Raltegravir

Raltegravir
Clinical data
Trade names	Isentress
Other names	RAL
AHFS/Drugs.com	Monograph
MedlinePlus	a608004
License data	EU EMA: by INN; US DailyMed: Raltegravir; US FDA: Raltegravir;
Pregnancy; category	AU: B3;
Routes of; administration	By mouth
ATC code	J05AJ01 (WHO) ;
Legal status
Legal status	UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	60% (FDA)
Protein binding	83%
Metabolism	Liver (UGT1A1)
Elimination half-life	9 hours
Excretion	feces and urine
Identifiers
	IUPAC name N-(4-Fluorobenzyl)-5-hydroxy-1-methyl-2-(2-{[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino}-2-propanyl)-6-oxo-1,6-dihydro-4-pyrimidinecarboxamide;
CAS Number	518048-05-0 ;
PubChem CID	54671008;
DrugBank	DB06817;
ChemSpider	16445111 ;
UNII	22VKV8053U;
KEGG	D06676; as salt: D07133;
ChEBI	CHEBI:82960;
ChEMBL	ChEMBL254316 ;
NIAID ChemDB	471309;
PDB ligand	RLT (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID2048660 ;
ECHA InfoCard	100.124.631
Chemical and physical data
Formula	C20H21FN6O5
Molar mass	444.423 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1nnc(o1)C(=O)NC(C)(C)C\3=N\C(C(=O)NCc2ccc(F)cc2)=C(\O)C(=O)N/3C;
	InChI InChI=1S/C20H21FN6O5/c1-10-25-26-17(32-10)16(30)24-20(2,3)19-23-13(14(28)18(31)27(19)4)15(29)22-9-11-5-7-12(21)8-6-11/h5-8,28H,9H2,1-4H3,(H,22,29)(H,24,30) ; Key:CZFFBEXEKNGXKS-UHFFFAOYSA-N ;

Raltegravir, sold under the brand name Isentress, is an antiretroviral medication used, together with other medication, to treat HIV/AIDS. It may also be used, as part of post exposure prophylaxis, to prevent HIV infection following potential exposure. It is taken by mouth.

Common side effects include trouble sleeping, feeling tired, nausea, high blood sugar, and headaches. Severe side effects may include allergic reactions including Stevens–Johnson syndrome, muscle breakdown, and liver problems. It is unclear if use during pregnancy or breastfeeding is safe. Raltegravir is an HIV integrase strand transfer inhibitor which blocks the functioning of HIV integrase which is needed for viral replication.

Raltegravir was approved for medical use in the United States in 2007. It is on the World Health Organization's List of Essential Medicines. Lamivudine/raltegravir, a combination with lamivudine, is also available.

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