Liraglutide Injection (recombinant Route), Diabetes Bulk and Pen 3ml：18mg CAS No.: 204656-20-2

DESCRIPTION

LIRGLUTIDE contains liraglutide, an analog of human GLP-1 and acts as a GLP-1 receptor agonist. The peptide precursor of liraglutide, produced by a process that includes expression of recombinant DNA in Saccharomyces cerevisiae, has been engineered to be 97% homologous to native human GLP-1 by substituting arginine for lysine at position 34. Liraglutide is made by attaching a C-16 fatty acid (palmitic acid) with a glutamic acid spacer on the remaining lysine residue at position 26 of the peptide precursor. The molecular formula of liraglutide is C172H265N43O51 and the molecular weight is 3751.2 Daltons. The structural formula (Figure 1) is:

LIRAGLUTIDE injection is a sterile, aqueous, clear, colorless or almost colorless solution for subcutaneous use. Each 1 mL of LIRAGLUTIDE solution contains 6 mg of liraglutide and the following inactive ingredients: disodium phosphate dihydrate, 1.42 mg; propylene glycol, 14 mg; phenol, 5.5 mg; and water for injection. LIRAGLUTIDE has a pH of approximately 8.15, hydrochloric acid or sodium hydroxide may be added to adjust pH. Each pre-filled pen contains a 3 mL solution of LIRAGLUTIDE equivalent to 18 mg liraglutide (free-base, anhydrous).

Mechanism of Action

Liraglutide is an acylated human Glucagon-Like Peptide-1 (GLP-1) receptor agonist with 97% amino acid sequence homology to endogenous human GLP-1(7-37). GLP-1(7-37) represents <20% of total circulating endogenous GLP-1. Like GLP-1(7-37), liraglutide activates the GLP-1 receptor, a membrane-bound cell-surface receptor coupled to adenylyl cyclase by the stimulatory G-protein, Gs, in pancreatic beta cells. Liraglutide increases intracellular cyclic AMP (cAMP) leading to insulin release in the presence of elevated glucose concentrations. This insulin secretion subsides as blood glucose concentrations decrease and approach euglycemia. Liraglutide also decreases glucagon secretion in a glucose-dependent manner. The mechanism of blood glucose lowering also involves a delay in gastric emptying. GLP-1(7-37) has a half-life of 1.5-2 minutes due to degradation by the ubiquitous endogenous enzymes, dipeptidyl peptidase IV (DPP-IV) and neutral endopeptidases (NEP). Unlike native GLP-1, liraglutide is stable against metabolic degradation by both peptidases and has a plasma half-life of 13 hours after subcutaneous administration. The pharmacokinetic profile of liraglutide, which makes it suitable for once daily administration, is a result of self-association that delays absorption, plasma protein binding and stability against metabolic degradation by DPP-IV and NEP.

Pharmacodynamics

LIRAGLUTIDE’s pharmacodynamic profile is consistent with its pharmacokinetic profile observed after single subcutaneous administration as LIRAGLUTIDE lowered fasting, premeal and postprandial glucose throughout the day

Fasting and postprandial glucose was measured before and up to 5 hours after a standardized meal after treatment to steady state with 0.6, 1.2 and 1.8 mg LIRAGLUTIDE or placebo. Compared to placebo, the postprandial plasma glucose AUC0-300min was 35% lower after LIRAGLUTIDE 1.2 mg and 38% lower after LIRAGLUTIDE 1.8 mg. Glucose−dependent insulin secretion

The effect of a single dose of 7.5 mcg/kg (~ 0.7 mg) LIRAGLUTIDE on insulin secretion rates (ISR) was investigated in 10 patients with type 2 diabetes during graded glucose infusion. In these patients, on average, the ISR response was increased in a glucose-dependent manner (Figure 2).

Glucagon secretion

LIRAGLUTIDE lowered blood glucose by stimulating insulin secretion and lowering glucagon secretion. A single dose of LIRAGLUTIDE 7.5 mcg/kg (~ 0.7 mg) did not impair glucagon response to low glucose concentrations.

Gastric emptying

LIRAGLUTIDE causes a delay of gastric emptying, thereby reducing the rate at which postprandial glucose

appears in the circulation.

Cardiac Electrophysiology (QTc)

The effect of LIRAGLUTIDE on cardiac repolarization was tested in a QTc study. LIRAGLUTIDE at steady state

concentrations with daily doses up to 1.8 mg did not produce QTc prolongation.

Name: Liraglutide

Liraglutide is a prescription medicine used to treat the symptoms of Type 2 Diabetes Mellitus. Liraglutide may be used alone or with other medications.

Dosage: Injection

Specification: 3ml:18mg

Indications

Liraglutide is indicated: as an adjunct to diet and exercise to improve glycemic control in patients 10 years and older with type 2 diabetes mellitus,

Liraglutide to reduce the risk of major adverse cardiovascular events (cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke) in adults with type 2 diabetes mellitus and established cardiovascular disease.

Entrepreneurship

1993

On December 31, Hangzhou Jiuyuan Gene Engineering Co., Ltd. was registered and established in Hangzhou High-tech Development Zone.

Year 2003

On September 18, the platelet-promoting drug-Jijufen (recombinant human interleukin-11 for injection), obtained the new drug certificate and production approval.

Year 2008

The company was named the first batch of national high-tech enterprises in 2008.

On December 19, the fifth new product Giotin (palonosetron hydrochloride bulk drug and injection) was officially approved for production.

Year 2010

The company's new product, recombinant human BMP-2 bone repair material (Bone Youdao), was officially put into production and sales.

2020 year

The company's R&D center settled in Hangzhou Pharmaceutical Town as a whole.

The company's sales exceeded 1 billion yuan.

Honor

National High-Tech Enterprise

Key High-tech Enterprise of National Torch Plan

National Intellectual Property Advantage Enterprise

Provincial high-tech research and development center

Zhejiang Provincial Enterprise Technology Center

Famous Trademark of Zhejiang Province

Zhejiang Jiuyuan Gene Biopharmaceutical Research Institute

FAQ

Q: Are you trading company or manufacturer?

A: We are professional manufacturer specialized in the research, development, manufacture and marketing of pharmaceuticals based on gene engineering and biochemical technology since 1993.

And we trade our products with our clients directly.

Q: Do you provide sample? Is it free?

A: If the sample is low value, we will provide the free sample with freight collect. But for some high value samples, we need to collect the sample charge.

Q: What is your term of payment?

A: 30% down payment before producing and 70% balance payment before shipping.

Q: Which certificate do you have?

A: GMP, EUGMP and ISO14001.

Q: Do you have the test and audit service?

A: Yes, we can assist to get the designated test report for product and the designated factory audit report.

http://www.jiuyuangene.net/