Drug intelligence / Profile preview

dolutegravir + rifabutin

Development stage
Phase 1
Lead developer
ViiV Healthcare
Modality
Small Molecules
Administration
Oral
01

Overview

**dolutegravir + rifabutin** is a combination of two drugs: dolutegravir (original code name GSK1349572) and rifabutin. Dolutegravir is a next-generation HIV integrase strand transfer inhibitor that prevents the integration of HIV DNA into the host genome by inhibiting the strand transfer step of the viral integrase enzyme. It is highly potent against wild-type and many integrase inhibitor-resistant HIV strains, developed for once-daily oral dosing without a pharmacokinetic booster. Rifabutin is an antibiotic of the rifamycin class used primarily for tuberculosis and mycobacterial infections; it inhibits bacterial DNA-dependent RNA polymerase. The combination may be used in patients co-infected with HIV and mycobacteria, as rifabutin is selected when avoiding strong CYP3A induction from rifampin. The interaction between dolutegravir and rifabutin is of clinical significance, as rifabutin is a moderate inducer of CYP3A, but dolutegravir is primarily glucuronidated and is less affected compared to other integrase inhibitors. Dolutegravir was developed via a collaboration between Shionogi and GSK and is marketed by ViiV Healthcare. The combination does not constitute a single marketed product with a unique brand name but represents a recognized regimen in specific clinical contexts.

Other names
dolutegravir + rifabutinS/GSK1349572 + rifabutinGSK1349572 + rifabutin
02

Targets

Integrase allosteric pocket (HIV)RNAP (Bacterial dna-dependent RNA polymerase)

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