Available EU DMF/CEP
API Status
Therapeutic Category
Alimentary tract & metabolism
Anti-infectives for systemic use
Antipyretic, analgesic and anti-inflammatory
Antineoplastic & immunomodulating agents
Blood & blood forming organs
Cardiovascular system
Genito-urinary system & sex hormones
Injectable forms
Musculo-skeletal system
Nervous system
Opthalmological preparations
Respiratory system
Available US DMF
Available Japanese/Chinese DMF
Japanese DMF
Chinese DMF
Korean DMF

Sitagliptin hydrochloride


69-09-0 (phosphate) 862156-92-1 (HCl)

Reference product


Polymorphic form

Crystalline monohydrate form III

Therapeutic Area

Alimentary tract and metabolism



EU DMF readiness

Q1 2020

US DMF readiness

Q1 2020

Drug description:

Sitagliptin phosphate/hydrochloride is an compound belongs to the beta amino acid derivative acts as anti-diabetic agent.
Sitagliptin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is used in combination treatment with all oral medications for type 2 diabetes and insulin products.
It is formulated as film coated tablets for oral route of administration.

Mechanism of Action:

Sitagliptin is a highly selective DPP-4 inhibitor exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones, thereby increasing the concentration and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner.

The above product is presented solely for informational purposes and does not constitute an offer in any sense. Products under patent (SPC) protection in Poland and/or other countries are not offered until expiration of the corresponding IP right.