 kilograms, every step of the way, we have stepped on the pit, filled in the soil, before we have this set of mature technology today. Nowadays, our eptifibatide APIs have been exported to Europe, Southeast Asia and other markets, and we have helped formulation companies to pass the consistency evaluation and ANDA declaration.

Eptifibatide (Eptifibatide Acetate, Eptifibatide Acetate) is a cyclic peptide consisting of 7 amino acids, which mimics the KGD (lysine-glycine-aspartic acid) sequence of the γ-chain of fibrinogen and competitively binds to the GP IIb/IIIa receptor on the surface of platelets, blocking the binding of fibrinogen to platelets and thus inhibiting platelet aggregation.

Eptifibatide is well positioned clinically: th:

• Individuals: Patients with non-ST-segment elevation acute coronary syndrome (NSTE-ACS), especially those planning to undergo PCI
• Mode of administration: intravenous push + continuous infusion, fast onset of action, platelet function recovery in 2-4 hours after stopping the drug
• Clinical status: One of the antithrombotic drugs recommended by domestic and international cardiovascular guidelines

For generic companies, efibatide is a classic variety. Its patent has long expired, but the market demand is stable, and the quality requirements for APIs are very high - the impurity profile must be consistent with that of the original, the process must be robust, and the supply must be reliable.

1. It has taken more than a decade for the process to move from "capable" to "stable"
In the early days of eptifibatide, the biggest difficulty was cyclization. How to form disulfide bonds, how to avoid mismatches, how to control impurities, it took us a few years to figure it out. The current process:

• Solid phase synthesis: Fmoc strategy, preferred resin, stable crude peptide yield above 85%
• Cyclization: precise control of pH and oxidation conditions, cyclization efficiency over 95%, disulfide bond pairing correct rate close to 100%.
• Purification: three-step preparative HPLC, cutting out key impurities (e.g. oxidized impurities, missing peptides, dimers) one by one
• Enlargement: from 20L to 3000L reactor, the process parameters are shifted, and the yield and purity are not degraded

2. Heterogeneous mass spectrometry, dare to compare with the original
We have done a detailed analysis of impurity profiles to identify all the impurities that may occur during the production of efibatide: oxidized impurities, deamidation impurities, dimers, missing peptides The impurity profiles of each batch of products are compared with those of the originator drugs to ensure consistency. Some domestic customers have used our APIs for consistency evaluation, and the impurity data passed the evaluation directly, without issuing supplement.

3. cGMP production, audited
Our Eptifibatide API CAS 881997-86-0 is produced in cGMP workshop, clean area ISO 7/8, each batch has complete batch production records.In QC lab, HPLC, LC-MS, GC, ICP-MS are available, and the methods are all validated. We have extensive experience with FDA, EMA, and NMPA audits. We can provide a full set of documents to support our customers when they need to be audited.

4. Stability of supply, with constant supply being our bottom line
The most fearful thing about doing APIs is that the supply will be cut off. We have set up a dual-source procurement system, with two suppliers for key materials such as amino acids and resins. For those with long procurement cycle, we set up safety stock. During the epidemic, a lot of manufacturers cut off goods, but we managed to keep all the orders. A European customer later told us that he had signed an annual contract with us because of the word "continuous supply".

Production site (10 acres)
Complying with FDA, EMA, NMPA cGMP requirements
ISO 9001:2015 certified
Automated solid-phase synthesis plant (100 kg)
Preparative HPLC Purification System (multiple sets)
Freeze-drying workshop (30㎡+)
Clean area ISO class 7/8

Quality system
Change control, deviation management, CAPA - it should be there
Supplier audits - every critical material is audited
Annual quality review - annual review, continuous improvement
Cooperating with customer audits - FDA, EMA, NMPA have all experienced, no major problems

Customer Cases

• Case 1: The consistency evaluation program of a domestic pharmaceutical company

They were doing the consistency evaluation of efibatide injection, and had searched for several API suppliers, but the impurity profiles did not match with those of the original researcher. When they found us, there were only a few months left before the deadline. We sent three batches of validation data to them, and the impurity profile was almost identical to that of the original study. They signed a contract directly and used our API to make preparations, which eventually passed the evaluation successfully. Now we have become the exclusive supplier of this product, which is purchased steadily every year.

• Case 2: Local registration of a client in Southeast Asia

A pharmaceutical company in Southeast Asia has a stable demand for efibatide injection in the local market, and they want to localize the production. We supplied three batches of APIs in a row, and the purity of each batch was above 99.2% with stable impurity profile. The preparations they made with these APIs have successfully

We don't want to be a "universal supplier", but we do have confidence in the variety of efebatide. The process is mature, the quality is stable, the documents are complete, and it has been sold both at home and abroad. If you are looking for efibatide API, whether it is for formulation production, generic drug declaration or R&D, you can have a chat first.