Insulin glargine
Long-acting insulin
From Wikipedia, the free encyclopedia
Insulin glargine sold, among others, under the brand name Lantus (manufactured and marketed by Sanofi) is a long-acting modified form of medical insulin, used in the management of type 1 and type 2 diabetes.[8] It is injected just under the skin.[8] Effects generally begin an hour after use.[8]
Toujeo branded insulin glargine | |
| Clinical data | |
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| Trade names | Lantus, others |
| Biosimilars | insulin glargine-aglr, insulin glargine-yfgn, Abasaglar, Rezvoglar, Semglee[1] |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a600027 |
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| Routes of administration | Subcutaneous |
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| Pharmacokinetic data | |
| Onset of action | ~1 hour[8] |
| Duration of action | 24–36 hours[8] |
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| ECHA InfoCard | 100.241.126 |
| Chemical and physical data | |
| Formula | C267H404N72O78S6 |
| Molar mass | 6062.96 g·mol−1 |
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Common side effects include low blood sugar, problems at the site of injection, itchiness, and weight gain.[8] Other serious side effects include low blood potassium.[8] NPH insulin rather than insulin glargine is generally preferred in pregnancy.[9] After injection, microcrystals slowly release insulin for about 24 hours.[8] This insulin causes body tissues to absorb glucose from the blood and decreases glucose production by the liver.[8]
Insulin glargine was patented, but the patent expired in most jurisdictions in 2014. It was approved for medical use in the United States in 2000.[8] It is on the World Health Organization's List of Essential Medicines.[10] In 2023, it was the 30th most commonly prescribed medication in the United States, with more than 18 million prescriptions.[11][12] In July 2021, the US Food and Drug Administration (FDA) approved an interchangeable biosimilar insulin product called Semglee (insulin glargine-yfgn) for the treatment of diabetes.[13]
Medical uses
The long-acting insulin class, which includes insulin glargine, do not appear much better than neutral protamine Hagedorn (NPH) insulin,[14] but do have a greater cost, making them, as of 2010, not cost effective for the treatment of type 2 diabetes.[15] In a previous review it was unclear if there is a difference in hypoglycemia, as there was not enough data to determine any differences with respect to long term outcomes,[16] however a more recent Cochrane systematic review did not find clinically significant difference when comparing insulin glargine to NPH insulin, insulin detemir or insulin degludec in the management of type 1 diabetes in either adults or children over periods of 6 months or longer.[14] It is not typically the recommended long-acting insulin in the United Kingdom.[9]
Semglee is indicated to improve glycemic control in adults and children with type 1 diabetes and in adults with type 2 diabetes.[13] Semglee is both biosimilar to, and interchangeable with, its reference product Lantus (insulin glargine), a long-acting insulin analog.[13]
Mixing with other insulins
The American Diabetes Association said in 2003 that, unlike some other longer-acting insulins, glargine should not be diluted or mixed with other insulin or solution in the same syringe, due to the low pH of its diluent.[17] However, a 2004 study found that mixing glargine with other insulins did not affect short-term glycemic profile.[18]
Adverse effects
Common side effects include low blood sugar, problems at the site of injection, itchiness, and weight gain.[8] Serious side effects include low blood potassium.[8]
As of 2012, tentative evidence shows no association between insulin glargine and cancer.[19] Previous studies had raised concerns.[20]
When comparing insulin glargine to NPH insulin, insulin detemir or insulin degludec, no significant adverse effects were found in the management of type 1 diabetes in either adults or children in periods of six months or longer.[14]
Pharmacology
Mechanism of action
Insulin glargine differs from human insulin by replacing asparagine with glycine in position 21 of the A-chain and by carboxy-terminal extension of B-chain by 2 arginine residues. The arginine amino acids shift the isoelectric point from a pH of 5.4 to 6.7, making the molecule more soluble at an acidic pH and less soluble at physiological pH. The isoelectric shift also allows for the subcutaneous injection of a clear solution. The glycine substitution prevents deamidation of the acid-sensitive asparagine at acidic pH. In the neutral subcutaneous space, higher-order aggregates form, resulting in a slow, peakless dissolution and absorption of insulin from the site of injection.[21]
History
Legal status
Biosimilars
Semglee (glargine-yfgn) received US Food and Drug Administration (FDA) approval in July 2021.[citation needed] The approval was granted to Mylan, which had merged with Upjohn into Viatris.[citation needed]
Rezvoglar (glargine-aglr) was approved by the FDA in December 2021 to be produced by Lilly.[citation needed]
Abasaglar (Eli Lilly and Boehringer Ingelheim) was authorized for medical use in the European Union in September 2014.[26][27]
Lusduna (Merck Sharp & Dohme (MSD)) was authorized for medical use in the European Union in January 2017.[28]
Semglee (Mylan and Biocon Biologics) was authorized for medical use in the European Union in March 2018.[29]
In November 2025, the Committee for Medicinal Products for Human Use of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Ondibta, intended for the treatment of diabetes.[30] The applicant for this medicinal product is Gan & Lee Pharmaceuticals Europe GmbH.[30] Ondibta is a biosimilar medicinal product that is highly similar to the reference product Lantus, which was authorized in the EU in June 2000.[30] Ondibta was authorized for medical use in the European Union in January 2026.[30][31]
Patent expiry
Patent protection for insulin glargine expired in the European Union and the United States in 2014.[32] Insulin glargine from competitor Eli Lilly became available in most countries during 2015, under the brand names Basaglar (as a follow-on in the US) and Abasaglar (as a biosimilar in the EU).[32]
Brand names
Insulin glargine is sold under various brand names including Basaglar[33], Lantus[34], and Toujeo[35].
