Johnson, Mark Jewell, Roxanne C Gan, Jianjun Dumont, Etienne Burns, Olivia Johns, Brian A
Published in
Clinical pharmacology in drug development
GSK2838232 is a novel, potent HIV-1 maturation inhibitor for use in regimen-based combination antiretroviral therapy from a once-daily oral dose boosted with a pharmacoenhancer (ritonavir or cobicistat). This phase 1 study in healthy participants was conducted in 2 parts. Part 1 (n = 14) assessed the relative bioavailability of single doses of a 20...
Yamada, Masanori Osamura, Minori Ogura, Hirofumi Onoue, Tomohiro Wakamatsu, Akira Numachi, Yotaro Caltabiano, Stephen Mahar, Kelly M
Published in
Clinical pharmacology in drug development
Daprodustat is a prolyl hydroxylase inhibitor that stimulates erythropoiesis in a manner similar to the natural response to hypoxia, whereby inhibition of hypoxia inducible factor (HIF) prolyl-4-hydroxylases by daprodustat ultimately results in increased levels of HIF-responsive genes. Daprodustat is under development as an emerging new class of ag...
Sidharta, Patricia N Dingemanse, Jasper
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Clinical pharmacology in drug development
Aprocitentan is an investigational, orally active, dual, endothelin receptor antagonist that targets a novel pathway in the treatment of difficult-to-control (resistant) hypertension. The drug-drug interaction potential of aprocitentan on the breast cancer resistance protein (BCRP) transporter substrate rosuvastatin was investigated in this single-...
Patel, Chirag Goel, Sanjay Patel, Manish R Rangachari, Lakshmi Wilbur, Jayson D Shou, Yaping Venkatakrishnan, Karthik Lockhart, A Craig
Published in
Clinical pharmacology in drug development
The aim of this phase 1 study was to determine the effects of sapanisertib on the heart rate-corrected QT (QTc) interval in patients with advanced solid tumors. Adult patients with advanced solid tumors were enrolled to receive a single sapanisertib 40-mg dose. Blood samples for pharmacokinetic analysis were collected and electrocardiogram readings...
Sesoko, Shogo Huang, Jinhong Okayama, Takashige Nishida, Erika Miyoshi, Kazuhisa
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Clinical pharmacology in drug development
TAC-302 stimulates neurite outgrowth activity and is expected to restore urinary function in patients with lower urinary tract dysfunction. We conducted 2 phase 1, randomized, placebo-controlled studies to confirm the safety and pharmacokinetics (PK) of TAC-302 in healthy adult Japanese male volunteers. In the first-in-human single-dose study (n = ...
Ino, Hiroko Shiramoto, Masanari Eto, Takashi Haranaka, Miwa Irie, Shin Terao, Takumi Ogura, Hirofumi Wakamatsu, Akira Hoyano, Keiko Nakano, Atsushi
...
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Clinical pharmacology in drug development
Levocetirizine is classified as a second-generation antihistamine. Levocetirizine is available for the treatment of allergic disorders such as allergic rhinitis and chronic idiopathic urticaria. This was a single-center, single-dose, open-label, randomized, 2-way crossover study in healthy Japanese male subjects consisting of 2 parts. Part 1 compar...
Sakamoto, Kei Matsuki, Shunji Irie, Shin Uchida, Naoki Hayashi, Nobuya Horiuchi, Masato Ren, Song
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Clinical pharmacology in drug development
Tezepelumab, a human immunoglobulin G2 monoclonal antibody against thymic stromal lymphopoietin, is currently under clinical development for the treatment of severe, uncontrolled asthma. This phase 1, randomized, placebo-controlled, single-ascending-dose study assessed the safety, tolerability, pharmacokinetics, and immunogenicity of subcutaneous t...
Pei, Tong Yang, Jing Hu, Chaoying Chen, Xiaoping Gong, Shili Hu, Xiao Li, Lin Zhang, Lan
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Clinical pharmacology in drug development
Clopidogrel is an antiplatelet drug with high intraindividual variability in systemic exposure and efficacy. It has been used for treating atherosclerosis and acute coronary syndrome and in preventing stent restenosis and thrombotic complications after stent implantation in clinical practice for nearly 20 years. In this study we aimed to evaluate t...
Xu, Yichao Lou, Honggang Chen, Jinliang Jiang, Bo Yang, Dandan Hu, Yin Ruan, Zourong
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Clinical pharmacology in drug development
A backpropagation artificial neural network (BPANN) model was established for the prediction of the plasma concentration and pharmacokinetic parameters of rosuvastatin (RVST) in healthy subjects. The data (demographic characteristics and results of clinical laboratory tests) were collected from 4 bioequivalence studies using reference 10-mg RVST ca...
Rizea-Savu, Simona Duna, Simona Nicoleta Ghita, Adrian Iordachescu, Adriana Chirila, Marinela
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Clinical pharmacology in drug development
Duloxetine is a combined serotonin and norepinephrine reuptake inhibitor indicated in adults for the treatment of major depressive disorder, diabetic peripheral neuropathic pain, and generalized anxiety disorder. The aim of these studies was to evaluate the effect of food on the pharmacokinetics and safety of duloxetine 60-mg gastroresistant hard c...
