调查研究的非核苷逆转录酶抑制剂(Nnrti)在小型研究中很有
ATHENS, Greece (Reuters Health) - An investigational nonnucleoside reverse transcriptase inhibitor (NNRTI) designed by Belgium-based biotech firm Tibotec-Virco to treat drug-resistant HIV has shown promising results in a phase IIa trial.
Twelve treatment-na patients receiving TMC125 monotherapy experienced an average reduction in plasma viral load of 99% after 1 week of treatment, Tibotec-Virco's Dr. Gerben van 't Klooster and colleagues reported on Monday at the 8th European Conference on Clinical Aspects and Treatment of HIV Infection (ECCATH).
Eight of the 12 participants who received TMC125 had viral loads below 400 copies/mL at the end of the study, the investigators reported. The drug was well tolerated with no apparent differences in side effects between TMC125 and placebo.
Dr. Neil Graham, vice president of the company's medical department told Reuters Health that the depth and speed of the drop in viral load was to his knowledge unique.
"These early clinical data suggest that TMC125 could become a major contributor to more effective HIV therapy in the future," he said.
TMC125 is a dianilinopyrimidine with single bonds between its three pyrimidine rings. This provides the molecule with flexibility that allows it to inactivate the HIV reverse transcriptase molecule, even if mutations have altered the structure of the binding site.
The company now wants to test the drug in treatment-experienced patients and a similar week-long proof-of-concept study is under way, the investigators said.
Dr. Graham also told Reuters Health that a 48-week study of TMC125, in combination with other antiretrovirals, should begin in the first half of next year. NNRTI-resistant patients enrolled in the trial would be treated with a combination of drugs to which their virus is sensitive, plus either TMC125 or placebo.
-London Newsroom +44 20 7542 7986, http://www.100md.com
Twelve treatment-na patients receiving TMC125 monotherapy experienced an average reduction in plasma viral load of 99% after 1 week of treatment, Tibotec-Virco's Dr. Gerben van 't Klooster and colleagues reported on Monday at the 8th European Conference on Clinical Aspects and Treatment of HIV Infection (ECCATH).
Eight of the 12 participants who received TMC125 had viral loads below 400 copies/mL at the end of the study, the investigators reported. The drug was well tolerated with no apparent differences in side effects between TMC125 and placebo.
Dr. Neil Graham, vice president of the company's medical department told Reuters Health that the depth and speed of the drop in viral load was to his knowledge unique.
"These early clinical data suggest that TMC125 could become a major contributor to more effective HIV therapy in the future," he said.
TMC125 is a dianilinopyrimidine with single bonds between its three pyrimidine rings. This provides the molecule with flexibility that allows it to inactivate the HIV reverse transcriptase molecule, even if mutations have altered the structure of the binding site.
The company now wants to test the drug in treatment-experienced patients and a similar week-long proof-of-concept study is under way, the investigators said.
Dr. Graham also told Reuters Health that a 48-week study of TMC125, in combination with other antiretrovirals, should begin in the first half of next year. NNRTI-resistant patients enrolled in the trial would be treated with a combination of drugs to which their virus is sensitive, plus either TMC125 or placebo.
-London Newsroom +44 20 7542 7986, http://www.100md.com