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Drug Evaluation

Efavirenz – Still First-line King?

, PharmD MAS & , MD
Pages 965-972 | Published online: 15 Jul 2008

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (2)

Andrea Giacomelli, Laura Pezzati & Stefano Rusconi. (2020) The crosstalk between antiretrovirals pharmacology and HIV drug resistance. Expert Review of Clinical Pharmacology 13:7, pages 739-760.
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Beatriz Larru, Jessica Eby & Elizabeth D Lowenthal. (2014) Antiretroviral treatment in HIV-1 infected pediatric patients: focus on efavirenz. Pediatric Health, Medicine and Therapeutics 5, pages 29-42.
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Bin Su, Guiju Gao, Min Wang, Yanqiu Lu, Linghua Li, Chen Chen, Yuanyuan Chen, Chuan Song, Fengting Yu, Ying Li, Yixin Liu, Yang Luo, Haolan He, Cong Cheng, Lixia Xu, Tong Zhang, Lijun Sun, An Liu, Wei Xia, Yuanyuan Qin, Qingxia Zhao, Hongxia Wei, Weiping Cai, Yaokai Chen, Fujie Zhang & Hao Wu. (2023) Efficacy and safety of ainuovirine versus efavirenz combination therapies with lamivudine/tenofovir disoproxil fumarate for medication of treatment-naïve HIV-1-positive adults: week 48 results of a randomized controlled phase 3 clinical trial followed by an open-label setting until week 96. The Lancet Regional Health - Western Pacific 36, pages 100769.
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Bárbara Costa & Nuno Vale. (2022) Efavirenz: History, Development and Future. Biomolecules 13:1, pages 88.
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Runji Zhang, Jian Bao, Jialu Qiao, Wenshuang Li, Feng Qian, Kanghong Hu & Binlian Sun. (2021) Long-term efavirenz exposure induced neuroinflammation and cognitive deficits in C57BL/6 mice. Biochemical and Biophysical Research Communications 584, pages 46-52.
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Susana Santos Braga, Firas El-Saleh, Karyna Lysenko & Filipe A. Almeida Paz. (2021) Inclusion Compound of Efavirenz and γ-Cyclodextrin: Solid State Studies and Effect on Solubility. Molecules 26:3, pages 519.
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Dhanashree H. Surve, Yugandhara B. Jirwankar, Vikas D. Dighe & Anil B. Jindal. (2020) Long-Acting Efavirenz and HIV-1 Fusion Inhibitor Peptide Co-loaded Polymer–Lipid Hybrid Nanoparticles: Statistical Optimization, Cellular Uptake, and In Vivo Biodistribution . Molecular Pharmaceutics 17:10, pages 3990-4003.
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CH. RAMESH, DHARMASOTH RAMA DEVI DEVI, M.N.B. SRINIVAS, S. RADHA KRISHNA, NAGARAJU RAJANA & K. BASAVAIAH. (2020) Development and Validation of RP-Chiral HPLC Method for Determination of (R)-Enantiomer Excess Content in Efavirenz. Asian Journal of Chemistry 32:9, pages 2208-2212.
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Ansgar Brüning, Julia Jückstock, Bernd Kost, Panagiotis Tsikouras, Tobias Weissenbacher, Sven Mahner & Ioannis Mylonas. (2017) Induction of DNA damage and apoptosis in human leukemia cells by efavirenz. Oncology Reports 37:1, pages 617-621.
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Mônica M. Bastos, Carolina C.P. Costa, Talitha C. Bezerra, Fernando de C. da Silva & Núbia Boechat. (2016) Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. European Journal of Medicinal Chemistry 108, pages 455-465.
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A Olagunju, O Bolaji, A Amara, L Else, O Okafor, E Adejuyigbe, J Oyigboja, D Back, S Khoo & A Owen. (2015) Pharmacogenetics of pregnancy-induced changes in efavirenz pharmacokinetics. Clinical Pharmacology & Therapeutics 97:3, pages 298-306.
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Alessandro Schipani, David Back, Andrew Owen, Gerry Davies, Saye Khoo & Marco Siccardi. (2014) Use of In Vitro to In Vivo Extrapolation to Predict the Optimal Strategy for Patients Switching from Efavirenz to Maraviroc or Nevirapine. Clinical Pharmacokinetics 54:1, pages 107-116.
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Steffen Wildum, Daniela Paulsen, Kai Thede, Helga Ruebsamen-Schaeff & Holger Zimmermann. (2013) In Vitro and In Vivo Activities of AIC292, a Novel HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor . Antimicrobial Agents and Chemotherapy 57:11, pages 5320-5329.
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Michael B Gatch, Alexey Kozlenkov, Ren-Qi Huang, Wenjuan Yang, Jacques D Nguyen, Javier González-Maeso, Kenner C Rice, Charles P France, Glenn H Dillon, Michael J Forster & John A Schetz. (2013) The HIV Antiretroviral Drug Efavirenz has LSD-Like Properties. Neuropsychopharmacology 38:12, pages 2373-2384.
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Nicholas A. Meanwell, Stanley V. D'Andrea, Christopher W. Cianci, Ira B. Dicker, Kap‐Sun Yeung, Makonen Belema & Mark Krystal. 2013. Drug Discovery. Drug Discovery 439 515 .
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Rodrigo Cristofoletti, Anita Nair, Bertil Abrahamsson, D.W. Groot, Sabine Kopp, Peter Langguth, James E. Polli, Vinod P. Shah & Jennifer B. Dressman. (2013) Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Efavirenz. Journal of Pharmaceutical Sciences 102:2, pages 318-329.
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Iris Usach, Virginia Melis & José-Esteban Peris. (2013) Non-nucleoside reverse transcriptase inhibitors: a review on pharmacokinetics, pharmacodynamics, safety and tolerability. Journal of the International AIDS Society 16:1, pages 18567.
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A. Habtewold, W. Amogne, E. Makonnen, G. Yimer, K.-D. Riedel, N. Ueda, A. Worku, W. E. Haefeli, L. Lindquist, G. Aderaye, J. Burhenne & E. Aklillu. (2011) Long-term effect of efavirenz autoinduction on plasma/peripheral blood mononuclear cell drug exposure and CD4 count is influenced by UGT2B7 and CYP2B6 genotypes among HIV patients. Journal of Antimicrobial Chemotherapy 66:10, pages 2350-2361.
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Jayakanthan Mannu, Pranitha Jenardhanan & Premendu P. Mathur. (2010) A computational study of CYP3A4 mediated drug interaction profiles for anti-HIV drugs. Journal of Molecular Modeling 17:8, pages 1847-1854.
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Ana Blas-García, Nadezda Apostolova, Daniel Ballesteros, Daniel Monleón, Jose M. Morales, Milagros Rocha, Victor M. Victor & Juan V. Esplugues. (2010) Inhibition of mitochondrial function by efavirenz increases lipid content in hepatic cells. Hepatology 52:1, pages 115-125.
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Marie-Pierre de Béthune. (2010) Non-nucleoside reverse transcriptase inhibitors (NNRTIs), their discovery, development, and use in the treatment of HIV-1 infection: A review of the last 20 years (1989–2009). Antiviral Research 85:1, pages 75-90.
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