Efavirenz
Efavirenz structure
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Common Name | Efavirenz | ||
|---|---|---|---|---|
| CAS Number | 154598-52-4 | Molecular Weight | 315.675 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 422.7±55.0 °C at 760 mmHg | |
| Molecular Formula | C14H9ClF3NO2 | Melting Point | 139-141ºC | |
| MSDS | Chinese USA | Flash Point | 209.4±31.5 °C | |
| Symbol |
GHS09 |
Signal Word | Warning | |
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Mitochondrial (dys)function - a factor underlying the variability of efavirenz-induced hepatotoxicity?
Br. J. Pharmacol. 172(7) , 1713-27, (2015) The non-nucleoside analogue reverse transcriptase inhibitor efavirenz is associated with hepatic toxicity and metabolic disturbances. Although the mechanisms involved are not clear, recent evidence has pinpointed a specific mitochondrial action of efavirenz a... |
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Evaluation of the in vitro/in vivo potential of five berries (bilberry, blueberry, cranberry, elderberry, and raspberry ketones) commonly used as herbal supplements to inhibit uridine diphospho-glucuronosyltransferase.
Food Chem. Toxicol. 72 , 13-9, (2014) In this study, we evaluated inhibitory potentials of popularly-consumed berries (bilberry, blueberry, cranberry, elderberry, and raspberry ketones) as herbal supplements on UGT1A1, UGT1A4, UGT1A6, UGT1A9, and UGT2B7 in vitro. We also investigated the potentia... |
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Evaluation of thein vitro/in vivodrug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition
Food Chem. Toxicol. 68 , 117-27, (2014) • BST204 is a purified dry extract of ginseng containing high amounts of Rh2 and Rg3. • BST204 had only weak inhibitory effects on nine CYPs and five UGTs. • It is unlikely that BST204 alter pharmacokinetics of drugs metabolized by CYPs/UGTs. |
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Metabolic drug-drug interaction potential of macrolactin A and 7-O-succinyl macrolactin A assessed by evaluating cytochrome P450 inhibition and induction and UDP-glucuronosyltransferase inhibition in vitro.
Antimicrob. Agents Chemother. 58(9) , 5036-46, (2014) Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureu... |
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Species differences and substrate specificity of CYP3A heteroactivation by efavirenz.
Xenobiotica 45(4) , 345-52, (2015) 1. The purpose of this study was to clarify species differences in the heteroactivation of CYP3A substrates by efavirenz, which is known from clinical studies to activate midazolam 1'-hydroxylation, and to assess the feasibility of an animal model. 2. In monk... |
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Optimization of a validated stability-indicating RP-LC method for the determination of fulvestrant from polymeric based nanoparticle systems, drugs and biological samples.
Biomed. Chromatogr. 28(10) , 1409-17, (2014) Fulvestrant is used for the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy. Several reversed-phase columns with variable silica materials, diameters, lengths, et... |
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Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein.
Antimicrob. Agents Chemother. 58(6) , 3168-76, (2014) Predicting drug-drug interactions (DDIs) related to cytochrome P450 (CYP), such as CYP3A4 and one of the major drug transporters, P-glycoprotein (P-gp), is crucial in the development of future chemotherapeutic regimens to treat tuberculosis (TB) and TB/AIDS c... |
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Tetronic® 904-containing polymeric micelles overcome the overexpression of ABCG2 in the blood-brain barrier of rats and boost the penetration of the antiretroviral efavirenz into the CNS.
Nanomedicine (Lond.) 10 , 2325-37, (2015) To assess the involvement of ABCG2 in the pharmacokinetics of efavirenz in the blood-brain barrier (BBB) and investigate a nanotechnology strategy to overcome its overexpression under a model of chronic oral administration. Materials & methods A model of chro... |
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Potential interactions between HIV drugs, ritonavir and efavirenz and anticancer drug, nilotinib--a study in primary cultures of human hepatocytes that is applicable to HIV patients with cancer.
J. Clin. Pharmacol. 54(11) , 1272-9, (2014) Nilotinib is used to treat chronic myeloid leukemia (CML), and is metabolized by CYP3A. With a black-box warning for QT prolongation, which is exposure dependent, controlling for drug interactions is clinically relevant. Treatments of HIV patients with CML ar... |
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A screen of approved drugs and molecular probes identifies therapeutics with anti-Ebola virus activity.
Sci. Transl. Med. 7 , 290ra89, (2015) Currently, no approved therapeutics exist to treat or prevent infections induced by Ebola viruses, and recent events have demonstrated an urgent need for rapid discovery of new treatments. Repurposing approved drugs for emerging infections remains a critical ... |