生物活性

Indinavir is a potent and specific protease inhibitor (PI) which has long been used as a component of the highly active antiretroviral therapy (HAART) for the treatment of HIV/AIDS. Although new drugs have recently been developed, indinavir remains a popular choice in many developing countries. The metabolism of indinavir has been extensively studied in human, rats, dogs, and monkeys. It is metabolized predominantly via CYP3A and is also a substrate of P-glycoprotein (P-gp), an efflux transporter that can limit the oral absorption of indinavir. Consequently, co-administration of foods, drugs or dietary supplements with influences on CYP3A and/or P-gp may affect the pharmacokinetics of indinavir, causing undesirable toxicity and/or diminishment of drug efficacy.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Jia-Ming Yang,et.al. Impact of the Herbal Medicine Sophora flavescens on the Oral Pharmacokinetics of Indinavir in Rats: The Involvement of CYP3A and P-Glycoprotein. PLoS One. 2012; 7(2): e31312. Published online 2012 Feb 16. doi: 10.1371/journal.pone.0031312. PMCID: PMC3281083.
[2] Evan D. Kharasch,et.al. Lack of Indinavir Effects on Methadone Disposition Despite Inhibition of Hepatic and Intestinal Cytochrome P4503A (CYP3A)Anesthesiology. Author manuscript; available in PMC 2013 Mar 4. Published in final edited form as: Anesthesiology. 2012 Feb; 116(2): 432–447. doi: 10.1097/ALN.0b013e3182423478. PMCID: PMC3586934.
[3] Swetha Bollam,et.al. Development of Indinavir Submicron Lipid Emulsions Loaded with Lipoamino Acids—In Vivo Pharmacokinetics and Brain-Specific Delivery. AAPS PharmSciTech. 2011 Mar; 12(1): 422–430. Published online 2011 Mar 1. doi: 10.1208/s12249-011-9604-3. PMCID: PMC3066383.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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