Dolutegravir sodium

CAS No.	1051375-19-9	Cat. No.	BCP11890
Name	Dolutegravir sodium
Synonyms	Dolutegravir sodium salt;S/GSK1349572 sodium;GSK 1349572A;GSK-1349572A;GSK1349572A;
Formula	C20H18F2N3NaO5	M. Wt	441.36

Description	Dolutegravir (DTG, GSK1349572) is metabolized primarily by uridine diphosphate glucuronyltransferase (UGT)1A1, with a minor role of cytochrome P450 (CYP)3A, and with renal elimination of unchanged drug being extremely low (< 1% of the dose). Fifty-three percent of the total oral dose is excreted unchanged in the feces but it is unknown if all or part of this is due to unabsorbed drug or some percentage of biliary excretion of the glucuronide conjugate which can be further degraded to form the parent compound in the gut lumen. The current Food and Drug Administration (FDA) draft guidance for renal impairment studies states that a pharmacokinetic (PK) study in patients with renal impairment should be conducted even for those drugs primarily metabolized or secreted in bile, because renal impairment can inhibit some pathways of hepatic and gut drug metabolism and transport.
Pathways	Protease/Metabolic Enzyme Microbiology/Virology
Targets	Integrase HIV

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