| 药品名称 |
Delavirdine
|
| 分子靶点 |
Reverse transcriptase/RNaseH
|
| 酶 |
Cytochrome P450 3A4;Cytochrome P450 2D6;Cytochrome P450 3A5;Cytochrome P450 3A7;Cytochrome P450 2C9;Cytochrome P450 2C19;Cytochrome P450 2C8
|
| 药物类型 |
Small Molecule
|
| 研发阶段 |
Approved
|
| 药物描述 |
A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.
|
| 结构式 |
 |
| 药物别名 |
(N-[2-[4-[3-(1-methylethylamino)pyridin-2-yl]piperazin-1-yl]carbonyl-1H-indol-5-yl] methanesulfonamide);1-(3-((1-methylethyl)amino)-2-pyridinyl)-4-((5-((methylsulfonyl)amino)-1H-indol-2-yl)carbonyl)piperazine;2-(4-(5-methanesulfonamido-1H-indol-2-ylcarbonyl)-1-piperazinyl)-N-(1-methylethyl)-3-pyridinamine;Delavirdin;Delavirdina;Delavirdine;Delavirdinum;N-(2-(1-(3-(isopropylamino)pyridin-2-yl)piperazine-4-carbonyl)-1H-indol-5-yl)methanesulfonamide;N-{2-[4-(3-Isopropylamino-pyridin-2-yl)-piperazine-1-carbonyl]-1H-indol-5-yl}-methanesulfonamide
|
| 治疗类别 |
Anti-HIV Agents;Anti-Infective Agents;Anti-Retroviral Agents;Antiinfectives for Systemic Use;Antiviral Agents;Antivirals for Systemic Use;Cytochrome P-450 CYP2C19 Inhibitors;Cytochrome P-450 CYP2C19 Inhibitors (strong);Cytochrome P-450 CYP2C8 Inhibitors;Cytochrome P-450 CYP2C9 Inhibitors;Cytochrome P-450 CYP2C9 Inhibitors (strong);Cytochrome P-450 CYP2D6 Inhibitors;Cytochrome P-450 CYP2D6 Inhibitors (moderate);Cytochrome P-450 CYP2D6 Substrates;Cytochrome P-450 CYP3A Inhibitors;Cytochrome P-450 CYP3A Inhibitors (strong);Cytochrome P-450 CYP3A Substrates;Cytochrome P-450 CYP3A4 Inhibitors;Cytochrome P-450 CYP3A4 Inhibitors (strong);Cytochrome P-450 CYP3A4 Substrates;Cytochrome P-450 CYP3A5 Inhibitors;Cytochrome P-450 CYP3A7 Inhibitors;Cytochrome P-450 Enzyme Inhibitors;Direct Acting Antivirals;Enzyme Inhibitors;Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor;Indoles;Non-Nucleoside Reverse Transcriptase Inhibitors;Nonnucleoside Reverse Transcriptase Inhibitors;Nucleic Acid Synthesis Inhibitors;Piperazines;Reverse Transcriptase Inhibitors
|
| UNII号 |
DOL5F9JD3E
|
| CAS号 |
136817-59-9
|
| 分子量 |
456.561
|
| 分子式 |
C22H28N6O3S
|
| 适应症 |
For the treatment of HIV-1 infection in combination with appropriate antiretroviral agents when therapy is warranted
|
| 药效学 |
Delavirdine is a non-nucleoside reverse transcriptase inhibitor (nNRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Delavirdine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of Delavirdine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases (such as human DNA polymerases alpha, beta, or sigma) are not inhibited by Delavirdine.
|
| 作用机制 |
Delavirdine binds directly to viral reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by disrupting the enzyme's catalytic site.
|
| 吸收 |
Rapidly absorbed
|
| 蛋白结合 |
98%
|
| 代谢 |
Hepatic
|
| 排泄 |
Delavirdine is extensively converted to several inactive metabolites by cytochrome P450 3A (CYP3A). Delavirdine was excreted in the milk of lactating rats at a concentration three to five times that of rat plasma.
|
| 半衰期 |
5.8 hours
|
| 毒理 |
Major toxicity of delavirdine is rash and should be advised to promptly notify their physician should rash occur. The majority of rashes associated with delavirdine occur within 1 to 3 weeks after initiating treatment with delavirdine. The rash normally resolves in 3 to 14 days and may be treated symptomatically while therapy with delavirdine is continued. Any patient experiencing severe rash or rash accompanied by symptoms such as fever, blistering, oral lesions, conjunctivitis, swelling, muscle or joint aches should discontinue medication and consult a physician.
|
| ATC代码 |
J05AG02
|
