Chemical structural formula:
C256H381N65O79S6
Insulin aspart is a rapid-acting insulin analogue that is modified by altering the B28 proline residue to aspartic acid residue from human insulin. As a result, Rapilin has a lower tendency to form hexamers than soluble human insulin.
Like other insulins, insulin aspart’s primary function is the regulation of glucose metabolism. Insulin and its analogues lower blood glucose by stimulating peripheral glucose uptake, especially by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin inhibits lipolysis and proteolysis, and enhances protein synthesis.
The faster absorption characteristic of insulin aspart depends on its fast release after subcutaneous injection and subsequent fast absorption into the blood.
In healthy subjects and diabetic patients, insulin serum concentrations indicated a faster absorption after subcutaneous injection of insulin aspart in comparison to human insulin.
The relative bioavailability of insulin aspart compared to regular human insulin indicates that two insulins are absorbed to a similar extent.
According to literature, diabetic patients were administered subcutaneously both insulin aspart and regular human insulin, and mean Cmax is much larger than that of regular human insulin.
The mean insulin clearance was similar for both insulin aspart and regular human insulin.
In clinical studies, subgroup analyses based on age and gender did not indicate any difference in safety and efficacy in insulin aspart-treated patients compared to the entire study population.
The following content is intended to answer your questions only and is not intended to be used for promotional purposes or as a clinical medication guidance.
※ Product Characteristics
● What is the basic information of Rapilin®?
The generic name of Rapilin® is insulin aspart injection, and it contains insulin aspart as the active ingredient. It is indicated for the treatment of diabetes and has been approved in China in 2020. Insulin aspart is a rapid-acting insulin product that is usually administered just before a meal, although it can also be used immediately after a meal if required. Dosage should be determined by the physician based on the individual needs of the patient. Rapilin® is classified as a biosimilar and shows a high degree of similarity in terms of quality, safety and efficacy when compared to the approved reference (originator) medicine.
● Will Rapilin® cause liver and kidney problems like some oral hypoglycemic drugs?
Raplin® is not associated with liver or kidney problems. The liver and kidneys are involved in the elimination of the body's own insulin. The introduction of exogenous insulin does not place an additional burden on these organs. In cases of liver or kidney dysfunction, the need for insulin may be reduced due to the reduced breakdown of endogenous insulin. Therefore, people using insulin should continue to monitor their blood glucose levels and adjust their dose if necessary.
● Is Rapilin® addictive? Could higher doses lead to dependence?
Rapilin® is not associated with addiction or dependence. Addiction is when an individual develops an intense craving for a substance to obtain psychological or physiological effects, leading to uncontrollable and compulsive use. Unlike addictive substances, Rapilin® is a form of insulin, a natural hormone that is essential for metabolic processes and the maintenance of life. The use of insulin is determined by factors such as blood glucose control and the functioning of the body's β cells. It is not addictive and its necessity is dictated by medical considerations rather than addictive tendencies.
● What are the precautions for the use of Rapilin® in special populations? Are there efficacy and safety data?
Pregnant and breastfeeding women: This product can be used by pregnant women. Two randomized controlled clinical trials have shown that it has no adverse effects on the health of pregnant women or on the health of their fetuses or newborns compared with soluble human insulin preparations (as stated in the prescribing information).
Children: Given the rapid onset of action of this product compared with soluble human insulin, it may be a favorable option for children who require rapid action. Studies in children and adolescents aged 2-17 years have shown that insulin aspart has pharmacodynamic behavior similar to that in adults. In general, doses of 0.5 to 1.0 U per kg of body weight per day are common in this age group (as stated in the prescribing information).
Older people: No special instructions, please refer to the [Dosage] in the prescribing information or follow the doctor's advice.
※ Clinical Study
● What are the pharmacokinetics/pharmacodynamics (PK/PD) of Rapilin®️ compared to the reference drug, the original insulin aspart?
In 2021, Gan & Lee Pharmaceuticals (the applicant) conducted a Phase 1 clinical trial using a randomized, double-blind, triple-crossover design with positive glucose clamp techniques. The results, reported by Plum-Mörschel et al. at the American Diabetes Association (ADA), showed that Rapilin®️ was bioequivalent to the original reference insulin aspart product available in the US and EU. This equivalence covered both pharmacokinetic (PK) and pharmacodynamic (PD) aspects. In addition, the study included 36 healthy male subjects and the safety profile of Rapilin®️ was very similar to that of the reference drug.
The key pharmacokinetic (PK) parameters, Cmax and AUC0-12h, showed PK bioequivalence between Rapilin®️ and the original reference drug. This equivalence was demonstrated by the 90% confidence intervals (CIs) falling entirely within the predefined PK similarity range of 80% to 125%.
Figure 1 Comparison of mean PK curves (±SEMs) and primary endpoints
The key pharmacodynamic (PD) measures, GIRmax and AUCGIR.0-24h, showed a comparable glucose infusion rate (GIR) pattern between Rapilin®️ and the original reference drug. The PD endpoints met bioequivalence criteria with both the 90% and 95% confidence intervals (CIs) ranging from 80.00% to 120.00% similarity.
Figure 2 Comparison of mean PD curves (±SEMs) and primary endpoints
Consistent and comparable safety was observed across the three treatment groups, with all insulin types being well tolerated. The incidence of adverse events was similar and there were minimal cases of injection site reactions.
● What is the glucose-lowering efficacy and safety profile of Rapilin® in combination with metformin?
A multi-center, randomized, open-label, non-inferiority Phase 3 confirmatory clinical trial in China. The study included 590 patients with type 2 diabetes who were randomized to receive metformin in combination with Rapilin® (n=441) or the reference drug (n=149) for a total of 24 weeks. The results showed that Rapilin® was not inferior to the original insulin arspart reference drug in terms of glycaemic control (glycaemic hemoglobin levels were reduced by 2.20% and 2.32% from baseline in the Rapilin® and reference drug groups, respectively). There was no statistically significant difference in the treatment difference between the two groups and that it had a comparable safety and immunogenicity profile to the reference drug (Yao et al. 2022).
※ Clinical Appication
● Does Rapilin®️ require a higher dosage than the original insulin aspart to achieve equivalent efficacy?
There is no difference in the dosage of Rapilin®️ compared to the original insulin aspart. A bioequivalence study conducted in Germany evaluated Rapilin®️ and originator insulin aspart and showed no discernible differences in pharmacokinetic and pharmacodynamic characteristics between the two. This was confirmed by a 12-hour glucose clamp study in humans (Plum-Mörschel et al., 2021).
● Can Rapilin® (cartridge) be used with an insulin pump?
Rapilin®️ can be administered via an insulin pump. The prescribing information introduces catheter occlusion and infusion site reactions when using insulin pumps with this product and human insulin.
© 2023 Gan & Lee Pharmaceuticals All Rights Reserved
Please enter the email address used for registration to receive password reset messages
We sent an email to XXXXXXXXXXX@qq.com with a link to reset the password. If you don't get one, try checking your spam folder.
