NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS IN DEVELOPMENT

NOTE: Several fact sheets describe drugs that are being tested against HIV: These drugs have not been approved by the Food and Drug Administration (FDA) for use against HIV.
NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
These drugs stop HIV from multiplying by blocking the reverse transcriptase enzyme. This enzyme changes HIV's genetic material (RNA) into the form of DNA. This step has to occur before HIV's genetic code gets combined with an infected cell's own genetic codes. Non-nucleoside reverse transcriptase inhibitors, called NNRTIs or non-nukes, physically prevent the reverse transcriptase enzyme from working.
NNRTIs IN DEVELOPMENT
NNRTIs (also called non-nukes) in development include BILR 355 BS, Calanolide A, Etravirine (TMC125), MIV-150, and Rilpivirine (TMC278).

BILR 355 BS by Boehringer Ingelheim is being developed against wild type virus and virus already resistant to NNRTIs. A Phase II study is in progress.

(+)-Calanolide A by Sarawak MediChem Pharmaceuticals was derived from a rain forest plant. It can easily cross the blood-brain barrier, and seems to stay in the bloodstream for a long time. It is in Phase II human trials.

Etravirine (TMC125) by Tibotec is active against some strains of HIV that are resistant to other NNRTIs. It takes longer for HIV to develop resistance to TMC125 than to the first NNRTI drugs. It is being studied in Phase III trials and is available through an expanded access program.

MIV-150 by Medivir and Chiron shows good results in the laboratory against HIV that is resistant to other NNRTIs. It takes a long time for HIV to develop resistance to MIV-150. Phase II trials are in progress.

Rilpivirine (TMC278) by Tibotec is active against some strains of HIV that are resistant to other NNRTIs. It is being developed as a once-daily medication. A Phase IIb dose finding study is in progress.

NNRTIs NO LONGER IN DEVELOPMENT
The following NNRTIs are no longer being developed for use against HIV:

  • Atevirdine by Upjohn
  • Capravirine by Pfizer / Agouron Pharmaceuticals
  • DPC083 by Bristol-Myers Squibb
  • Emivirine (Coactinon) by Triangle Pharmaceuticals
  • GW5634, GW678248 by GlaxoSmithKline
  • Loviride by Janssen Pharmaceuticals
  • HBY-097 by Hoechst-Bayer
  • PNU142721 by Pharmacia & Upjohn
  • TMC120 by Tibotec