Merck’s day again : Januvia (sitagliptin) enters EU

Januvia (sitagliptin), Merck’s oral DPP 4 inhibitor got the EU approval. This license makes Januvia, the only one DPP 4 inhibitor available in the prime markets (US & EU), atleast for a year to come. The prime contender for the DPP4 inhibitor market, Galvus (Vidagliptin) of Novartis, is going through an additional round of clinical trials before FDA approval. Even though Galvus has a presence in some pockets like Mexico, the actual entry into the big markets will be delayed.

Sitagliptin is indicated in type 2 diabetes mellitus patients to improve glycaemia control in combination with biguanides like metformin when diet and exercise with other oral hypoglycemics do not provide adequate glycaemia control. The recommended dose of Januvia is 100 mg once daily. Dosage needs to be adjusted in case of patients with renal insufficiency depending on the creatinine clearance. Januvia should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.

Gliptins, the DPP – 4 inhibitors are considered to be the ninth class of antidiabetic medications. The concept behind these dipeptidyl peptidase IV (DPP-IV) inhibitors, known as the gliptins, derives from the recognition that glucagon-like peptide (GLP) — a naturally occurring gastrointestinal peptide that stimulates insulin secretion, suppresses glucagon levels, and slows gastric emptying — is rapidly inactivated by DPP-IV. (
David M Nathan, N Engl J Med 2007 356: 437-440).

picture source: wikipedia

Dr Nathan gives a word of caution stating, “….Given that the main therapeutic effectiveness of the gliptins is mediated by their ability to increase levels of GLP, which is not a very effective glucose-lowering agent, it is not surprising that these agents are relatively ineffective in lowering glycated hemoglobin levels. Moreover, although they have been developed to be relatively specific for the GLP substrate and not to increase the levels of the many other DPP-IV substrates, none of them is so selective as to preclude alteration of the other substrates, including proteins involved in immunity and other hormones. The potential for unexpected consequences thus remains relatively high.” Please read my previous post on the safety of DPP-4 inhibitors in diabetics. Dr Nathan was very critical of FDA for approving Januvia, given the paucity of available data.

Whatever the case may be, Januvia now has a presence in 42 countries which includes the EU, the United states, Mexico and Philippines. Merck also has enough time to capture the market.

Seeji, Pharm House


  1. Anonymous says

    My husband has been on Jaunvia for only 10 days while still taking his metformin but no longer taking glibizide.
    His glocuse levels have risen significantly both fasting and post food intake. In fact he is eating very very little and has numbers consitenlty 250 - 399.
    Something is wrong with this drug!