Sitagliptin Phosphate

(USAN, rINNM)
Sitagliptin Phosphate Chemical formula
Synonyms: Fosfato de sitagliptina; MK-431; MK-0431; Ono-5435; Sitagliptine, Phosphate de; Sitagliptini Phosphas. 7-[(3R)-3-Amino-4(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazinemonophosphate monohydrate.
Cyrillic synonym: Ситаглиптина Фосфат.

💊 Chemical information

Chemical formula: C16H15F6N5O,H3O4P, H2O = 523.3.
CAS — 486460-32-6 (sitagliptin); 654671-78-0 (sitagliptin phosphate); 654671-77-9 (sitagliptin phosphate monohydrate).

💊 Profile

Like vildagliptin, sitagliptin is an inhibitor of the enzyme dipeptidylpeptidase-4, an enzyme responsible, among other roles, for the degradation of the incretin hormone glucagon-like peptide-1 (GLP-1; insulinotropin), which plays a role in regulating insulin secretion. It is used in the treatment of type 2 diabetes mellitus, as monotherapy or as dual therapy with metformin, a sulfonylurea, or a thiazolidinedione. Triple therapy using sitagliptin with metformin and a sulfonylurea may be given if dual therapy is inadequate. Sitagliptin is given as the phosphate, but doses are in terms of the base; 128.5 mg of sitagliptin phosphate is equivalent to about 100 mg of sitagliptin. The usual oral dose is the equivalent of 100 mg of sitagliptin once daily, as monotherapy or in combination. When given with metformin in a combination preparation, sitagliptin may be given in 2 divided doses. The dose of sulfonylurea may need to be lowered when used with sitagliptin. Sitagliptin may be taken with or without food. Dosage should be adjusted in patients with renal impairment (see below). Adverse effects reported with sitagliptin include upper respiratory-tract infections, headache, and nasopharyngitis. Hypersensitivity reactions including anaphylaxis, angioedema, urticaria, rash, and Stevens-Johnson syndrome have also been reported.
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Administration in renal impairment.

US licensed product information suggests the following oral doses of sitagliptin in patients with renal impairment, based on creatinine clearance (CC):
mild impairment (CC 50 mL/minute or more): no adjustment necessary, 100 mg daily
moderate impairment (CC 30 to less than 50 mL/minute): 50 mg daily
severe impairment (CC less than 30 mL/minute): 25 mg daily. It may be given without regard to the timing of haemodialysis

💊 Preparations

Proprietary Preparations

Austral.: Januvia; Braz.: Januvia; Cz.: Januvia; Tesavel; Xelevia; Fr.: Januvia; Gr.: Januvia; Xelevia; Malaysia: Januvia; Mex.: Januvia; Port.: Januvia; Tesavel; Xelevia; UK: Januvia; USA: Januvia. Multi-ingredient: USA: Janumet.
Published November 29, 2018.