生物活性 | |||
---|---|---|---|
描述 | Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Didanosine demonstrated linear pharmacokinetic behavior over the dose ranges of 0.4 to 16.5 mg/kg intravenously and 0.8 to 10.2 mg/kg orally. Bioavailability of didanosine when administered as a solution with an antacid was approximately 43% for doses from 0.8 to 10.2 mg/kg in patients with AIDS and advanced AIDS-related complex[3]. In the target cell for HIV, didanosine is converted to its active moiety, dideoxyadenosine-5'-triphosphate (ddATP), which inhibits HIV reverse transcriptase and terminates viral DNA growth. Didanosine is an effective and generally well tolerated drug in previously untreated and antiretroviral therapy-experienced patients with HIV infection[4]. Didanosine (100 mg/kg/day) induced a loss of mtDNA (to 48% of the control level) similar to that induced by fosalvudine tidoxil[5]. |
临床研究 | |||||
---|---|---|---|---|---|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00000924 | HIV Infections | Phase 2 | Completed | - | - |
NCT00618176 | HIV Infections | Phase 4 | Completed | - | China ... 展开 >> Peking Union Medical College Hospital Beijing, China, 100730 收起 << |
NCT00214435 | HIV Infection ... 展开 >> AIDS 收起 << | Phase 4 | Unknown | - | Australia, New South Wales ... 展开 >> 407 Doctors Recruiting Sydney, New South Wales, Australia, 2010 Contact: David A Baker, MB ChB 02 9332 2531 db@407.com.au Principal Investigator: David A Baker, MB ChB 收起 << |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.23mL 0.85mL 0.42mL |
21.17mL 4.23mL 2.12mL |
42.33mL 8.47mL 4.23mL |
参考文献 |
---|