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Page 1
Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: Insights from mathematical modeling and meta-analysis.
Garami A, Shimansky YP, Rumbus Z, Vizin RCL, Farkas N, Hegyi J, Szakacs Z, Solymar M, Csenkey A, Chiche DA, Kapil R, Kyle DJ, Van Horn WD, Hegyi P, Romanovsky AA. Garami A, et al. Pharmacol Ther. 2020 Apr;208:107474. doi: 10.1016/j.pharmthera.2020.107474. Epub 2020 Jan 9. Pharmacol Ther. 2020. PMID: 31926897 Free article. Review.
We also conducted a meta-analysis of T(b) data from human trials and found that polymodal TRPV1 antagonists (ABT-102, AZD1386, and V116517) increase T(b), whereas the mode-selective blocker NEO6860 does not. ...
We also conducted a meta-analysis of T(b) data from human trials and found that polymodal TRPV1 antagonists (ABT-102, AZD1386, …
Transient Receptor Potential Vanilloid 1 Antagonists Prevent Anesthesia-induced Hypothermia and Decrease Postincisional Opioid Dose Requirements in Rodents.
Garami A, Ibrahim M, Gilbraith K, Khanna R, Pakai E, Miko A, Pinter E, Romanovsky AA, Porreca F, Patwardhan AM. Garami A, et al. Anesthesiology. 2017 Nov;127(5):813-823. doi: 10.1097/ALN.0000000000001812. Anesthesiology. 2017. PMID: 28806222 Free article.
METHODS: General anesthesia was induced in rats and mice with either isoflurane or ketamine, and animals were treated with transient receptor potential vanilloid 1 antagonists (AMG 517 or ABT-102). The core body temperature and oxygen consumption were monitored duri …
METHODS: General anesthesia was induced in rats and mice with either isoflurane or ketamine, and animals were treated with transient recepto …
Solid state drug-polymer miscibility studies using the model drug ABT-102.
Jog R, Gokhale R, Burgess DJ. Jog R, et al. Int J Pharm. 2016 Jul 25;509(1-2):285-295. doi: 10.1016/j.ijpharm.2016.05.068. Epub 2016 Jun 3. Int J Pharm. 2016. PMID: 27265312
An extensive solid state miscibility study was conducted to aid in understanding the mechanisms involved in drug/stabilizer interactions. ABT-102 (model drug) and nine different polymers with different molecular weights and viscosities were selected to investigate d …
An extensive solid state miscibility study was conducted to aid in understanding the mechanisms involved in drug/stabilizer interactions. …
Formulation design and evaluation of amorphous ABT-102 nanoparticles.
Jog R, Kumar S, Shen J, Jugade N, Tan DC, Gokhale R, Burgess DJ. Jog R, et al. Int J Pharm. 2016 Feb 10;498(1-2):153-69. doi: 10.1016/j.ijpharm.2015.12.033. Epub 2015 Dec 15. Int J Pharm. 2016. PMID: 26705150
A DoE approach was applied to investigate formulation and spray drying process parameters for the preparation of spray dried amorphous ABT-102 nanoparticles. Stability studies were performed on the optimized formulations to monitor physical and chemical changes unde …
A DoE approach was applied to investigate formulation and spray drying process parameters for the preparation of spray dried amorphous AB …
What is the mechanism behind increased permeation rate of a poorly soluble drug from aqueous dispersions of an amorphous solid dispersion?
Frank KJ, Westedt U, Rosenblatt KM, Hölig P, Rosenberg J, Mägerlein M, Fricker G, Brandl M. Frank KJ, et al. J Pharm Sci. 2014 Jun;103(6):1779-86. doi: 10.1002/jps.23979. Epub 2014 Apr 24. J Pharm Sci. 2014. PMID: 24764046
In contrast, Caco-2 permeation of ABT-102 was independent of the ASD concentration, but three times faster than that of crystalline suspensions. Molecular solubility of ABT-102 (equilibrium dialysis) was also independent of the ASD concentration, but b …
In contrast, Caco-2 permeation of ABT-102 was independent of the ASD concentration, but three times faster than that of crysta …
Disturbances in slow-wave sleep are induced by models of bilateral inflammation, neuropathic, and postoperative pain, but not osteoarthritic pain in rats.
