Gilead acquires HIV integrase inhibitor from Japan Tobacco

This article is more than 20 years old. Click here for more recent articles on this topic

Gilead Sciences today announced that it has acquired the development rights to a drug from a new class. The product, an integrase inhibitor, has been licensed from Japan Tobacco.

JTK-303 has already undergone phase I human studies in healthy volunteers in Japan, and Gilead will get phase I/II trials underway in HIV-positive volunteers later this year, the company says.

HIV’s integrase enzyme is needed for integration of HIV DNA into the DNA of human cells, so it represents a new target for drug discovery in addition to the various steps in viral entry, and the reverse transcriptase and protease enzymes already targeted by licensed drugs.

Glossary

phase I

The first stage of human testing of a new drug or intervention, typically involving a small number (10-100) of participants who do not have the condition the drug is intended to treat. Phase I clinical trials evaluate safety, side-effects, dosage and how a drug is metabolised and excreted in the body.

deoxyribonucleic acid (DNA)

The material in the nucleus of a cell where genetic information is stored.

integrase inhibitors (INI, INSTI)

A class of antiretroviral drugs. Integrase strand transfer inhibitors (INSTIs) block integrase, which is an HIV enzyme that the virus uses to insert its genetic material into a cell that it has infected. Blocking integrase prevents HIV from replicating.

reverse transcriptase

A retroviral enzyme which converts genetic material from RNA into DNA, an essential step in the lifecycle of HIV. Several classes of anti-HIV drugs interfere with this stage of HIV’s life cycle: nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). 

enzyme

A protein which speeds up a chemical reaction.

Other companies working on integrase inhibitors include Merck, which already has a product in phase I/II trials, Pfizer, Bristol Myers Squibb, Glaxo SmithKline and Avexa, an Australian company.