Second Generation HIV Maturation Inhibitor Presented in USA
Dr. Edwin De Jesus of the Orlandian Center for Immunology (USA) presented the results of phase IIa clinical trials of the innovative second-generation HIV maturation inhibitor GSK2838232. The drug, which previously demonstrated a clearly defined preclinical virological profile and excellent pharmacokinetics, as well as safety and tolerability in HIV-negative volunteers, showed a high result in evaluating antiviral activity.
According to Dr. De Jesus, in a two-part study evaluating the pharmacokinetics, efficacy, and safety of HIV-positive people, 33 patients were divided into 4 groups (200 mg - 8 people, 100 mg - 10 people, 50 mg - 8 and 20 mg - 7) in order to study the antiviral effect and tolerance profile when using different dosages of GSK2838232 plus cobicistat (150 mg) once a day. Sample data was collected and analyzed within 10 days of taking the composition and 11 days after completion of therapy (21 days).
Following the completion of the study in the 1st cohort (100 mg), the specialists conducted a preliminary analysis of the pharmacokinetics and safety of the drug, and later evaluated the data of other cohorts.
In the course of studying the obtained information, scientists noticed a proportional increase in the dose of the antiviral effect of the composition. The level of pharmacokinetics for all dosages ranged from moderate to high with a steady state by the 8th day after administration and an average geometric plasma value of t½ to 10th.
By the time the study was completed (day 11), GSK2838232 monotherapy showed an average maximum decrease of HIV-1 RNA in plasma from the initial level by 1.70; 1.32; 1.56 and 0.67 log10 copies / ml at dosages of 200, 100, 50 and 20 mg, respectively.
Of the 33 participants, only one showed phenotypic resistance to the drug.
The test composition was well tolerated and did not cause clinically significant adverse reactions. Only five participants had headaches associated with the use of the drug, drowsiness and sleep disturbance, skin rash and itching.
Considering the data obtained from the study of each group, the experts concluded that GSK2838232 showed short-term tolerance and antiviral activity with the maximum response in the cohort with the highest dosage. Thus, preliminary results of the study of the effectiveness of the drug confirmed the validity of its further studies.