Leys LJ, Chu KL, Xu J, Pai M, Yang HS, Robb HM, Jarvis MF, Radek RJ, McGaraughty S. Leys LJ, et al. Pain. 2013 Jul;154(7):1092-102. doi: 10.1016/j.pain.2013.03.019. Epub 2013 Mar 15. Pain. 2013. PMID: 23664655
Sleep disturbances lasted for approximately 3 to 14days, depending on the model, and were resolved despite continued hypersensitivity to evoked stimulation. Morphine, gabapentin, diclofenac, and ABT-102 (TRPV1 antagonist) all improved sleep in the bilateral CFA assa …
Sleep disturbances lasted for approximately 3 to 14days, depending on the model, and were resolved despite continued hypersensitivity to evo …
The amorphous solid dispersion of the poorly soluble ABT-102 forms nano/microparticulate structures in aqueous medium: impact on solubility.
Frank KJ, Westedt U, Rosenblatt KM, Hölig P, Rosenberg J, Mägerlein M, Fricker G, Brandl M. Frank KJ, et al. Int J Nanomedicine. 2012;7:5757-68. doi: 10.2147/IJN.S36571. Epub 2012 Nov 12. Int J Nanomedicine. 2012. PMID: 23166440 Free PMC article.
The ASD, prepared by hot melt extrusion, contained the poorly soluble ABT-102 (solubility in buffer, 0.05 mug/mL), a hydrophilic polymer, and three surfactants. The apparent solubility of ABT-102 from the ASD-formulation was enhanced up to 200 times in …
The ASD, prepared by hot melt extrusion, contained the poorly soluble ABT-102 (solubility in buffer, 0.05 mug/mL), a hydrophil …
Effects of the TRPV1 antagonist ABT-102 on body temperature in healthy volunteers: pharmacokinetic/ pharmacodynamic analysis of three phase 1 trials.
Othman AA, Nothaft W, Awni WM, Dutta S. Othman AA, et al. Br J Clin Pharmacol. 2013 Apr;75(4):1029-40. doi: 10.1111/j.1365-2125.2012.04405.x. Br J Clin Pharmacol. 2013. PMID: 22966986 Free PMC article. Clinical Trial.
RESULTS: The developed body temperature model included additive components of baseline, circadian rhythm (cosine function of time) and ABT-102 effect (Emax function of plasma concentration) with tolerance development (decrease in ABT-102 Emax over time …
RESULTS: The developed body temperature model included additive components of baseline, circadian rhythm (cosine function of time) and AB …
Amorphous solid dispersion enhances permeation of poorly soluble ABT-102: true supersaturation vs. apparent solubility enhancement.
Frank KJ, Rosenblatt KM, Westedt U, Hölig P, Rosenberg J, Mägerlein M, Fricker G, Brandl M. Frank KJ, et al. Int J Pharm. 2012 Nov 1;437(1-2):288-93. doi: 10.1016/j.ijpharm.2012.08.014. Epub 2012 Aug 20. Int J Pharm. 2012. PMID: 22951865
We explored the formulation-related impact of ASDs on permeation rate, apparent solubility and molecular solubility of the poorly soluble drug ABT-102. The influence of fasted state simulated intestinal fluid (FaSSIF) as dispersion medium was also studied. ...Appare …
We explored the formulation-related impact of ASDs on permeation rate, apparent solubility and molecular solubility of the poorly soluble dr …
An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UV(B)-inflamed and normal skin.
Schaffler K, Reeh P, Duan WR, Best AE, Othman AA, Faltynek CR, Locke C, Nothaft W. Schaffler K, et al. Br J Clin Pharmacol. 2013 Feb;75(2):404-14. doi: 10.1111/j.1365-2125.2012.04377.x. Br J Clin Pharmacol. 2013. PMID: 22775239 Free PMC article. Clinical Trial.
ABT-102 6 mg was superior to active controls over the 8 h period (P < 0.05) whereas ABT-102 2 mg was comparable. Improvements in VAS scores compared with placebo were observed with ABT-102 6 mg (P < 0.001) and ABT-102 …
ABT-102 6 mg was superior to active controls over the 8 h period (P < 0.05) whereas ABT-102 2 mg was comparab …
19 results